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公开(公告)号:US20060205676A1
公开(公告)日:2006-09-14
申请号:US11240867
申请日:2005-09-30
申请人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy Lowinger , Karl Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy Lowinger , Karl Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号: A61K31/7052 , A61K31/444 , A61K31/4436
CPC分类号: C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要: Pyrimidine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
摘要翻译: 其中R 1表示其中R 11为氢,C 1-6烷基,卤素,羟基,C 1 -C 6烷基, 1-12烷氧基,硝基,氨基,C 1-6烷基磺酰基氨基,C 1-6烷氧基羰基,C 1-6烷基, (C 1-6烷基)氨基,C 1-6烷酰基氨基,苯基C 1-6烷基氨基,苯基磺酰基氨基,C 1 -C 6烷基氨基, ,或-O-(CH 2)n - n - R 111; R 2表示氢或卤素; R 3表示氢,-CR 31,32,32,33, R 4是氢,氨基甲酰基,CN,羧基等; R 5是氨基,C 1-6烷基氨基,C 1-6烷基氨基等,或其盐。 该化合物具有优异的抗炎活性和其他生物活性。
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公开(公告)号:US20060100246A1
公开(公告)日:2006-05-11
申请号:US11240728
申请日:2005-09-30
申请人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy Lowinger , Karl Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy Lowinger , Karl Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号: A61K31/444 , A61K31/4436 , C07D409/02 , C07D401/02
CPC分类号: C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要: This invention is to provide a process for producing 2-amino-4,6-disubstituted nicotinic acid ester analogs and salts thereof, comprising the reaction shown by the following scheme. The ester analogs can be prepared in one pot, and in good yield by using tertiary alkyl cyanoacetate. Furthermore, the method is useful for preparing derivatives of various analogs of the ester, e.g. alkyl substituted and aryl substituted analogs.
摘要翻译: 本发明提供一种制备2-氨基-4,6-二取代的烟酸酯类似物及其盐的方法,其包括如下方案所示的反应。 酯类似物可以在一锅中制备,并且通过使用氰基乙酸叔烷酯以良好的产率制备。 此外,该方法可用于制备酯的各种类似物的衍生物,例如。 烷基取代和芳基取代的类似物。
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公开(公告)号:US06984649B1
公开(公告)日:2006-01-10
申请号:US10402500
申请日:2003-03-28
申请人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号: A61K31/4545 , C07D409/14 , C07D211/68 , C07D213/73
CPC分类号: C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents 1.2.3.6-tetrahydro-pyridine, or —CR31R32R33 wherein R31 represents H or C1-6 alkyl and R32 and R33 are joined to form a 5-8 membered saturated ring optionally containing up to three heteroatoms; R4 is carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
摘要翻译: 吡啶化合物,其通式如下:其中R 1表示其中R 11为氢,C 1-6烷基,卤素,羟基,C 1-12烷氧基,硝基,氨基,C 1-6烷基磺酰基氨基,C 1-6烷氧基羰基,C 1-6烷基, (C 1-6烷基)氨基,C 1-6烷酰基氨基,苯基C 1-6烷基氨基,苯基磺酰基氨基,C 1 -C 6烷基氨基, ,或-O-(CH 2)n - n - R 111; R 2表示氢或卤素; R 3表示1.2.3.6-四氢 - 吡啶或-CR 31,其中R 1,R 2,R 3, SUP> 31表示H或C 1-6烷基,R 32和R 33连接形成5-8 任选地含有至多三个杂原子的饱和环; R 4是氨基甲酰基,CN,羧基等; R 5是氨基,C 1-6烷基氨基,C 1-6烷基氨基等,或其盐。 该化合物具有优异的抗炎活性和其他生物活性。
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公开(公告)号:US06562811B1
公开(公告)日:2003-05-13
申请号:US09956618
申请日:2001-09-18
申请人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号: A61K3154
CPC分类号: C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di(C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33, or —NR34R35; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
摘要翻译: 吡啶化合物,其通式如下:其中-R 1表示其中R 11为氢,C 1-6烷基,卤素,羟基,C 1-12烷氧基,硝基,氨基,C 1-6烷基磺酰基氨基,C 1-6烷氧基羰基,C 1-6烷基氨基,二( C 1-6烷酰基氨基,C 1-6烷酰基氨基,苯基C 1-6烷基氨基,苯磺酰基氨基或-O-(CH 2)n -R 111; R2代表氢或卤素; R3表示氢,-CR31R32R33或-NR34R35; R4是氢,氨基甲酰基,CN,羧基等; R5是氨基,C1-6烷基氨基,二C1-6烷基氨基等或其盐。 该化合物具有优异的抗炎活性和其他生物活性。
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公开(公告)号:US07435743B2
公开(公告)日:2008-10-14
申请号:US11240867
申请日:2005-09-30
申请人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshiro , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuiyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshiro , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuiyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号: A61K31/4418 , A61K31/444 , A61K31/4436 , C07D213/22 , C07D409/04 , C07D213/73
CPC分类号: C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要: Pyrimidine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
摘要翻译: 其中R 1表示其中R 11为氢,C 1-6烷基,卤素,羟基,C 1 -C 6烷基, 1-12烷氧基,硝基,氨基,C 1-6烷基磺酰基氨基,C 1-6烷氧基羰基,C 1-6烷基, (C 1-6烷基)氨基,C 1-6烷酰基氨基,苯基C 1-6烷基氨基,苯基磺酰基氨基,C 1 -C 6烷基氨基, ,或-O-(CH 2)n - n - R 111; R 2表示氢或卤素; R 3表示氢,-CR 31,32,32,33, R 4是氢,氨基甲酰基,CN,羧基等; R 5是氨基,C 1-6烷基氨基,C 1-6烷基氨基等,或其盐。 该化合物具有优异的抗炎活性和其他生物活性。
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公开(公告)号:US07232909B2
公开(公告)日:2007-06-19
申请号:US11240728
申请日:2005-09-30
申请人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshiro , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuiyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人: Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshiro , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuiyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号: C07D213/73
CPC分类号: C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要: This invention is to provide a process for producing 2-amino-4,6-disubstituted nicotinic acid ester analogs and salts thereof, comprising the reaction shown by the following scheme. The ester analogs can be prepared in one pot, and in good yield by using tertiary alkyl cyanoacetate. Furthermore, the method is useful for preparing derivatives of various analogs of the ester, e.g. alkyl substituted and aryl substituted analogs.
摘要翻译: 本发明提供一种制备2-氨基-4,6-二取代的烟酸酯类似物及其盐的方法,其包括如下方案所示的反应。 酯类似物可以在一锅中制备,并且通过使用氰基乙酸叔烷酯以良好的产率制备。 此外,该方法可用于制备酯的各种类似物的衍生物,例如。 烷基取代和芳基取代的类似物。
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公开(公告)号:US07410986B2
公开(公告)日:2008-08-12
申请号:US10433377
申请日:2001-11-19
申请人: Toshiki Murata , Sachiko Sasaki , Takashi Yoshino , Yuka Ikegami , Tsutomu Masuda , Mitsuyuki Shimada , Takuya Shintani , Makoto Shimazaki , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Masaomi Umeda , Hiroshi Komura , Nagahiro Yoshida
发明人: Toshiki Murata , Sachiko Sasaki , Takashi Yoshino , Yuka Ikegami , Tsutomu Masuda , Mitsuyuki Shimada , Takuya Shintani , Makoto Shimazaki , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Masaomi Umeda , Hiroshi Komura , Nagahiro Yoshida
IPC分类号: A61K31/4412 , A61K31/4418 , C07D213/61 , C07D213/62
CPC分类号: C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85 , C07D401/10 , C07D401/12 , C07D405/12
摘要: 4-aryl pyrimidine compounds of general formula and salts thereof: wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is hydrogen or hydroxy; R3 is hydrogen, C1-6 alkyl, etc.; R4 is hydrogen, hydroxy, halogen, amino, etc.; R5 is hydroxy, amino, carboxy, etc.; R6 is hydrogen, carbamoyl, cyano, carboxy, C1-6 alkoxycarbonyl, etc. and R7 is amino or C1-6 alkanoylamino. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and the like.
摘要翻译: 通式为4-芳基嘧啶化合物及其盐:其中X为CH或N; R1是氢,卤素,C1-6烷基,C1-6烷氧基等; R2是氢或羟基; R3是氢,C1-6烷基等; R4是氢,羟基,卤素,氨基等; R5是羟基,氨基,羧基等; R6是氢,氨基甲酰基,氰基,羧基,C1-6烷氧基羰基等,R7是氨基或C1-6烷酰基氨基。 化合物(I)或其盐具有优异的抗炎活性等。
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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。
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9.
公开(公告)号:US20120277238A1
公开(公告)日:2012-11-01
申请号:US13388296
申请日:2010-07-29
IPC分类号: A61K31/496 , C07D471/04 , C07D491/052 , C07D487/04 , A61K31/4985 , A61K31/404 , A61K31/437 , A61P11/06 , A61P37/08 , A61P11/00 , A61P29/00 , A61P17/06 , A61P1/00 , A61P9/10 , A61P25/00 , C07D403/06
CPC分类号: A61K31/404 , A61K9/0019 , A61K9/1652 , A61K9/2054 , A61K9/4866 , A61K31/496 , A61K31/4985 , C07C2601/02 , C07D207/34 , C07D209/42 , C07D209/52 , C07D235/24 , C07D401/06 , C07D403/06 , C07D471/04 , C07D487/04 , C07D491/052
摘要: The present invention provides a compound which indicates a histamine H4 receptor modulating activity.A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is —O—, etc., n is an integer of 0 to 6; X is —N(R7)— or —O—; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is —C(R8)═ or —N═; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is ═O, ═S, etc.; B ring is a ring represented by the following formula: wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译: 本发明提供了表示组胺H 4受体调节活性的化合物。 由式(I)表示的化合物:其中A环是由下式表示的环:其中R1是取代或未取代的烷基等,W是-O-等,n是0-6的整数 ; X是-N(R 7) - 或-O-; R7是氢,取代或未取代的烷基等; Y是-C(R8)=或-N =; R8是氢,取代或未取代的烷基等; Z是═O,═S等; B环是由下式表示的环:其中R 10各自独立地是取代或未取代的烷基,卤素,羟基,取代或未取代的烷氧基,取代或未取代的氨基; R11,R12a和R12b各自独立地为氢或取代或未取代的烷基等; p为0〜4的整数,或其药学上可接受的盐或其溶剂合物。
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公开(公告)号:US08173841B2
公开(公告)日:2012-05-08
申请号:US13052482
申请日:2011-03-21
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 , A61K31/17
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 an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and 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, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
摘要翻译: 本发明涉及可用作药物制剂活性成分的四氢萘衍生物及其盐。 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,膀胱过度活动症,急迫性尿失禁,慢性疼痛,神经性疼痛 ,手术后疼痛,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。
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