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1. 发明申请

WO1997040027A1 SUBSTITUTED BENZYLAMINES AND THEIR USE FOR THE TREATMENT OF DEPRESSION 审中-公开
标题翻译：替代苯甲酸酯及其用于治疗呕吐的用途
公开(公告)号：WO1997040027A1
公开(公告)日：1997-10-30
申请号：PCT/EP1997001904
申请日：1997-04-15
申请人： AKZO NOBEL N.V. , LEYSEN, Dirk, Casimir, Maria , RUIGT, Gerardus, Stephanus, Franciscus , LINDERS, Joannes, Theodorus, Maria , DIJCKS, Fredericus, Antonius , GROVE, Simon, James, Anthony , RAE, Duncan, Robertson
发明人： AKZO NOBEL N.V.
IPC分类号： C07D261/20
CPC分类号： C07D413/10 , C07D231/56 , C07D261/20 , C07D413/12 , C07D417/12
摘要： The present invention relates to certain novel benzylamine derivatives of formula (I) wherein R and R , which may be the same or different, are each selected from C6-12aryl, C2-14heteroaryl, C6-12arylC1-6alkyl, C2-14heteroarylC1-6alkyl (where the alkyl, aryl or heteroaryl moiety may be optionally substituted by one or more substituents selected from C1-6alkoxy, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-12aryl, C2-14heteroaryl, halogen, amino, hydroxy, haloC1-6alkyl, nitro, C1-6alkylthio, sulphonamide, C1-6alkylsulphonyl, hydroxy-C1-6alkyl, C1-6alkoxycarbonyl, carboxyl, carboxyC1-6alkyl, carboxamide and C1-6alkylcarboxamide), hydrogen, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C2-6alkenyl, C2-6alkynyl and C1-6alkoxyC1-6alkyl (where the alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl, or alkoxyalkyl moieties may be optionally substituted by one or more substituents selected from amino, halogen, hydroxy, C1-6alkylcarboxamide, carboxamide, carboxy, C1-6alkoxycarbonyl, C1-6alkylcarboxy and carboxyC1-6alkyl) or one of R and R are as hereinbefore defined and one is hydroxy; R and R , which may be the same or different, are each selected from C6-12aryl, C2-14heteroaryl, C6-12arylC1-6alkyl, C2-14heteroarylC1-6alkyl (where the alkyl, aryl or heteroaryl moiety may be optionally substituted by one or more substituents selected from C1-6alkoxy, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-12aryl, C2-14heteroaryl, halogen, amino, hydroxy, haloC1-6alkyl, nitro, C1-6alkylthio, sulphonamide, C1-6alkylsulphonyl, hydroxyC1-6alkyl, C1-6alkoxycarbonyl, carboxyl, carboxyC1-6alkyl, C1-6alkylcarboxamide and carboxamide), hydrogen, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-6alkyl, C4-6cycloalkenyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy-C1-6alkyl, haloC1-6alkyl, haloC2-6alkenyl, haloC2-6alkynyl, cyano, carboxyl, C1-6alkylcarboxy and carboxyC1-6alkyl (where the alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl, or alkoxyalkyl moieties may be optionally substituted by one or more substituents selected from amino, hydroxy, C1-6alkylcarboxamide, carboxamide, carboxy, C1-6alkoxycarbonyl, C1-6alkylcarboxy and carboxyC1-6alkyl); or one of R or R together with one of R or R and the N atom to which it is attached form a 5- or 6-membered heterocyclic ring. R represents one or more ring substituents selected from halogen, hydrogen C1-6alkyl and C1-6alkoxy; and R represents a single ring substituent of formula (A) wherein the dotted line represents an optional bond; Y is oxygen or -NR (where R is hydrogen or C1-6alkyl) and R represents one or more substituents selected from hydrogen, halogen, haloC1-6alkyl, C1-6alkyl and C1-6alkoxy; or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
摘要翻译：本发明涉及一些式（I）的新型苄胺衍生物，其中R 1和R 2可以相同或不同，各自选自C 6-12芳基，C 2-4芳基，C 6-12芳基C 1-6烷基，其中烷基，芳基或杂芳基部分可以任选地被一个或多个选自C 1-6烷氧基，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 6-12芳基，C 2-4杂芳基，卤素，氨基，羟基，卤代C 1-6烷基，硝基，C 1-6烷硫基，磺酰胺，C 1-6烷基磺酰基，羟基-C 1-6烷基，C 1-6烷氧基羰基，羧基，羧基C 1-6烷基，羧酰胺和C 1-6烷基羧酰胺），氢，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 2-6烯基，C 2-6炔基和C 1-6烷氧基C 1-6烷基（其中烷基，环烷基，环烯基，烯基，炔基或烷氧基烷基部分可以任选地被一个或多个选自氨基，卤素，羟基，C 1-6烷基羧酰胺，羧酰胺，羧基，C 1-6烷氧基羰基，C 1-6a 烷基羧基和羧基C 1-6烷基）或R 1和R 2中的一个如上文所定义，一个是羟基; R 3和R 4可以相同或不同，各自选自C 6-12芳基，C 2-14杂芳基，C 6-12芳基C 1-6烷基，C 2-4杂芳基C 1-6烷基（其中烷基，芳基或杂芳基部分可以任选地被一个或多个选自C 1-6烷氧基，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 6-12芳基，C 2-4杂芳基，卤素，氨基，羟基，卤代C 1-6烷基，硝基，C 1-6烷硫基，磺酰胺，C 1-6烷基磺酰基，羟基C 1-6烷基，C 1-6烷氧基羰基，羧基，羧基C 1-6烷基，C 1-6烷基羧酰胺和甲酰胺），氢，C 1-6烷基，C 3-6环烷基，C 3-6环烷基C 1-6烷基，C 4-6环烯基， C 1-6烷氧基-C 1-6烷基，卤代C 1-6烷基，卤代C 2-6烯基，卤代C 2-6炔基，氰基，羧基，C 1-6烷基羧基和羧基C 1-6烷基（其中烷基，环烷基，环烯基，链烯基，炔基，或烷氧基烷基部分可以任选地被一个或多个选自氨基，羟基，C 1-6烷基羧酰胺，甲酰胺，羧基，C 1-6烷氧基羰基，C 1-6烷基羧基和羧基C 1-6烷基）; 或R 3或R 4中的一个与R 1或R 2中的一个以及与其连接的N原子形成5-或6-元杂环。 R 5表示一个或多个选自卤素，C 1-6烷基和C 1-6烷氧基的环取代基; 并且R 6表示式（A）的单环取代基，其中虚线表示任选的键; Y是氧或-NR 8（其中R 8是氢或C 1-6烷基），R 7代表一个或多个选自氢，卤素，卤代C 1-6烷基，C 1-6烷基和C 1-6烷氧基的取代基; 或其药学上可接受的盐或溶剂合物。本发明还涉及其制备方法，含有它们的药物制剂及其在药物治疗中的用途，特别是治疗抑郁症。

2. 发明申请

WO2010142705A1 SUBSTITUTED 16,17-ANNELLATED STEROID COMPOUNDS FOR USE IN WOMEN'S HEALTHCARE 审中-公开
标题翻译：用于妇女健康服用的16,17-ANNELLATED STEROID化合物
公开(公告)号：WO2010142705A1
公开(公告)日：2010-12-16
申请号：PCT/EP2010/058042
申请日：2010-06-09
申请人： N.V. ORGANON , DIJCKS, Fredericus, Antonius , LOOZEN, Hubert, Jan, Jozef , ADDO, Samira , EDERVEEN, Antonius, Gerardus, Hendrikus
发明人： DIJCKS, Fredericus, Antonius , LOOZEN, Hubert, Jan, Jozef , ADDO, Samira , EDERVEEN, Antonius, Gerardus, Hendrikus
IPC分类号： C07J53/00 , A61K31/57 , A61P5/30 , A61P5/32 , A61P5/34 , A61P5/36
CPC分类号： C07J53/002
摘要： The present invention relates to substituted steroid compounds having the formula (I) Wherein R 1 is H or halogen; R 2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R 3 is H or halogen; R 4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R 5 is methyl or ethyl; R 6 is H or methyl; R 7 is H or methyl; R 8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.
摘要翻译：本发明涉及具有式（I）的取代的类固醇化合物，其中R1是H或卤素; R2是H，（1C-4C）烷基，（1C-4C）酰基，葡糖醛酸或氨磺酰基; R3是H或卤素; R4是H，（1C-4C）烷基，（2C-4C）烯基或（2C-4C）炔基; R5是甲基或乙基; R6是H或甲基; R7是H或甲基; R8是H或酰基，用于治疗和预防子宫内膜异位，避孕，绝经期和绝经后妇女的激素治疗，治疗骨质疏松症和治疗子宫肌瘤和其他月经相关疾病，如功能障碍崩漏。

3. 发明申请

WO2006027347A1 15β-SUBSTITUTED STEROIDS HAVING SELECTIVE ESTROGENIC ACTIVITY 审中-公开
标题翻译：具有选择性雌激素活性的15β-取代的甾族化合物
公开(公告)号：WO2006027347A1
公开(公告)日：2006-03-16
申请号：PCT/EP2005/054368
申请日：2005-09-05
申请人： AKZO NOBEL N.V. , LOOZEN, Hubert, Jan, Jozef , EDERVEEN, Antonius, Gerardus, Hendrikus , DIJCKS, Fredericus, Antonius
发明人： LOOZEN, Hubert, Jan, Jozef , EDERVEEN, Antonius, Gerardus, Hendrikus , DIJCKS, Fredericus, Antonius
IPC分类号： C07J1/00 , A61K31/56 , A61P5/00
CPC分类号： A61K31/56 , C07J1/00
摘要： The invention provides 15β-substituted steroidal compounds having selective estrogen receptor activity according to Formula (I) wherein, R 1 is H, C 1-5 alkyl, C 1-12 acyl, di-(C 1-5 alkyl)aminocarbonyl, (C 1-5 alkyl)oxycarbonyl or sulfamoyl, R 2 is H, C 1-3 alkyl, C 2-3 alkenyl or C 2-3 alkynyl, each of which may be optionally substituted with a halogen, R 3 is C 1-2 alkyl, ethenyl or ethynyl, each of which may be optionally substituted with a halogen, and R 4 is H or C 1-12 acyl.
摘要翻译：本发明提供了具有根据式（I）的选择性雌激素受体活性的15β-取代的甾族化合物，其中R 1是H，C 1-5烷基，C 1 -C 6烷基， 1-12酰基，二 - （C 1-5烷基）氨基羰基，（C 1-5烷基）氧基羰基或氨磺酰基，R 2 是H，C 1-3烷基，C 2-3-3烯基或C 1-3-3炔基，其中每一个可以任选被卤素取代，R 3是C 1-12烷基，乙烯基或乙炔基，其各自可以任选被卤素取代，R 1， 4是H或C 1-12酰基。

4. 发明申请

WO9918941A3 Ih-MODULATORS 审中-公开
标题翻译： IH-调节剂
公开(公告)号：WO9918941A3
公开(公告)日：2000-01-13
申请号：PCT/EP9806651
申请日：1998-10-14
申请人： AKZO NOBEL NV , DIJCKS FREDERICUS ANTONIUS , GROVE SIMON JAMES ANTHONY , CARLYLE IAN CRAIG , THORN SIMON NICHOLAS , RAE DUNCAN ROBERTSON , RUIGT GERARDUS STEPHANUS FRANC , LEYSEN DIRK
发明人： DIJCKS FREDERICUS ANTONIUS , GROVE SIMON JAMES ANTHONY , CARLYLE IAN CRAIG , THORN SIMON NICHOLAS , RAE DUNCAN ROBERTSON , RUIGT GERARDUS STEPHANUS FRANC , LEYSEN DIRK
IPC分类号： G01N33/50 , A61K31/00 , A61K31/085 , A61K31/121 , A61K31/135 , A61K31/137 , A61K31/15 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/416 , A61K31/42 , A61K31/423 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/47 , A61K31/472 , A61K31/496 , A61K31/505 , A61K45/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07C47/55 , C07C47/575 , C07C211/28 , C07C211/29 , C07C217/56 , C07C255/58 , C07D213/48 , C07D213/61 , C07D215/12 , C07D217/14 , C07D231/56 , C07D239/26 , C07D261/08 , C07D261/20 , C07D263/56 , C07D263/57 , C07D277/28 , C07D277/66 , C07D307/52 , C07D307/80 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/56 , C07D333/58 , C07D413/04 , C07D498/04 , G01N33/15 , A61K31/34 , A61K31/38 , A61K31/425 , A61K31/435
CPC分类号： C07D413/04 , A61K31/00 , A61K31/085 , A61K31/121 , A61K31/137 , A61K31/15 , A61K31/381 , A61K31/416 , A61K31/423 , A61K31/426 , A61K31/437 , A61K31/472 , C07C211/28 , C07C211/29 , C07C217/56 , C07C255/58 , C07D213/61 , C07D215/12 , C07D217/14 , C07D231/56 , C07D239/26 , C07D261/08 , C07D261/20 , C07D263/57 , C07D277/28 , C07D277/66 , C07D307/52 , C07D307/80 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/58
摘要： The present invention relates to the use of an Ih channel modulator in the manufacture of a medicament for use in psychiatry. To certain novel methanamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly for use in psychiatry.
摘要翻译：本发明涉及Ih通道调节剂在制造用于精神病学的药物中的用途。某些新的甲胺衍生物，其制备方法，含有它们的药物制剂及其在药物治疗中的用途，特别是用于精神病学。

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