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1. 发明授权

US06777414B1 Nitrogen-containing heterocyclic compounds and benamide compounds and drugs containing the same 失效
标题翻译：含氮杂环化合物和苯甲酰胺化合物及含有其的药物
公开(公告)号：US06777414B1
公开(公告)日：2004-08-17
申请号：US09958296
申请日：2001-10-05
申请人： Naoto Ohkura , Yukiko Hiraiwa , Tetsuya Matsushima , Kazue Sasaki , Takehiro Yamamoto , Masaharu Shiotani , Shigeki Suzuki , Yuuko Nakatani , Chizuko Kuroda , Mieko Nagasawa , Kiyoaki Katano
发明人： Naoto Ohkura , Yukiko Hiraiwa , Tetsuya Matsushima , Kazue Sasaki , Takehiro Yamamoto , Masaharu Shiotani , Shigeki Suzuki , Yuuko Nakatani , Chizuko Kuroda , Mieko Nagasawa , Kiyoaki Katano
IPC分类号： C07D20946
CPC分类号： C07D213/40 , C07D209/46 , C07D295/155 , C07D309/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04
摘要： Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases. In formula (I), R1 and R2 represent alkyl, alkoxy, cycloalkyl, phenyl, alkenyl, alkynyl, or a five- or six-membered saturated or unsaturated heterocyclic ring, or R1 and R2, together with a nitrogen atom to which R1 and R2 are attached, may form a ring; R3 and R4 represent a hydrogen atom, alkyl, a halogen atom, hydroxyl, nitrile, alkoxycarbonyl, alkoxy, or carboxyl; or R2 and R3 may be attached to each other to form —(CH2)m—, —N═CH—, —CH═N—, or —(C1-6 alkyl)C═N—; A, D, E, and G each represent a carbon atom, or any one of A, D, E, and G represents a nitrogen atom with the other three each representing a carbon atom; Q represents a nitrogen atom or a carbon atom; Y represents a group represented by formula (II) wherein X represents a hydrogen atom, group —C(═O)N(R5)R6 or group —C(═O)OR7, R8 is absent or represents a bond, an oxygen atom, a sulfur atom, —SO2—, —SO—, —CH2—CH2—, or —CH═CH—, and R9 and R10 represent a hydrogen atom, alkyl, alkoxy, a halogen atom, or hydroxyl; and Z represents —(CH2)n—, —O—(CH2)i—, or —C(═O)NH—(CH2)i—.
摘要翻译：公开了在肝脏中具有甘油三酯生物合成抑制活性的由式（I）表示的化合物，并且对来自肝脏的含载脂蛋白B的脂蛋白的分泌具有抑制活性，特别是对含有载脂蛋白B的脂蛋白的分泌具有优异的抑制活性。没有肝脏中脂质积累的副作用，可用于治疗和预防高脂血症和动脉硬化性疾病。在式（I）中，R 1和R 2表示烷基，烷氧基，环烷基，苯基，烯基，炔基或五元或六元饱和或不饱和杂环，或R 1和R 2， 2>与R 1和R 2连接的氮原子一起形成环; R 3和R 4表示氢原子，烷基，卤素原子，羟基，腈，烷氧基羰基，烷氧基或羧基; 或R 2和R 3可以彼此连接形成 - （CH 2）m - ， - N = CH - ， - CH = N-或 - （C 1-6烷基）C = N-; A，D，E和G各自表示碳原子，A，D，E和G中的任一个表示氮原子，其余三个表示碳原子; Q表示氮原子或碳原子; Y表示由式（II）表示的基团，其中X表示氢原子，-C（= O）N（R 5）R 6或-C（= O）OR 7， 8>不存在或表示键，氧原子，硫原子，-SO 2 - ， - SO - ， - CH 2 -CH 2 - 或-CH = CH-，R 9和R 10表示氢原子，烷基，烷氧基，卤素原子或羟基; 并且Z表示 - （CH 2）n - ， - O-（CH 2）i - 或-C（= O）NH-（CH 2）i - 。

2. 发明授权

US07030120B2 Nitrogen-containing heterocyclic compounds and benzamide compounds and drugs containing the same 失效
公开(公告)号：US07030120B2
公开(公告)日：2006-04-18
申请号：US10868006
申请日：2004-06-16
申请人： Naoto Ohkura , Yukiko Hiraiwa , Tetsuya Matsushima , Kazue Sasaki , Takehiro Yamamoto , Masaharu Shiotani , Shigeki Suzuki , Yuuko Nakatani , Chizuko Kuroda , Mieko Nagasawa , Kiyoaki Katano
发明人： Naoto Ohkura , Yukiko Hiraiwa , Tetsuya Matsushima , Kazue Sasaki , Takehiro Yamamoto , Masaharu Shiotani , Shigeki Suzuki , Yuuko Nakatani , Chizuko Kuroda , Mieko Nagasawa , Kiyoaki Katano
IPC分类号： C07D209/46 , C07D213/81 , C07D213/82 , C07D217/22 , C07D237/30
CPC分类号： C07D213/40 , C07D209/46 , C07D295/155 , C07D309/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04
摘要： Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases. In formula (I), R1 and R2 represent alkyl, alkoxy, cycloalkyl, phenyl, alkenyl, alkynyl, or a five- or six-membered saturated or unsaturated heterocyclic ring, or R1 and R2, together with a nitrogen atom to which R1 and R2 are attached, may form a ring; R3 and R4 represent a hydrogen atom, alkyl, a halogen atom, hydroxyl, nitrile, alkoxycarbonyl, alkoxy, or carboxyl; or R2 and R3 may be attached to each other to form —(CH2)m—, —N═CH—, —CH═N—, or —(C1-6 alkyl)C═N—; A, D, E, and G each represent a carbon atom, or any one of A, D, E, and G represents a nitrogen atom with the other three each representing a carbon atom; Q represents a nitrogen atom or a carbon atom; Y represents a group represented by formula (II) wherein X represents a hydrogen atom, group —C(═O)N(R5)R6 or group —C(═O)OR7, R8 is absent or represents a bond, an oxygen atom, a sulfur atom, —SO2—, —SO—, —CH2—CH2—, or —CH═CH—, and R9 and R10 represent a hydrogen atom, alkyl, alkoxy, a halogen atom, or hydroxyl; and Z represents —(CH2)n—, —O—(CH2)i—, or —C(═O)NH—(CH2)i—

3. 发明授权

US06583144B2 Nitrogen-containing heterocyclic compounds and therapeutic agents for hyperlipidemia comprising the same 失效
标题翻译：含氮杂环化合物和包含其的高脂血症治疗剂
公开(公告)号：US06583144B2
公开(公告)日：2003-06-24
申请号：US10127491
申请日：2002-04-23
申请人： Naoto Ohkura , Takashi Tsuruoka , Takayuki Usui , Yukiko Hiraiwa , Tetsuya Matsushima , Masaharu Shiotani , Tetsutaro Niizato , Yuuko Nakatani , Shigeki Suzuki , Chidsuko Kuroda , Kiyoaki Katano
发明人： Naoto Ohkura , Takashi Tsuruoka , Takayuki Usui , Yukiko Hiraiwa , Tetsuya Matsushima , Masaharu Shiotani , Tetsutaro Niizato , Yuuko Nakatani , Shigeki Suzuki , Chidsuko Kuroda , Kiyoaki Katano
IPC分类号： A61K31495
CPC分类号： C07D409/12 , C07D209/46 , C07D217/24 , C07D265/22 , C07D279/08 , G03F7/2049 , Y10S977/915
摘要： Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia. wherein A represents group —CR1R2—(CH2)i— where R1 and R2 each represent a hydrogen atom or alkyl, —CH═CH—, —O—CH2—, or —S(O)j—CH2—; B represents a hydrogen or halogen atom; X represents —CR3R4R5, —NR6R7, —(CH2—CH═C(CH3)—CH2)p—CH2CH═C(CH3)2, alkyl, cycloalkyl, phenyl, cinnamyl, or heteroaromatic ring; Y represents —(CH2)q—, —CH═CH—, —NR8—, an oxygen atom, or a bond; Z represents carbonyl or a bond; K represents alkylene or a bond; L represents —CH═CH— or a bond; and M represents a hydrogen atom, alkyl, cycloalkyl, phenyl, heterocyclic ring, biphenyl, or diphenylmethyl.
摘要翻译：公开了由式（I）表示的化合物及其药学上可接受的盐和溶剂化物。该化合物可以抑制肝脏中甘油三酯的生物合成，并可以抑制含有载脂蛋白B的脂蛋白从肝脏的分泌。因此，它们可用于预防或治疗由高脂血症引起的高脂血症（特别是超低密度脂蛋白血症）和动脉硬化疾病如心肌梗死或胰腺炎。其中A代表基团-CR1R2-（CH2）i - 其中R1和R2各自表示氢原子或烷基，-CH = CH-，-O-CH2-或-S（O）j-CH2-; B表示氢或卤素原子; X代表-CR3R4R5，-NR6R7， - （CH2-CH = C（CH3）-CH2）p-CH2CH = C（CH3）2，烷基，环烷基，苯基，肉桂基或杂芳族环; Y表示 - （CH 2）q - ， - CH = CH - ， - NR 8 - ，氧原子或键; Z表示羰基或键; K表示亚烷基或键; L表示-CH = CH-或键; M代表氢原子，烷基，环烷基，苯基，杂环，联苯基或二苯基甲基。

4. 发明授权

US06417362B1 Nitrogenous heterocyclic compounds and hyperlipemia remedy containing the same 失效
标题翻译：含氮杂环化合物和含有相同的高脂血症药物
公开(公告)号：US06417362B1
公开(公告)日：2002-07-09
申请号：US09424708
申请日：1999-11-30
申请人： Naoto Ohkura , Takashi Tsuruoka , Takayuki Usui , Yukiko Hiraiwa , Tetsuya Matsushima , Masaharu Shiotani , Tetsutaro Niizato , Yuuko Nakatani , Shigeki Suzuki , Chidsuko Kuroda , Kiyoaki Katano
发明人： Naoto Ohkura , Takashi Tsuruoka , Takayuki Usui , Yukiko Hiraiwa , Tetsuya Matsushima , Masaharu Shiotani , Tetsutaro Niizato , Yuuko Nakatani , Shigeki Suzuki , Chidsuko Kuroda , Kiyoaki Katano
IPC分类号： C07D24104
CPC分类号： C07D409/12 , C07D209/46 , C07D217/24 , C07D265/22 , C07D279/08 , G03F7/2049 , Y10S977/915
摘要： Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia. wherein A represents group —CR1R2—(CH2)i— where R1 and R2 each represent a hydrogen atom or alkyl, —CH═CH—, —O—CH2—, or —S(O)j—CH2—; B represents a hydrogen or halogen atom; X represents —CR3R4R5, —NR6R7, —(CH2—CH═C(CH3)—CH2)p—CH2CH═C(CH3)2, alkyl, cycloalkyl, phenyl, cinnamyl, or heteroaromatic ring; Y represents —(CH2)q—, —CH═CH—, —NR8—, an oxygen atom, or a bond; Z represents carbonyl or a bond; K represents alkylene or a bond; L represents —CH═CH— or a bond; and M represents a hydrogen atom, alkyl, cycloalkyl, phenyl, heterocyclic ring, biphenyl, or diphenylmethyl.
摘要翻译：公开了由式（I）表示的化合物及其药学上可接受的盐和溶剂化物。该化合物可以抑制肝脏中甘油三酯的生物合成，并可以抑制含有载脂蛋白B的脂蛋白从肝脏的分泌。因此，它们可用于预防或治疗由高脂血症引起的高脂血症（特别是超低密度脂蛋白血症）和动脉硬化疾病如心肌梗死或胰腺炎。其中A代表基团-CR1R2-（CH2）i - 其中R1和R2各自表示氢原子或烷基，-CH = CH-，-O-CH2-或-S（O）j-CH2-; B表示氢或卤素原子; X代表-CR3R4R5，-NR6R7， - （CH2-CH = C（CH3）-CH2）p-CH2CH = C（CH3）2，烷基，环烷基，苯基，肉桂基或杂芳族环; Y表示 - （CH 2）q - ， - CH = CH - ， - NR 8 - ，氧原子或键; Z表示羰基或键; K表示亚烷基或键; L表示-CH = CH-或键; M代表氢原子，烷基，环烷基，苯基，杂环，联苯基或二苯基甲基。

5. 发明授权

US5814636A Compounds with platelet aggregation inhibitor activity 失效
标题翻译：具有血小板聚集抑制活性的化合物
公开(公告)号：US5814636A
公开(公告)日：1998-09-29
申请号：US615227
申请日：1996-07-10
申请人： Kiyoaki Katano , Shokichi Ohuchi , Tomoaki Miura , Eiki Shitara , Masaro Shimizu , Kazue Yaegashi , Naoto Ohkura , Yasuko Isomura , Hiroyuki Iida , Midori Ishikawa , Kenji Asai , Emiko Hatsushiba
发明人： Kiyoaki Katano , Shokichi Ohuchi , Tomoaki Miura , Eiki Shitara , Masaro Shimizu , Kazue Yaegashi , Naoto Ohkura , Yasuko Isomura , Hiroyuki Iida , Midori Ishikawa , Kenji Asai , Emiko Hatsushiba
IPC分类号： A61K31/445 , A61K31/495 , C07D211/58 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/14
CPC分类号： C07D401/04 , C07D211/58 , C07D401/14 , C07D405/14
摘要： A compound represented by the general formula (I) and a pharmaceutically acceptable salt and solvate thereof having an effect for inhibiting the aggregation of platelets is disclosed: ##STR1## wherein A, B and C represent independently CH.sub.2 or C.dbd.O; X and Y are different from each other, and each of them is CH or N; D is --(CH.sub.2).sub.k -- or --(CH.sub.2).sub.m --CO-- where k is an integer of 1 to 4; and m is an integer of 0 to 3; E is the following group (II) or (III): ##STR2## wherein n is an integer of 1 to 3; and Z is --W--(CH.sub.2).sub.p --COOR.sup.3 (wherein W is --O-- or a bond; p is an integer of 1 to 4; and R.sup.3 is hydrogen, lower alkyl or an ester residue which can be removed under physiological conditions); R.sup.1 is hydrogen or lower alkyl; and R.sup.2 is hydrogen atom or lower alkyl.
摘要翻译： PCT No.PCT / JP95 / 01419 Sec。 371日期：1996年7月10日 102（e）日期1996年7月10日PCT提交1995年7月17日PCT公布。公开号WO96 / 02503 日本1996年2月1日公开了具有抑制血小板聚集作用的由通式（I）表示的化合物及其药学上可接受的盐和溶剂合物：＆lt; IMAGE＆gt; CH2或C = O; X和Y彼此不同，它们各自为CH或N; D是 - （CH 2）k - 或 - （CH 2）m -CO-，其中k是1至4的整数; m为0〜3的整数。 E为下列组（II）或（III）：其中n为1至3的整数;（II）其中n为1至3的整数; Z为-W-（CH 2）p -COOR 3（其中W为-O-或键; p为1〜4的整数; R 3为氢，低级烷基或可在生理条件下除去的酯残基）; R1是氢或低级烷基; R2是氢原子或低级烷基。

6. 发明授权

US06451800B1 Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists 失效
标题翻译：苯基哌嗪衍生物作为整合素α2β拮抗剂
公开(公告)号：US06451800B1
公开(公告)日：2002-09-17
申请号：US09601176
申请日：2000-07-28
申请人： Keiichi Ajito , Shoichi Murakami , Minoru Ishikawa , Mikio Yamamoto , Dai Kubota , Shuichi Gomi , Mitsugu Hachisu , Kiyoaki Katano
发明人： Keiichi Ajito , Shoichi Murakami , Minoru Ishikawa , Mikio Yamamoto , Dai Kubota , Shuichi Gomi , Mitsugu Hachisu , Kiyoaki Katano
IPC分类号： A61K31497
CPC分类号： C07D239/42 , C07D235/30 , C07D239/14
摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin &agr;v&bgr;3-mediated diseases and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.
摘要翻译：本发明的目的是提供具有整合素α2拮抗活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗整合素α1β介导的疾病和抑制血小板聚集的治疗剂。根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂化物：其中A表示含有两个氮原子等的5-至7-元杂环; X和Z表示CH或氮原子; R4和R5代表烷基，卤素等; Q表示> C = O，> CH2等; R6表示H，烷基，芳烷基等; R 7表示H，炔基等; R8表示H，取代的氨基等; R9代表H或烷基; m为0〜5; n为0〜4; p为2或3; q为0或1。

7. 发明授权

US4785090A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4785090A
公开(公告)日：1988-11-15
申请号：US704077
申请日：1985-02-21
申请人： Takashi Tsuruoka , Seiji Shibahara , Katsuyoshi Iwamatsu , Tsuneo Okonogi , Satoru Nakabayashi , Yasushi Murai , Hiroko Ogino , Kiyoaki Katano , Takashi Yoshida , Shigeharu Inoue , Shunzo Fukatsu , Shinichi Kondo
发明人： Takashi Tsuruoka , Seiji Shibahara , Katsuyoshi Iwamatsu , Tsuneo Okonogi , Satoru Nakabayashi , Yasushi Murai , Hiroko Ogino , Kiyoaki Katano , Takashi Yoshida , Shigeharu Inoue , Shunzo Fukatsu , Shinichi Kondo
IPC分类号： C07D213/64 , C07D213/68 , C07D221/04 , C07D501/36 , C07D501/38 , A61K31/545
CPC分类号： C07D221/04 , C07D213/64 , C07D213/68
摘要： This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group ##STR6## wherein R.sup.8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.
摘要翻译：这是一类具有下式的抗菌化合物：其中Y是直链或支链烷基或烯基链，3-6个碳原子的环烷基甲基，每个基团任选被卤素取代，或基团< 其中n为0或1-3的整数，A为基团-COR 3，其中R 3为羟基，其中R 4和R 5可以相同或不同，为氢或1-5碳的烷基原子，基团或含有氮和/或硫的5-或6-元杂环基，R 1和R 2可以相同或不同，为氢，1-5个碳原子的烷基或R1 并且R 2可以组合在一起形成3-5个碳原子的亚烷基，Z是下式的基团：其中m是0或3-5的整数，R6是氢或1-3个碳的烷基原子和R 7，当m是3-5的整数时，是1-5个碳原子的烷基，烯基，环丙基，基团 - （CH 2）pB，其中p是0或1-3的整数，B是氨基，烷基取代的氨基羟基，羧基，氨基甲酰基，三氟甲基，磺酸，磺酸酰胺，烷硫基或氰基，或当m为0时，其为1-5个碳原子的烷基，其可任选被卤素，链烯基，基团其中R8是氢，1-4个碳原子的烷基或苯基，或环丙基及其盐。

8. 发明授权

US4485235A Process for preparing 7-.alpha.-methoxycephem compounds 失效
标题翻译：制备7-甲氧基头孢烯化合物的方法
公开(公告)号：US4485235A
公开(公告)日：1984-11-27
申请号：US373700
申请日：1982-04-30
申请人： Kiyoaki Katano , Kunio Atsumi , Fumio Kai , Ken Nishihata , Eiichi Akita
发明人： Kiyoaki Katano , Kunio Atsumi , Fumio Kai , Ken Nishihata , Eiichi Akita
IPC分类号： C07D501/16 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/18 , C07D501/20 , C07D501/24 , C07D501/36 , C07D501/57
CPC分类号： C07D501/20 , Y02P20/55
摘要： Disclosed is a novel cephem compound represented by the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n are as defined in the specification, which is a useful intermediate for synthesizing various cephalosporin antibiotics having a methoxy group at the 7.alpha.-position thereof. Also disclosed is a process for preparing the same.
摘要翻译：公开了由下式表示的新型头孢烯化合物：其中R 1，R 2，R 3，R 4和n如说明书中所定义，其是用于合成具有在7α-甲基的甲氧基的各种头孢菌素抗生素的有用中间体，的位置。还公开了其制备方法。

9. 发明授权

US06420558B1 Aminopiperidine derivates as integrin &agr;v&bgr;3 antagonists 有权
标题翻译：氨基哌啶衍生物作为整联蛋白α2β拮抗剂
公开(公告)号：US06420558B1
公开(公告)日：2002-07-16
申请号：US09673017
申请日：2000-10-10
申请人： Minoru Ishikawa , Shoichi Murakami , Mikio Yamamoto , Dai Kubota , Mitsugu Hachisu , Kiyoaki Katano , Keiichi Ajito
发明人： Minoru Ishikawa , Shoichi Murakami , Mikio Yamamoto , Dai Kubota , Mitsugu Hachisu , Kiyoaki Katano , Keiichi Ajito
IPC分类号： C07D23902
CPC分类号： C07D235/14 , C07D401/12
摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic group containing two nitrogen atoms or the like; D represents >NH2, >CH2 or the like; X and Z represent CH or a nitrogen atom; R7 and R8 represent alkyl, halogen or the like; Q represents >C═O, >CH2 or the like; R9 represents H, alkyl, aralkyl or the like; R10 represents H, alkynyl or the like; R11 represents H, substituted amino or the like; R12 represents H or alkyl; m is 0 to 5; n is 0 to 4; p and q are each 1 to 3; and r is 0 or 1.
摘要翻译：本发明的目的是提供具有整合素α噬菌体拮抗活性，细胞粘附抑制活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗心血管疾病，血管发生相关疾病脑血管疾病等，并用于抑制血小板聚集。根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂合物：其中A表示含有两个氮原子等的5-至7-元杂环基; D表示> NH 2，> CH 2等; X和Z表示CH或氮原子; R 7和R 8表示烷基，卤素等; Q表示> C = O，> CH2等; R 9表示H，烷基，芳烷基等; R 10表示H，炔基等; R11表示H，取代的氨基等; R 12表示H或烷基; m为0〜5; n为0〜4; p和q各自为1至3; r为0或1。

10. 发明授权

US5141946A Azole derivatives and anti-ulcerative composition containing same 失效
标题翻译：唑衍生物和含有其的抗溃疡组合物
公开(公告)号：US5141946A
公开(公告)日：1992-08-25
申请号：US716622
申请日：1991-06-14
申请人： Kiyoaki Katano , Tamako Tomomoto , Hiroko Ogino , Naoki Yamazaki , Fumiya Hirano , Yasukatsu Yuda , Fukio Konno , Motohiro Nishio , Tomoya Machinami , Seiji Shibahara , Takashi Tsuruoka , Shigeharu Inouye
发明人： Kiyoaki Katano , Tamako Tomomoto , Hiroko Ogino , Naoki Yamazaki , Fumiya Hirano , Yasukatsu Yuda , Fukio Konno , Motohiro Nishio , Tomoya Machinami , Seiji Shibahara , Takashi Tsuruoka , Shigeharu Inouye
IPC分类号： C07D487/04 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61P1/04 , C07D471/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D513/04
摘要： Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in whichA, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represnts a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-memebered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integrer from 0 to 2.The compounds are useful in treating ulcers.
摘要翻译：通式（I）的化合物：其中A，B，C和D各自表示-CH =或-N =，条件是其中至少一个为 -N =; X表示-NH-，-O-或-S-; Y表示 - （CH 2）p - ，其中p是0至4的整数，-C（CH 3）2 - ， - CH 2 CH = CH - ， - CH 2 CO - ， - CF 2 - 或-CH 2 COCH 2 - R1表示氢原子，C1-4烷基，卤素原子或C1-4烷氧基; R2表示氢原子，羟基，饱和或不饱和的C1-6烷基，C1-6烷氧基，羧基，可以任意取代的饱和或不饱和的C 1-12烷氧基羰基，环烷氧基羰基，含有至少一个氮原子的饱和或不饱和五元或六元杂环基团，任选具有一个或多个氮原子和/或氧原子，其可以任选地被缩合和/或取代，-CONR 3 R 4，-NR 3 R 4，-OCOR 3或 - NHCONHR 3其中R3和R4可以相同或不同，表示可以任选被取代的C 1-6烷基或环烷基，m和n各自表示0至2的整数。该化合物可用于处理溃疡

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