5096-73-1Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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Paragraph 0370; 0379-0384, (2021/06/26)
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.
Piperazine derivatives and their use as therapeutic agents
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Paragraph 0103, (2016/03/19)
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.
6-methoxy diazine-3-carboxylic acid synthesis process
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Paragraph 0010, (2016/12/01)
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.
1 -(PYRIDAZIN-3-YL)-IMIDAZOLIDIN-2-ONE DERIVATIVES AS HERBICIDES
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Page/Page column 44, (2015/05/26)
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
SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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Page/Page column 78, (2013/05/09)
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.
AMIDE DERIVATIVE
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Page/Page column 45, (2012/02/05)
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.
Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors
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
scheme or table, p. 479 - 483 (2011/02/28)
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
Organic compounds
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Page/Page column 29, (2009/05/29)
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.
Heterocyclic Derivatives and Their Use as Strearoyl-Coa Desaturase Inhibitors
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Page/Page column 15, (2008/12/05)
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.
Pyridazine Derivatives for Inhibiting Human Stearoyl-Coa-Desaturase
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Page/Page column 14, (2008/12/08)
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,
