专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06172067B2 2-substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists 失效
标题翻译： 2-取代-1-哌啶基苯并咪唑化合物作为ORL1-受体激动剂
公开(公告)号：US06172067B2
公开(公告)日：2001-01-09
申请号：US09369208
申请日：1999-08-05
申请人： Fumitaka Ito , Hirohide Noguchi , Hiroshi Kondo
发明人： Fumitaka Ito , Hirohide Noguchi , Hiroshi Kondo
IPC分类号： A61K31454
CPC分类号： C07D401/04 , C07D211/58 , C07D401/14
摘要： A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5 )alkenyl, or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, Y is hydrogen, halo, amino or mercapto, or unsubstituted, mono-, di- or tri- substituted (C1-C10)alkyl-M—, (C3-C7)cycloalkyl-M—, (C2-C6)alkenyl-M—, (C1-C4)alkyl-NH-((C1-C4)alkyl)-M—, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M—, aryl-M—, aromatic or non-aromatic heterocyclic-M—, aryl-(C1-C5)alkyl-M— or aromatic non-aromatic heterocyclic-(C1-C5)alkyl-M—, wherein M is a covalent bond O, S, NH or the like, or the like; Z1, Z2, Z3 and Z4 are hydrogen or the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.
摘要翻译：一种下式的化合物或其药学上可接受的盐，其中R是未取代的一价，二或三取代的（C 3 -C 11）环烷基或（C 3 -C 11）环烯基等，A是未取代的（C1- C7）烷基或（C2-C5）烯基或未取代的单，二或三取代的芳基或芳族杂环等，Y是氢，卤素，氨基或巯基，或未取代的单，二 - （C 1 -C 6）烷基-M-，（C 3 -C 7）环烷基M - ，（C 2 -C 6）烯基-M-，（C 1 -C 4）烷基-NH-（（C 1 -C 4）烷基）-M-，二（C 1 -C 4）烷基-N - （（C 1 -C 4）烷基）-M-，芳基M-，芳族或非芳族杂环M-，芳基 - （C 1 -C 5）烷基-M-或芳族非芳族杂环 - （C1-C5）烷基-M-，其中M是共价键O，S，NH等; Z1，Z2，Z3和Z4为氢等具有ORL1-受体激动剂活性，并且可用作哺乳动物受试者中的止痛剂等。

2. 发明授权

US06423725B1 4-(2-keto-1-benzimidazolinyl)piperidine compounds as ORL1-receptor agonists 失效
标题翻译： 4-（2-酮-1-苯并咪唑啉基）哌啶化合物作为ORL1-受体激动剂
公开(公告)号：US06423725B1
公开(公告)日：2002-07-23
申请号：US09403408
申请日：2000-03-06
申请人： Fumitaka Ito , Hirohide Noguchi , Yoriko Ohashi , Hiroshi Kondo , Tatsuya Yamagishi
发明人： Fumitaka Ito , Hirohide Noguchi , Yoriko Ohashi , Hiroshi Kondo , Tatsuya Yamagishi
IPC分类号： A61K31454
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14
摘要： A compound of the formula: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined above are useful as ORL1-receptor agonists, and useful as analgesics or the like in mammalian subjects.
摘要翻译：下式化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如上定义，可用作ORL1-受体激动剂，并且可用作哺乳动物受试者中的止痛剂等。

3. 发明授权

US06313302B2 Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists 失效
标题翻译：吡咯烷基和吡咯啉基乙胺化合物作为κ激动剂
公开(公告)号：US06313302B2
公开(公告)日：2001-11-06
申请号：US09770513
申请日：2001-01-26
申请人： Fumitaka Ito , Hiroshi Kondo
发明人： Fumitaka Ito , Hiroshi Kondo
IPC分类号： C07C23724
CPC分类号： C07D213/82 , C07D207/10 , C07D207/12 , C07D207/20 , C07D207/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.
摘要翻译：下式的化合物及其盐，其中A是氢，卤素或羟基; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar1是任选取代的苯基; Ar2是选自苯基，萘乙基或吡啶基的芳基或杂芳基，芳基或杂芳基任选被取代; R1是氢，羟基或C1-C4烷基; 并且R 2和R 3独立地选自任选取代的C 1 -C 7烷基，C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基或R 2和R 3与它们所连接的氮原子一起形成任选取代的吡咯烷。这些化合物可用作κ激动剂。

4. 发明授权

US06294569B2 Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists 失效
公开(公告)号：US06294569B2
公开(公告)日：2001-09-25
申请号：US09770514
申请日：2001-01-26
申请人： Fumitaka Ito , Hiroshi Kondo
发明人： Fumitaka Ito , Hiroshi Kondo
IPC分类号： A61K314025
CPC分类号： C07D213/82 , C07D207/10 , C07D207/12 , C07D207/20 , C07D207/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

5. 发明授权

US5886009A Quinuclidine derivative as a substance P antagonist 失效
标题翻译：奎宁环衍生物作为P物质拮抗剂
公开(公告)号：US5886009A
公开(公告)日：1999-03-23
申请号：US500958
申请日：1995-06-19
申请人： Fumitaka Ito , Hiroshi Kondo , Masami Nakane , Kaoru Shimada
发明人： Fumitaka Ito , Hiroshi Kondo , Masami Nakane , Kaoru Shimada
IPC分类号： A61K31/435 , A61P1/00 , A61P9/08 , A61P9/12 , A61P11/00 , A61P17/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D453/02
CPC分类号： A61K31/435 , C07D453/02
摘要： This invention relates to the quinuclidine derivative (2S, 3S)-N-(5-n-propyl-2-methoxyphenyl)methyl-2-diphenylmethyl-1-azabicyclo�2.2.2!octan-3-amine and its pharmaceutically acceptable salts. These compounds are substance P antagonists and are useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.
摘要翻译： PCT No.PCT / US93 / 06624 Sec。 371日期：1995年6月19日 102（e）1995年6月19日PCT PCT 1993年7月19日PCT公布。公开号WO94 / 11368 日期：5月26日，本发明涉及奎宁环衍生物（2S，3S）-N-（5-正丙基-2-甲氧基苯基）甲基-2-二苯基甲基-1-氮杂双环[2.2.2]辛-3-胺和其药学上可接受的盐。这些化合物是物质P拮抗剂，可用于治疗胃肠道疾病，炎性疾病，中枢神经系统疾病和疼痛。

6. 发明授权

US5859011A Dihydropyridine derivatives as bradykinin antagonist 失效
标题翻译：二氢吡啶衍生物作为缓激肽拮抗剂
公开(公告)号：US5859011A
公开(公告)日：1999-01-12
申请号：US793561
申请日：1997-07-01
申请人： Fumitaka Ito , Hiroshi Kondo , David L. Hageman , John A. Lowe, III , Susumu Nakanishi , Fredric J. Vinick
发明人： Fumitaka Ito , Hiroshi Kondo , David L. Hageman , John A. Lowe, III , Susumu Nakanishi , Fredric J. Vinick
IPC分类号： C07D487/08 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/495 , A61K31/505 , A61P9/00 , A61P11/00 , A61P17/00 , A61P25/04 , A61P29/00 , A61P31/12 , A61P37/08 , A61P43/00 , C07D211/90 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D451/04 , C07D453/02 , C07D471/08 , A61K31/50
CPC分类号： C07D451/04 , C07D211/90 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D453/02
摘要： Compound of formula (1) and their pharmaceutically acceptable salts wherein A1,A2,R1, R2,R3,R4,X are as defined in the specification have excellent bradykinin antagonistic activity. ##STR1##
摘要翻译： PCT No.PCT / IB95 / 00400 Sec。 371日期1997年7月1日 102（e）日期1997年7月1日PCT提交1995年5月26日PCT公布。出版物WO96 / 06082 日期：1996年2月29日，式（1）化合物及其药学上可接受的盐，其中A1，A2，R1，R2，R3，R4，X如说明书中所定义，具有优异的缓激肽拮抗活性。（一）

7. 发明授权

US5807867A Quinuclidine derivatives 失效
标题翻译：奎宁环衍生物
公开(公告)号：US5807867A
公开(公告)日：1998-09-15
申请号：US211120
申请日：1994-05-23
申请人： Fumitaka Ito , Hiroshi Kondo , Masami Nakane , Kaoru Shimada , John Adams Lowe, III , Terry Jay Rosen
发明人： Fumitaka Ito , Hiroshi Kondo , Masami Nakane , Kaoru Shimada , John Adams Lowe, III , Terry Jay Rosen
IPC分类号： C07D453/02 , A01N43/90 , A61K20060101 , A61K31/395 , A61K31/435 , A61K31/439 , A61K31/44 , A61K31/445 , A61P1/00 , A61P1/16 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P29/00 , A61P43/00 , C07D20060101 , C07D453/00 , C07D453/04 , C07D471/10
CPC分类号： C07D453/02
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is methoxy and R.sup.2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.
摘要翻译： PCT No.PCT / US92 / 03317。 371日期1994年5月23日 102（e）日期1994年5月23日PCT提交1992年4月28日PCT公布。出版物WO92 / 21677 日期：1992年12月10日化学式为其中R 1为甲氧基且R 2选自甲基，乙基，异丙基，仲丁基和叔丁基的式和这些化合物的药学上可接受的盐。这些化合物是物质P拮抗剂，可用于治疗胃肠道疾病，炎性疾病，中枢神经系统疾病和疼痛。

8. 发明授权

US5939433A Quinuclidine derivatives 失效
标题翻译：奎宁环衍生物
公开(公告)号：US5939433A
公开(公告)日：1999-08-17
申请号：US846909
申请日：1997-04-30
申请人： Fumitaka Ito , Hiroshi Kondo , Masami Nakane , Kaoru Shimada , John Adams Lowe, III , Terry Jay Rosen
发明人： Fumitaka Ito , Hiroshi Kondo , Masami Nakane , Kaoru Shimada , John Adams Lowe, III , Terry Jay Rosen
IPC分类号： C07D453/02 , A01N43/90 , A61K20060101 , A61K31/395 , A61K31/435 , A61K31/439 , A61K31/44 , A61K31/445 , A61P1/00 , A61P1/16 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P29/00 , A61P43/00 , C07D20060101 , C07D453/00 , C07D453/04 , C07D471/10
CPC分类号： C07D453/02
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is methoxy and R.sup.2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.
摘要翻译：下式的化合物其中R1是甲氧基，R2选自甲基，乙基，异丙基，仲丁基和叔丁基; 和这些化合物的药学上可接受的盐。这些化合物是物质P拮抗剂，可用于治疗胃肠道疾病，炎性疾病，中枢神经系统疾病和疼痛。

9. 发明授权

US06303602B1 Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists 失效
标题翻译：吡咯烷基和吡咯啉基乙胺化合物作为κ激动剂
公开(公告)号：US06303602B1
公开(公告)日：2001-10-16
申请号：US09770512
申请日：2001-01-26
申请人： Fumitaka Ito , Hiroshi Kondo
发明人： Fumitaka Ito , Hiroshi Kondo
IPC分类号： A61K31401
CPC分类号： C07D213/82 , C07D207/10 , C07D207/12 , C07D207/20 , C07D207/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： A compound of the following formula: or a salt thereof, wherein A is hydrogen, halo, hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, furanyl or thienyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
摘要翻译：下式的化合物或其盐，其中A是氢，卤素，羟基; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar1是任选取代的苯基; Ar 2是选自苯基，萘乙基，呋喃基或噻吩基的芳基或杂芳基，芳基或杂芳基任选被取代; R1是氢，羟基或C1-C4烷基; 并且R 2和R 3独立地选自任选取代的C 1 -C 7烷基，C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基或R 2和R 3与它们所连接的氮原子一起形成任选取代的吡咯烷，哌啶或吗啉环。这些化合物可用作κ激动剂。

10. 发明授权

US06294557B1 Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists 失效
标题翻译：吡咯烷基和吡咯啉基乙胺化合物作为κ激动剂
公开(公告)号：US06294557B1
公开(公告)日：2001-09-25
申请号：US09771030
申请日：2001-01-26
申请人： Fumitaka Ito , Hiroshi Kondo
发明人： Fumitaka Ito , Hiroshi Kondo
IPC分类号： A61K314439
CPC分类号： C07D213/82 , C07D207/10 , C07D207/12 , C07D207/20 , C07D207/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
摘要翻译：下式的化合物及其盐，其中A是氢，卤素，羟基等; 虚线表示任选的双键，条件是如果虚线是双键，则A不存在; Ar1是任选取代的苯基等; Ar 2是选自苯基，萘乙基，吡啶基等的芳基或杂芳基，芳基或杂芳基任选被取代; R1是氢，羟基，C1-C4烷基等; 并且R2和R3独立地选自任选取代的C 1 -C 7烷基，C 3 -C 6环烷基，C 2 -C 6烯基，C 2 -C 6炔基等，或者R 2和R 3与它们所连接的氮原子一起形成任选取代的吡咯烷，哌啶或吗啉环。这些化合物可用作κ激动剂。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式