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1. 发明授权

US5798357A Agent for prophylaxis and treatment of thromboxane A.sub.2 -mediated diseases 失效
标题翻译：用于预防和治疗血栓素A2介导的疾病的药剂
公开(公告)号：US5798357A
公开(公告)日：1998-08-25
申请号：US687604
申请日：1996-08-08
申请人： Ruriko Ikegawa , Teruaki Imada , Norifumi Nakamura , Keizo Tanikawa , Nobutomo Tsuruzoe
发明人： Ruriko Ikegawa , Teruaki Imada , Norifumi Nakamura , Keizo Tanikawa , Nobutomo Tsuruzoe
IPC分类号： C07D401/12 , A61K31/50 , A61P7/02 , A61P9/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P43/00 , A61K31/495
CPC分类号： A61K31/501 , A61K31/50
摘要： An agent for the prophylaxis or treatment of TXA.sub.2 -mediated diseases, particularly, a TXA.sub.2 synthetase inhibitor, which comprises a pyridazinone compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof as an active ingredient. The pyridazinone compound (I) and pharmacologically acceptable salts thereof used in the present invention have prophylactic and therapeutic activities against TXA.sub.2 -mediated diseases, particularly a TXA.sub.2 synthetase inhibitory action and are useful as an agent for the prophylaxis or treatment of TXA.sub.2 -mediated diseases, particularly as TXA.sub.2 synthetase inhibitors.
摘要翻译： PCT No.PCT / JP95 / 00244 Sec。 371日期：1996年8月8日 102（e）日期1996年8月8日PCT提交1995年2月20日PCT公布。第WO95 / 22329号公报日期1995年8月24日用于预防或治疗TXA2介导的疾病的药剂，特别是TXA2合成酶抑制剂，其包含式（I）的哒嗪酮化合物（I）其中每个符号如说明书或其药理学上可接受的盐作为活性成分。用于本发明的哒嗪酮化合物（I）及其药理学上可接受的盐具有抗TXA2介导的疾病，特别是TXA2合成酶抑制作用的预防和治疗活性，可用作预防或治疗TXA2介导的疾病，特别是作为TXA2合成酶抑制剂。

2. 发明授权

US5318968A 5-heteroarylamino-6-oxy-substituted 3(2H)-pyridazinones 失效
标题翻译： 5-杂芳基氨基-6-氧基取代的3（2H） - 哒嗪酮
公开(公告)号：US5318968A
公开(公告)日：1994-06-07
申请号：US994413
申请日：1992-12-21
申请人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
发明人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
IPC分类号： A61K31/50 , A61K31/501 , A61P7/02 , C07D237/22 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , C07D237/22 , C07D405/12
摘要： A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.
摘要翻译：式（Ⅰ）化合物或其药学上可接受的盐，其制备方法和药物组合物的特征在于含有这些化合物作为有效成分。这些化合物具有强的抗血栓形成活性，强心剂活性，血管扩张剂活性和抗SRS-A活性，可用作各种血栓形成，充血性心力衰竭，高血压，哮喘，立即型过敏性疾病等的预防或治疗剂。

3. 发明授权

US5314883A 5-heteroarylamino-6-oxy-substituted 3(2H)-pyridazinones 失效
标题翻译： 5-杂芳基氨基-6-氧基取代的3（2H） - 哒嗪酮
公开(公告)号：US5314883A
公开(公告)日：1994-05-24
申请号：US994404
申请日：1992-12-21
申请人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
发明人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
IPC分类号： A61K31/50 , A61K31/501 , A61P7/02 , C07D237/22 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , C07D237/22 , C07D405/12
摘要： A compound of the formula: ##STR1## or its pharmaceutically acceptable salt and pharmaceutical compositions containing these compounds as effective ingredients. These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic afflictions, congestive heart failure, hypertension, asthma, immediate-type allergy diseases and the like.
摘要翻译：下式的化合物：其含有这些化合物作为有效成分的药学上可接受的盐和药物组合物。这些化合物具有强的抗血栓活性，强心剂活性，血管扩张剂活性和抗SRS-A活性，可用作各种血栓形成疾病，充血性心力衰竭，高血压，哮喘，立即型过敏性疾病等的预防或治疗剂。

4. 发明授权

US5856327A Pyridazinone derivatives 失效
标题翻译：哒嗪酮衍生物
公开(公告)号：US5856327A
公开(公告)日：1999-01-05
申请号：US936600
申请日：1997-09-24
申请人： Keizo Tanikawa , Takashi Matsumoto , Hiroo Matsumoto , Nobutomo Tsuruzoe , Hitoshi Nakabeppu
发明人： Keizo Tanikawa , Takashi Matsumoto , Hiroo Matsumoto , Nobutomo Tsuruzoe , Hitoshi Nakabeppu
IPC分类号： C07D237/22 , C07D401/12 , A61K31/50
CPC分类号： C07D401/12 , C07D237/22
摘要： Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## �wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, Y is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!. These compounds have strong antiplatelet effects, are excellently safe, and can be used as active ingredients of prophylactic and therapeutic drugs for various thrombotic diseases.
摘要翻译：由式（I）表示的哒嗪酮衍生物和含有它们的抗血小板剂：其中R是氢原子或C1-C4烷基，X是氢原子，氯原子或溴原子， Ar是吡啶基或被OR 1取代的苯基（其中R1是氢原子或C1-C4烷基）和A {其中A是氢原子，卤素原子，C1-C4烷基或OR2（其中R 2是氢原子或C 1 -C 4烷基），Y是直链上的一个碳原子被一个OR 1基团取代的C 1 -C 8亚烷基（其中R 1与上述相同），Z 1和 Z2独立地为氢原子，卤素原子，C1-C4烷基或OR1基团（其中R1与上述定义相同）]。这些化合物具有很强的抗血小板作用，非常安全，可用作各种血栓性疾病的预防和治疗药物的活性成分。

5. 发明授权

US5750523A Pyridazinone derivatives 失效
标题翻译：哒嗪酮衍生物
公开(公告)号：US5750523A
公开(公告)日：1998-05-12
申请号：US676227
申请日：1996-07-23
申请人： Keizo Tanikawa , Takashi Matsumoto , Hiroo Matsumoto , Nobutomo Tsuruzoe , Hitoshi Nakabeppu
发明人： Keizo Tanikawa , Takashi Matsumoto , Hiroo Matsumoto , Nobutomo Tsuruzoe , Hitoshi Nakabeppu
IPC分类号： C07D237/22 , C07D401/12 , A61K31/50
CPC分类号： C07D401/12 , C07D237/22
摘要： Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## �wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!. These compounds have strong antiplatelet effects, are excellently safe, and can be used as active ingredients of prophylactic and therapeutic drugs for various thrombotic diseases.
摘要翻译： PCT No.PCT / JP95 / 00069 Sec。 371日期：1996年7月23日 102（e）日期1996年7月23日PCT提交1995年1月24日PCT公布。 WO95 / 19969 PCT公开日期：1997年7月27日由式（I）表示的哒嗪酮衍生物和含有它们的抗血小板剂：其中R是氢原子或C1-C4烷基，X是氢原子，氯原子或溴原子，Ar是吡啶基或被OR 1取代的苯基（其中R1是氢原子或C1-C4烷基）和A {其中A是氢原子，卤原子，C1-C4 烷基或OR 2（其中R 2是氢原子或C 1 -C 4烷基）}是其中一个碳原子被一个OR 1基团取代的C 1 -C 8亚烷基（其中R 1与上述定义相同），Z 1和Z 2独立地为氢原子，卤素原子，C 1 -C 4烷基或OR 1基（其中R 1与上述定义相同）]。这些化合物具有很强的抗血小板作用，非常安全，可用作各种血栓性疾病的预防和治疗药物的活性成分。

6. 发明授权

US5202323A 5-arylmethylamino-6-oxy-substituted 3(2H)-pyridazinones 失效
标题翻译： 5-氨基甲酰胺-6-氧代替3（2H） - 吡啶并[
公开(公告)号：US5202323A
公开(公告)日：1993-04-13
申请号：US768182
申请日：1991-10-16
申请人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
发明人： Keizo Tanikawa , Akira Saito , Takashi Matsumoto , Ryozo Sakoda , Nobutomo Tsuruzoe , Ken-ichi Shikada
IPC分类号： A61K31/50 , A61K31/501 , A61P7/02 , C07D237/22 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , C07D237/22 , C07D405/12
摘要： A compound of the formula, ##STR1## or its pharmaceutically acceptable salt, and its preparation process and pharmaceutical compositions characterized by containing these compounds as effective ingredients.These compounds have strong antithrombotic activity, cardiotonic activity, vasodilator activity and anti-SRS-A activity, and are useful as prophylactic or therapeutic agents for various thrombotic affections, congestive heart failure, hypertension, asthma, immediate type allergy diseases and the like.

7. 发明授权

US4654348A Pyrazolo[4,3-d]pyrimidine derivative, process for its production, antihyperlipidemic agent containing it, its intermediate, and process for the production of the intermediate 失效
标题翻译：吡唑并[4,3-d]嘧啶衍生物，其制备方法，含有它的抗高血脂药，其中间体和中间体的制备方法
公开(公告)号：US4654348A
公开(公告)日：1987-03-31
申请号：US718377
申请日：1985-04-01
申请人： Yoshihiro Fujikawa , Mikio Suzuki , Mitsuaki Sakashita , Nobutomo Tsuruzoe , Tadashi Miyasaka
发明人： Yoshihiro Fujikawa , Mikio Suzuki , Mitsuaki Sakashita , Nobutomo Tsuruzoe , Tadashi Miyasaka
IPC分类号： A61K31/505 , A61P3/06 , C07D487/04 , A61K31/415
CPC分类号： C07D487/04
摘要： A pyrazolo[4,3-d]pyrimidine derivative having the formula: ##STR1## wherein R.sup.1 is lower alkyl or phenyl, R.sup.2 is --A--CO.sub.2 R.sup.21 (wherein A is alkylene having from 1 to 10 carbon atoms which is unsubstituted or substituted by alkyl having from 1 to 3 carbon atoms; and R.sup.21 is lower alkyl having from 1 to 4 carbon atoms), --CH.sub.2 CO-phenyl, a saturated or unsaturated, straight chain or branched aliphatic group having from 3 to 16 carbon atoms, phenyl-lower alkyl, --CH.sub.2 CN, chloro substituted phenyl-lower alkyl or ##STR2## (wherein R.sup.22 is hydrogen or lower alkyl), and R.sup.3 is a saturated or unsaturated, straight chain or branched aliphatic group having from 2 to 22 carbon atoms, phenyl-lower alkyl, benzyloxy substituted phenyl-lower alkyl, lower alkyl substituted or unsubstituted 2-(phenylmethyloxy)ethyl, cyclohexylcyclohexyl, methylcyclohexyl, 3-thia-n-heptyl, 3,6-dioxa-n-decyl, 4-oxo-n-pentyl or 2-hydroxyethyl. Intermediates and processes of making the compounds of formula I are also disclosed. The compounds of formula I are useful as antihyperlipidemic agents.
摘要翻译：具有下式的吡唑并[4,3-d]嘧啶衍生物：其中R 1是低级烷基或苯基，R 2是-A-CO 2 R 21（其中A是具有1至10个碳原子的亚烷基，其是未取代的或由具有1至3个碳原子的烷基取代; R 21是具有1至4个碳原子的低级烷基），-CH 2 CO-苯基，具有3至16个碳原子的饱和或不饱和的直链或支链脂族基团，苯基 - 低级烷基，-CH 2 CN，氯代取代的苯基 - 低级烷基或者其中R 22是氢或低级烷基，R 3是具有2至22个碳原子的饱和或不饱和的直链或支链脂族基团，苯基 - 低级烷基，苄氧基取代的苯基 - 低级烷基，低级烷基取代或未取代的2-（苯基甲氧基）乙基，环己基环己基，甲基环己基，3-硫杂 - 正庚基，3,6-二氧杂 - 正戊基或2-羟乙基。还公开了制备式I化合物的中间体和方法。式I的化合物可用作抗高血脂药物。

8. 发明申请

US20090155187A1 DRUG FOR INHIBITING VASCULAR INTIMAL HYPERPLASIA 审中-公开
标题翻译：用于抑制血管紧张素血症的药物
公开(公告)号：US20090155187A1
公开(公告)日：2009-06-18
申请号：US12353646
申请日：2009-01-14
申请人： Hiroshi Nishiyama , Norimasa Shudo , Nobutomo Tsuruzoe
发明人： Hiroshi Nishiyama , Norimasa Shudo , Nobutomo Tsuruzoe
IPC分类号： A61K9/12 , A61K31/501
CPC分类号： A61K31/501 , C07D237/14
摘要： To provide an intimal hyperplasia inhibitor useful for prevention of restenosis after percutaneous transluminal coronary angioplasty (PTCA) or vascular stent placement or treatment of its progress.An intimal hyperplasia inhibitor containing a 3(2H)-pyridazinone compound represented by the formula (I): [wherein each of R1, R2 and R3 is independently a hydrogen atom or a C1-6 alkyl group, X is a halogen atom, cyano or a hydrogen atom, Y is a halogen atom, trifluoromethyl or a hydrogen atom, and A is a C1-8 alkylene which may be substituted with a hydroxyl group] or a pharmacologically acceptable salt thereof.
摘要翻译：提供内皮增生抑制剂，可用于预防经皮腔内冠状动脉成形术（PTCA）或血管支架置入或治疗其进展后的再狭窄。含有由式（I）表示的3（2H） - 哒嗪酮化合物的内膜增生抑制剂：其中R 1，R 2和R 3各自独立地为氢原子或C 1-6烷基，X为卤素原子，氰基或氢原子，Y为卤素原子，三氟甲基或氢原子，A为可被羟基取代的C 1-8亚烷基]或其药理学上可接受的盐。

9. 发明授权

US4639444A 3,5-dialkyl-4,6-diaryl-tetrahydro-2H-13,5-thiadiazine-2-thione derivative, process for its production and antihyperlipidemic agent containing it 失效
标题翻译： 3,5-二烷基-4,6-二芳基 - 四氢-2H-13,5-噻二嗪-2-硫酮衍生物，其制备方法和含有它的抗高血脂药
公开(公告)号：US4639444A
公开(公告)日：1987-01-27
申请号：US800025
申请日：1985-11-20
申请人： Yoshihiro Fujikawa , Mitsuaki Sakashita , Nobutomo Tsuruzoe
发明人： Yoshihiro Fujikawa , Mitsuaki Sakashita , Nobutomo Tsuruzoe
IPC分类号： A61K31/54 , A61P3/06 , C07D285/34 , C07D317/00 , C07D417/14 , C07D407/10
CPC分类号： C07D417/14 , C07D285/34
摘要： A compound of the formula: ##STR1## wherein R is methyl or ethyl, X is hydrogen (provided R is ethyl), lower alkyl, lower alkoxy, lower alkylthio, fluorine, bromine, phenoxy or substituted phenoxy, X.sub.m is methylenedioxy or --CH.dbd.CH--CH.dbd.CH--, and m is 1, 2 or 3.
摘要翻译：下式的化合物，其中R是甲基或乙基，X是氢（提供R是乙基），低级烷基，低级烷氧基，低级烷硫基，氟，溴，苯氧基或取代的苯氧基，Xm是亚甲二氧基或-CH = CH-CH = CH-，m为1,2或3。

10. 发明申请

US20080306080A1 NEUTROPHILIA INHIBITOR 审中-公开
标题翻译：中性抑制剂
公开(公告)号：US20080306080A1
公开(公告)日：2008-12-11
申请号：US12188638
申请日：2008-08-08
申请人： Takehisa Iwama , Nobutomo Tsuruzoe
发明人： Takehisa Iwama , Nobutomo Tsuruzoe
IPC分类号： A61K31/501 , A61P11/00
CPC分类号： C07D401/12 , A61K31/501
摘要： To provide an antineutrophilia agent effective for treatment of development and progress of acute infections, collagen diseases (chronic rheumatoid arthritis, Wegener's granulomatosis and Behcet's disease), chronic obstructive pulmonary disease (COPD), chronic bronchitis, pulmonary emphysema, small airway disease, gout, Cushing's syndrome, myelofibrosis, neoplastic neutrophilia, polycythemia vera and diseases caused by administration of steroid drugs.An antineutrophilia agent containing a 3(2H)-pyridazinone compound represented by the formula (I) or a pharmaceutically acceptable salt thereof [wherein each of R1, R2 and R3 is independently a hydrogen atom or a C1-6 is alkyl group, X is a halogen atom, cyano or a hydrogen atom, Y is a halogen atom, trifluoromethyl or a hydrogen atom, and A is a C1-8 alkylene which may be substituted with a hydroxyl group].
摘要翻译：为了提供一种有效治疗急性感染发展和进展的抗营养药物，胶原病（慢性类风湿关节炎，韦格纳肉芽肿病和白塞病），慢性阻塞性肺病（COPD），慢性支气管炎，肺气肿，小气道疾病，痛风，库兴综合征，骨髓纤维化，肿瘤性嗜中性粒细胞增多症，真性红细胞增多症和由类固醇药物引起的疾病。含有式（I）所示的3（2H） - 哒嗪酮化合物或其药学上可接受的盐的抗中毒药，其中R1，R2和R3各自独立地为氢原子或C1-6为烷基，X为卤原子，氰基或氢原子，Y为卤素原子，三氟甲基或氢原子，A为可被羟基取代的C 1-8亚烷基]。

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