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21. 发明授权

US07166608B2 N-aroyl piperazine derivatives as orexin receptor antagonists 失效
标题翻译： N-芳酰哌嗪衍生物作为食欲素受体拮抗剂
公开(公告)号：US07166608B2
公开(公告)日：2007-01-23
申请号：US10492250
申请日：2002-10-09
申请人： Clive Leslie Branch , Christopher Norbert Johnson , David John Nash , Geoffrey Stemp
发明人： Clive Leslie Branch , Christopher Norbert Johnson , David John Nash , Geoffrey Stemp
IPC分类号： A61K31/496 , C07D413/06 , C07D417/06
CPC分类号： C07D413/10 , C07D241/04 , C07D417/06
摘要： This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR2; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C═O, SO2, or CH═CH—; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar2 represents phenyl or a 5- or 6-membered heterocyclyl group containing 1 to 3 heteroatoms selected from N, O and S, wherein the phenyl heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing 1 to 4 heteroatoms selected from N, O and S; R1 represents optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S; R2 represents hydrogen, optionally substituted (C1-4)alkyl, optionally substituted (C1-6)alkanoyl, optionally subtituted (C1-6)alkanoxycarbonyl or optionally substituted aryl(C1-6)alkyloxycarbonyl; and their use as orexin receptor-antagonists.
摘要翻译：本发明涉及式（I）的N-芳酰基哌嗪衍生物，其中：Y表示NR 2; m表示1,2或3; p表示0或1; X是O，S，C-O，SO 2 H或CH-CH-; Ar 1是芳基或含有至多4个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; Ar 2表示苯基或含有1至3个选自N，O和S的杂原子的5-或6-元杂环基，其中苯基杂环基被R 1 O取代和另外任选的取代基; 或者Ar 2表示含有1至4个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 1表示任选取代的（C 1-4 - ）烷氧基，卤素，任选取代的（C 1-6 - ）烷基，任选取代的苯基，或含有1至4个选自N，O和S的杂原子的任选取代的5或6元杂环; R 2表示氢，任选取代的（C 1-4 - ）烷基，任选取代的（C 1-6 - ）烷酰基，任选取代的（C 烷氧基羰基或任选取代的芳基（C 1-6 - ）烷氧基羰基; 以及它们作为食欲肽受体拮抗剂的用途。

22. 发明授权

US06465485B1 Tetrahydroisoquinoline derivatives as modulators of dopamine D3 receptors 失效
标题翻译：四氢异喹啉衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US06465485B1
公开(公告)日：2002-10-15
申请号：US09656379
申请日：2000-09-06
申请人： Clive Leslie Branch , Christopher Norbert Johnson , Geoffrey Stemp
发明人： Clive Leslie Branch , Christopher Norbert Johnson , Geoffrey Stemp
IPC分类号： C07D21704
CPC分类号： C07D401/12 , C07D217/04 , C07D217/26 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Compounds of formula (I): and their salts having affinity for dopamine receptors, in particular the D3 receptor, and thus potential in the treatment of conditions wherein modulation of the D3 receptor is beneficial, e.g., as antipsychotic agents.
摘要翻译：式（I）的化合物及其对多巴胺受体，特别是D3受体具有亲和性的盐，因此在治疗D3受体的调节作为抗精神病药有利的条件下具有潜力。

23. 发明授权

US06943160B2 Morpholine derivatives as antagonists of orexin receptors 失效
标题翻译：吗啉衍生物作为食欲素受体的拮抗剂
公开(公告)号：US06943160B2
公开(公告)日：2005-09-13
申请号：US10432421
申请日：2001-11-22
申请人： Clive Leslie Branch , Christopher Norbert Johnson , Alexander B. Smith , Geoffrey Stemp , Kevin Thewlis
发明人： Clive Leslie Branch , Christopher Norbert Johnson , Alexander B. Smith , Geoffrey Stemp , Kevin Thewlis
IPC分类号： C07D417/06 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P15/00 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/30 , A61P43/00 , C07D417/12 , C07D417/14 , C07D413/06 , C07D413/12 , C07D413/14
CPC分类号： C07D417/12 , C07D417/14
摘要： This invention relates to morpholine derivatives of formula (I) and their use as antagonists of orexin receptors.
摘要翻译：本发明涉及式（I）的吗啉衍生物及其作为食欲素受体拮抗剂的用途。

24. 发明授权

US06855717B2 Tetrahydroisoquinoline derivatives as modulators of dopamine D3 receptors 失效
标题翻译：四氢异喹啉衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US06855717B2
公开(公告)日：2005-02-15
申请号：US10367306
申请日：2003-02-14
申请人： Clive Leslie Branch , Christopher Norbert Johnson , Geoffrey Stemp
发明人： Clive Leslie Branch , Christopher Norbert Johnson , Geoffrey Stemp
IPC分类号： C07D401/12 , C07D405/12 , A61K31/47
CPC分类号： C07D401/12 , C07D405/12
摘要： Compounds of formula (I): wherein: R2 represents a hydrogen atom or a C1-4alkyl group; q is 1 or 2; A represents a group of formula (a) or (b) wherein T, U, V and Y independently represent CH or a nitrogen atom; R5 is a group selected from: a hydrogen or halogen atom, cyano, C1-4 alkyl or C1-4 alkoxy group s is 1 or 2; Ar2 represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; and salts thereof. The compounds are useful for the treatment of conditions which require modulaton of a dopamine receptor such as schizophrenia.
摘要翻译：式（I）化合物：其中：R 2表示氢原子或C 1-4烷基; q为1或2; A表示式（a）或（b）的基团，其中T，U，V和Y 独立地表示CH或氮原子; R 5是选自：氢或卤素原子，氰基，C 1-4烷基或C 1-4烷氧基的基团是1或2; Ar 2表示任选取代的苯基环或任选取代的5或6元芳族杂环; 及其盐。该化合物可用于治疗需要调节多巴胺受体如精神分裂症的病症。

25. 发明授权

US06677354B2 Piperdines for use as orexin receptor antagonists 失效
标题翻译：用作食欲肽受体拮抗剂的Pi子
公开(公告)号：US06677354B2
公开(公告)日：2004-01-13
申请号：US10311445
申请日：2002-12-16
申请人： Clive Leslie Branch , Christopher Norbert Johnson , Geoffrey Stemp , Kevin Thewlis
发明人： Clive Leslie Branch , Christopher Norbert Johnson , Geoffrey Stemp , Kevin Thewlis
IPC分类号： A61K314545
CPC分类号： C07D401/06 , C07D211/26 , C07D401/10 , C07D405/06 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/04
摘要： Disclosed are compounds of formula (I): wherein: Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered heteroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R5 represents an optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to 3 heteroatoms selected from N, O and S; or pharmaceutically acceptable salts thereof.
摘要翻译：公开了式（I）的化合物：其中：Y表示基团（CH 2）n，其中n表示0,1或2; R 1是苯基，萘基，含有至多3个选自杂原子的单或双环杂芳基来自N，O和S; 或NR 3或R 4基团，其中R 3和R 4中的一个是氢或任选取代的（C 1-4）烷基，另一个是苯基，萘基或含有上述的单或双环杂芳基至3个选自N，O和S的杂原子，或R 3和R 4与它们所连接的N原子一起形成具有任选稠合的苯环的5至7元环胺; 任何R 1可以任选被取代; R 2表示苯基或含有至多3个选自N，O和S的杂原子的5-或6-元杂芳基，其中苯基或杂芳基被取代 R 5和另外任选的取代基; 或R 2表示含有至多3个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 5表示任选取代的（C 1-4）烷氧基，卤素，任选取代的（C1- 6）烷基，任选取代的苯基或含有至多3个选自N，O和S的杂原子的任选取代的5或6元杂环; 或其药学上可接受的盐。

26. 发明授权

US4108992A Cephalosporin analogues and compositions 失效
标题翻译： CEPHALOSPORIN类似物和组合物
公开(公告)号：US4108992A
公开(公告)日：1978-08-22
申请号：US766213
申请日：1977-02-07
申请人： Michael John Pearson , Clive Leslie Branch
发明人： Michael John Pearson , Clive Leslie Branch
IPC分类号： C07D205/085 , C07D505/00 , C07F9/568 , A01N9/00 , A01N9/22 , C07D265/00 , C07D273/00
CPC分类号： C07D505/00 , C07D205/085 , C07F9/5683
摘要： Novel cephalosporin analogues, salts and esters thereof, their preparation, intermediates and antibacterial compositions containing them. The compositions are formulated for human use into unit dosage form containing 100-4,000 mg of antibacterial compound. The cephem analogues are characterized by having a ring O-heteroatom instead of a ring N-heteroatom and are designated as oxacephems.

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