- COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.
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Paragraph 0370; 0379-0384
(2021/06/26)
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- Piperazine derivatives and their use as therapeutic agents
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Compounds for treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the compounds are of formula (I): where x y, W, V, R 2 , R 3 , R 4 , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , R 8a , R 9 and R 9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
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Paragraph 0103
(2016/03/19)
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- 6-methoxy diazine-3-carboxylic acid synthesis process
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The present invention discloses a 6-methoxy diazine-3-carboxylic acid synthesis process, which comprises: 1) under ice bath, adding 3-chloro-6-methyl diazine to sulfuric acid, adding an oxidizing agent under stirring, carrying out a reaction at a temperature of 50-90 DEG C, cooling, adding ice water, diluting, extracting, combining the extraction liquid, drying, carrying out pressure reducing to achieve a dried state, and re-crystallizing the residue to obtain 6-chloro diazine-3-carboxylic acid; and 2) adding sodium methoxide and the 6-chloro diazine-3-carboxylic acid to the solvent in a stirring manner, carrying out a reflux reaction on the system, carrying out pressure reducing on the reaction liquid to remove the excess solvent, adding ice water, adjusting the pH value with concentrated hydrochloric acid, standing overnight, filtering, and re-crystallizing the filter cake by using water to obtain the 6-methoxy diazine-3-carboxylic acid. According to the present invention, the starting raw material is changed, is subjected to the domestic industrial production, and is easy to obtain, the synthetic steps are reduced, the operation process is reduced, and the 6-methoxy diazine-3-carboxylic acid synthesis is suitable for industrial production.
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Paragraph 0010
(2016/12/01)
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- 1 -(PYRIDAZIN-3-YL)-IMIDAZOLIDIN-2-ONE DERIVATIVES AS HERBICIDES
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The invention relates to pyrrolone compounds of the formula (I) wherein R1, R2, R3, Rb, Rc and Rd are as defined in the specification. Furthermore, the present invention relates to processe
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Page/Page column 44
(2015/05/26)
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- SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided, are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Page/Page column 78
(2013/05/09)
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- AMIDE DERIVATIVE
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The present invention relates to a compound or a pharmacologically acceptable salt thereof that has an excellent antagonistic effect on a neurokinin NK1 receptor, a neurokinin NK2 receptor, and a muscarine M3 receptor and is useful as a therapeutic agent for bronchial asthma, chronic obstructive pulmonary disease, or the like. A compound represented by general formula (I): [wherein R1 represents a hydrogen atom, a C1-C6 alkyl group, or the like; R2 represents a hydrogen atom, a C1-C6 alkyl group, or the like; R3 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group A, or the like; R4 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group A, or the like; L1 represents a C1-C10 alkylene group or the like; L2 represents a carbonyl group, a group represneted by the formula -N(R5)-C(=O)-, a group represented by the formula -C(=O)-N(R5)-, or the like; R5 represents a hydrogen atom, a C1-C6 alkyl group, or the like; E represents a phenylene group that may be substituted with 1 to 4 group(s) independently selected from Substituent Group A, or the like; m is an integer of 1 to 4; n is an integer of 0 to 4; p is an integer of 0 to 2; q is an integer of 1 to 10; r is 1 or 2; s is 0 or 1; and Substituent Group A represents the group consisting of a halogen atom, a C1-C6 alkyl group, C1-C6 halogenated alkyl group, or the like] or a pharmacologically acceptable salt thereof.
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Page/Page column 45
(2012/02/05)
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- Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors
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Potent and orally bioavailable SCD inhibitors built on an azetidinyl pyridazine scaffold were identified. In a one-month gDIO mouse model of obesity, we demonstrated that there was no therapeutic index even at low doses; efficacy in preventing weight gain
- Isabel, Elise,Powell, David A.,Black, W. Cameron,Chan, Chi-Chung,Crane, Sheldon,Gordon, Robert,Guay, Jocelyne,Guiral, Sebastien,Huang, Zheng,Robichaud, Jo?l,Skorey, Kathryn,Tawa, Paul,Xu, Lijing,Zhang, Lei,Oballa, Renata
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scheme or table
p. 479 - 483
(2011/02/28)
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- Organic compounds
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The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the formula (I): in which the substitutents are as defined in claim 1 and salts, solvates, hydrates and N-oxides thereof.
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Page/Page column 29
(2009/05/29)
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- Pyridazine Derivatives for Inhibiting Human Stearoyl-Coa-Desaturase
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Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a,
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Page/Page column 15
(2008/12/08)
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- Heterocyclic Derivatives and Their Use as Strearoyl-Coa Desaturase Inhibitors
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Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, W, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
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Page/Page column 15
(2008/12/05)
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- NICOTINIC ACID DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
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The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the Formula (I): in which the substitutents are as defined in claim 1 and and salts, solvates, hydrates and N- oxides thereof.
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Page/Page column 66
(2008/12/08)
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- HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
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Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and
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Page/Page column 42-43
(2008/06/13)
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- HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
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Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and
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Page/Page column 34
(2008/06/13)
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- AZETIDINE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
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Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)
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Page/Page column 36
(2008/06/13)
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- NEW COMPOUNDS
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The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
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Page 148-149
(2010/02/06)
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- Amide derivative
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A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1is hydogen atom, optionally substituted alkyl, etc.; R2and R3are independently optionally substituted alkyl, etc.; R4and R5are independently hydrogen atom or optionally substituted alkyl; R6is hydrogen atom, hydroxy or alkyl; or a pharmaceutically acceptable salt thereof is useful as a medicament for treating retinal degenerative disorders and the like.
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