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1. 发明授权

US07410986B2 4-6-diphenyl pyridine derivatives as antiinflammatory agents 失效
标题翻译： 4-二苯基吡啶衍生物作为抗炎剂
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。

2. 发明授权

US06562811B1 Pyridine derivatives 失效
标题翻译：吡啶衍生物
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。

3. 发明授权

US06984649B1 Pyridine derivatives 失效
标题翻译：吡啶衍生物
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。

4. 发明授权

US07232909B2 Pyridine derivatives 失效
标题翻译：吡啶衍生物
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。

5. 发明授权

US07435743B2 Pyridine derivatives 失效
标题翻译：吡啶衍生物
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。

6. 发明申请

US20060100246A1 Pyridine derivatives 失效
标题翻译：吡啶衍生物
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。

7. 发明申请

US20060205676A1 Pyridine derivatives 失效
标题翻译：吡啶衍生物
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。

8. 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。

9. 发明申请

US20060247260A1 Bis (hetero) aryl carboxamide derivatives for use as PG12 antagonists 审中-公开
标题翻译：用作PG12拮抗剂的双（杂）芳基甲酰胺衍生物
公开(公告)号：US20060247260A1
公开(公告)日：2006-11-02
申请号：US10544033
申请日：2004-01-28
申请人： Toshiki Murata , Takuya Shintani , Masaomi Umeda , Takashi Iino , Toshiya Moriwaki
发明人： Toshiki Murata , Takuya Shintani , Masaomi Umeda , Takashi Iino , Toshiya Moriwaki
IPC分类号： A61K31/513 , A61K31/4412 , A61K31/42 , A61K31/4152 , A61K31/195
CPC分类号： C07D207/325 , C07D211/14 , C07D213/64 , C07D213/82 , C07D231/12 , C07D231/14 , C07D239/34 , C07D261/18 , C07D333/38
摘要： This invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) in which Ar1 and Ar2 independently represent phenyl or a 5 or 6-membered heteroaromatic ring, R6 represents carboxyl or tetrazolyl, and the remaining variables are as defined in the text and claims, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 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, 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 the diseases also relate to PGI2.
摘要翻译：本发明涉及式（I）的芳基或杂芳基酰氨基烷烃衍生物，其中Ar 1和Ar 2独立地表示苯基或5或6元杂芳环R 6是代表羧基或四唑基，其余的变量如本文和权利要求中所定义，其可用作药物制剂的活性成分。本发明的芳基或杂芳基酰氨基烷烃具有PGI 2拮抗活性，可用于预防和治疗与PGI2活性相关的疾病。这些疾病包括泌尿系统疾病或紊乱，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，膀胱反应过度，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，因为这些疾病也与PGI2有关。

10. 发明申请

US20060135613A1 Carboxamides derivatives 审中-公开
标题翻译：甲酰胺衍生物
公开(公告)号：US20060135613A1
公开(公告)日：2006-06-22
申请号：US10517646
申请日：2003-06-12
申请人： Makoto Shimazaki , Osamu Sakurai , Kanako Hirai , Klaus Urbahns , Noriyuki Yamamoto , Satoru Yoshikawa , Masaomi Umeda , Masaomi Tajimi
发明人： Makoto Shimazaki , Osamu Sakurai , Kanako Hirai , Klaus Urbahns , Noriyuki Yamamoto , Satoru Yoshikawa , Masaomi Umeda , Masaomi Tajimi
IPC分类号： A61K31/198 , A61K31/195 , C07C237/38
CPC分类号： C07C235/34
摘要： The present invention relates to carboxamides which are useful as an active ingredient of pharmaceutical preparations. The carboxamides 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 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, 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 the diseases are 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羧酰胺。本发明的甲酰胺具有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紊乱，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，膀胱反应过度，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，因为通过用IP受体拮抗剂治疗来减轻疾病。

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