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1. 发明申请

WO2005092858A3 ALPHA ARYL OR HETEROARYL METHYL BETA PIPERIDINO PROPANAMIDE COMPOUNDS AS ORL1-RECEPTOR ANTAGONIST 审中-公开
公开(公告)号：WO2005092858A3
公开(公告)日：2005-10-06
申请号：PCT/IB2005/000751
申请日：2005-03-16
申请人： PFIZER JAPAN INC. , PFIZER INC. , HASHIZUME, Yoshinobu , HIROTA, Masako , MIHARA, Sachiko , NAKAMURA, Hiroshi , KOIKE, Hiroki , MATSUMOTO, Yukari
发明人： HASHIZUME, Yoshinobu , HIROTA, Masako , MIHARA, Sachiko , NAKAMURA, Hiroshi , KOIKE, Hiroki , MATSUMOTO, Yukari
IPC分类号： C07D221/20
摘要： This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 independently represent a hydrogen atom or the like; R 3 represents a hydrogen atom, or the like; R 4 represents a hydrogen atom or the like; (formula II) represents one of the following or the like; R 5 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxgen atom or the like and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

2. 发明申请

WO2006134486A2 ALPHA-(ARYL-OR HETEROARYL-METHYL)-BETA PIPERIDINO PROPANAMIDE COMPOUNDS AS ORL1-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为ORL1受体拮抗剂的ALPHA-（芳基或异丁基 - 甲基）-BETA哌啶丙酰胺化合物
公开(公告)号：WO2006134486A2
公开(公告)日：2006-12-21
申请号：PCT/IB2006/001642
申请日：2006-06-09
申请人： PFIZER JAPAN INC. , PFIZER INC. , HASHIZUME, Yoshinobu , HIROTA, Masako , KOIKE, Hiroki , MATSUMOTO, Yukari , MIHARA, Sachiko , NAKAMURA, Hiroshi
发明人： HASHIZUME, Yoshinobu , HIROTA, Masako , KOIKE, Hiroki , MATSUMOTO, Yukari , MIHARA, Sachiko , NAKAMURA, Hiroshi
IPC分类号： C07D451/06 , A61K31/46 , A61P25/04
CPC分类号： C07D451/06
摘要： This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 independently represent hydrogen or the like; R 3 and R 4 independently represents hydrogen or the like; R 5 represents aryl or the like; -X-Y- represents -CH 2 O- or the like; and n represents 0, 1 or 2.These compounds have ORL1 -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盐，其中R 1和R 2独立代表氢或类似物; R 3和R 4独立地表示氢等; R 5表示芳基等; -X-Y-表示-CH 2 O-等; 并且n代表0,1或2.这些化合物具有ORL1-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。

3. 发明申请

WO2006134485A1 ALPHA-(ARYL-OR HETEROARYL-METHYL)-BETA-PIPERIDINOPROPANOIC ACID COMPOUNDS AS ORL1-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为ORL1受体拮抗剂的ALPHA-（芳基或杂芳基 - 甲基） - 哌嗪 - 哌嗪二磷酸化合物
公开(公告)号：WO2006134485A1
公开(公告)日：2006-12-21
申请号：PCT/IB2006/001624
申请日：2006-06-08
申请人： PFIZER JAPAN INC. , PFIZER INC. , HASHIZUME, Yoshinobu , HIROTA, Masako , KOIKE, Hiroki , MATSUMOTO, Yukari , MIHARA, Sachiko , NAKAMURA, Hiroshi
发明人： HASHIZUME, Yoshinobu , HIROTA, Masako , KOIKE, Hiroki , MATSUMOTO, Yukari , MIHARA, Sachiko , NAKAMURA, Hiroshi
IPC分类号： C07D491/10 , A61K31/343
摘要： This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester or salt thereof, wherein R 1 and R 2 independently represent hydrogen or the like; R 3 represents aryl or the like; -X-Y- represents -CH 2 O- or the like; and n represents 0, 1 or 2. These compounds have ORL1 -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酯或盐，其中R 1和R 2独立代表氢或类似物; R 3表示芳基等; -X-Y-表示-CH 2 O-等; 并且n表示0,1或2.这些化合物具有ORL1-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。

4. 发明申请

WO2005092895A2 ALPHA ARYL OR HETEROARYL METHYL BETA PIPERIDINO PROPANOIC ACID COMPOUNDS AS ORL1-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为ORL1受体拮抗剂的ALPHA ARYL或HETEROARYL METHYL BETA PIPERIDINO丙酸化合物
公开(公告)号：WO2005092895A2
公开(公告)日：2005-10-06
申请号：PCT/IB2005/000679
申请日：2005-03-16
申请人： PFIZER JAPAN INC. , PFIZER INC. , HASHIZUME, Yoshinobu , HIROTA, Masako , MIHARA, Sachiko , NAKAMURA, Hiroshi , KOIKE, Hiroki , MATSUMOTO, Yukari
发明人： HASHIZUME, Yoshinobu , HIROTA, Masako , MIHARA, Sachiko , NAKAMURA, Hiroshi , KOIKE, Hiroki , MATSUMOTO, Yukari
IPC分类号： C07D491/00
CPC分类号： C07D221/20 , C07D401/06 , C07D471/06 , C07D471/10 , C07D491/10 , C07D513/10
摘要： This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 independently represent a hydrogen atom or the like; R 3 represents an aryl group having from 6 to 10 ring atoms or the like ; X represents an oxygen atom , or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonists activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译：本发明提供了式（I）化合物或这类化合物或其药学上可接受的盐的药学上可接受的酯，其中R 1和R 2独立地表示氢原子等; R 3表示具有6〜10个环原子等的芳基; X表示氧原子等; Y表示氧原子等; 并且n表示整数0,1或2.这些化合物具有ORL1-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。

5. 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。

6. 发明申请

WO2008090434A1 SUBSTITUTED N-BICYCLICALKYL BICYCLIC CARBOXYAMIDE COMPOUNDS 审中-公开
标题翻译：取代的N-双羟基苄基双环羧酰胺化合物
公开(公告)号：WO2008090434A1
公开(公告)日：2008-07-31
申请号：PCT/IB2008/000125
申请日：2008-01-16
申请人： PFIZER JAPAN INC. , PFIZER INC. , ANDO, Koji , MIHARA, Sachiko , MAGAYAMA, Satoshi , NAKAO, Kuzanari
发明人： ANDO, Koji , MIHARA, Sachiko , MAGAYAMA, Satoshi , NAKAO, Kuzanari
IPC分类号： C07D215/14 , C07D217/04 , C07D401/12 , A61K31/44 , A61P25/00
CPC分类号： C07D401/12 , C07D215/14 , C07D217/04
摘要： This invention provides compounds of the formula (I): and their use for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. The invention also provides pharmaceutical compositions comprising the above compounds.
摘要翻译：本发明提供式（I）化合物及其用于治疗哺乳动物VR1受体如过度活化如疼痛等引起的疾病状况的用途。本发明还提供包含上述化合物的药物组合物。

7. 发明申请

WO2007010390A1 INDAZOLECARBOXAMIDE DERIVATIVES AS 5HT4 RECEPTOR AGONISTS 审中-公开
标题翻译：作为5HT4受体激动剂的异吲哚酰胺衍生物
公开(公告)号：WO2007010390A1
公开(公告)日：2007-01-25
申请号：PCT/IB2006/002120
申请日：2006-07-14
申请人： PFIZER JAPAN INC. , PFIZER INC. , ISHIBASHI, Asako , KAWAMURA, Kiyoshi , KATO, Tomoki , MIHARA, Sachiko , MORITA, Mikio
发明人： ISHIBASHI, Asako , KAWAMURA, Kiyoshi , KATO, Tomoki , MIHARA, Sachiko , MORITA, Mikio
IPC分类号： C07D403/12 , C07D401/12 , A61K31/435 , A61K31/41 , A61P1/00 , A61P9/00 , A61P25/06 , A61P25/28 , A61P3/10
CPC分类号： C07D401/12 , C07D403/12 , C07D405/14
摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R 1 , R 2 , R 3 , A and m are each as described herein and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT 4 agonistic activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中：R 1，R 2，R 3， A和m各自如本文所述，含有这些化合物的组合物和这些化合物在治疗由5-HT 4激动剂活性介导的病症（例如但不限于胃食管反流）疾病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病和呼吸暂停综合征。

8. 发明申请

WO2003057688A2 OXO OR OXY-PYRIDINE COMPOUNDS AS 5-HT4 RECEPTOR MODULATORS 审中-公开
标题翻译： OXO或OXY-吡啶化合物作为5-HT4受体调节剂
公开(公告)号：WO2003057688A2
公开(公告)日：2003-07-17
申请号：PCT/IB2002/005600
申请日：2002-12-20
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , UCHIDA, Chikara , MIHARA, Sachiko , MORITA, Mikio , KAWAMURA, Kiyoshi , NUKUI, Seiji , STOBIE, Alan , GYMER, Geoffrey, Edward
发明人： UCHIDA, Chikara , MIHARA, Sachiko , MORITA, Mikio , KAWAMURA, Kiyoshi , NUKUI, Seiji , STOBIE, Alan , GYMER, Geoffrey, Edward
IPC分类号： C07D401/12
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14
摘要： This invention provides compounds of the formula (I) and (II) or the phannaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R 1 is hydrogen or halo; R 2 and R 3 are independently hydrogen or C 1-6 alkyl; R 4 and R 5 are independently hydrogen or C 1-6 alkyl; R 6 is hydrogen, C l-12 alkyl, C 1-6 alkoxy (C 1-6 )alkyl or C 1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C 3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R 7 and R 8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R 9 is C 1-6 alkyl or C 3-8 cycloalkyl; R 10 is C 1-6 alkyl or NR 11 R 12 ; L is (CR 11 R 12 )n or NR 11 ; M is NR 11 or (CR 11 R 12 )n ; R 11 and R 12 are independently hydrogen or C 1-6 alkyl; n is an integer from 0 to 5; and. m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C 1-6 alkyl; with the proviso that when R 9 is C 1-6 alkyl, L is not NR 11 . These compounds have 5-HT 4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）和（II）化合物或其药学上可接受的酯及其药学上可接受的盐：其中R 1是氢或卤素; R 2和R 3独立地是氢或C 1-6烷基; R 4和R 5独立地是氢或C 1-6烷基; R 6是氢，C 1-12烷基，C 1-6烷氧基（C 1-6）烷基或被至多3个选自C 3-8环烷基，芳基，杂芳基和杂环基; R 7和R 8是氢或一起可以形成具有一个或两个碳原子的亚烷基链; R 9是C 1-6烷基或C 3-8环烷基; R 10是C 1-6烷基或NR 11 R 12; L是（CR 11 R 12）n或NR 11; M是NR 11或（CR 11 R 12）n; R 11和R 12独立地是氢或C 1-6烷基; n为0〜5的整数，和。 m为0〜2的整数; 所述杂环，芳基和杂芳基是未取代的或被至少一个选自卤素和C 1-6烷基的取代基取代; 条件是当R 9为C 1-6烷基时，L不为NR 11。这些化合物具有5-HT 4受体的结合活性，因此可用于治疗哺乳动物，特别是人类的胃食管反流病，非溃疡性消化不良，肠易激综合征等。本发明还提供了包含上述化合物的药物组合物。

9. 发明申请

WO2003057688A3 OXO OR OXY-PYRIDINE COMPOUNDS AS 5-HT4 RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2003057688A3
公开(公告)日：2003-07-17
申请号：PCT/IB2002/005600
申请日：2002-12-20
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC. , UCHIDA, Chikara , MIHARA, Sachiko , MORITA, Mikio , KAWAMURA, Kiyoshi , NUKUI, Seiji , STOBIE, Alan , GYMER, Geoffrey, Edward
发明人： UCHIDA, Chikara , MIHARA, Sachiko , MORITA, Mikio , KAWAMURA, Kiyoshi , NUKUI, Seiji , STOBIE, Alan , GYMER, Geoffrey, Edward
IPC分类号： C07D401/12
摘要： This invention provides compounds of the formula (I) and (II) or the phannaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R 1 is hydrogen or halo; R 2 and R 3 are independently hydrogen or C 1-6 alkyl; R 4 and R 5 are independently hydrogen or C 1-6 alkyl; R 6 is hydrogen, C l-12 alkyl, C 1-6 alkoxy (C 1-6 )alkyl or C 1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C 3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R 7 and R 8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R 9 is C 1-6 alkyl or C 3-8 cycloalkyl; R 10 is C 1-6 alkyl or NR 11 R 12 ; L is (CR 11 R 12 )n or NR 11 ; M is NR 11 or (CR 11 R 12 )n ; R 11 and R 12 are independently hydrogen or C 1-6 alkyl; n is an integer from 0 to 5; and. m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C 1-6 alkyl; with the proviso that when R 9 is C 1-6 alkyl, L is not NR 11 . These compounds have 5-HT 4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

10. 发明公开

EP1896479A1 ALPHA-(ARYL-OR HETEROARYL-METHYL)-BETA-PIPERIDINOPROPANOIC ACID COMPOUNDS AS ORL1-RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ALPHA（芳基或杂芳基甲基）-β-PIPERIDINOPROPANSÄUREVERBINDUNGENAS ORL1受体的拮抗剂
公开(公告)号：EP1896479A1
公开(公告)日：2008-03-12
申请号：EP06765538.1
申请日：2006-06-08
申请人： Pfizer, Inc.
发明人： HASHIZUME, Yoshinobu , HIROTA, Masako , KOIKE, Hiroki , MATSUMOTO, Yukari , MIHARA, Sachiko , NAKAMURA, Hiroshi
IPC分类号： C07D491/10 , A61K31/343
摘要： This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester or salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 represents aryl or the like; -X-Y- represents -CH2O- or the like; and n represents 0, 1 or 2. These compounds have ORL1 -receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

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