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公开(公告)号:US4197241A
公开(公告)日:1980-04-08
申请号:US961087
申请日:1978-11-15
申请人: John F. Cavalla , Alan C. White
发明人: John F. Cavalla , Alan C. White
IPC分类号: C07D207/12 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K31/451 , A61K31/55 , A61P25/04 , C07D207/08 , C07D207/26 , C07D211/22 , C07D211/76 , C07D221/22 , C07D223/04 , C07D223/08 , C07D223/10
CPC分类号: C07D207/08 , C07D207/26 , C07D211/22 , C07D211/76 , C07D223/04 , C07D223/10
摘要: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine derivatives of formula (I) and their aromatized derivatives of formula (II) ##STR1## where n is 2, 3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl, R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.3 is hydrogen, lower alkyl, aryl(lower)alkyl, lower alkenyl or lower alkynyl. The compounds are useful as intermediates for preparing 3,3-disubstituted -hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
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公开(公告)号:US4060609A
公开(公告)日:1977-11-29
申请号:US518811
申请日:1974-10-29
申请人: Erich Schacht , Werner Mehrhof , Rochus Jonas , Herbert Nowak , Zdenek Simane
发明人: Erich Schacht , Werner Mehrhof , Rochus Jonas , Herbert Nowak , Zdenek Simane
IPC分类号: C07D295/08 , C07C217/32 , C07D211/22 , C07D211/42 , C07D223/08 , C07D295/092 , A61K31/535
CPC分类号: C07D295/088
摘要: Biphenylyl ethers of the formula R--O--CH.sub.2 --CR.sub.1 (OH)--CH.sub.2 Z wherein R.sub.1 is H or CH.sub.3 ; Z is dialkylamino of 2-8 carbon atoms, morpholino, pyrrolidino, piperidino, homopiperidino, hydroxypyrrolidino, hydroxypiperidino or hydroxyhomopiperidino; R is either biphenylyl substituted by at least one of F, Cl, Br, I, CF.sub.3, NO.sub.2 and piperidino or, when R.sub.1 is CH.sub.3 or when Z is homopiperidino, hydroxypyrrolidino, hydroxypiperidino or hydroxyhomopiperidino, unsubstituted biphenyl, and the physiologically acceptable acid addition salts thereof, possess cholesterol blood-level-lowering activity and can be produced by reacting a compound of the formula R--O--CH.sub.2 --Y wherein Y is ##STR1## or --CR.sub.1 (OH)--CH.sub.2 X, X being Cl, Br, I or a free or functionally modified OH-group, with an amine of the formula H-Z.
摘要翻译: 式R-O-CH 2 -CR 1(OH)-CH 2 Z的联苯基醚,其中R 1是H或CH 3; Z是2-8个碳原子的二烷基氨基,吗啉代,吡咯烷子基,哌啶子基,高哌啶基,羟基吡咯烷基,羟基哌啶子基或羟基高哌啶子基; R是由F,Cl,Br,I,CF 3,NO 2和哌啶子中至少一种取代的联苯基,或当R 1为CH 3或Z为高哌啶基,羟基吡咯烷基,羟基哌啶子基或羟基高哌啶子基,未取代的联苯基和生理上可接受的酸加成 其盐具有胆固醇血液中降低水平的活性,并且可以通过使式RO-CH2-Y的化合物(其中Y是或-CR1(OH)-CH2X,X是Cl,Br,I或 游离的或官能改性的OH-基团与式HZ的胺反应。
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公开(公告)号:US3622565A
公开(公告)日:1971-11-23
申请号:US3622565D
申请日:1968-01-17
申请人: RHONE POULENC SA
IPC分类号: C07D223/22 , C07D223/08 , C07D41/08
CPC分类号: C07D223/08
摘要: The invention provides new 10-amino-10,11-dihydrodibenzo(b, f)azepine derivatives and their salts which are useful as antidepressants, analgesics, anticonvulsants and tranquillizers.
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公开(公告)号:US10940154B2
公开(公告)日:2021-03-09
申请号:US16408718
申请日:2019-05-10
发明人: Jae U. Jeong , Deepak Bandyopadhyay , Patrick M. Eidam , Philip Anthony Harris , Jianxing Kang , Bryan Wayne King , Ami Lakdawala Shah , Lara Kathryn Leister , Attiq Rahman , Joshi M. Ramanjulu , Clark A. Sehon , Robert Singhaus, Jr. , Daohua Zhang
IPC分类号: A61K31/553 , A61K31/55 , C07D413/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D267/14 , C07D498/04 , C07D281/10 , A61K31/551 , C07D403/12 , C07D223/08
摘要: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
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公开(公告)号:US10933070B2
公开(公告)日:2021-03-02
申请号:US16299254
申请日:2019-03-12
发明人: Jae U. Jeong , Deepak Bandyopadhyay , Patrick M. Eidam , Philip Anthony Harris , Jianxing Kang , Bryan Wayne King , Ami Lakdawala Shah , Lara Kathryn Leister , Attiq Rahman , Joshi M. Ramanjulu , Clark A. Sehon , Robert Singhaus, Jr. , Daohua Zhang
IPC分类号: A61K31/55 , A61K31/551 , A61K31/553 , C07D413/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D267/14 , C07D498/04 , C07D281/10 , C07D403/12 , C07D223/08
摘要: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
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公开(公告)号:US20190382342A1
公开(公告)日:2019-12-19
申请号:US15740437
申请日:2016-07-01
IPC分类号: C07D211/58 , C07D211/46 , C07D211/54 , C07D223/08 , C07D205/04 , C07D207/12 , C07D223/12 , C07D451/06 , A61P25/28
摘要: Provided herein are compounds and methods for inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
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公开(公告)号:US09873671B2
公开(公告)日:2018-01-23
申请号:US15277421
申请日:2016-09-27
发明人: George D. Hartman , Scott Kuduk
IPC分类号: C07D223/08 , A61K31/55 , A61K45/06 , C07D267/10 , A61K31/553 , C07D223/32 , A61K31/439 , A61K31/551 , C07D221/22 , C07D223/06 , C07D243/08 , A61K38/21 , A61K47/48 , A61K31/554 , C07D283/00 , C07D295/26 , C07D403/12
CPC分类号: C07D223/08 , A61K31/439 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61K38/21 , A61K45/06 , A61K47/60 , C07D221/22 , C07D223/06 , C07D223/32 , C07D243/08 , C07D267/10 , C07D283/00 , C07D295/26 , C07D403/12 , A61K2300/00
摘要: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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公开(公告)号:US09339510B2
公开(公告)日:2016-05-17
申请号:US14856761
申请日:2015-09-17
发明人: George D. Hartman , Scott Kuduk
IPC分类号: A61K31/55 , C07D223/08 , C07D267/10 , A61K31/675 , A61K38/21 , A61K39/29 , A61K45/06
CPC分类号: A61K31/675 , A61K31/439 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/553 , A61K31/554 , A61K38/21 , A61K38/212 , A61K38/215 , A61K38/217 , A61K39/292 , A61K45/06 , C07D221/24 , C07D223/06 , C07D223/08 , C07D223/32 , C07D243/08 , C07D267/10 , C07D281/06 , C07F9/5532 , C07F9/6527 , A61K2300/00
摘要: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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公开(公告)号:US07405209B2
公开(公告)日:2008-07-29
申请号:US11152745
申请日:2005-06-14
申请人: Robert Wells Marquis, Jr. , Yu Ru , Daniel Frank Veber , Maxwell David Cummings , Scott Kevin Thompson , Dennis Shinji Yamashita
发明人: Robert Wells Marquis, Jr. , Yu Ru , Daniel Frank Veber , Maxwell David Cummings , Scott Kevin Thompson , Dennis Shinji Yamashita
IPC分类号: A61P19/00 , A61K31/55 , A61K31/00 , C07D223/08 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号: C07D405/14 , A61K38/00 , C07D223/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07K5/06139
摘要: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
摘要翻译: 本发明提供了抑制蛋白酶的4-氨基 - 氮杂-3-酮蛋白酶抑制剂及其药学上可接受的盐,水合物和溶剂化物,包括组织蛋白酶K,这些化合物的药物组合物,这些化合物的新中间体,以及治疗疾病的方法 骨质疏松过多或软骨或基质降解,包括骨质疏松症; 牙龈疾病包括牙龈炎和牙周炎; 关节炎,更具体地,骨关节炎和类风湿性关节炎; 佩吉特病 恶性高钙血症; 和代谢性骨病,其包括通过向有需要的患者施用本发明的化合物来抑制所述骨丢失或过度软骨或基质降解。
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公开(公告)号:US06914140B1
公开(公告)日:2005-07-05
申请号:US09546143
申请日:2000-04-10
IPC分类号: C07D223/08 , C07D223/12 , C07D498/04 , C07D201/16
CPC分类号: C07D223/12 , C07D223/08
摘要: A novel process for the manufacture of compounds of the formula wherein R1 and R2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.
摘要翻译: 用于制备下式化合物的新方法其中R 1和R 2独立地代表芳酰基。 本发明还涉及用于制备式I化合物的新方法中的新型中间体。
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