专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

31. 发明授权

US07615557B2 Tetrahydro-naphthalene and urea derivatives 失效
标题翻译：四氢萘和脲衍生物
公开(公告)号：US07615557B2
公开(公告)日：2009-11-10
申请号：US10574122
申请日：2004-09-22
申请人： Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmuller , Jean De Vry , Muneto Mogi , Klaus Urbahns , Takeshi Yura , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto , Yasuhiro Tsukimi , Hiroaki Yuasa , Jang Gupta , Fumihiko Hayashi
发明人： Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmuller , Jean De Vry , Muneto Mogi , Klaus Urbahns , Takeshi Yura , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto , Yasuhiro Tsukimi , Hiroaki Yuasa , Jang Gupta , Fumihiko Hayashi
IPC分类号： A01N43/40 , A61K31/445 , A61K31/4965 , C07D295/00 , C07D241/04
CPC分类号： C07D295/215 , C07D211/62 , C07D401/04
摘要： This invention relates to a hydroxy-tetrahydro-naphthalene or an urea derivative formula (I) and salts thereof which are useful as active ingredients of pharmaceutical preparations, wherein A represents formula (II) or (III) wherein # represents the connection position to the molecule and Q1a, Q2a, Q3a and Q4a are defined, and E represents formula (IV) or (V) wherein # represents the connection position to the molecule and Q1b, Q2b, Q3b, Q4b, Q5b, R1b, na, ma, Xa and Ra are defined.
摘要翻译：本发明涉及用作药物制剂活性成分的羟基 - 四氢 - 萘或脲衍生物式（I）及其盐，其中A表示式（II）或（III），其中＃表示与分子和Q1a，Q2a，Q3a和Q4a，E表示式（IV）或（V），其中＃表示与分子的连接位置，Q1b，Q2b，Q3b，Q4b，Q5b，R1b，na，ma，Xa 和Ra。

32. 发明申请

US20070129355A1 Pyrimidine derivatives useful for the treatment of diseases mediated by crth2 有权
标题翻译：可用于治疗由crth2介导的疾病的嘧啶衍生物
公开(公告)号：US20070129355A1
公开(公告)日：2007-06-07
申请号：US10554668
申请日：2004-04-14
申请人： Tai-wei Ly , Yuji Koriyama , Takashi Yoshino , Hiroki Sato , Kazuho Tanaka , Hiromi Sugimoto , Yoshihisa Manabe , Kevin Bacon , Klaus Urbahns , Masanori Seki , Takuya Shintani
发明人： Tai-wei Ly , Yuji Koriyama , Takashi Yoshino , Hiroki Sato , Kazuho Tanaka , Hiromi Sugimoto , Yoshihisa Manabe , Kevin Bacon , Klaus Urbahns , Masanori Seki , Takuya Shintani
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/506 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D239/42 , C07D239/30 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12
摘要： The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.
摘要翻译：本发明涉及式（I）的嘧啶衍生物及其盐，其可用作药物制剂的活性成分。本发明的嘧啶衍生物具有优异的CRTH2（G蛋白偶联化学引诱物受体，在Th2细胞上表达）拮抗活性，可用于预防和治疗与CRTH2活性相关的疾病，特别是用于治疗过敏性疾病，如哮喘，过敏性鼻炎，特应性皮炎和过敏性结膜炎; 嗜酸性粒细胞相关疾病，如中华综合征和鼻窦炎; 嗜碱性粒细胞相关疾病，如嗜碱性白血病，慢性荨麻疹和人类和其他哺乳动物的嗜碱性白细胞增多症; 以T淋巴细胞为特征的炎性疾病和白血球浸润如银屑病，湿疹，炎性肠病，溃疡性结肠炎，克罗恩病，COPD（慢性阻塞性肺病）和关节炎等。

33. 发明授权

US07094911B2 Biphenyl and biphenyl-analogous compounds as integrin antagonists 失效
标题翻译：联苯和联苯类似物作为整联蛋白拮抗剂
公开(公告)号：US07094911B2
公开(公告)日：2006-08-22
申请号：US10285073
申请日：2002-10-31
申请人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
发明人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
IPC分类号： C07D333/24 , C07D333/36 , C07D409/06 , A61K31/38 , A61P19/10
CPC分类号： C07D213/40 , C07C237/36 , C07C271/22 , C07C275/42 , C07C311/06 , C07C311/09 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/43 , C07C311/47 , C07C317/14 , C07C323/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/34 , C07D213/38 , C07D213/55 , C07D213/74 , C07D213/75 , C07D213/82 , C07D231/18 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/30 , C07D235/32 , C07D261/10 , C07D263/58 , C07D277/42 , C07D277/54 , C07D277/82 , C07D285/10 , C07D285/135 , C07D285/14 , C07D295/096 , C07D295/13 , C07D295/15 , C07D295/215 , C07D307/52 , C07D333/34 , C07D333/48 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
摘要翻译：本发明涉及联苯和联苯类似物，其作为药物组合物的制备和用途，作为整联蛋白拮抗剂，特别涉及用于治疗和预防癌症，动脉硬化，再狭窄，溶骨性疾病如骨质疏松和眼科疾病根据本发明的化合物具有式（1）其中R 1，R 2，U，V，A，B，W，R 3， SUP，C和R 4具有如权利要求中所定义的含义。

34. 发明申请

US20060166989A1 2-naphthamide derivatives 审中-公开
标题翻译： 2-萘甲酰胺衍生物
公开(公告)号：US20060166989A1
公开(公告)日：2006-07-27
申请号：US10517677
申请日：2003-05-30
申请人： Makoto Shimazaki , Osamu Sakurai , Toshiki Murata , Klaus Urbahns , Noriyuki Yamamoto , Satoru Yoshikawa , Masaomi Umeda , Masaomi Tajimi , Tsutomu Masuda , Takuya Shintani , Haruka Shimizu
发明人： Makoto Shimazaki , Osamu Sakurai , Toshiki Murata , Klaus Urbahns , Noriyuki Yamamoto , Satoru Yoshikawa , Masaomi Umeda , Masaomi Tajimi , Tsutomu Masuda , Takuya Shintani , Haruka Shimizu
IPC分类号： A61K31/537 , A61K31/44 , A61K31/195 , C07D213/55 , C07D265/30 , C07C237/40
CPC分类号： C07C235/66
摘要： The present invention relates to 2-naphthamides, which are useful as an active ingredient of pharmaceutical preparations. The 2-naphthamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benign prostatic hypertrophy (BPH), pro-statitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the disease is also alleviated by treatment with an IP receptor antagonist.
摘要翻译：本发明涉及可用作药物制剂活性成分的2-萘甲酰胺。本发明的2-萘甲酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体活性相关的疾病。这些疾病包括尿路疾病或病症如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱高反应性，良性前列腺肥大），pro-statitis，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺增生症，膀胱炎或自发性膀胱过敏反应。本发明的化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压血友病和出血; 和炎症，因为该疾病也通过用IP受体拮抗剂治疗而缓解。

35. 发明申请

US20060089371A1 Phenyl or heteroaryl amino alkane derivatives as ip receptor antagonist 审中-公开
标题翻译：苯基或杂芳基氨基烷烃衍生物作为ip受体拮抗剂
公开(公告)号：US20060089371A1
公开(公告)日：2006-04-27
申请号：US10534174
申请日：2003-10-29
申请人： Toshiki Murata , Masami Umeda , Satoru Yoshikawa , Klaus Urbahns , Jang Gupta , Osamu Sakurai
发明人： Toshiki Murata , Masami Umeda , Satoru Yoshikawa , Klaus Urbahns , Jang Gupta , Osamu Sakurai
IPC分类号： A61K31/506 , C07D403/02
CPC分类号： C07D213/64 , C07C229/36 , C07D213/74 , C07D231/38 , C07D239/42 , C07D241/20 , C07D261/14 , C07D277/42 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/10
摘要： The present invention relates to phenyl or heteroaryl amino alkane derivatives of formula (I) in which the groups Q1-Q4, Ar, and R1-R7 are as defined in the specification and claims. These materials are useful as active ingredients of pharmaceutical preparations. The phenyl or heteroaryl amino alkanes of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic activity. Such diseases include urological diseases or disorders as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since these diseases also are alleviated by treatment with an IP receptor antagonist. The application claims the compounds, pharmaceutical compositions containing them, and methods of treatment using them.
摘要翻译：本发明涉及式（I）的苯基或杂芳基氨基烷烃衍生物，其中基团Q 1，Q 4，Ar和R 1， SUP> -R 7如说明书和权利要求中所定义。这些材料可用作药物制剂的活性成分。本发明的苯基或杂芳基氨基烷烃具有IP受体拮抗活性，可用于预防和治疗与IP受体拮抗活性相关的疾病。这些疾病包括泌尿系统疾病或疾病如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱高反应性，良性前列腺肥大），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏。本发明的化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压血友病和出血; 和炎症，因为这些疾病也通过用IP受体拮抗剂治疗而缓解。本申请要求化合物，含有它们的药物组合物和使用它们的治疗方法。

36. 发明授权

US08129386B2 Fused azole-pyrimidine derivatives 有权
标题翻译：熔融唑 - 嘧啶衍生物
公开(公告)号：US08129386B2
公开(公告)日：2012-03-06
申请号：US12414257
申请日：2009-03-30
申请人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Jishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
发明人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Jishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.
摘要翻译：本发明涉及新型稠合吡唑嘧啶衍生物，其制备方法和含有它们的药物制剂。本发明的稠合唑类嘧啶衍生物对磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是PI3K-γ抑制作用，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节疾病，自身免疫疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性学科。

37. 发明申请

US20100322980A1 PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES MEDIATED BY CRTH2 有权
标题翻译：用于治疗由CRTH2介导的疾病的吡咯烷衍生物
公开(公告)号：US20100322980A1
公开(公告)日：2010-12-23
申请号：US12868663
申请日：2010-08-25
申请人： Tai-wei Ly , Yuji Koriyama , Takashi Yoshino , Hiroki Sato , Kazuho Tanaka , Hiromi Sugimoto , Yoshihisa Manabe , Kevin Bacon , Klaus Urbahns , Masanori Seki , Takuya Shintani
发明人： Tai-wei Ly , Yuji Koriyama , Takashi Yoshino , Hiroki Sato , Kazuho Tanaka , Hiromi Sugimoto , Yoshihisa Manabe , Kevin Bacon , Klaus Urbahns , Masanori Seki , Takuya Shintani
IPC分类号： A61K9/00 , A61K31/505 , A61K31/5377 , A61K31/506
CPC分类号： C07D239/42 , C07D239/30 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12
摘要： The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.
摘要翻译：本发明涉及式（I）的嘧啶衍生物及其盐，其可用作药物制剂的活性成分。本发明的嘧啶衍生物具有优异的CRTH2（G蛋白偶联化学引诱物受体，在Th2细胞上表达）拮抗活性，可用于预防和治疗与CRTH2活性相关的疾病，特别是用于治疗过敏性疾病，如哮喘，过敏性鼻炎，特应性皮炎和过敏性结膜炎; 嗜酸性粒细胞相关疾病，如中华综合征和鼻窦炎; 嗜碱性粒细胞相关疾病，如嗜碱性白血病，慢性荨麻疹和人类和其他哺乳动物的嗜碱性白细胞增多症; 以T淋巴细胞为特征的炎性疾病和白血球浸润如银屑病，湿疹，炎性肠病，溃疡性结肠炎，克罗恩病，COPD（慢性阻塞性肺病）和关节炎等。

38. 发明申请

US20090270388A1 FUSED AZOLE-PYRIMIDINE DERIVATIVES 有权
标题翻译：熔融的偶氮吡啶衍生物
公开(公告)号：US20090270388A1
公开(公告)日：2009-10-29
申请号：US12414257
申请日：2009-03-30
申请人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
发明人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
IPC分类号： A61K31/519 , C07D487/04 , A61K31/5377 , A61P29/00 , A61P37/00 , A61P3/10 , A61P35/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.
摘要翻译：本发明涉及新的稠合唑吡喃衍生物，其制备方法和含有它们的药物制剂。本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节疾病，自身免疫疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性学科。

39. 发明授权

US07544716B2 Tetrahydro-naphthalene derivatives as vanilloid receptor antagonists 失效
标题翻译：四氢萘衍生物作为香草素受体拮抗剂
公开(公告)号：US07544716B2
公开(公告)日：2009-06-09
申请号：US10537217
申请日：2003-11-28
申请人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： A61K31/17
CPC分类号： C07C275/32 , C07C2602/10 , C07D207/27 , C07D211/22 , C07D211/46 , C07D211/62 , C07D295/135
摘要： This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.
摘要翻译：本发明涉及式（I）的四氢 - 萘衍生物，其中可变基团如说明书和权利要求中所定义，以及其可用作药物制剂活性成分的互变异构体和立体异构形式及其盐。本发明的四氢 - 萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，敦促性尿失禁，膀胱过度活动症，慢性疼痛，神经性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎症性疾病，哮喘和COPD。公开并要求保护所述化合物，含有它们的药物组合物和使用它们的治疗方法。

40. 发明授权

US07381840B2 Tetrahydro-naphthalene derivatives 失效
标题翻译：四氢萘衍生物
公开(公告)号：US07381840B2
公开(公告)日：2008-06-03
申请号：US10537482
申请日：2003-11-28
申请人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： C07C273/00
CPC分类号： C07D295/088 , C07C233/29 , C07C233/75 , C07C235/42 , C07C237/40 , C07C275/32 , C07C275/38 , C07C275/40 , C07C275/42 , C07C317/32 , C07C323/44 , C07C2602/10 , C07D207/27 , C07D211/22 , C07D211/46 , C07D211/62 , C07D295/135
摘要： This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. They have the general formula (I) in which R1 represents hydrogen or C1-6 alkyl, and X represents —N(H)Y1, —(H)—C1-6 alkyleneY1, biphenyl or C1-6 alkyl substituted by biphenyl, and the group Y1 is an optionally substituted biphenyl. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
摘要翻译：本发明涉及四氢萘衍生物及其盐，其可用作药物制剂的活性成分。它们具有其中R 1表示氢或C 1-6烷基的通式（I），X表示-N（H）Y 1，， - （H）-C 1-6亚烷基，由联苯取代的联苯基或C 1-6烷基，以及基团 Y 1是任选取代的联苯。本发明的四氢 - 萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，膀胱过度活动症，急迫性尿失禁，慢性疼痛，神经性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎性疾病，哮喘和COPD。

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