- Preparation, use, and safety of 0-mesitylenesulfonylhydroxylamine
-
The aminating reagent O-mesitylsulfonylhydroxylamine (MSH) has a known potential hazard since it contains high-energy functional groups in its structure. There are references in the literature that report several incidents involving the use of pure and crystalline MSH. The preparation and safe use of this reagent at kilo scale are described herein.
- Mendiola, Javier,Rincon, Juan A.,Mateos, Carlos,Soriano, Jose Francisco,De Frutos, Oscar,Niemeier, Jeffry K.,Davis, Edward M.
-
-
Read Online
- SUBSTITUTED 1,5-NAPHTHYRIDINES OR QUINOLINES AS ALK5 INHIBITORS
-
The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
- -
-
Paragraph 226; 254; 258
(2021/05/29)
-
- N-(4-FLUOROPHENYL)-5-PHENYL-[1,2,4] TRIAZOLO [1,5-A] PYRIDINE-2-CARBOXAMIDE DERIVATIVES AND THEIR SYNTHESIS THEREOF
-
The present invention relates to the development of novel N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for their different pharmacological activities. It particularly relates to the development of N-(4-fluorophenyl)-5-phenyl- [1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives as antiviral, anticancer, antifungal, hypoglycemic, anti-tubercular, sedative, anti-type 2 diabetes activity. It specifically relates to the N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives for treatment of H37Rv and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). The present invention also relates to the process for synthesis of N-(4-fluorophenyl)- 5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives. The invention further relates to method for treatment of method for treatment of diseases such as tuberculosis, type 2 diabetes, bacterial, viral and fungal infections. Invention addresses the challenges in working with chemical processes and products by inventing novel reaction methodology that can maximize the desired products and minimize by-products, designing new synthetic schemes that can simplify operations in chemical productions and seeking nontoxic reagent that are inherently environmentally and ecologically benign. Synthesis of novel N-(4- fluorophenyl)-5-phenyl-[1,2,4]triazolo[1,5-a]pyridine-2-carboxamide derivatives is being employed to develop a novel synthetic methodology and their pharmacological applications. Novel series of N-(4-fluorophenyl)-5-phenyl-[1,2,4]triazolo[l,5-a]pyridine-2-carboxamide derivatives were designed synthesized evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of mycobacterium tuberculosis (MTB). All the synthesized compounds were characterized by spectroscopic methods like Mass, NMR and elemental analysis.
- -
-
Page/Page column 9; 15
(2021/08/20)
-
- Pyrimidine-4 (3H)-ketone heterocyclic compound, preparation method thereof and application of pyrimidine-4 (3H)-ketone heterocyclic compound in medicine
-
The invention relates to pyrimidine-4 (3H)-ketone heterocyclic compounds suitable for inhibiting or regulating SHP2, a preparation method of the pyrimidine-4 (3H)-ketone heterocyclic compounds and application of the pyrimidine-4 (3H)-ketone heterocyclic compounds in medicine. Specifically, the invention relates to a compound as shown in a general formula (I) and a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, a method for treating and/or preventing related diseases mediated by SHP2, especially cancers by using the compound or the pharmaceutically acceptable salt thereof, and a preparation method of the compound or the pharmaceutically acceptable salt thereof. The invention also relates to application of the compound or the pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof in preparation of drugs for treating and/or preventing SHP2-mediated related diseases. Wherein each substituent in the general formula (I) is as defined in the specification.
- -
-
Paragraph 0280-0282; 0284-0287
(2021/07/21)
-
- PYRIMIDINYL GROUP-CONTAINING TRICYCLIC COMPOUND SERVING AS C-MET INHIBITOR
-
Disclosed are a pyrimidinyl group-containing tricyclic compound and applications thereof in preparing a cancer-treating medicament. Specifically disclosed are a compound as represented by formula (I), a pharmaceutically acceptable salt of same, or an isomer thereof.
- -
-
Paragraph 0427-0429
(2021/12/18)
-
- AROMATIC RING DERIVATIVE AS IMMUNOREGULATION AND PREPARATION METHOD AND APPLICATION OF AROMATIC RING DERIVATIVE
-
Relating to a compound represented by formula (I) and a pharmaceutically acceptable salt of the compound, and an application of the compound as an S1P1 agonist.
- -
-
Paragraph 0137-0138
(2021/10/15)
-
- Pyrazole formaldoxime ether compound as well as preparation method and application thereof
-
The invention discloses a pyrazole formaldoxime ether compound as well as a preparation method and application thereof. The structural formula of the pyrazole formaldoxime ether compound is shown as the following formula I shown in the specification, wherein in the formula I, R1 represents at least one of hydrogen, C1-C6 alkyl, C1-C6 alkyl monosubstituted by halogen and C1-C6 alkyl polysubstitutedby halogen; R2 represents at least one of hydrogen, C1-C6 alkyl, C1-C6 alkyl monosubstituted or polysubstituted by halogen, aryl and substituted aryl; R3 represents at least one of phenyl, benzyl, substituted benzyl, substituted phenyl, an unsubstituted nitrogen and/or oxygen-containing heterocyclic group, a substituted nitrogen and/or oxygen-containing heterocyclic group, an unsubstituted C3-C8cycloalkyl group and a substituted C3-C8 cycloalkyl group. The pyrazole formaldoxime ether compound takes oxime ether as a main skeleton structure, is simple in preparation method, can be used for efficiently preventing and treating fungal diseases and oomycete diseases of farmland crops, and can be used for disease resistance management.
- -
-
Paragraph 0051-0053
(2020/09/09)
-
- Direct synthesis of secondary amides from ketones through Beckmann rearrangement using O-(mesitylsulfonyl)hydroxylamine
-
The Beckmann rearrangement is a versatile method for the preparation of secondary amides from ketones via oxime intermediates and has been widely used in the synthesis of bioactive natural products and pharmaceuticals. Herein, we have developed a highly efficient direct method for the preparation of secondary amides and lactams from ketones using O-(mesitylsulfonyl)hydroxylamine (MSH). The reactions proceed rapidly at room temperature under mild condition without requiring any additive, and tolerate multiple functional groups. A simple aqueous work-up often furnished the products in excellent yield with high purity.
- Chandra, Dinesh,Verma, Saumya,Pandey, Chandra Bhan,Yadav, Ajay K.,Kumar, Puneet,Tiwari, Bhoopendra,Jat, Jawahar L.
-
supporting information
(2020/03/23)
-
- Substituted pyrazole fused ring derivative as well as preparation method and application thereof
-
The invention relates to the field of medicinal chemistry, and mainly relates to a compound represented by a formula I, a stereoisomer, a despinner, a tautomer, an isotope marker, NOx or a pharmaceutically acceptable salt thereof, a preparation method of the compound, and an application of the compound in preparation of a medicine for treating RET kinase mediated diseases.
- -
-
Paragraph 0185-0190
(2020/04/17)
-
- FUSED PYRAZINE DERIVATIVES AS A2A / A2B INHIBITORS
-
This application relates to compounds of Formula (I) or pharmaceutically acceptable salts thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.
- -
-
Page/Page column 129
(2020/01/31)
-
- INHIBITORS OF CGAS FOR TREATING AUTOINFLAMMATORY DISEASES AND CANCER METASTASIS
-
Tri-cyclyl nitrogen-containing heterocyclic compounds are disclosed. The compounds are inhibitors of human cGAS in interferon-producing cell types. They are thus useful as therapeutic agents for treating cGAS-related autoimmune diseases in humans.
- -
-
Paragraph 0216
(2020/09/30)
-
- INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX KINASE ("NACK") AND METHODS FOR USE OF THE SAME
-
Disclosed herein are Notch transcriptional activation complex kinase ("NACK") inhibitors, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein include compounds of Formula (la) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
- -
-
Paragraph 00152
(2019/08/29)
-
- Synthesis of pyrazol [1,5-alpha] pyridine-3-carboxylic acid derivatives
-
The invention relates to synthesis of pyrazol [1,5-alpha] pyridine-3-carboxylic acid derivatives, and belongs to the field of organic synthesis. Trimethylsulfonyl chloride is used as a raw material toreact with tert-butoxycarbonyl hydroxylamine to obtain a compound 3; then the compound 3 reacts with trifluoroacetic acid to obtain a mixed solution of a compound 4; the mixed solution directly reacts with pyrazine to obtain a compound 6 without carrying out separation, washing and drying; an ethyl propiolate reaction is continuously performed; a water phase obtained after the reaction is extracted by ethyl acetate; an organic extract obtained after extraction is dried by anhydrous MgSO4 and evaporated; remaining residues are subjected to recrystallization (ethyl acetate, methylbenzene or petroleum ether), separation, washing and drying to obtain a compound 8; the compound 8 further reacts with NaOH to obtain a compound 9. In the route, the second step and the third step are continuouslycarried out, so that not only is the risk of the process reduced, but also yield is over 70%. No matter whether the raw material is of a symmetrical structure, the target product can be accurately obtained. The synthesis is suitable for industrial production.
- -
-
Paragraph 0008; 0043; 0045; 0046; 0047; 0048; 0049
(2019/02/04)
-
- SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
-
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
- -
-
Paragraph 000474; 000484; 000577; 000615; 000685
(2019/06/05)
-
- FORMULATIONS COMPRISING 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZAB ICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE
-
6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.
- -
-
Page/Page column 303
(2019/05/06)
-
- CRYSTALLINE FORMS
-
Provided herein are compound of Formula I-IV and pharmaceutically acceptable salts thereof which exhibit rearranged during transfection (RET) kinase inhibition. In particular, provided herein are novel crystalline forms of 4-(6-(4-((6-methoxypyridin-3-yl)methyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula I), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula II), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-(6-methoxynicotinoyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula III), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(4-hydroxy-4-(pyridin-2-ylmethyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula IV), and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds, processes for making the compounds, and the use of the compounds in therapy. More particularly, the application relates to novel crystalline forms of Formula I-IV and pharmaceutically acceptable salts thereof useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
- -
-
Paragraph 00587
(2019/05/02)
-
- 3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR
-
The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
- -
-
Page/Page column 48
(2019/01/16)
-
- INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
-
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
- -
-
-
- HETEROAROMATIC COMPOUNDS HAVING ACTIVITY AGAINST RSV
-
The invention concerns compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.
- -
-
Page/Page column 24
(2019/11/12)
-
- 1-Aminopyridinium Ylides as Monodentate Directing Groups for sp3 C-H Bond Functionalization
-
1-Aminopyridinium ylides are efficient directing groups for palladium-catalyzed β-arylation and alkylation of sp3 C-H bonds in carboxylic acid derivatives. The efficiency of these directing groups depends on the substitution at the pyridine moiety. The unsubstituted pyridine-derived ylides allow functionalization of primary C-H bonds, while methylene groups are unreactive in the absence of external ligands. 4-Pyrrolidinopyridine-containing ylides are capable of C-H functionalization in acyclic methylene groups in the absence of external ligands, thus rivaling the efficiency of the aminoquinoline directing group. Preliminary mechanistic studies have been performed. A cyclopalladated intermediate has been isolated and characterized by X-ray crystallography, and its reactivity was studied.
- Le, Ky Khac Anh,Nguyen, Hanh,Daugulis, Olafs
-
supporting information
p. 14728 - 14735
(2019/10/11)
-
- SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS
-
Provided herein are compounds of the Formula I and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
- -
-
Paragraph 00802; 00803
(2018/04/27)
-
- SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS
-
Provided herein are compounds of the Formula I: (I) or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
- -
-
Paragraph 00929; 00932
(2018/04/27)
-
- SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
-
Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.
- -
-
Paragraph 00882
(2018/08/20)
-
- Rhodium(III)-Catalyzed Redox-Neutral Cascade [3 + 2] Annulation of N-Phenoxyacetamides with Propiolates via C-H Functionalization/Isomerization/Lactonization
-
A Rh(III)-catalyzed cascade [3 + 2] annulation of N-phenoxyacetamides with propiolates under mild conditions using the internal oxidative O-N bond as the directing group has been achieved. This catalytic system provides a regio- and stereoselective access to benzofuran-2(3H)-ones bearing exocyclic enamino motifs with exclusive Z configuration selectivity, acceptable to good yields and good functional group compatibility. Mechanistic investigations by experimental and density functional theory studies suggest that a consecutive process of C-H functionalization/isomerization/lactonization is likely to be involved in the reaction.
- Pan, Jin-Long,Chen, Chao,Hao, Yu,Liu, Chang,Bai, He-Yuan,Ding, Jun,Zhang, Shu-Yu,Wang, Li-Ren,Xie, Peipei,Xia, Yuanzhi
-
supporting information
p. 7131 - 7136
(2018/12/14)
-
- SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS
-
Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.
- -
-
Paragraph 00687; 00688; 00689
(2017/02/09)
-
- ISOPROPYL TRIAZOLO PYRIDINE COMPOUNDS
-
The present invention provides a compound of the Formula (I) below: Wherein R1 is selected from the group consisting of H, CH3, CN, CH2CN, C(CH3)2CN, and F; R2 is selected from the group consisting of H, O(C1-C3alkyl)R5, CH2CN, and CN; R3 is selected from the group consisting of H, OCH3, CN, C(CH3)2CN, and CH2CN; R4 is selected from the group consisting of H and CH3; R5 is selected from the group consisting of H, CN, C(CH3)2CN, OCH3, S(O)2CH3, and C(CH3)2OH; provided that at least one selected from the group consisting of R1, R2, R3 and R4 is H; or a pharmaceutically acceptable salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.
- -
-
Paragraph 0052-0053
(2016/12/01)
-
- TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
-
The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
- -
-
Page/Page column 58
(2016/10/31)
-
- PYRAZOLOPYRIDINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
-
A series of substituted pyrazolo[1,5-a]pyridine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
- -
-
Page/Page column 81
(2015/06/25)
-
- ISOPROPYL TRIAZOLO PYRIDINE COMPOUNDS
-
The present invention provides a compound of the Formula (I) below: Wherein R1 is selected from the group consisting of H, CH3, CN, CH2CN, C(CH3)2CN, and F; R2 is selected from the group consisting of H, O(C1-C3alkyl)R5, CH2CN, and CN; R3 is selected from the group consisting of H, OCH3, CN, C(CH3)2CN, and CH2CN; R4 is selected from the group consisting of H and CH3; R5 is selected from the group consisting of H, CN, C(CH3)2CN, OCH3, S(O)2CH3, and C(CH3)2OH; provided that at least one selected from the group consisting of R1, R2, R3 and R4 is H; or a pharmaceutically acceptable salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.
- -
-
Page/Page column 14
(2015/07/23)
-
- HETEROARYLS AND USES THEREOF
-
The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
- -
-
Paragraph 00240
(2015/08/03)
-
- HETEROARYLS AND USES THEREOF
-
The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
- -
-
Paragraph 0328-0329
(2015/09/22)
-
- BENZENE SULFONAMIDES AS CCR9 INHIBITORS
-
The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).
- -
-
Page/Page column 102
(2015/07/15)
-
- 8 - SUBSTITUTED 2 -AMINO - [1,2,4] TRIAZOLO [1, 5 -A] PYRAZINES AS SYK TRYROSINE KINASE INHIBITORS AND GCN2 SERIN KINASE INHIBITORS
-
Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and / or systemic lupus
- -
-
Page/Page column 80; 81
(2013/09/12)
-
- TRIAZOLOPYRAZINE DERIVATIVES
-
Compounds of the formula (I) in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
- -
-
Page/Page column 95; 96
(2013/09/26)
-
- TRIAZOLOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
-
This invention relates to triazolopyridyl compounds of the structural formula: [Formula should be inserted here] or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
- -
-
Page/Page column 38
(2013/04/10)
-
- COMPOUNDS
-
The present invention features compounds of formula (I): and salts thereof, pharmaceutical compositions comprising said compounds, and uses of such compounds in treating or preventing viral infections, such as HCV infections, and diseases associated with such infections.
- -
-
Page/Page column 42-43
(2012/06/01)
-
- TRIAZOLOPYRAZINE DERIVATIVES
-
Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment rheumatoid arthritis
- -
-
Page/Page column 70
(2012/03/26)
-
- HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
-
Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
- -
-
Page/Page column 41
(2012/07/27)
-
- Osmium-catalyzed vicinal oxyamination of alkenes by N-(4- toluenesulfonyloxy)carbamates
-
N-(4-Toluenesulfonyloxy)carbamates based on a range of common amine protecting groups serve as preformed nitrogen sources in the intermolecular osmium-catalyzed oxyamination reaction of a variety of mono-, di-, and trisubstituted alkenes. The reactions occur with low catalyst loadings and good yields and afford high regioselectivity for unsymmetrically substituted alkenes.
- Masruri,Willis, Anthony C.,McLeod, Malcolm D.
-
p. 8480 - 8491
(2012/11/13)
-
- HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
-
Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes
- -
-
Page/Page column 121
(2011/12/14)
-
- Synthesis, larvicidal activity, and SAR studies of new benzoylphenylureas containing oxime ether and oxime ester group
-
A series of new structural benzoylphenylureas (BPUs) containing oxime ether and oxime ester group were designed and synthesized. The larvicidal activities against Oriental armyworm and mosquito of these benzoylphenylureas were evaluated and the result of bioassay displayed specific structure-activity relationship (SAR). Most of the compounds exhibited excellent larvicidal activities against Oriental armyworm and mosquito. Interestingly, some compounds showed different structure-activity relationship towards diamondback moth, beet armyworm, and corn borer although three tested insects all belong to the same insect order.
- Sun, Ranfeng,Li, Yongqiang,Lue, Maoyun,Xiong, Lixia,Wang, Qingmin
-
scheme or table
p. 4693 - 4699
(2010/10/02)
-
- Design, synthesis, bioactivity, and structure-activity relationship (SAR) studies of novel benzoylphenylureas containing oxime ether group
-
Novel benzoylphenylureas containing an oxime ether group were designed and synthesized by four schemes. These benzoylphenylureas were identified by 1H NMR spectroscopy and element analysis (or HRMS). The bioactivities of the new compounds were evaluated. These benzoylphenylureas exhibited excellent larvicidal activities against oriental armyworm, some of which were much better in comparison with the commercial Flucycloxuron. In particular, the larvicidal activities against oriental armyworm of compounds 1 and 23 were 5-10 times better than that of Flucycloxuron. Most of these benzoylphenyureas exhibited excellent larvicidal activities against mosquito. At the same time, some of these compounds have good plant growth regulatory activities as well.
- Sun, Ranfeng,Lue, Maoyun,Chen, Li,Li, Qingshan,Song, Haibin,Bi, Fuchun,Huang, Runqiu,Wang, Qingmin
-
scheme or table
p. 11376 - 11391
(2010/04/02)
-
- Herbicidal 3-(bicyclic nitrogen-containing heterocycle)-substituted-1-methyl-6-trifluoromethyluracils
-
Herbicidal 3-(bicyclic nitrogen-containing heterocycle)-substituted-1-methyl-6-trifluoromethyluracils, compositions containing them, and methods of using them to control undesired plant growth are disclosed. The herbicidal compounds of the present invention are defined by the following generic structure: STR1 in which V is N or C--R1 ; R is hydrogen, straight or branched chain alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, alkoxycarbonylalkyl, arylalkyl, optionally substituted with halogen, or aminocarbonylalkyl in which the amino nitrogen is substituted with arylalkyl or one or two alkyl; R1 is hydrogen, alkyl, haloalkyl, or cyano; R2 is lower alkyl or amino; and X is hydrogen or halogen, with the proviso that each aliphatic component has not more than six carbon atoms.
- -
-
-
- 3-(benzofuran-7-yl)-6-haloalkyluracils
-
Herbicidal 3-(benzofuran-7-yl)-6-haloalkyluracils of the formula STR1 in which M is fluoroalkyl (C1-6); D is hydrogen, alkyl (C1-6), or alkoxy(C1-6)-carbonyl; E is hydrogen or alkyl (C1-6), or D and E taken together are --CH2 CH2 --; R is hydrogen, amino, alkyl (C1-6), 2-alkenyl (C3-6), 2-alkynyl (C3-6), alkoxy(C1-6)methyl, benzyl, amino, fluoroalkyl (C1-6), alkoxy (C1-6)-carbonylmethyl; or cyanoalkyl (C1-6) having preferably one cyano group; X is hydrogen, fluorine, chlorine, bromine, cyano, alkyl(C1-6), haloalkyl(C1-6), haloalkoxy(C1-6), or alkoxy(C1-6); Y is hydrogen, alkyl (C1-6), fluorine, chlorine, or bromine; and Z is CH2, C=O, C=S, --CH(OH)--, --CH2 CH2 --, --CH=CH--, --(C=O)CH2 --; or C=N--O--R' wherein R' is alkyl(C1-6).
- -
-
-
- Compositions of retinoids substituted with a dithiane ring, their use, and process for preparing the compounds
-
The invention relates to a stereospecific derivative of formula: STR1 in which R is hydrogen or a C 1 -C 4 thioalkyl. The invention also relates to the use of these compounds for the manufacture of stereospecific retinal or retinoic acid, as well as to a process for preparing the retinoids of formula (I). The invention finally relates to a cosmetic or pharmaceutcial composition which contains at least one compound of formula (I) in a suitable vehicle; the pharmaceutical composition according to the invention may be used for treating dermatological, rheumatic, respiratory or ophthalmological conditions.
- -
-
-