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1. 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。

2. 发明申请

US20070167458A1 Tetrahydro-naphthalene and urea derivatives 失效
标题翻译：四氢萘和脲衍生物
公开(公告)号：US20070167458A1
公开(公告)日：2007-07-19
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 , Hiroaki Yuasa , Jang Gupta , Yasuhiro Tsukimi , 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 , Hiroaki Yuasa , Jang Gupta , Yasuhiro Tsukimi , Fumihiko Hayashi
IPC分类号： A61K31/495 , C07D211/40 , 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Q 1a，Q 2a，Q 3a和Q 4a定义，E表示式（IV ）或（V）其中＃表示与分子的连接位置和Q 1b，Q 2b，Q 3b，Q 4b α，α，α，α，α，α，α，α，α和R a a都被定义。

3. 发明申请

US20080058377A1 Bicyclic Amide, Carbamate or Urea Derivatives as Vanilloid Receptor Modulators 审中-公开
标题翻译：双环酰胺，氨基甲酸酯或尿素衍生物作为香草酸受体调节剂
公开(公告)号：US20080058377A1
公开(公告)日：2008-03-06
申请号：US10578490
申请日：2004-10-26
申请人： Muneto Mogi , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto , Klaus Urbahns , Fumihiko Hayashi , Yasuhiro Tsukimi , Jang Gupta , Hiroaki Yuasa
发明人： Muneto Mogi , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto , Klaus Urbahns , Fumihiko Hayashi , Yasuhiro Tsukimi , Jang Gupta , Hiroaki Yuasa
IPC分类号： A61K31/445 , A61K31/16 , A61K31/17 , A61P29/00 , C07C275/28 , C07C233/00 , A61P13/00 , A61K31/195
CPC分类号： C07D295/155 , C07C235/38 , C07C275/32 , C07C2601/14 , C07C2602/08 , C07C2602/10
摘要： This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
摘要翻译：本发明涉及可用作药物制剂活性成分的双环酰胺，氨基甲酸酯或脲衍生物及其盐。本发明的双环酰胺，氨基甲酸酯或尿素衍生物具有香草素受体（VR1）拮抗活性，可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗泌尿系统疾病或病症，例如逼尿肌过度活动症（膀胱过度活动症），尿失禁，神经源性逼尿肌过敏反应（逼尿肌hyperflexia），特发性逼尿肌过度活动（逼尿肌不稳定），良性前列腺增生和下尿路症状; 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，中风和炎性疾病如哮喘和慢性阻塞性肺（或气道）疾病（COPD）。

4. 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。

5. 发明申请

US20080045546A1 Tetradydro-Naphthalene And Urea Derivatives 审中-公开
标题翻译：十四氢萘和尿素衍生物
公开(公告)号：US20080045546A1
公开(公告)日：2008-02-21
申请号：US10575027
申请日：2004-10-02
申请人： Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pemerstorfer , Elke Reissmuller , Muneto Mogi , Takeshi Yura , Hiroshi Fujishima , Masanori Seki , Yuji Koriyama , Kayo Yasoshima , Keiko Misawa , Masaomi Tajimi , Noriyuki Yammoto , Klaus Urbahns , Fumihiko Hayashi , Yasuhiro Tsukimi , Jang Gupta
发明人： Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pemerstorfer , Elke Reissmuller , Muneto Mogi , Takeshi Yura , Hiroshi Fujishima , Masanori Seki , Yuji Koriyama , Kayo Yasoshima , Keiko Misawa , Masaomi Tajimi , Noriyuki Yammoto , Klaus Urbahns , Fumihiko Hayashi , Yasuhiro Tsukimi , Jang Gupta
IPC分类号： A61K31/519 , A61K31/44 , C07D211/68 , C07D213/06
CPC分类号： C07C275/32 , A61K31/167 , A61K31/17 , A61K31/357 , A61K31/42 , A61K31/433 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/455 , A61K31/4706 , A61K31/472 , A61K31/517 , A61K47/54 , C07C233/29 , C07C233/75 , C07C235/24 , C07C235/38 , C07C235/56 , C07C235/64 , C07C237/04 , C07C275/30 , C07C275/38 , C07C2602/08 , C07C2602/10 , C07D209/18 , C07D213/40 , C07D213/56 , C07D213/89 , C07D215/46 , C07D217/22 , C07D239/94 , C07D261/14 , C07D285/06 , C07D317/66
摘要： This invention relates to tetrahydro-naphthalene and urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene and urea derivatives of the present invention have vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
摘要翻译：本发明涉及四氢萘和脲衍生物及其盐，其可用作药物制剂的活性成分。本发明的四氢萘和脲衍生物具有香草素受体（VR1）拮抗活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗泌尿系统疾病或病症，如逼尿肌过度活动（膀胱过度活动），尿失禁，神经源性逼尿肌过度活动（逼尿肌hyperflexia），特发性逼尿肌过度活动（逼尿肌不稳定），良性前列腺增生和下尿路症状; 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，中风和炎性疾病如哮喘和慢性阻塞性肺（或气道）疾病（COPD）。

6. 发明申请

US20070010568A1 Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists 审中-公开
标题翻译：取代的氮杂双环己烷衍生物作为毒蕈碱受体拮抗剂
公开(公告)号：US20070010568A1
公开(公告)日：2007-01-11
申请号：US10544520
申请日：2003-02-07
申请人： Anita Mehta , Bruhaspathy Miriyala , Naresh Kumar , Jang Gupta
发明人： Anita Mehta , Bruhaspathy Miriyala , Naresh Kumar , Jang Gupta
IPC分类号： A61K31/403 , C07D209/02
CPC分类号： C07D471/08
摘要： This invention relates to derivatives of substituted azabicyclo hexanes. The compound of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.
摘要翻译：本发明涉及取代的氮杂双环己烷的衍生物。本发明化合物可用作毒蕈碱受体拮抗剂，可用于治疗通过毒蕈碱受体介导的呼吸道，尿路和胃肠道系统的各种疾病。本发明还涉及制备本发明化合物的方法，含有本发明化合物的药物组合物以及通过毒蕈碱受体介导的疾病的治疗方法。

7. 发明申请

US20060247225A1 3,6-Disubstituted azabicyclo hexane derivatives as muscarinic receptor antagonists 失效
公开(公告)号：US20060247225A1
公开(公告)日：2006-11-02
申请号：US10543585
申请日：2003-01-23
申请人： Anita Mehta , Arundutt Silamkoti , Naresh Kumar , Jang Gupta
发明人： Anita Mehta , Arundutt Silamkoti , Naresh Kumar , Jang Gupta
IPC分类号： A61K31/55 , A61K31/46
CPC分类号： C07D401/04 , C07D209/52 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06 , C07D409/04
摘要： This invention generally relates to derivatives of 3,6 disubstituted azabicyclo hexanes. The compounds of this invention can function as muscarinic receptor antagonists and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.

8. 发明申请

US20060122253A1 3,6-disubstituted azabicyclo [3.1.0]hexane derivatives useful as muscarinic receptor antagonists 失效
标题翻译：用作毒蕈碱受体拮抗剂的3,6-二取代的氮杂双环[3.1.0]己烷衍生物
公开(公告)号：US20060122253A1
公开(公告)日：2006-06-08
申请号：US10523208
申请日：2002-07-31
申请人： Anita Mehta , Arundutt Silamkoti , Kirandeep Kaur , Jang Gupta
发明人： Anita Mehta , Arundutt Silamkoti , Kirandeep Kaur , Jang Gupta
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D209/52
摘要： This invention generally relates to the derivatives of 3,6 disubstituted azabicyclo[3.1.0]hexanes. The compounds of this invention are muscarinic receptor antagonists which are useful, inter-alia, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.
摘要翻译：本发明一般涉及3,6-二取代的氮杂双环[3.1.0]己烷的衍生物。本发明的化合物是毒蕈碱受体拮抗剂，其特别用于治疗通过毒蕈碱受体介导的呼吸，尿和胃肠道系统的各种疾病。本发明还涉及制备本发明化合物的方法，含有本发明化合物的药物组合物和通过毒蕈碱受体介导的疾病的治疗方法。

9. 发明申请

US20060004083A1 Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo (3.1.0) hexane derivatives as muscarinic receptor antagonists 失效
标题翻译：含有3,6-二取代的氮杂二环（3.1.0）己烷衍生物的氟磺酰氨基作为毒蕈碱受体拮抗剂
公开(公告)号：US20060004083A1
公开(公告)日：2006-01-05
申请号：US10525439
申请日：2002-08-23
申请人： Anita Mehta , Jang Gupta
发明人： Anita Mehta , Jang Gupta
IPC分类号： A61K31/403 , C07D209/02
CPC分类号： C07D209/94 , C07D209/52
摘要： This invention generally relates to the derivatives of novel 3,6 disubstituted azabicyclo[3.1.0] hexane's. The compounds of this invention are MUSCARINIC receptor antagonists which are useful, inter-ail for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through MUSCARINIC receptors. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through MUSCARINIC receptors.
摘要翻译：本发明一般涉及新的3,6-二取代的氮杂双环[3.1.0]己烷的衍生物。本发明的化合物是MUSCARINIC受体拮抗剂，其可用于治疗通过MUSCARINIC受体介导的呼吸，尿和胃肠道系统的各种疾病。本发明还涉及制备本发明化合物的方法，含有本发明化合物的药物组合物和通过MUSCARINIC受体介导的疾病的治疗方法。

10. 发明申请

US20070287732A1 Substituted Azabicyclo Hexane Derivatives as Muscarinic Receptor Antagonists 失效
标题翻译：取代的氮杂双环己烷衍生物作为毒蕈碱受体拮抗剂
公开(公告)号：US20070287732A1
公开(公告)日：2007-12-13
申请号：US10552617
申请日：2003-04-10
申请人： Anita Mehta , Arundutt Silamkoti , Jang Gupta
发明人： Anita Mehta , Arundutt Silamkoti , Jang Gupta
IPC分类号： A61K31/445 , A61P11/00 , A61P13/00 , C07D211/22
CPC分类号： C07D209/52 , C07D405/06
摘要： This invention generally relates to derivatives of substituted azabicyclo hexanes of formula I. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.
摘要翻译：本发明一般涉及式I的取代的氮杂二环己烷的衍生物。本发明的化合物可用作毒蕈碱受体拮抗剂，并且可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病。本发明还涉及制备本发明化合物的方法，含有本发明化合物的药物组合物和通过毒蕈碱受体介导的疾病的治疗方法。

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