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1. 发明申请

WO2004089366A1 BICYCLIC COMPOUNDS AS NR2B RECEPTOR ANTAGONISTS 审中-公开
标题翻译：双环化合物作为NR2B受体拮抗剂
公开(公告)号：WO2004089366A1
公开(公告)日：2004-10-21
申请号：PCT/IB2004/001177
申请日：2004-04-01
申请人： PFIZER JAPAN, INC. , PFIZER INC. , ANDO, Kazuo , KAWAI, Makoto , KAWAMURA, Mitsuhiro , MATSUMIZU, Miyako , MORITA, Asato , SAKURADA, Isao
发明人： ANDO, Kazuo , KAWAI, Makoto , KAWAMURA, Mitsuhiro , MATSUMIZU, Miyako , MORITA, Asato , SAKURADA, Isao
IPC分类号： A61K31/4184
CPC分类号： C07D239/94 , C07D209/08 , C07D215/12 , C07D215/26 , C07D231/56 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/26 , C07D261/20 , C07D263/56 , C07D471/04
摘要： This invention provides a compound of the formula (I) wherein R 1 and R 2 independently represent a hydrogen atom or the like; X represents a covalent bond or the like: A represents a bicyclic, aromatic, saturated or partially unsaturated heterocyclic or carbocyclic group having from 8 to 12 ring atoms; or the like: B represents a phenyl group or a heteroaryl group having from 5 to 6 ring atoms or the like: These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物，其中R 1和R 2独立地表示氢原子等; X表示共价键或类似物：A表示具有8至12个环原子的双环，芳族，饱和或部分不饱和的杂环或碳环基团; B表示苯基或具有5〜6个环原子的杂芳基等：这些化合物可用于治疗NMDA NR2B受体过度活化引起的疾病状况，例如哺乳动物的疼痛等。本发明还提供了包含上述化合物的药物组合物。

2. 发明申请

WO2005080317A2 THERAPEUTIC AMIDE DERIVATIVES 审中-公开
标题翻译：治疗酰胺衍生物
公开(公告)号：WO2005080317A2
公开(公告)日：2005-09-01
申请号：PCT/IB2005/000258
申请日：2005-02-01
申请人： PFIZER JAPAN, INC. , PFIZER INC. , KAWAI, Makoto , KAWAMURA, Mitsuhiro , SAKURADA, Isao , MORITA, Asato
发明人： KAWAI, Makoto , KAWAMURA, Mitsuhiro , SAKURADA, Isao , MORITA, Asato
IPC分类号： C07C235/00
CPC分类号： C07C235/48 , C07C2601/14 , C07D207/34 , C07D209/34 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/227 , C07D215/48 , C07D231/14 , C07D231/56 , C07D233/90 , C07D235/26 , C07D237/04 , C07D237/24 , C07D249/04 , C07D263/38 , C07D277/68 , C07D303/22 , C07D309/06 , C07D317/72 , C07D401/12 , C07D405/06 , C07D405/12
摘要： The present invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: A and B independently represent CH 2 or O, with the proviso that A and B are not simultaneously O; Cy represents one of the following Formula (II) optionally substituted by one to three groups selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl, C 1-6 alkylamino and amino; R 1 and R 2 are independently selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl and C 3-8 cycloalkyl; n represents an integer from 0-4; X is hydrogen, hydroxy, halogen or C 1-6 alkoxy; Y is oxy, thio, a 1-4 membered alkylene, a 2-4 membered alkylene ether, 2-4 membered alkylene thioether or an oxyethyleneoxy group, optionally substituted by 1 to 4 groups independently selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy and C 1-6 haloalkyl; Z is CH or N; and p represents an integer from 0-5 when Z is CH or 0-4 when Z is N; when p represents 2 or more, two of R 2 s may be taken together with the carbon atoms to which they are attached to form a 5-8 membered cycloalkyl ring to processes for the preparation of, intermediates used in the preparation of, compositions containing such compounds and the uses of such compounds as antagonists of the NMDA NR2B receptor.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：A和B独立地表示CH 2或O，条件是A和B不同时为O; Cy表示任选被一至三个选自羟基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6烷基氨基和氨基的基团取代的下式（II）之一。 R 1和R 2独立地选自羟基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基和C 3-8环烷基; n表示0-4的整数; X是氢，羟基，卤素或C 1-6烷氧基; Y是氧基，硫代，1-4元亚烷基，2-4元亚烷基醚，2-4元亚烷基硫醚或氧化乙烯氧基，任选被1至4个独立地选自羟基，卤素，C 1-6烷基， C 1-6烷氧基和C 1-6卤代烷基; Z是CH或N; 当Z为CH时，p表示0-5的整数，Z为N时为0〜4的整数。当p表示2或更多时，R 2中的两个可以与它们所连接的碳原子一起形成5-8元环烷基环，以制备用于制备中间体的中间体，含有这些化合物的组合物以及这些化合物作为NMDA NR2B受体的拮抗剂的用途。

3. 发明申请

WO2006097808A1 BENZIMIDAZOLONE DERIVATIVES AS CB2 RECEPTOR LIGANDS 审中-公开
标题翻译：苯并咪唑衍生物作为CB2受体配体
公开(公告)号：WO2006097808A1
公开(公告)日：2006-09-21
申请号：PCT/IB2006/000521
申请日：2006-03-02
申请人： PFIZER JAPAN INC. , PFIZER INC. , ANDO, Kazuo , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
发明人： ANDO, Kazuo , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
IPC分类号： C07D235/26 , C07D401/06 , C07D403/12 , C07D413/12 , C07D417/12 , C07D405/06 , C07D471/04 , A61K31/4168 , A61P29/00
CPC分类号： C07D471/04 , C07D235/26 , C07D401/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R 1 , R 2 and R 3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or bronchitis.
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：A，B，R 1，R 2和R 3， / SUP>各自如本文所述，并且含有这些化合物的组合物和这些化合物在治疗由CB2受体结合活性介导的病症（例如但不限于炎性疼痛，伤害性疼痛，神经性疼痛，纤维肌痛）慢性腰痛，内脏痛，急性脑缺血，疼痛，慢性疼痛，急性疼痛，疱疹后神经痛，神经病，神经痛，糖尿病性神经病，HIV相关神经病，神经损伤，类风湿性关节炎疼痛，骨关节炎疼痛，背痛，癌症疼痛，牙痛，纤维肌痛，神经炎，坐骨神经痛，炎症，神经变性疾病，咳嗽，支气管收缩，肠易激综合征（IBS），炎性肠病（IBD），结肠炎，脑血管缺血，呕吐如癌症化疗诱发呕吐，类风湿关节炎哮喘，克罗恩病，溃疡性结肠炎，哮喘，皮炎，季节性过敏性鼻炎，胃食管反流病（GERD），便秘，腹泻，功能性胃肠道疾病，皮肤T细胞淋巴瘤，多发性硬化症，骨关节炎，牛皮癣，系统性红斑狼疮，糖尿病青光眼，骨质疏松症，肾小球性肾炎，肾缺血，肾炎，肝炎，脑卒中，血管炎，心肌梗塞，脑缺血，可逆性气道梗阻，成人呼吸道疾病综合征，慢性阻塞性肺病（COPD），隐源性纤维化性肺泡炎或支气管炎。

4. 发明申请

WO2005035523A1 FUSED LACTAM COMPOUNDS 审中-公开
标题翻译： FUSED LACTAM化合物
公开(公告)号：WO2005035523A1
公开(公告)日：2005-04-21
申请号：PCT/IB2004/003125
申请日：2004-09-27
申请人： PFIZER JAPAN INC. , PFIZER INC. , ANDO, Kazuo , HIROTA, Masako , KAWAI, Makoto , SHIMOKAWA, Hirohisa
发明人： ANDO, Kazuo , HIROTA, Masako , KAWAI, Makoto , SHIMOKAWA, Hirohisa
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： This invention provides a compound the formula (I), wherein R 1 represents an aryl group having from 6 to 10 ring carbon atoms etc.; R 2 represents a hydrogen atom etc., n epresents 0, 1 or 2; said heteroaryl group is unsubstituted or substituted and said ary is substituted by at least one substituer,t selected from the group consisting of substituents a; said substituents a are selected from the group 10 consisting of halogen ate ms, alkyl groups having from 1 to 6 carbon atoms etc.; or a pharmaceutically ac eptable ester of such compound, or a pharmaceutically ac eptable salt thereof. These compou ds are useful for the treatment of disease conditions caused 15 by overactivation of N DA NR2B receptor such of pain, stroke, traumatic brain injury, Parkinson's disease, Alzheimer's disease, depression, anxiety, migraine, or the like in mammalian, especially humans. This invention also provides a pharmaceutical composi ion comprising the above compound.
摘要翻译：本发明提供式（I）化合物，其中R 1表示具有6〜10个环碳原子的芳基等; R 2表示氢原子等，n表示0,1或2; 所述杂芳基是未取代的或取代的，并且所述芳基被至少一个取代基取代，t选自取代基a; 所述取代基a选自卤素原子团组成的组10，具有1至6个碳原子的烷基等; 或这种化合物的药学上可接受的酯，或其药学上可接受的盐。这些药物可用于治疗由哺乳动物特别是人类中的NDA NR2B受体过度活化引起的疾病状况，例如疼痛，中风，创伤性脑损伤，帕金森病，阿尔茨海默氏病，抑郁症，焦虑症，偏头痛等。。本发明还提供了包含上述化合物的药物组合物。

5. 发明申请

WO2004054579A1 2-PYRIDYL AND 2-PYRIMIDYL CYCLOALKYLENE AMIDE COMPOUNDS AS NR2B RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NR2B受体拮抗剂的2-吡啶基和2-吡啶基环丙烯酰胺化合物
公开(公告)号：WO2004054579A1
公开(公告)日：2004-07-01
申请号：PCT/IB2003/005757
申请日：2003-12-05
申请人： PFIZER JAPAN INC. , PFIZER INC. , KAWAI, Makoto , NAKAMURA, Hiroshi , SHIMOKAWA, Hirohisa
发明人： KAWAI, Makoto , NAKAMURA, Hiroshi , SHIMOKAWA, Hirohisa
IPC分类号： A61K31/4418
CPC分类号： C07D213/65
摘要： This invention provides a compound of the Formula (I), wherein R 1 represents Formula (II), wherein R 5 represents a hydroxy group or the like; R 6 represents a hydrogen atom or the like. Z represents a carbon or a nitrogen atom: R 2 represents a hydrogen atom or the like: R 3 represents a hydrogen or the like: A represents a cycloalkylene or the like: X represents a covalent bond or the like: R 4 represents an aryl or the like. These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such as pain, or the like in mammals. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物，其中R 1表示式（II），其中R 5表示羟基等; R 6表示氢原子等。 Z表示碳原子或氮原子：R 2表示氢原子等：R 3表示氢原子等：A表示亚环烷基等：X表示共价键等：R 4代表芳基等。这些化合物可用于治疗哺乳动物中NMDA NR2B受体（例如疼痛）的过度活化引起的疾病状况。本发明还提供了包含上述化合物的药物组合物。

6. 发明申请

WO2008032164A2 BENZIMIDAZOLONE DERIVATIVES 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO2008032164A2
公开(公告)日：2008-03-20
申请号：PCT/IB2007/002583
申请日：2007-09-03
申请人： PFIZER PRODUCTS INC. , ANDO, Kazuo , BUCHLER, Ingrid, Price , HEDGE, Shridhar Gajanan , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
发明人： ANDO, Kazuo , BUCHLER, Ingrid, Price , HEDGE, Shridhar Gajanan , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
CPC分类号： C07D413/06 , A61K31/16 , C07D235/26 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D413/14 , C07D471/04
摘要： This invention relates to compounds and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) or pharmaceutically acceptable salts thereof, wherein: A, B, R 1 , R 2 and R 3 are each as described herein. These compounds are useful in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, spasticity, epilepsy, Tourette's syndrome, Parkinson's disease, neuroprotection, anxiety, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, cachexia, nausea, emesis, chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasodialation, hypertension, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis and bronchitis.
摘要翻译：本发明涉及用于治疗哺乳动物受试者（包括人）中由CB1受体活性介导的病症的化合物和方法，其包括向需要这种治疗的哺乳动物施用治疗有效量的式（I）化合物或其药学上可接受的盐，其中：A，B，R 1，R 2和R 3各自如本文所述。这些化合物可用于治疗由CB2受体结合活性介导的病症，例如但不限于炎性疼痛，伤害性疼痛，神经性疼痛，纤维肌痛，慢性腰痛，内脏痛，急性脑缺血，疼痛，慢性疼痛，急性疼痛，疱疹后神经痛，神经病，神经痛，糖尿病性神经病，HIV相关神经病，神经损伤，类风湿性关节炎疼痛，骨关节炎疼痛，背痛，癌症疼痛，牙痛，纤维肌痛，神经炎，坐骨神经痛，炎症，神经变性疾病，痉挛性，癫痫，Tourette综合征，帕金森病，神经保护，焦虑，咳嗽，支气管收缩，肠易激综合征（IBS），炎性肠病（IBD），结肠炎，脑血管缺血，恶病质，恶心，呕吐，化疗诱发呕吐，类风湿关节炎，哮喘，克罗恩病，溃疡性结肠炎，哮喘，皮炎，季节性过敏性鼻炎，胃食管反流病（GERD），便秘功能性胃肠道疾病，皮肤T细胞淋巴瘤，多发性硬化，骨关节炎，牛皮癣，系统性红斑狼疮，糖尿病，青光眼，骨质疏松症，肾小球性肾炎，肾缺血，肾炎，肝炎，脑中风，血管扩张，高血压，血管炎，心肌梗死，脑缺血，可逆性气道阻塞，成人呼吸道疾病综合征，慢性阻塞性肺疾病（COPD），隐源性纤维化肺泡炎和支气管炎。

7. 发明公开

EP1861377A1 BENZIMIDAZOLONE DERIVATIVES AS CB2 RECEPTOR LIGANDS 有权
标题翻译：苯并咪唑酮衍生物CB2受体配体
公开(公告)号：EP1861377A1
公开(公告)日：2007-12-05
申请号：EP06710527.0
申请日：2006-03-02
申请人： Pfizer, Inc.
发明人： ANDO, Kazuo , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
IPC分类号： C07D235/26 , C07D401/06 , C07D403/12 , C07D413/12 , C07D417/12 , C07D405/06 , C07D471/04 , A61K31/4168 , A61P29/00
CPC分类号： C07D471/04 , C07D235/26 , C07D401/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or bronchitis.

8. 发明公开

EP0790981A1 ARYLOXYCYCLOALKENYL AND ARYLOXYIMINOCYCLOALKENYLHYDROXYUREAS AS 5-LIPOXYGENASE INHIBITORS 失效
标题翻译：作为5-脂氧合酶抑制剂的芳氧基环烷基和芳氧基亚氨基环烷基甲基氢氧化物
公开(公告)号：EP0790981A1
公开(公告)日：1997-08-27
申请号：EP95918112.0
申请日：1995-05-26
申请人： PFIZER PHARMACEUTICALS INC. , PFIZER INC.
发明人： KAWAI, Akiyoshi , KAWAI, Makoto , STEVENS, Rodney, W.
IPC分类号： A61K , C07C , C12N , C07C275 , A01N47 , A61K31 , A61P29 , C07C67 , C07C69 , C07C273 , C07C309 , C07C313 , C07C317 , C07C323 , C07D213 , C07D215 , C07D307 , C07D333
CPC分类号： C07C275/64
摘要： The present invention provides a compound of formula (I), wherein Ar is (a) phenyl, naphthyl and biphenyl, each optionally substituted with C1-4 alkyl, C1-4 haloalkyl, C1-4 hydroxyalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C2-4 alkoxyalkoxy, C1-4 alkylthio, hydroxy, halo, cyano, amino, C1-4 alkylamino, di (C2-8) alkylamino, C2-6 alkanoylamino, carboxy, C2-6 alkoxycarbonyl, or optionally substituted phenyl, phenoxy, phenylthio or phenylsulfinyl or (b) furyl, benzo[b]furyl, thienyl, benzo[b]thienyl, pyridyl or quinolyl, each optionally substituted with C1-4 alkyl, C1-4 haloalkyl, halo, C1-4 alkoxy, optionally-substituted phenyl, phenoxy or phenylthio, X is C1-C4 alkylene, C2-C4 alkenylene, -(CHR1)m-Q?1-(CHR2)¿n-, -O-(CHR1)jQ2- and -(CHR1)-O-N = in which the N = moiety is attached to the cycloakene ring; and in which Q1 is O, S, SO, SO¿2, NR?3, CH = N-O or CO, Q2 is O, S, SO, SO¿2? or NR?3, and R1, R2 and R3¿ are each hydrogen or C¿1?-C4 alkyl, m and n are each an integer from 0 to 4 and j is an integer from 1 to 4; p is an integer of 1 or 2; Y is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C2-4 alkoxyalkyl, C1-4 alkylthio, hydroxy, halo, cyano or amino; Z is hydrogen or C1-4 alkyl; and M is hydrogen, a pharmaceutically acceptable cation or a pharmaceutically acceptable metabolically cleavable group. Further the invention provides a pharmaceutical composition for treating a medical condition for which a 5-lipoxygenase inhibitor is needed in a mammalian subject which comprises a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. Preferably the medical condition is an inflammatory disease, allergy or cardiovascular diseases.
摘要翻译：本发明提供了式（I）化合物，其中Ar是（a）各自任选被C 1-4烷基，C 1-4卤代烷基，C 1-4羟基烷基，C 1-4烷氧基，C 1 -C 4烷氧基， C1-4烷基硫基，羟基，卤素，氰基，氨基，C1-4烷基氨基，二（C2-8）烷基氨基，C2-6烷酰基氨基，羧基，C2-6烷氧基羰基或任选取代的苯基，苯氧基，苯硫基或苯基亚磺酰基或（b）各自任选被C 1-4烷基，C 1-4卤代烷基，卤素，C 1-4烷氧基任选取代的呋喃基，苯并[b]呋喃基，噻吩基，苯并[b]噻吩基，吡啶基或喹啉基，任选取代的苯基，苯氧基或苯硫基，X为C 1 -C 4亚烷基，C 2 -C 4亚烯基， - （CHR 1）m Q 1 1-（CHR 2）n - ， - O-（CHR 1）j Q 2 - 和 - （CHR 1） -ON =其中N =部分与环烯环连接; 其中Q1是O，S，SO，SO2，NR3，CH = N-O或CO，Q2是O，S，SO，SO2- 或NR 3 3，且R 1，R 2和R 3各自为氢或C 1 -C 4烷基，m和n各自为0-4的整数，j为1-4的整数; p是1或2的整数; Y是氢，C1-4烷基，C1-4卤代烷基，C1-4烷氧基，C2-4烷氧基烷基，C1-4烷硫基，羟基，卤素，氰基或氨基; Z是氢或C 1-4烷基; M是氢，药学上可接受的阳离子或药学上可接受的代谢可裂解基团。此外，本发明提供了用于治疗哺乳动物受试者中需要5-脂氧合酶抑制剂的医学病症的药物组合物，其包含治疗有效量的本发明化合物和药学上可接受的载体。优选的医学病症是炎性疾病，变态反应或心血管疾病。

9. 发明授权

EP1861377B1 BENZIMIDAZOLONE DERIVATIVES AS CB2 RECEPTOR LIGANDS 有权
标题翻译：苯并咪唑酮衍生物CB2受体配体
公开(公告)号：EP1861377B1
公开(公告)日：2010-12-29
申请号：EP06710527.0
申请日：2006-03-02
申请人： Pfizer, Inc.
发明人： ANDO, Kazuo , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
IPC分类号： C07D235/26 , C07D401/06 , C07D403/12 , C07D413/12 , C07D417/12 , C07D405/06 , C07D471/04 , A61K31/4168 , A61P29/00
CPC分类号： C07D471/04 , C07D235/26 , C07D401/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or bronchitis.

10. 发明授权

EP0790981B1 ARYLOXYCYCLOALKENYL AND ARYLOXYIMINOCYCLOALKENYLHYDROXYUREAS AS 5-LIPOXYGENASE INHIBITORS 失效
标题翻译：作为5-脂氧合酶抑制剂的芳氧基环烷基和芳氧基亚氨基环烷基甲基氢氧化物
公开(公告)号：EP0790981B1
公开(公告)日：1999-09-08
申请号：EP95918112.4
申请日：1995-05-26
申请人： PFIZER INC.
发明人： KAWAI, Akiyoshi , KAWAI, Makoto , STEVENS, Rodney, W.
IPC分类号： C07C275/64 , A61K31/17
CPC分类号： C07C275/64
摘要： The present invention provides a compound of formula (I), wherein Ar is (a) phenyl, naphthyl and biphenyl, each optionally substituted with C1-4 alkyl, C1-4 haloalkyl, C1-4 hydroxyalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C2-4 alkoxyalkoxy, C1-4 alkylthio, hydroxy, halo, cyano, amino, C1-4 alkylamino, di (C2-8) alkylamino, C2-6 alkanoylamino, carboxy, C2-6 alkoxycarbonyl, or optionally substituted phenyl, phenoxy, phenylthio or phenylsulfinyl or (b) furyl, benzo[b]furyl, thienyl, benzo[b]thienyl, pyridyl or quinolyl, each optionally substituted with C1-4 alkyl, C1-4 haloalkyl, halo, C1-4 alkoxy, optionally-substituted phenyl, phenoxy or phenylthio, X is C1-C4 alkylene, C2-C4 alkenylene, -(CHR )m-Q -(CHR )n-, -O-(CHR )jQ - and -(CHR )-O-N = in which the N = moiety is attached to the cycloakene ring; and in which Q is O, S, SO, SO2, NR , CH = N-O or CO, Q is O, S, SO, SO2 or NR , and R , R and R are each hydrogen or C1-C4 alkyl, m and n are each an integer from 0 to 4 and j is an integer from 1 to 4; p is an integer of 1 or 2; Y is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C2-4 alkoxyalkyl, C1-4 alkylthio, hydroxy, halo, cyano or amino; Z is hydrogen or C1-4 alkyl; and M is hydrogen, a pharmaceutically acceptable cation or a pharmaceutically acceptable metabolically cleavable group. Further the invention provides a pharmaceutical composition for treating a medical condition for which a 5-lipoxygenase inhibitor is needed in a mammalian subject which comprises a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. Preferably the medical condition is an inflammatory disease, allergy or cardiovascular diseases.
摘要翻译：本发明提供了式（I）化合物，其中Ar是（a）各自任选被C 1-4烷基，C 1-4卤代烷基，C 1-4羟基烷基，C 1-4烷氧基，C 1 -C 4烷氧基， C1-4烷基硫基，羟基，卤素，氰基，氨基，C1-4烷基氨基，二（C2-8）烷基氨基，C2-6烷酰基氨基，羧基，C2-6烷氧基羰基或任选取代的苯基，苯氧基，苯硫基或苯基亚磺酰基或（b）各自任选被C 1-4烷基，C 1-4卤代烷基，卤素，C 1-4烷氧基任选取代的呋喃基，苯并[b]呋喃基，噻吩基，苯并[b]噻吩基，吡啶基或喹啉基，任选取代的苯基，苯氧基或苯硫基，X为C1-C4亚烷基，C2-C4亚烯基， - （CHR1）mQ1-（CHR2）n-，-O-（CHR'1 其中N =部分与环烯环连接;并且 - （CHR 1）-ON = 并且其中Q 1是O，S，SO，SO 2，NR 3，CH = NO或CO，Q 2是O，S，SO，SO 2或NR 3，并且R 1， R 2和R 3各自为氢或C 1 -C 4烷基，m和n各自为0-4的整数，j为1-4的整数; p是1或2的整数; Y是氢，C1-4烷基，C1-4卤代烷基，C1-4烷氧基，C2-4烷氧基烷基，C1-4烷硫基，羟基，卤素，氰基或氨基; Z是氢或C 1-4烷基; M是氢，药学上可接受的阳离子或药学上可接受的代谢可裂解基团。此外，本发明提供了用于治疗哺乳动物受试者中需要5-脂氧合酶抑制剂的医学病症的药物组合物，其包含治疗有效量的本发明化合物和药学上可接受的载体。优选的医学病症是炎性疾病，变态反应或心血管疾病。

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