- CYCLOBUTYL AMIDE MONOACYLGLYCEROL LIPASE MODULATORS
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Compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to depression, major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, and bipolar disorder), cancers and eye conditions: wherein R1, , R3, and L are as defined herein.
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- Non-Cryogenic, Ammonia-Free Reduction of Aryl Compounds
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A method of reducing an aromatic ring or a cyclic, allylic ether in a compound includes preparing a reaction mixture including a compound including an aromatic moiety or a cyclic, allylic ether moiety, an alkali metal, and either ethylenediamine, diethylenetriamine, triethylenetetramine, or a combination thereof, in an ether solvent; and reacting the reaction mixture at from ?20° C. to 30° C. for a time sufficient to reduce a double bond in the aromatic moiety to a single bond or to reduce the cyclic, allylic ether moiety.
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- COMPOUND FOR INHIBITING PGE2/EP4 SIGNALING TRANSDUCTION INHIBITING, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF
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A compound of formula (I), a preparation method therefor, a pharmaceutical composition containing a derivative thereof, and the therapeutic uses thereof, especially inhibiting PGE2/EP4 signalling transduction and the uses thereof for treating cancer, acute or chronic pain, migraine, osteoarthritis, rheumatoid arthritis, gout, bursitis, ankylosing spondylitis, primary dysmenorrhea, tumour or arteriosclerosis.
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- CROSSLINKED ARTIFICIAL NUCLEIC ACID ALNA
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The present invention provides a novel bridged artificial nucleic acid and an oligomer containing the same as a monomer. The present invention provides specifically a compound represented by general formula (I) (wherein each symbol is the same as defined in the specification) or salts thereof; as well as an oligonucleotide compound represented by general formula (I′) (wherein each symbol is the same as defined in the specification) or salts thereof.
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- TEMPERATURE-SENSITIVE NANO SILVER CONTROLLED-RELEASE SMART ANTIBACTERIAL COATING AND PREPARATION METHOD THEREFOR
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This present invention discloses a temperature-sensitive nano-silver controlled release antibacterial coating composite, which is comprises: water, acrylic, polyurethane resin, temperature-sensitive nano-silver controlled release antibacterial agent, dispersant, curing agent, defoamer, filming additive and leveling agent. By adsorbing nano silver particles into the pores of mesoporous SiO2 modified by poly N-isopropyl acrylamide, we successfully prepared a temperature-sensitive nano-silver controlled release antibacterial agent. By adding the prepared agent to the conventional coating composite, we achieved “on-off” control of the antibacterial properties of coating composite. Through the control of temperature, the release of nano-silver in the mesoporous nano-silica of the coating film layer is controlled. This control method is not only to protect the nano-silver, but also to adjust the strength of the anti-bacterial properties according to the actual demands and improve the use-efficiency of nano silver particles. This invention is in line with the new concept of “Intelligent Age” in the 21st century.
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- BICYCLIC HETEROARYL COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN
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Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
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- Thermoreversible reactions on inorganic nanoparticle surfaces: Diels-alder reactions on sterically crowded surfaces
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Organically surface-functionalized nanoparticles are important cross-linkers for nanocomposites. In the past, many cross-linking reactions were based on simple radical additions. However, novel smart materials require reversible reactions. These reactions, such as the Diels-Alder reaction, often have a specific sterical demand, e.g., a six-centered transition state. In this study, 5 nm silica particles were functionalized with maleimide groups, and their reactivity with regard to Diels-Alder reactions were investigated, applying various techniques. A new method for the surface modification of silica nanoparticles is presented, minimizing agglomeration in organic solvents and thus increasing the accessibility of the functional groups on the particle surface. Kinetic studies of substituted model compounds were carried out to evaluate the reactivity of the maleimide functionality. The Diels-Alder reaction between 2,5-dimethylfuran and N-propylmaleimide, N-ethyl(N-propylcarbamato) maleimide, and N-phenylmaleimide was followed by UV/Vis spectroscopy. The reaction rate increases in this order, showing the effect of maleimide substitution. Afterwards N-((3-triethoxysilyl)propyl)maleimide was used to graft maleimidopropyl functional groups onto the nanoparticle surface. 3-Aminopropyltriethoxysilane, which could then be reacted with 1,1′-(methylenedi-4,1-phenylene)bismaleimide, was used to attach phenyl-substituted maleimide functionality to the surface. 3- Isocyanatopropyltriethoxysilane introduced the electron-drawing carbamato functionality into the system. The surface coverage of the samples was characterized applying CHN analysis, TGA-FTIR coupling, and FTIR spectroscopy. All analytical methods revealed that the functional groups are covalently bonded to the silica surface and the maleimide rings remain intact. Diels-Alder reactions of the surface groups show that the reactivity of the molecules attached to the particles depends on sterical crowding, but the reaction rate is not significantly changed by surface effects.
- Engel, Tom,Kickelbick, Guido
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p. 149 - 157
(2013/08/24)
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- NANOPARTICLES THAT PREFERENTIALLY ASSOCIATE WITH AND KILL DISEASED CELLS FOR DIAGNOSTIC AND THERAPEUTIC APPLICATIONS
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Of the many compositions and methods provided herein, one composition includes a nanoparticle having a first oxide of a first metal and a dopant that includes an ion or an atom of a second metal. A method includes a method comprising providing a plurality of nanoparticles comprising a first oxide of a first metal and a dopant that comprises an ion or an atom of a second metal; providing a diseased cell and a healthy cell; contacting the diseased cell and the healthy cell with the nanoparticle; and allowing the nanoparticle to preferentially associate with the diseased cell.
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- INHIBITORS OF HEMOPOIETIC CELL KINASE (P59-HCK) AND THEIR USE IN THE TREATMENT OF INFLUENZA INFECTION
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The present invention relates inter alia to the treatment or prevention of influenza virus infection (including subtypes influenza A virus, influenza B virus, avian strain H5N1, A/H1N1, H3N2 and/or pandemic influenza) using compounds which inhibit the activity of p59-HCK and to a method of screening for a candidate drug substance intended to prevent or treat influenza virus infection in a subject, said method comprising identifying a test substance capable of inhibiting p59-HCK activity.
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- Compounds and Compositions as Protein Kinase Inhibitors
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The present invention provides compounds of Formula I or II: wherein R1, R1b, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds of Formula (I) or (II) and pharmaceutical compositions thereof are useful for the treatment of B-Raf-associated diseases.
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- Alkaloids
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The present invention provides novel alkaloid compounds and collections of these compounds, and provides methods for the synthesis of these compounds using biomimetic synthetic strategies. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as bacterial infections, proliferative diseases, and reproductive disorders, to name a few.
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- AROMATIC AMIDES
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This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
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- Thiazole compounds and their pharmaceutical use
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Compounds of formula (I) and pharmaceutically-acceptable and -cleavable esters thereof and acid addition salts thereof, wherein the symbols are as defined are MAP kinase inhibitors, useful pharmaceutically for treating TNFα and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.
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- Antithrombotic agents
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The invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts, as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.
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- N-ureidoheterocycloalkyl-piperidines as modulators of chemokine receptor activity
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The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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- Phenylpiperazines
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The invention relates to novel phenylpiperazine derivatives of the formula wherein: —R represents the group (a) or (b) as indicated in the description. These compounds are (partial) D2 receptor agonists and are usefull for treating CNS disorders, in particular Parkinson's disease.
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- Inhibitors of papilloma virus
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A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DN
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- Benzimidazolidinone derivatives as muscarinic agents
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Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
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- Heterocyclic aromatic compounds useful as growth hormone secretagogues
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Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xais heteroaryl, preferably, ?and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5and R5aare as defined herein.
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- Heterocyclic aromatic compounds usefuls as growth hormone secretagogues
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Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof,wherein Xa is heteroaryl, preferably, ?and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.
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- 6,11-3C-bicyclic 9a-azalide derivatives
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The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
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- Hydantoin compounds useful as anti-inflammatory agents
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Compounds having the formula (I): 1and pharmaceutically-acceptable salts thereof, are useful for treating inflammatory or immune diseases, in which A is a four to seven membered heterocyclic or carbocyclic saturated ring; L and K are O or S; M is N or CH; Y is N or CH; Z is hydrogen, alkyl or substituted alkyl; and R1-R4 are as defined in the specification.
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- Methods for forming combinatorial libraries combining amide bond formation with epoxide opening
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The invention relates to methods for forming combinatorial libraries. The invention provides methods suitable for the rapid and convenient synthesis of very large combinatorial libraries of small organic molecules. In particular, the invention provides a
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- Indazole derivatives as JNK inhibitors and compositions and methods related thereto
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Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
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- Hepatitis C virus inhibitors
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The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.
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- Thrombin inhibitors
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This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.
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- Compounds which mimic the chemical and biological properties of discodermolide
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Compounds which mimic the chemical and/or biological activity of discodermolide are provided and intermediates useful in their preparation.
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- Chemical Compounds
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A compound of formula (I) which is an agonist at the adenosine A1 receptor wherein R2represents C1-3alkyl, halogen or hydrogen; R3represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the adenosine A1 receptor.
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- 2-(Purin -9-yl)-tetrahydrofuran-3,4-diol derivatives
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A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2areceptor are described.
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- Nematicidal pyrazoles
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Novel pyrazoles of formula (1) wherein R1 represents halogen, C1-6 alkyl, C1-5 haloalkyl, C2-6 alkoxy, C1-4 alkylthio, C2-5 alkenyloxy, C3-5 alkynyloxy, C2-6 (total carbon number) alkoxyalkyl, C2-6 (total carbon number) alkylthioalkyl, C1-5 haloalkoxy, C2-6 (total carbon number) alkoxyalkoxy, hydroxy or optionally substituted phenyl, R2 represents hydrogen, halogen, C1-5 alkyl, C2-6 (total carbon number) alkoxyalkyl, C2-6 (total carbon number) alkylthioalkyl, C2-6 (total carbon number) alkylsulfinylalkyl, C2-6 (total carbon number alkylsulfonylalkyl or C1-5 haloalkyl, R3 represents hydrogen, C1-5 alkyl, —COR4, COOR5, CH(OR6)2 or CH2Si(R7)3, R4 represents C1-10 alkyl, C1-6 haloalkyl, C2-6 alkenyl, optionally substituted C3-6 cycloalkyl, C2-6 (total carbon number) alkoxyalkyl, C2-6 (total carbon number alkylthioalkyl, optionally substituted phenyl, C1-6 haloalkyl, alkylamino, di-(C1-6 alkyl)amino or optionally substituted phenylamino, R5 represents C1-7 alkyl, R6 and R7 represent C1-6 alkyl, and n is 1, 2 or 3, and when n is 2 or 3, the corresponding number (n) of R1 radicals may be the same or different, processes for preparing these compounds and their use as nematicides and anthelmintics.
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- Cytokine production inhibitors
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A compound selected from the group consisting of a 5,6-dihydro-α-pyrone of formula (I): wherein bond a is oriented eitheror; X is O or NH; R1is selected from the group consisting of: a group R3(O)C— wherein R3is selected from the group consisting of: (i) a group of formula R4—CH═CH— wherein R4is C1-C20alkyl, C2-C20alkenyl, an aryl group, or a 5- or 6-membered unsaturated heterocyclic ring containing one or two O, N or S atoms, (ii) C2-C20alkyl; and (iii) an aryl group or a substituent which is a fused ring system of formula (1) or (2): ?wherein each of R′ and R″, which are the same or different and may occupy any position on ring a or ring b of said fused ring system, is H or C1-C6alkyl; a group ArCH2— wherein Ar is an aryl group; and a group R5O—CH2— wherein R5is C1-C6alkyl optionally interrupted by one or two O atoms; and R2is CH3or, when R1is a group of formula (A) as defined below, R2is R6OOC— or R6NOC— wherein R6is C1-C6alkyl; and the pharmaceutically and veterinarily acceptable salts and esters thereof; with the exception of compounds wherein bond a is oriented, X is O and R1is a group of formula (A): ?wherein R11and R21are H when R2in formula (I) is CO2H or CH3, or one of R11and R21is H and the other is OH when R2in formula (I) is CO2H.
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- Biologically active analogs of discodermolide
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The subject invention provides novel compositions of biologically active discodermolide compounds which can advantageously be used for immunomodulation and/or treating cancer. The compounds of the subject invention have utility for use in the treatment of cancer, as tubulin polymerizers and as microtubule stabilization agents. The present invention also pertains to the identification of regions of the discodermolide molecule which are responsible for certain aspects of the bioactivity of discodermolide compounds.
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- Transition metal aerogel-supported catalyst
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A process for preparing a supported catalyst comprising a transition metal selected from palladium, platinum, nickel, cobalt or copper on an aerogel support, which includes the steps of providing a mixture containing an alkoxide precursor of the aerogel, a chelate complex of the transition metal with a chelating agent having Si(OR)3anchor groups, and an organic solvent in which the chelate complex is soluble; hydrolyzing the mixture by admixing it with water to form a gel; and converting the gel under supercritical conditions into the transition metal aerogel-supported catalyst. The supported catalyst has an especially homogeneous distribution of the metal component and is suitable, for example, for use as a hydrogenation catalyst.
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- Benzyloxy-substituted, fused N-heterocycles, processes for their preparation, and their use as bradykinin receptor antagonists
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Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of liver cirrhosis or Alzheimer''s disease. This application describes such compounds, as well as processes for their preparation and use. The compounds according to this invention include compounds of formula (I) STR1in which B, D, R 1, and R 2 have the meanings indicated herein.
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- Piperazine compounds, their preparation, and methods of using them
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Novel piperazine and piperidine derivative compounds having interesting and advantageous pharmacological properties. The disdosed compounds have the general formula (a) and salts thereof. These compounds have high affinity for both the dopamine D2receptors and serotonine 5-HT1Areceptors, rendering them useful for the treatment of CNS-disorders, in particular schizophrenia.
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- 2,3,5-substituted biphenyls useful in the treatment of insulin resistance and hyperglycemia
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This invention provides compounds of Formula I having the structure wherein:B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
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- Heteroaryl alkyl alpha substituted peptidylamine calcium channel blockers
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The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
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- Precursors for deoxyribonucleotides containing non-standard nucleosides
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The disclosure describes building blocks for preparing oligonucleotides carrying non-standard nucleobases that can pair with complementary non-standard nucleobases so as to fit the Watson-Crick geometry, in that the resulting base pair joins a monocyclic six membered ring pairing with a fused bicyclic heterocyclic ring system composed of a five member ring fused with a six member ring, with the orientation of the heterocycles with respect to each other and with respect to the backbone chain analogous to that found in DNA and RNA, but with a pattern of hydrogen bonds holding the base pair together different from that found in the AT and GC base pairs (a "non-standard base pair").
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- Antithrombotic diamines
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This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.
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- SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
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This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: STR1 This invention also provides pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
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- Anti-viral compounds
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PCT No. PCT/US97/07531 Sec. 371 Date Jan. 6, 1999 Sec. 102(e) Date Jan. 6, 1999 PCT Filed May 2, 1997 PCT Pub. No. WO97/42155 PCT Pub. Date Nov. 13, 1997The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
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- Process for producing unsaturated glycol diester using tellurium and rhodium catalyst
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A method for production of unsaturated glycol diester, such as 1,4-diacetoxy-2-butene, is formed of reacting conjugated diene with carboxylic acid and molecular oxygen in the presence of a solid catalyst in the liquid phase under pressure. The catalyst is formed of rhodium and tellurium, which are supported on an inorganic porous carrier. The catalyst is stable, and the unsaturated glycol diester is prepared in high conversion and selectivity.
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- Anti-viral compounds
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PCT No. PCT/US97/07438 Sec. 371 Date Jan. 6, 1999 Sec. 102(e) Date Jan. 6, 1999 PCT Filed May 2, 1997 PCT Pub. No. WO97/42156 PCT Pub. Date Nov. 13, 1997The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
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- Anti-viral method
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PCT No. PCT/US97/07525 Sec. 371 Date Jan. 6, 1999 Sec. 102(e) Date Jan. 6, 1999 PCT Filed May 2, 1997 PCT Pub. No. WO97/41849 PCT Pub. Date Nov. 13, 1997A method of inhibiting an envelope virus selected from the group consisting of influenza bovine diarrheal, hepatitis C and tick borne encephalitis virus that udergoes hemagglutinin-mediated fusion with a host cell is disclosed which comprises administering to a virus-infected cell, a cell susceptible of infection or a mammal in need thereof, an effective amount of a compound as defined by Formula I in the specification.
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- Anti-viral compounds
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PCT No. PCT/US97/07526 Sec. 371 Date Jan. 6, 1999 Sec. 102(e) Date Jan. 6, 1999 PCT Filed May 2, 1997 PCT Pub. No. WO97/41860 PCT Pub. Date Nov. 13, 1997The present invention provides compounds which inhibit. an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
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- BENZIMIDAZOLE DERIVATIVES HAVING DOPAMINERGIC ACTIVITY
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Pharmaceutically active benzimidazole derivatives are disclosed comprising compounds of the formula: STR1 particularly wherein X is nitrogen, R. sup.1 is phenyl or heteroaryl, and one of R 2 or R 3 is hydroxy. Said compounds have D4 dopaminergic receptor binding activity and consequently are useful as active ingredients in pharmaceutical compositions and methods of treatment for sleep disorders, sexual disorders, gastrointestinal disorders, psychosis, affective psychosis, nonorganic psychosis, personality disorders, psychiatric mood disorders, conduct and impulse disorders, schizophrenic and schizoaffective disorders, polydipsia, bipolar disorders, dysphoric mania, anxiety and related disorders, obesity, emesis, bacterial infections of the CNS, learning disorders, memory disorders, Parkinson's disease, depression, extrapyramidal side effects from neuroleptic agents, neuroleptic malignant syndrome, hypothalamic pituitary disorders, ocular disorders, congestive heart failure, chemical dependencies, vascular and cardiovascular disorders, dystonia, tardive dyskinesia, Gilles De La Tourette's syndrome and other hyperkinesias, dementia, ischemia, Parkinson's disease, akathesia and other movement disorders, hypertension and diseases caused by a hyperactive immune system such as allergies and inflammation in a mammal.
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- BENZIMIDAZOLONE DERIVATIVES WITH CENTRAL DOPAMINERGIC ACTIVITY
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This invention relates to novel, pharmaceutically active benzimidazolone derivatives of the formula STR1 wherein the dashed line, R 0 through R 6 and X 1 through X 3 are defined as in the specification. These compounds exhibit central dopaminergic activity and are u in the treatment of CNS disorders.
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- Supported Lewis acid catalyst polymerization process
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A supported Lewis acid catalyst, which comprises an inorganic oxide substrate having immobilized thereon at least one Lewis acid and a modifying agent containing at least one functional moiety capable of reacting with surface hydroxyl groups originally present on said substrate and which is effective as a catalyst for hydrocarbon conversion reactions including cationic polymerization, alkylation, isomerization and cracking reactions is disclosed.
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- Benzofurans and benzopyrans as chronobiological agents
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The invention thus provides compounds of Formula (I) STR1 wherein R 1 and R 2 which may be the same or different represent H, C 1-6 alkyl or substituted alkyl or C 3-7 cycloalkyl; or aryl;R 3, and R 4 which may be the same or different represent H, halogen, C 1-6 alkyl; or substituted aryl;R 5 is H or C 1-6 alkyl;n is an integer 0, 1 or 2and m is an integer 1, 2, 3, or 4;the dotted line indicates the presence or absence of an additional bond; and pharmaceutically acceptable solvates (e.g. hydrates) thereof.
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- Adenosine derivatives
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This invention relates to novel adenosine derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. Thus the invention provides compounds of formula (I) which are agonists at the adenosine A1 receptor. STR1 wherein R1 represents phenyl optionally substituted by one or more substituents selected from halogen, C1-3 alkyl, trifluoromethyl, nitro, cyano, --CO2 Ra1 --CONRa Rb, --CORa, --SORc, --SO2 Rc, --SO3 H, --SO2 NRa Rb, --ORa, --NHSO2 Rc, --NHCORa and --NRa Rb, R2 represents a C1-6 alkyl or C3-6 alkenyl group; R3 represents C1-3 alkyl; Ra and Rb may each independently represent hydrogen or C1-3 alkyl or, when --NRa Rb is directly attached to said phenyl, Ra and Rb together with the nitrogen atom may form a -5 or -6 or membered heterocyclic ring optionally containing a second heteroatom selected from oxygen or nitrogen, which second nitrogen heteroatom may optionally be further substituted by hydrogen or C1-3 alkyl; Rc represents C1-3 alkyl; and salts and solvates thereof, in particular physiologically acceptable salts and solvates thereof.
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