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1. 发明专利

BG104670A 4-(2-KETO-1-BENZIMIDAZOLINYL)PIPERIDINNE COMPOUNDS AS ORL1-RECEPTOR AGONISTS 未知
公开(公告)号：BG104670A
公开(公告)日：2001-05-31
申请号：BG10467000
申请日：2000-08-07
申请人： ITO FUMITAKA , KONDO HIROSHI , NOGUCHI HIROHIDE , OHASHI YORIKO , YAMAGISHI TATSUYA
发明人： ITO FUMITAKA , KONDO HIROSHI , NOGUCHI HIROHIDE , OHASHI YORIKO , YAMAGISHI TATSUYA
IPC分类号： A61K31/4427 , A61K31/4433 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P7/12 , A61P9/12 , A61P23/00 , A61P25/04 , A61P25/22 , A61P29/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D409/14 , A61K31/445
摘要： A compound of formula or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined above and are useful as ORL-1-receptor agonists, and useful as analgesics or the like in mammalian subjects. 7 claims

2. 发明专利

SK278788B6 THE QUINUCLIDINE DERIVATIVES, PREPARATION METHOD AND USE THEREOF 未知
公开(公告)号：SK278788B6
公开(公告)日：1998-02-04
申请号：SK390692
申请日：1992-04-28
申请人： ITO FUMITAKA , KONDO HIROSHI , SHIMADA KAORU , NAKANE MASAMI , LOWE JOHN ADAMS III. , ROSEN TERRY J.
发明人： ITO FUMITAKA , KONDO HIROSHI , SHIMADA KAORU , NAKANE MASAMI , LOWE JOHN ADAMS III , ROSEN TERRY J
IPC分类号： A01N43/90 , A61K20060101 , C07D453/02 , 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
摘要： The quinuclidine derivatives with a general formula (I), where R1 means methoxygroup and R2 represents substituent selected based on the file containing isopropyl group, terc.-buthyl group, methyl group, methyl group, ethyl group and sec.-buthyl group together with salts derived based on these compounds and acceptable from pharmaceutical point of view. These components represent the antagonistic substances closed to the substance P and they can be applied, when healing gastrointestinal failures, inflammation diseases, failures closed to the central nervous system, and when healing pains. The basis for preparation of these compounds is the compound with a general formula (II), being undertaken to hydrolytic or hydrogenolitic removal of methoxybenzyl group and as a result of the subsequent step the reaction with aldehyde is provided or the intermediate product is converted to amine and after that the reaction with a reductive agent or with other compounds, explained in the description is provided, while the requested product is prepared.

3. 发明申请

WO1996006082A1 DIHYGROPYRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS 审中-公开
标题翻译：二氢吡啶衍生物作为BRADYKININ ANTAGONISTS
公开(公告)号：WO1996006082A1
公开(公告)日：1996-02-29
申请号：PCT/IB1995000400
申请日：1995-05-26
申请人： PFIZER INC. , PFIZER PHARMACEUTICALS INC. , ITO, Fumitaka , KONDO, Hiroshi , HAGEMAN, David, L. , LOWE, John, A., III , NAKANISHI, Susumu , VINICK, Fredric, J.
发明人： PFIZER INC. , PFIZER PHARMACEUTICALS INC.
IPC分类号： C07D211/90
CPC分类号： C07D451/04 , C07D211/90 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D453/02
摘要： A compound of formula (I) and its pharmaceutically acceptable salts, wherein A and A are each halo; X is direct bond, CH2, CO, O, S, S(O) or S(O)2; R is selected from a variety of groups such as hydrogen; substituted or unsubstituted C1-4 alkyl; substituted or unsubstituted piperidinyl; substituted or unsubstituted C5-14 cycloalkyl, bicycloalkyl or tricycloalkyl; substituted or unsubstituted C7-14 azacyclo-, azabicyclo- or azatricyclo-alkyl; bicyclo C7-10 alkenyl; benzocyclo C5-7 alkyl; and heterocyclic; R is hydrogen, C1-4 alkyl, substituted or unsubstituted phenyl or heterocyclic; and R and R are each C1-5 alkyl. The novel dihydropyridine compounds of this invention have excellent bradykinin antagonistic activity and are thus useful for the treatment of inflammation, cardiovascular disease, pain, common cold, allergies, asthma, pancreatitis, burns, virus infection, head injury, multiple trauma or the like in mammalian, especially humans.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中A 1和A 2各自为卤素; X是直接键，CH2，CO，O，S，S（O）或S（O）2; R 1选自各种基团，例如氢; 取代或未取代的C 1-4烷基; 取代或未取代的哌啶基; 取代或未取代的C 5-14环烷基，双环烷基或三环烷基; 取代或未取代的C7-14氮杂环，氮杂双环或氮杂三环烷基; 双环C7-10烯基; 苯并环C5-7烷基; 和杂环; R 2是氢，C 1-4烷基，取代或未取代的苯基或杂环; R 3和R 4各自为C 1-5烷基。本发明的新型二氢吡啶化合物具有优异的缓激肽拮抗活性，因此可用于治疗炎症，心血管疾病，疼痛，感冒，过敏，哮喘，胰腺炎，烧伤，病毒感染，头部损伤，多发性创伤等哺乳动物，特别是人类。

4. 发明申请

WO1994008997A1 SUBSTITUTED BENZYLAMINOQUINUCLIDINES AS SUBSTANCE P ANTAGONISTS 审中-公开
标题翻译：作为物质的拮抗剂的取代苄基氨基
公开(公告)号：WO1994008997A1
公开(公告)日：1994-04-28
申请号：PCT/US1993009168
申请日：1993-09-30
申请人： PFIZER INC. , ITO, Fumitaka , SATAKE, Kunio , SHIMADA, Kaoru
发明人： PFIZER INC.
IPC分类号： C07D453/02
CPC分类号： C07F9/6561 , C07D453/02
摘要： Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I), and the pharmaceutically acceptable salts thereof, wherein Ar and Ar are each independently aryl or substituted aryl; R is alkyl having from 1 to 6 carbon atoms; R is hydrogen or alkyl having from 1 to 6 carbon atoms; and either X and Y are taken separately and they are each, independently, hydrogen, dialkylphosphoryl having 2 to 12 carbon atoms, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms or alkynyl having from 2 to 6 carbon atoms; or X and Y are taken together and they represent a hydrocarbon chain having 3, 4, or 5 carbon atoms, optionally containing up to 2 double bonds and optionally having 1 or 2 substituents selected from oxo, hydroxy and alkyl having from 1 to 6 carbon atoms; provided that when X and Y are taken together they are attached to adjacent carbon atoms; and provided that if either X or Y is hydrogen, then the other one must be alkenyl or alkynyl.
摘要翻译：用于治疗炎性疾病，中枢神经系统疾病和式（I）的其它病症的化合物及其药学上可接受的盐，其中Ar 1和Ar 2各自独立地为芳基或取代的芳基; R 1是具有1至6个碳原子的烷基; R 2是氢或具有1至6个碳原子的烷基; X和Y分别取代，它们各自独立地为氢，具有2至12个碳原子的二烷基磷酰基，具有1至6个碳原子的烷基，具有2至6个碳原子的烯基或具有2至6个碳原子的炔基原子; 或X和Y一起并且它们表示具有3,4或5个碳原子的烃链，任选地含有至多2个双键并且任选地具有1或2个选自氧代，羟基和具有1至6个碳原子的烷基的取代基原子; 条件是当X和Y一起取代时，它们连接到相邻的碳原子上; 并且条件是如果X或Y是氢，则另一个必须是烯基或炔基。

5. 发明申请

WO1992020676A1 SUBSTITUTED 3-AMINOQUINUCLIDINES 审中-公开
标题翻译：取代的3-氨基胆碱
公开(公告)号：WO1992020676A1
公开(公告)日：1992-11-26
申请号：PCT/US1992004002
申请日：1992-05-19
申请人： PFIZER INC. , ITO, Fumitaka , KOKURA, Toshihide , NAKANE, Masami , SATAKE, Kunio , WAKABAYASHI, Hiroaki
发明人： PFIZER INC.
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Compounds of formula (I), wherein W, Ar , Ar and Ar are defined as below; 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：其中W，Ar 1，Ar 2和Ar 3的式（I）化合物定义如下：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。

6. 发明申请

WO2005016913A8 TETRAHYDROISOQUINOLINE OR ISOCHROMAN COMPOUNDS AS ORL-1 RECEPTOR LIGANDS FOR THE TREATMENT OF PAIN AND CNS DISORDERS 审中-公开
标题翻译：作为用于治疗疼痛和中枢神经疾病的ORL-1受体配体的四氢喹诺酮或异喹啉化合物
公开(公告)号：WO2005016913A8
公开(公告)日：2006-04-20
申请号：PCT/IB2004002662
申请日：2004-08-09
申请人： PFIZER JAPAN INC , PFIZER , ITO FUMITAKA , HAYASHI SHIGEO , HASHIZUME YOSHINOBU , MIHARA SACHIKO
发明人： ITO FUMITAKA , HAYASHI SHIGEO , HASHIZUME YOSHINOBU , MIHARA SACHIKO
IPC分类号： C07D401/06 , A61K31/4747 , C07D407/06 , C07D471/10 , C07D471/12 , C07D471/20 , C07D491/10
CPC分类号： C07D401/06 , C07D471/10 , C07D471/20 , C07D491/10
摘要： This invention provides the compounds of formula (I), or its a pharmaceutically acceptable ester or amide of such compound, or a pharmaceutically acceptable salt thereof, wherein X 1 is NH; R 1 , R 2 , R 4 through R 6 and R 7 through R 11 are all hydrogen; R 3 is hydroxy; X 2 and X 3 are methylene; X 4 is a bond; and X 5 is a carbon atom, and the like. These compounds have ORLI -receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的这种化合物的酯或酰胺或其药学上可接受的盐，其中X 1是NH; R 1，R 2，R 4，R 4和R 7通过R 6和R 7通过 R 11都是氢; R 3是羟基; X 2和X 3是亚甲基; X 4是一个键; 和X 5是碳原子等。这些化合物具有ORLI-受体拮抗剂活性; 因此，可用于治疗诸如疼痛，各种CNS疾病等疾病或病症。

7. 发明申请

WO2003064425A1 N-SUBSTITUTED SPIROPIPERIDINE COMPOUNDS AS LIGANDS FOR ORL-1 RECEPTOR 审中-公开
标题翻译： N-取代的螺吡啶化合物作为ORL-1受体的配体
公开(公告)号：WO2003064425A1
公开(公告)日：2003-08-07
申请号：PCT/IB2003/000203
申请日：2003-01-16
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , ITO, Fumitaka , KOIKE, Hiroki , MORITA, Asato
发明人： ITO, Fumitaka , KOIKE, Hiroki , MORITA, Asato
IPC分类号： C07D487/06
CPC分类号： C07D401/06 , C07D487/06 , C07D487/10 , C07D491/10
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, ester or ether thereof, wherein R 1 through R 12 are independently hydrogen or the like; X 1 and X 2 are independently CH 2 or the like; R 13 is hydrogen or the like; or R 12 and R 13 taken together with three ring atoms of the quinoline ring separating said substituents form a heterocyclic ring; R 14 and R 15 are hydrogen or the like or these groups taken together form oxo; and the dotted line represents a single or double bond. These compounds are ligands for ORL-1 receptor and especially are antagonists for said receptor.
摘要翻译：式（I）化合物或其药学上可接受的盐，酯或醚，其中R 1至R 12独立地为氢等; X 1和X 2独立地是CH 2等; R 13是氢等; 或R 12和R 13与分离所述取代基的喹啉环的三个环原子一起形成杂环; R 14和R 15是氢等，或这些基团一起形成氧代; 虚线表示单键或双键。这些化合物是ORL-1受体的配体，特别是用于所述受体的拮抗剂。

8. 发明申请

WO1996030339A1 PYRROLIDINYL HYDROXAMIC ACID COMPOUNDS AND THEIR PRODUCTION PROCESS 审中-公开
标题翻译：吡咯烷酮酸式化合物及其制备方法
公开(公告)号：WO1996030339A1
公开(公告)日：1996-10-03
申请号：PCT/JP1996000820
申请日：1996-03-28
申请人： PFIZER INC. , PFIZER PHARMACEUTICALS INC. , ITO, Fumitaka
发明人： PFIZER INC. , PFIZER PHARMACEUTICALS INC.
IPC分类号： C07D207/12
CPC分类号： C07D213/54 , C07D207/12 , C07D295/13 , C07D307/79 , C07D405/12 , C07D409/12 , Y02P20/55
摘要： A compound of formula (I) and its pharmaceutically acceptable salt, wherein A is hydrogen, hydroxy or OY, wherein Y is a hydroxy protecting group; Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C1-C4 alkyl, C1-C4 alkoxy, CF3, C1-C4 alkoxy-C1-C4 alkyloxy, and carboxy-C1-C4 alkyloxy; X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl, C1-C4 alkylenedioxy, pyridyl, furyl and thienyl, these groups optionally being substituted with up to three substituents selected from halo, C1-C4 alkyl, C1-C4 alkoxy, hydroxy, NO2, CF3 and SO2CH3; and R is hydrogen, C1-C4 alkyl or a hydroxy protecting group. These compounds and pharmaceutical compositions containing them are useful as analgesic, anti-inflammatory, diuretic, anesthetic or neuroprotective agents, or an agent for stroke or treatment of functional bowel diseases such as abdominal pain, for the treatment of a mammalian subject, especially a human subject. Further, the present invention provides processes for producing the hydroxamic compounds of formula (I) and their intermediate compounds of formula (II).
摘要翻译：式（I）化合物及其药学上可接受的盐，其中A为氢，羟基或OY，其中Y为羟基保护基; Ar是任选被一个或多个选自卤素，羟基，C 1 -C 4烷基，C 1 -C 4烷氧基，CF 3，C 1 -C 4烷氧基-C 1 -C 4烷氧基和羧基-C 1 -C 4烷氧基的取代基取代的苯基; X是苯基，萘基，联苯基，茚满基，苯并呋喃基，苯并噻吩基，1-四氢萘酮-6-基，C 1 -C 4亚烷基二氧基，吡啶基，呋喃基和噻吩基，这些基团任选被至多三个选自卤素，C 1 -C 4 烷基，C 1 -C 4烷氧基，羟基，NO 2，CF 3和SO 2 CH 3; 和R是氢，C 1 -C 4烷基或羟基保护基。这些化合物和含有它们的药物组合物可用作止痛剂，抗炎药，利尿剂，麻醉剂或神经保护剂，或用于中风或治疗功能性肠病如腹痛的药剂，用于治疗哺乳动物受试者，特别是人学科。此外，本发明提供了制备式（I）的异羟肟酸化合物及其中间体式（II）化合物的方法。

9. 发明申请

WO2005016913A1 TETRAHYDROISOQUINOLINE OR ISOCHROMAN COMPOUNDS AS ORL-1 RECEPTOR LIGANDS FOR THE TREATMENT OF PAIN AND CNS DISORDERS 审中-公开
标题翻译：作为用于治疗疼痛和中枢神经疾病的ORL-1受体配体的四氢喹诺酮或异喹啉化合物
公开(公告)号：WO2005016913A1
公开(公告)日：2005-02-24
申请号：PCT/IB2004/002662
申请日：2004-08-09
申请人： PFIZER JAPAN, INC. , PFIZER, Inc. , ITO, Fumitaka , HAYASHI, Shigeo , HASHIZUME, Yoshinobu , MIHARA, Sachiko
发明人： ITO, Fumitaka , HAYASHI, Shigeo , HASHIZUME, Yoshinobu , MIHARA, Sachiko
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D471/10 , C07D471/20 , C07D491/10
摘要： This invention provides the compounds of formula (I), or its a pharmaceutically acceptable ester or amide of such compound, or a pharmaceutically acceptable salt thereof, wherein X 1 is NH; R 1 , R 2 , R 4 through R 6 and R 7 through R 11 are all hydrogen; R 3 is hydroxy; X 2 and X 3 are methylene; X 4 is a bond; and X 5 is a carbon atom, and the like. These compounds have ORLI -receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的这种化合物的酯或酰胺或其药学上可接受的盐，其中X 1是NH; R 1，R 2，R 4至R 6和R 7至R 11均为氢; R 3是羟基; X 2和X 3是亚甲基; X 4是一个键; X 5为碳原子等。这些化合物具有ORLI-受体拮抗剂活性; 因此，可用于治疗诸如疼痛，各种CNS疾病等疾病或病症。

10. 发明申请

WO2002088082A2 PROCESS FOR PREPARING HYDROXYPYRROLIDINYL ETHYLAMINE COMPOUNDS USEFUL AS KAPPA AGONISTS 审中-公开
标题翻译：用于制备羟基吡咯烷酮乙酰胺化合物的方法可用作KAPPA激动剂
公开(公告)号：WO2002088082A2
公开(公告)日：2002-11-07
申请号：PCT/IB2002/000924
申请日：2002-03-25
申请人： PFIZER PRODUCTS INC. , DEVRIES, Keith, Michael , COUTURIER, Michel, Andre , TUCKER, John, Lloyd , ANDRESEN, Brian, Michael , ITO, Fumitaka
发明人： DEVRIES, Keith, Michael , COUTURIER, Michel, Andre , TUCKER, John, Lloyd , ANDRESEN, Brian, Michael , ITO, Fumitaka
IPC分类号： C07D207/00
CPC分类号： C07D207/12
摘要： A process of preparing compounds having the formula I: (I) or an optical isomer or racemic or optically active mixture thereof, which are useful as selective kappa-receptor agonists.
摘要翻译：制备具有式I（I）的化合物或其旋光异构体或外消旋或光学活性混合物的方法，其可用作选择性κ-受体激动剂。

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