- Retro-aza-Michael reaction in continuous flow. Approaches to synthesis of adaline and euphococcinine related products
-
A retro-aza-Michael ring opening reaction of tropinone and granatanone (pseudopelletierine) in flow setup was investigated and the resulting products were utilized as key intermediates in approaches to adaline and its analogues. The enantioselective flow-reaction gave products of ring opening of granatanone with enantiopurity up to 98% ee. Attempts to elaborate the retro-aza-Michael product to alkaloids are described. Lithiated carbamate derivative of tropane was converted to a tropane analogue of euphococcinine, an adaline related alkaloid (a methyl and tropane homologue of adaline 19). Reactivity of the retro-aza-Michael product under Morita-Baylis-Hillman conditions was also briefly investigated.
- Sienkiewicz, Michal,Pawelski, Damian,Podgorska, Katarzyna,Lazny, Ryszard
-
-
- Decarboxylative Oxygenation via Photoredox Catalysis
-
The direct conversion of aliphatic carboxylic acids to their dehomologated carbonyl analogues has been accomplished through photocatalytic decarboxylative oxygenation. This transformation is applicable to an array of carboxylic acid motifs, producing ketones, aldehydes, and amides in excellent yields. Preliminary results demonstrate that this methodology is further amenable to aldehyde substrates via in situ oxidation to the corresponding acid and subsequent decarboxylative oxygenation. We have exploited this strategy for the sequential oxidative dehomologation of linear aliphatic chains.
- Faraggi, Tomer M.,Li, Wei,MacMillan, David W. C.
-
p. 410 - 415
(2019/12/24)
-
- CHROMEN-4-ONE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS DISEASE
-
The present invention provides novel compounds having the general formula (I) wherein R1 to R6, and m are as described herein, compositions including the compounds and methods of using the compounds.
- -
-
Page/Page column 80
(2020/05/21)
-
- METHODS AND COMPOSITIONS FOR MODULATING SPLICING
-
Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
- -
-
Paragraph 01005
(2020/08/22)
-
- Tropane alkaloid compounds and method of manufacturing using sequential oxidation reactions
-
The present invention relates to a tropane alkaloid compound sequentially using an oxidative Mannich ring reaction and a method for producing the same. The present invention provides a tropane alkaloid compound having a structure of chemical formula 1 in
- -
-
-
- Compound and application thereof
-
The invention provides a novel compound. The novel compound has certain inhibitory activity for indoleamine 2,3-dioxygenase (IDO) which is oxido-reductase, and accordingly the novel compound can be used for treating diseases related to the indoleamine 2,3-dioxygenase and can be applied to cancer and immunity related diseases.
- -
-
Paragraph 0245-0248
(2019/04/17)
-
- Construction of 8-Azabicyclo[3.2.1]octanes via Sequential DDQ-Mediated Oxidative Mannich Reactions of N-Aryl Pyrrolidines
-
A concise synthesis of 8-azabicyclo[3.2.1]octanes via sequential oxidative Mannich reactions is described. This approach involves an intermolecular oxidative Mannich coupling reaction between N-aryl pyrrolidines with TMS enol ether and a subsequent intramolecular oxidative Mannich cyclization of the corresponding silyl enol ether. DDQ is used as a key oxidant for both reactions.
- Jo, Hanbyeol,Hassan, Ahmed H. E.,Jung, Seung Young,Lee, Jae Kyun,Cho, Yong Seo,Min, Sun-Joon
-
p. 1175 - 1178
(2018/02/23)
-
- CDK kinase inhibitors
-
The present invention belongs to the technical field of medicine, and particularly relates to a CDK kinase inhibitor represented by a general formula (I), a pharmaceutically acceptable salt of the CDK kinase inhibitor, an ester of the CDK kinase inhibitor, a solvate of the CDK kinase inhibitor and stereoisomers of the CDK kinase inhibitor, the pharmaceutically acceptable salt, the ester and the solvate, wherein R1, R2, R3, R4, R5 and n are defined in the specification. The present invention further relates to preparation methods of the compounds, pharmaceutical formulations containing the compounds, pharmaceutical compositions containing the compounds, and applications of the compound, the pharmaceutically acceptable salt, the ester, the solvate and the stereoisomers in preparation of treatment and/or preparation of CDK kinase-mediated cancer associated diseases. The formula (I) is defined in the specification.
- -
-
Paragraph 0417; 0419-0421
(2017/08/02)
-
- Tyrosine Kinase Inhibitor And Uses Thereof
-
Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.
- -
-
Paragraph 0516-0517
(2017/05/15)
-
- 7H-Pyrrolo[2,3-d]pyrimidine-4-thiol derivatives using as JAK-3 inhibitors
-
The present invention relates to a method for preparing a novel 7H-pyrrolo[2,3-d]pyrimidine-4-thiol derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient. The composition containing the novel 7H-pyrrolo[2,3-d]pyrimidine-4-thiol derivative according to the present invention can be useful for preventing or treating diseases caused by the overactivity of a Janus kinase (JAK).
- -
-
Paragraph 0139-0141
(2017/10/21)
-
- Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer
-
After a high-throughput screening campaign identified thioether 1 as an antagonist of the nuclear androgen receptor, a zone model was developed for structure-activity relationship (SAR) purposes and analogues were synthesized and evaluated in a cell-based luciferase assay. A novel thioether isostere, cyclopropane (1S,2R)-27, showed the desired increased potency and structural properties (stereospecific SAR response, absence of a readily oxidized sulfur atom, low molecular weight, reduced number of flexible bonds and polar surface area, and drug-likeness score) in the prostate-specific antigen luciferase assay in C4-2-PSA-rl cells to qualify as a new lead structure for prostate cancer drug development.
- Johnson, James K.,Skoda, Erin M.,Zhou, Jianhua,Parrinello, Erica,Wang, Dan,O'Malley, Katherine,Eyer, Benjamin R.,Kazancioglu, Mustafa,Eisermann, Kurtis,Johnston, Paul A.,Nelson, Joel B.,Wang, Zhou,Wipf, Peter
-
supporting information
p. 785 - 790
(2016/08/24)
-
- Highly chemoselective aerobic oxidation of amino alcohols into amino carbonyl compounds
-
The direct oxidation of unprotected amino alcohols to their corresponding amino carbonyl compounds has often posed serious challenges in organic synthesis and has constrained chemists to adopting an indirect route, such as a protection/deprotection strategy, to attain their goal. Described herein is a highly chemoselective aerobic oxidation of unprotected amino alcohols to their amino carbonyl compounds in which 2-azaadamantane N-oxyl (AZADO)/copper catalysis is used. The catalytic system developed leads to the alcohol-selective oxidation of various unprotected amino alcohols, carrying a primary, secondary, or tertiary amino group, in good to high yield at ambient temperature with exposure to air, thus offering flexibility in the synthesis of nitrogen-containing compounds. Strong as an ox: The highly chemoselective aerobic oxidation of unprotected amino alcohols to their corresponding amino carbonyl compounds has been achieved by using 2-azaadamantane N-oxyl (AZADO)/copper catalysis. This catalytic system oxidizes not only alcohols with tertiary amino groups but also those with secondary and primary amines in good to high yield at ambient temperature in air. bpy=2,2-bipyridyl, DMAP=4-(N,N-dimethylamino)pyridine.
- Sasano, Yusuke,Nagasawa, Shota,Yamazaki, Mai,Shibuya, Masatoshi,Park, Jaiwook,Iwabuchi, Yoshiharu
-
supporting information
p. 3236 - 3240
(2014/04/03)
-
- Synthesis and pharmacological evaluation of novel 1′-[2- (difluoromethoxy)benzyl]-2′H,5′H-spiro[8-azabicyclo[3.2.1]octane-3, 4′-imidazolidine]-2′,5′-diones and their derivatives
-
A series of novel 1′-[2-(difluoromethoxy)benzyl]-2′H,5′H- spiro[8-azabicyclo[3.2.1]octane-3,4′-imidazolidine]-2′, 5′-dione substituted hydantoins (5-32) were synthesized using an appropriate synthetic route and characterized by elemental analysis and spectral data. The novel molecules were screened for anticonvulsant activity in mice by maximal electroshock (MES) and subcutaneous pentylenetetrazol (ScPTZ)-induced seizure tests. The neurotoxicity was assessed using the rotarod method. Compounds 9, 10, 18, 30, and 31 exhibited anticonvulsant potency against MES seizure and in the ScPTZ model, with lesser neurotoxicity. Some title compounds showed lesser central nervous system depression compared to phenytoin.
- Madaiah, Malavalli,Prashanth, Maralekere K.,Revanasiddappa, Hosakere D.,Veeresh, Bantal
-
p. 370 - 380
(2014/05/20)
-
- Iron-catalyzed oxidative amidation of tertiary amines with aldehydes
-
Unconventional couple: A new oxidative coupling protocol for amide bond formation has been developed (see scheme). The method provides an efficient and practical route for the synthesis of tertiary amides from readily available tertiary amines and aldehydes in the presence of a simple FeCl2 catalyst. Mechanistic studies indicated that a peroxide and an iminium ion act as the reactive intermediates in this oxidative amidation.
- Li, Yuanming,Jia, Fan,Li, Zhiping
-
supporting information
p. 82 - 86
(2013/03/13)
-
- Amide bond formation through iron-catalyzed oxidative amidation of tertiary amines with anhydrides
-
A general and efficient method for amide bond synthesis has been developed. The method allows for synthesis of tertiary amides from readily available tertiary amines and anhydrides in the presence of FeCl2 as catalyst and tert-butyl hydroperoxide in water (T-Hydro) as oxidant. Mechanistic studies indicated that the in situ-generated α-amino peroxide of tertiary amine and iminium ion act as key intermediates in this oxidative transformation.
- Li, Yuanming,Ma, Lina,Jia, Fan,Li, Zhiping
-
p. 5638 - 5646
(2013/07/26)
-
- Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators
-
The metabotropic glutamate receptor subtype 5 has evolved into a promising target for the treatment of various diseases of the central nervous system, such as Fragile X and l-DOPA induced dyskinesia. One of the most advanced clinical compound is Novartis'
- Kubas, Holger,Meyer, Udo,Hechenberger, Mirko,Klein, Kai-Uwe,Plitt, Patrick,Zemribo, Ronalds,Spexgoor, Harm W.,Van Assema, Sander G.A.,Abel, Ulrich
-
supporting information
p. 6370 - 6376
(2013/11/19)
-
- METABOTROPIC GLUTAMATE RECEPTOR MODULATORS
-
The invention relates to heterocyclic derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.
- -
-
Page/Page column 36-37
(2012/12/13)
-
- 8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXAMIDE DERIVATIVE
-
Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R1a and R1b may be the same or different and each independently represents a C1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X1 represents a hydroxyl group or an aminocarbonyl group; Z1 represents a single bond or the like; and R2 represents an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group or the like.)
- -
-
Page/Page column 32
(2012/09/11)
-
- CYCLOHEXANE ANALOGUES AS GPR119 AGONISTS
-
This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.
- -
-
Page/Page column 33
(2012/03/12)
-
- An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: The discovery of N -{(1 S)-1-(3-fluorophenyl)-3-[(3- endo)-3-(5-isobutyryl-2- methyl-4,5,6,7-tetrahydro-1 H -imidazo[4,5- c ]pyridin-1-yl)-8-azabicyclo[3.2.1] oct-8-yl]propyl}acetamide (PF-232798)
-
Preventing entry of HIV into human host cells has emerged as an attractive approach to controlling viral replication. Maraviroc 1 is an approved antagonist of the human CCR5 receptor which prevents the entry of HIV. Herein, we report the design and discovery of a series of imidazopiperidine CCR5 antagonists which retain the attractive antiviral profile and window over hERG activity of maraviroc 1, combined with improved absorption profiles in rat and dog. Furthermore, this series of compounds has been shown to retain activity against a laboratory generated maraviroc-resistant HIV-1 strain, which indicates an alternative resistance profile to that of maraviroc 1. Compound 41f (PF-232798) was selected as a clinical candidate from the imidazopiperidine series and is currently in phase II clinical trials.
- Stupple, Paul A.,Batchelor, David V.,Corless, Martin,Dorr, Patrick K.,Ellis, David,Fenwick, David R.,Galan, Sébastien R. G.,Jones, Rhys M.,Mason, Helen J.,Middleton, Donald S.,Perros, Manos,Perruccio, Francesca,Platts, Michelle Y.,Pryde, David C.,Rodrigues, Deborah,Smith, Nicholas N.,Stephenson, Peter T.,Webster, Robert,Westby, Mike,Wood, Anthony
-
-
- 4-SULFONYLPIPERIDINE DERIVATIVES
-
[PROBLEMS] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [MEANS FOR SOLVING PROBLEMS] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms -CH2-CH2- or the like, or M4 together with M2 or M3 forms -CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one -CH2- or - CH2-CH2- group is formed thereamong.
- -
-
Page/Page column 16
(2010/07/10)
-
- Aryl pyrrolidinyl and piperidinyl ketone derivatives and uses thereof
-
Aryl and heteroaryl ketone compounds substituted with pyrrolidines and piperidines, that modulate serotonin norepinephrine and/or dopamine neurotransmission. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the com
- -
-
Page/Page column 41-42
(2009/12/28)
-
- Secondary Amines as Renin Inhibitors
-
The invention relates to novel secondary amine derivatives of formula (I) and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
- -
-
Page/Page column 28
(2009/07/18)
-
- N-LINKED HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS
-
Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
- -
-
Page/Page column 124-125
(2009/03/07)
-
- Process for preparing an intermediate to opioid receptor antagonists
-
The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1 ]oct-2-en-3-yl)benzamide intermediate in which the amino-prot
- -
-
-
- Anti-tumor and anti-angiogenic activity of novel hydantoin derivatives: Inhibition of VEGF secretion in liver metastatic osteosarcoma cells
-
A series of new azaspiro bicyclic hydantoin derivatives has been designed and synthesized. Initially, the anti-proliferative effect of the hydantoin derivatives was evaluated against human ovarian cancer cells (SKOV-3 and OVSAHO) and murine osteosarcoma c
- Basappa,Ananda Kumar,Nanjunda Swamy,Sugahara, Kazuyuki,Rangappa, Kanchugarakoppal S.
-
experimental part
p. 4928 - 4934
(2009/12/03)
-
- Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol
-
Discovering dopamine D2-like receptor subtype-selective ligands has been a focus of significant investigation. The D2R-selective antagonist 3-[4-(4-chlorophenyl)-4-hydroxypiperidinyl]methylindole (1, L741,626; K i(D2R/D3R) = 11.2:163 nM) has previously provided a lead template for chemical modification. Herein, analogues have been synthesized where the piperidine was replaced by a tropane ring that reversed the selectivity seen in the parent compound, in human hD2LR- or hD3R-transfected HEK 293 cells (31, Ki(D2R/D3R) = 33.4: 15.5 nM). Further exploration of both N-substituted and aryl ring-substituted analogues resulted in the discovery of several high affinity D2R/D3R ligands with 3-benzofurylmethyl-substituents (e.g., 45, Ki(D2R/D3R) = 1.7:0.34 nM) that induced high affinity not achieved in similarly N-substituted piperidine analogues and significantly (470-fold) improved D3R binding affinity compared to the parent ligand 1. X-ray crystallographic data revealed a distinctive spatial arrangement of pharmacophoric elements in the piperidinol vs tropine analogues, providing clues for the diversity in SAR at the D2 and D3 receptor subtypes.
- Paul, Noel M.,Taylor, Michelle,Kumar, Rakesh,Deschamps, Jeffrey R.,Luedtke, Robert R.,Newman, Amy Hauck
-
body text
p. 6095 - 6109
(2009/10/01)
-
- NOVEL COMPOUNDS
-
Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
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Page/Page column 68
(2008/12/08)
-
- Prokinetic agent for bowel preparation
-
The invention provides methods of bowel preparation before a diagnostic, surgical or therapeutic procedure, in particular, bowel preparation before a colonoscopy procedure, using a 5-HT4 receptor agonist as a prokinetic agent.
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-
- Heteroaryl pyrrolidinyl and piperidinyl ketone derivatives and uses thereof
-
Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of pre
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Page/Page column 114-115
(2008/12/06)
-
- SECONDARY AMINES AS RENIN INHIBITORS
-
The invention relates to novel secondary amine derivatives of formula (I) and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
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Page/Page column 75-76
(2010/11/28)
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- Chemical compounds
-
Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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Page/Page column 45
(2008/06/13)
-
- CARBAMATE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS
-
The invention provides novel benzoimidazolone-carboxamide-derived carbamate 5-HT4 receptor agonist compounds of formula (I): wherein R1, R2, R3, R4, a, and b are defined in the disclosure. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 7; 16
(2008/06/13)
-
- Quinolinone-carboxamide compounds
-
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 18
(2008/06/13)
-
- Indazole-carboxamide compounds
-
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 23
(2008/06/13)
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- 5-HT4 receptor agonist compounds
-
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 21
(2008/06/13)
-
- Quinolinone compounds as 5-HT4 receptor agonists
-
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 23
(2008/06/13)
-
- Benzoimidazolone-carboxamide compounds as 5-HT4 receptors agonists
-
The invention provides novel benzoimidazolone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 19
(2010/11/25)
-
- CYCLOALKANOPYRIDINE DERIVATIVE
-
Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.
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- BICYCLIC FIVE-MEMBERED HETEROARYL DERIVATIVES AND THEIR USE AS RENIN INHIBITORS
-
The invention relates to novel five-membered heteroaryl derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions comprising one or more of those compounds and especially their use as inhibitors of renin.
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Page/Page column 28-29
(2010/11/23)
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- Crystalline form of an indazole-carboxamide compound
-
The invention provides crystalline halide salts of 1-isopropyl-1H-indazole-3-carboxylic acid {(1S,3R,5R)-8-[2-(4-acetylpiperazin-1-yl)ethyl]-8-azabicyclo[3.2.1]oct-3-yl}amide and solvates thereof. The invention also provides pharmaceutical compositions comprising such salts, methods of using such crystalline salts to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salts.
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Page/Page column 9-10
(2008/06/13)
-
- Crystalline form of a quinolinone-carboxamide compound
-
The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
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Page/Page column 9
(2010/11/24)
-
- PIPERAZINO DERIVATIVES AS NEUROKININ ANTAGONISTS
-
The invention relates to compounds of formula (I) wherein Z, Rc, y, m, u, Ar2, n, X, Rc', l and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
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Page/Page column 65
(2010/11/08)
-
- INDAZOLE-CARBOXAMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS
-
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 39
(2010/02/13)
-
- Quinolinone-carboxamide compounds as 5-HT4 receptor agonists
-
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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Page/Page column 16
(2008/06/13)
-
- Chemical compounds
-
The present invention provides compounds of formula (I) wherein R1 and R2 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
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Page/Page column 17-18
(2010/02/13)
-
- IMIDAZOPYRIDINE SUBSTITUTED TROPANE DERIVATIVES WITH CCR5 RECEPTOR ANTAGONIST ACTIVITY FOR THE TREATMENT OF HIV AND INFLAMMATION
-
The present invention provides compounds of formula (I) wherein R1 and R2 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
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Page/Page column 38
(2010/02/11)
-
- Bridged bicyclic amine derivatives useful as CCR-3 receptor antagonists
-
Compounds having the formula (I), Ar—(F)(E)-(CR3R4)—(CHR5)m-(T)-(Q)-Ar1, are useful as CCR-3 receptor antagonists, wherein T is a bridged heterocyclyl group having one N atom and a bridge of one to two bridgehead carbon atoms; Ar and Ar1 are aryl or heteroaryl; F is alkylene, alkenylene, or a bond; E is —C(═O)N(R10)—, —SO2N(R10)—, —N(R11)C(═O)N(R10O)—, —N(R11)SO2N(R10)—, —N(R11)C(═S)N(R10)—, —N(R11)C(═O)—, —N(R11)SO2—, —N(R12)C(═O)CH(R13)—, or CH(R13)C(═O)N(R12)—; Q is —C(═O)— or C1-2alkylene; and R3, R4, R5, R9, R10, R11, R12, and R13 are defined as set forth in the specification.
- -
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Page/Page column 9; 11
(2010/02/08)
-
- Tropane derivatives useful in therapy
-
The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
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