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1. 发明授权

US6166221A Production method of optically active imidazole compound, synthetic intermediate therefor and production method thereof 失效
标题翻译：光学活性咪唑化合物的制备方法及其合成中间体及其制备方法
公开(公告)号：US6166221A
公开(公告)日：2000-12-26
申请号：US511782
申请日：2000-02-23
申请人： Kazuyuki Kawasaki , Haruhito Kobayashi , Syuji Ehara , Hideaki Sato
发明人： Kazuyuki Kawasaki , Haruhito Kobayashi , Syuji Ehara , Hideaki Sato
IPC分类号： A61K31/415 , A61P3/10 , A61P43/00 , C07D233/58 , C07D233/60 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention provides a method for producing an optically active 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof, which includes subjecting a compound of the formula (I) wherein each symbol in the formula is as defined in the specification, to optical resolution by fractional crystallization to give an optically active compound thereof and subjecting the compound to hydrolysis reaction. According to this method, a resolution method useful for industrial large-scale production of the optically active compound of 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid, which is useful as a thromboxane synthetase inhibitor and an agent for the prophylaxis and treatment of diabetic complications, can be obtained.
摘要翻译：本发明提供了一种制备光学活性的4- [α-羟基-5-（1-咪唑基）-2-甲基苄基] -3,5-二甲基苯甲酸或其药学上可接受的盐的方法，其包括使其中式中每个符号如本说明书中所定义的式（I）通过分级结晶得到其光学活性化合物并使该化合物进行水解反应的光学拆分。根据该方法，可以用于工业大规模生产4- [α-羟基-5-（1-咪唑基）-2-甲基苄基] -3,5-二甲基苯甲酸的光学活性化合物的分辨方法，其为可用作血栓素合成酶抑制剂和用于预防和治疗糖尿病并发症的药剂。

2. 发明授权

US6066739A Process for producing optically active imidazole compounds, intermediates for synthesizing the same, and process for producing the same 失效
标题翻译：光学活性咪唑化合物的制造方法，其合成用中间体及其制造方法
公开(公告)号：US6066739A
公开(公告)日：2000-05-23
申请号：US355096
申请日：1999-07-23
申请人： Kazuyuki Kawasaki , Haruhito Kobayashi , Syuji Ehara , Hideaki Sato
发明人： Kazuyuki Kawasaki , Haruhito Kobayashi , Syuji Ehara , Hideaki Sato
IPC分类号： A61K31/415 , A61P3/10 , A61P43/00 , C07D233/58 , C07D233/60 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention provides a method for producing an optically active 4-[.alpha.-hydro-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof, which includes subjecting a compound of the formula (I) ##STR1## wherein each symbol in the formula is as defined in the specification, to optical resolution by fractional crystallization to give an optically active compound thereof and subjecting the compound to hydrolysis reaction. According to this method, a resolution method useful for industrial large-scale production of the optically active compound of 4-[.alpha.-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid, which is useful as a thromboxane synthetase inhibitor and an agent for the prophylaxis and treatment of diabetic complications, can be obtained.
摘要翻译： PCT No.PCT / JP98 / 00150 Sec。 371日期：1999年7月23日 102（e）日期1999年7月23日PCT提交1998年1月14日PCT公布。第WO98 / 32740号公报日期：1998年7月30日本发明提供了一种光学活性的4- [α-氢-5-（1-咪唑基）-2-甲基苄基] -3,5-二甲基苯甲酸或其药学上可接受的盐的制备方法，包括使式（I）化合物（其中式中的每个符号如说明书中所定义）通过分级结晶进行光学拆分，得到其光学活性化合物并使化合物进行水解反应。根据该方法，可以用于工业大规模生产4- [α-羟基-5-（1-咪唑基）-2-甲基苄基] -3,5-二甲基苯甲酸的光学活性化合物的分辨方法，其为可用作血栓素合成酶抑制剂和用于预防和治疗糖尿病并发症的药剂。

3. 发明授权

US5760032A Thienylazole compound and thienotriazolodiazepine compound 失效
标题翻译：噻吩唑化合物和噻吩并三唑并噻嗪类化合物
公开(公告)号：US5760032A
公开(公告)日：1998-06-02
申请号：US750025
申请日：1996-11-22
申请人： Hiroshi Kitajima , Syuji Ehara , Hideaki Sato , Minoru Moriwaki , Kenichi Onishi
发明人： Hiroshi Kitajima , Syuji Ehara , Hideaki Sato , Minoru Moriwaki , Kenichi Onishi
IPC分类号： C07D409/04 , C07D409/14 , C07D495/14 , A61K31/55 , C07D491/00 , C07D513/00 , C07D515/00
CPC分类号： C07D409/14 , C07D409/04 , C07D495/14
摘要： Thienylazole compounds (I) and thienotriazolodiazepine compounds (II) of the formulas ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen, halogen, C.sub.1 -C.sub.5 alkyl and the like; --A.dbd.B-- is --N.dbd.N-- and the like; R.sup.3 and R.sup.19 are hydrogen, C.sub.1 -C.sub.5 alkyl and the like; Y is --NHCO--, --NHCONH--, --NHCOO-- and the like; Z.sup.1 and Z.sup.2 are aryl, heteroaryl and the like; Ar is halogen-substituted phenyl and the like; and m is 0 or an integer of 1-5. The compounds of the present invention have CCK antagonistic action and gastrin antagonistic action, particularly potent antagonistic action against CCK-A receptor, and are useful as agents for the prophylaxis and treatment of central and peripheral nervous system diseases (e.g., anxiety, schizophrenia, and the like) and digestive diseases (e.g., pancreatitis, gastric ulcer, enterelcosis, irritable bowel syndrome, constipation, and the like).
摘要翻译： PCT No.PCT / JP95 / 01071 Sec。 371日期：1996年11月22日 102（e）日期1996年11月22日PCT归档1995年6月1日PCT公布。公开号WO95 / 32964 日期：1995年12月7日式（I）其中R 1和R 2为氢，卤素，C 1 -C 5烷基等的噻吩唑化合物（I）和噻吩并三唑并二氮杂化合物（Ⅱ） -A = B-是-N = N-等; R3和R19是氢，C1-C5烷基等; Y是-NHCO-，-NHCONH-，-NHCOO-等; Z 1和Z 2是芳基，杂芳基等; Ar是卤素取代的苯基等; m为0或1-5的整数。本发明的化合物具有CCK拮抗作用和胃泌素拮抗作用，特别是针对CCK-A受体的强效拮抗作用，可用作预防和治疗中枢和周围神经系统疾病（例如焦虑，精神分裂症和类似物）和消化疾病（例如胰腺炎，胃溃疡，入侵性肠易激综合征，便秘等）。

4. 发明授权

US5721231A Thienotriazolodiazepine compound and pharmaceutical use thereof 失效
标题翻译：噻吩并三唑并噻嗪类化合物及其药物用途
公开(公告)号：US5721231A
公开(公告)日：1998-02-24
申请号：US535913
申请日：1995-09-28
申请人： Minoru Moriwaki , Hiroyuki Kitani , Syuji Ehara , Hirotsugu Komatsu , Mariko Amano
发明人： Minoru Moriwaki , Hiroyuki Kitani , Syuji Ehara , Hirotsugu Komatsu , Mariko Amano
IPC分类号： C07D495/14 , A61K31/55
CPC分类号： C07D495/14
摘要： N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno �3,2-f!�1,2,4!triazolo�4,3-a!�1,4!diazepin-6-yl )-N'- (2-methoxyphenyl)urea, optical isomers thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention strongly and selectively inhibit the expression of VCAM-1 and have an inhibitory effect on leukocyte adhesion to vascular endothelial cells. Accordingly, the compounds of the present invention can be used as cell adhesion inhibitors for prophylaxis or treatment of various diseases in which cell adhesion is involved in the onset and progress thereof.
摘要翻译： N-（4-（4-氯苯基）-2,3,9-三甲基-6H-噻吩并〔3,2-f〕〔1,2,4〕三唑并〔4,3-a〕〔1,4〕二氮杂 -6-基）-N'-（2-甲氧基苯基）脲，其旋光异构体和其药学上可接受的盐。本发明化合物强烈和选择性地抑制VCAM-1的表达，并且对白细胞对血管内皮细胞的粘附具有抑制作用。因此，本发明的化合物可以用作细胞粘附抑制剂，用于预防或治疗其起因和进展中涉及细胞粘附的各种疾病。

5. 发明授权

US06288061B1 Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US06288061B1
公开(公告)日：2001-09-11
申请号：US09598216
申请日：2000-06-21
申请人： Hiroyuki Sueoka , Jouji Yasuoka , Akira Nishiyama , Masatoshi Kiuchi , Katsuya Yamamoto , Kunio Sugahara , Syuji Ehara , Kei Sakata
发明人： Hiroyuki Sueoka , Jouji Yasuoka , Akira Nishiyama , Masatoshi Kiuchi , Katsuya Yamamoto , Kunio Sugahara , Syuji Ehara , Kei Sakata
IPC分类号： A61K314178
CPC分类号： C07D401/04 , C07D233/66 , C07D403/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof. The compounds of the formulas (I) and (XII) and pharmaceutically acceptable salts thereof of the present invention inhibit IL-4 and IL-5 production by Th2 cells and are effective for the prophylaxis and treatment of allergic diseases such as atopic dermatitis, bronchial asthma, allergic rhinitis and the like.
摘要翻译：本发明涉及下式（I）的咪唑衍生物，其中R 1是氢，任选取代的烷基等，R 2是氢，任选取代的烷基等，R 3是任选取代的杂芳基，R 4是任选取代的环烷基，任选地取代的苯基等，条件是当R 1为氢时，R 2和R 4相同或不同，并且各自为苯基或被卤素原子取代的苯基，低级烷基或低级烷氧基，R 3为被苯基取代的苯并噻唑基或噻唑基，咪唑下式（Ⅻ）的衍生物，其中R 6是任选取代的苯基或任选取代的杂芳基且R 7是取代的苯基，及其药学上可接受的盐。本发明的式（I）和（XII）化合物及其药学上可接受的盐抑制Th2细胞的IL-4和IL-5产生，对预防和治疗变应性疾病如特应性皮炎，支气管哮喘，过敏性鼻炎等。

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