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公开(公告)号:US20230150951A1
公开(公告)日:2023-05-18
申请号:US17909589
申请日:2021-03-08
申请人: OM PHARMA SA
发明人: Jacques BAUER , Olivier MARTIN
IPC分类号: C07D251/20 , C07C235/64 , C07C229/38 , C07C233/51 , C07C275/42 , C07C309/51 , C07C317/46 , C07D235/18
CPC分类号: C07D251/20 , C07C235/64 , C07C229/38 , C07C233/51 , C07C275/42 , C07C309/51 , C07C317/46 , C07D235/18
摘要: The present invention provides novel hydroquinone derivatives of formula (I), processes of preparation, as well as pharmaceutical compositions and methods of treating and/or preventing e.g. autoimmune, immunological, rheumatology, vascular disorders, ophthalmologic disorders, fibrotic disorders, metabolic and gastrointestinal disorders, neuroinflammatory and neurodegenerative diseases, neoplasms and cancer associated disorders, hormone related diseases and immunological disorders resulting from viral and bacterial infectious diseases and complications thereof. wherein R1 is COOR4, (CH2)nCOOR4, SO3H, (CH2)nSO3H or CONH—R10; one of R2 and R3 is H and the other is R5.
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公开(公告)号:US20230002326A1
公开(公告)日:2023-01-05
申请号:US17582851
申请日:2022-01-24
IPC分类号: C07D231/16 , A61K31/4192 , A61K9/00 , A61K45/06 , C07D207/34 , A61K31/40 , C07D233/68 , A61K31/4164 , C07D207/06 , C07D295/15 , A61K31/5375 , C07D249/08 , A61K31/4196 , C07D213/84 , A61K31/44 , C07D239/74 , A61K31/517 , C07C255/60 , A61K31/277 , C07D401/12 , A61K31/4439 , C07D249/04 , A61K31/415 , C07C317/46 , C07D209/08
摘要: This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
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公开(公告)号:US11161809B2
公开(公告)日:2021-11-02
申请号:US16854143
申请日:2020-04-21
发明人: Weiming Xu , Wanmei Li , Lianzhi Tao , Pengfei Zhang , Hongyun Shen , Dongxiang Feng
IPC分类号: C07C315/02 , C07C253/22 , C07C317/46 , C07C255/35
摘要: The disclosure provides processes for preparing 5-fluoro-2-methyl-1-(4-methylthiobenzylidene)-3-indanacetonitrile and for preparing sulindac, relating to the field of medicine. The former comprises mixing 6-fluoro-2-methyl-1-indanone, cyanoacetic acid, a first organic solvent and an acetic acid-based catalyst to proceed with a first condensation reaction to give a first condensation reaction solution, which contains 5-fluoro-2-methyl-3-indanacetonitrile; and mixing the first condensation reaction solution, per se, with a base, a second organic solvent and 4-(methylthio)benzaldehyde to proceed with a second condensation reaction to give 5-fluoro-2-methyl-1-(4-methylthiobenzylidene)-3-indanacetonitrile. The process is a one-pot process without separation of 5-fluoro-2-methyl-3-indanacetonitrile from the solvent, shortening the synthetic route, simplifying the preparation process and improving the 5-fluoro-2-methyl-1-(4-methylthiobenzylidene)-3-indanacetonitrile yield.
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公开(公告)号:US20200299243A1
公开(公告)日:2020-09-24
申请号:US16783161
申请日:2020-02-05
IPC分类号: C07D231/16 , A61K31/4192 , A61K9/00 , A61K45/06 , C07D207/34 , A61K31/40 , C07D233/68 , A61K31/4164 , C07D207/06 , C07D295/15 , A61K31/5375 , C07D249/08 , A61K31/4196 , C07D213/84 , A61K31/44 , C07D239/74 , A61K31/517 , C07C255/60 , A61K31/277 , C07D401/12 , A61K31/4439 , C07D249/04 , A61K31/415 , C07C317/46 , C07D209/08
摘要: This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
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公开(公告)号:US10597366B2
公开(公告)日:2020-03-24
申请号:US16164653
申请日:2018-10-18
发明人: Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: C07B39/00 , C07C43/295 , A61K31/09 , C07D213/85 , C07C43/285 , C07C43/205 , C07C43/263 , C07C43/23 , C07C43/225 , A61K31/10 , C07C255/54 , C07C255/56 , C07C205/22 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07D213/89 , C07D231/56 , C07D213/65 , C07C311/29 , A61K41/00 , A61P35/00 , C07C43/275 , C07C43/29
摘要: The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
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公开(公告)号:US10144711B2
公开(公告)日:2018-12-04
申请号:US15805390
申请日:2017-11-07
发明人: Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: A61P35/00 , A61K41/00 , A61K31/09 , C07C43/29 , C07C43/275 , C07D213/85 , C07C43/285 , C07C43/205 , C07C43/263 , C07C43/23 , C07C43/225 , A61K31/10 , C07C255/54 , C07C255/56 , C07C205/22 , C07C311/29 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07D213/89 , C07D231/56 , C07D213/65
摘要: The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
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公开(公告)号:US10023532B2
公开(公告)日:2018-07-17
申请号:US15091125
申请日:2016-04-05
发明人: Kei Domon , Keiji Toriyabe , Yutaka Ogawa , Junichiro Bessho , Kei Kawamoto , Akira Watanabe , Masaaki Komatsu , Takeshi Matsuda , Seisuke Ito
IPC分类号: C07C321/28 , C07C317/14 , A01N41/12 , C07D249/08 , C07D239/26 , C07C323/25 , C07D213/34 , C07D231/12 , C07D233/64 , C07D277/26 , C07C323/18 , A01N37/10 , A01N37/38 , C07C317/32 , C07C323/12 , C07C323/20 , C07C331/10 , A01N33/20 , A01N31/16 , C07C317/46 , C07C317/22 , A01N55/00 , A01N47/48 , A01N47/02 , A01N43/78 , A01N43/653 , A01N43/56 , A01N43/54 , A01N43/40 , A01N43/08 , A01N41/10 , A01N39/00 , A01N37/34 , A01N37/32 , C07C323/62 , A01N43/50
摘要: An alkyl phenyl sulfide derivative represented by the general formula [I] or an agriculturally acceptable salt thereof, and a pest control agent containing the derivative or the salt as an active ingredient. [in the above formula, R1 is, for example, a C1˜C6 alkyl group which is mono- or poly-substituted with halogen atom; R2 is, for example, a halogen atom or a C1˜C6 alkyl group; R3 is, for example, a hydrogen atom or a halogen atom; and R4 is, for example, a hydrogen atom or a C1˜C12 alkyl group.] The derivative or the salt has an excellent pest control effect.
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公开(公告)号:US20180155279A1
公开(公告)日:2018-06-07
申请号:US15805390
申请日:2017-11-07
发明人: Darryl David Dixon , Jonas Grina , John A. Josey , James P. Rizzi , Stephen T. Schlachter , Eli M. Wallace , Bin Wang , Paul Wehn , Rui Xu , Hanbiao Yang
IPC分类号: C07C311/29 , C07D231/56 , C07D213/89 , A61K31/09 , A61K31/10 , C07C43/205 , C07D213/85 , C07D213/65 , C07C381/10 , C07C323/22 , C07C317/48 , C07C317/46 , C07C317/44 , C07C317/42 , C07C317/40 , C07C317/36 , C07C317/34 , C07C317/32 , C07C317/24 , C07C317/22 , C07C313/06 , C07C255/56 , C07C255/54 , C07C205/22 , C07C43/285 , C07C43/263 , C07C43/23 , C07C43/225
CPC分类号: C07D213/85 , A61K31/09 , A61K31/10 , A61K41/0038 , A61P35/00 , C07C43/205 , C07C43/225 , C07C43/23 , C07C43/263 , C07C43/275 , C07C43/285 , C07C43/29 , C07C205/22 , C07C255/54 , C07C255/56 , C07C311/29 , C07C313/06 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/34 , C07C317/36 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/22 , C07C381/10 , C07C2602/04 , C07C2602/08 , C07C2602/10 , C07C2603/94 , C07D213/65 , C07D213/89 , C07D231/56
摘要: The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.
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公开(公告)号:US09815802B2
公开(公告)日:2017-11-14
申请号:US15319161
申请日:2015-06-26
发明人: Hartmut Ahrens , Ines Heinemann , Joerg Tiebes , Christian Waldraff , Simon Doerner-Rieping , Elmar Gatzweiler , Christopher Hugh Rosinger , Dirk Schmutzler , Hansjoerg Dietrich
IPC分类号: A01N43/713 , C07D257/06 , C07C317/44 , C07C317/46
CPC分类号: C07D257/06 , A01N43/713 , C07C317/44 , C07C317/46 , C07C2601/02
摘要: N-(1-Methyltetrazol-5-yl)benzamides of the general formula (I) are described as herbicides. In this formula (I), X, Z and R are radicals such as alkyl and cycloalkyl.
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公开(公告)号:US09708253B2
公开(公告)日:2017-07-18
申请号:US15109733
申请日:2015-01-05
发明人: Jingwu Duan , T. G. Murali Dhar , Bin Jiang , Ananta Karmakar , Arun Kumar Gupta , Zhonghui Lu , Carolyn A. Weigelt
IPC分类号: C07C317/20 , C07C317/24 , C07C317/30 , C07D205/04 , C07D207/27 , C07D211/46 , C07D211/78 , C07D213/30 , C07D231/12 , C07D213/81 , C07D213/82 , C07D309/08 , C07D231/14 , C07D231/56 , C07D401/04 , C07D403/04 , C07D237/08 , C07D237/20 , C07D237/24 , C07D405/04 , C07D239/28 , C07C317/46 , C07D241/24 , C07D249/04 , C07D471/04 , C07D207/277 , C07D277/60 , C07D295/096 , C07D211/48 , C07D211/62 , C07D295/185 , C07D213/56 , C07D213/71 , C07D213/75 , C07D309/04 , C07D335/02 , C07D401/06 , C07D401/12 , C07D295/205 , C07D213/40 , C07D231/54 , C07D237/22 , C07D249/06 , C07D277/82 , C07D295/16 , C07D295/195
CPC分类号: C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07D205/04 , C07D207/27 , C07D207/277 , C07D211/46 , C07D211/48 , C07D211/62 , C07D211/78 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/71 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/14 , C07D231/54 , C07D231/56 , C07D237/08 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/28 , C07D241/24 , C07D249/04 , C07D249/06 , C07D277/60 , C07D277/82 , C07D295/096 , C07D295/16 , C07D295/185 , C07D295/195 , C07D295/205 , C07D309/04 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D405/04 , C07D471/04
摘要: Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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