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1. 发明授权

US5158963A 1-4-dihydropyridine derivative, process for preparing the same and pharmaceutical composition containing the same 失效
标题翻译： 1-4-二氢吡啶衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5158963A
公开(公告)日：1992-10-27
申请号：US557816
申请日：1990-07-26
申请人： Michio Nakanishi , Katsuhiro Uchida , Terutake Nakagawa , Kiyoharu Ukai , Michiko Nagahara , Jun Nakano , Kazuhiko Kimura
发明人： Michio Nakanishi , Katsuhiro Uchida , Terutake Nakagawa , Kiyoharu Ukai , Michiko Nagahara , Jun Nakano , Kazuhiko Kimura
IPC分类号： C07D211/90
CPC分类号： C07D211/90
摘要： A 1,4-dihydropyridine derivative having the formula (I): ##STR1## wherein X is oxygen atom or nitrogen atom; when X is oxygen atom, R.sup.1 is hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group or magnesium atom, when X is nitrogen atom, X-R.sup.1 group is NH.sub.2, NHR.sup.1', NR.sup.1' R.sup.1" or ##STR2## in which R.sup.1' is a lower alkyl group or a lower alkoxyalkyl group, R.sup.1" is a lower alkyl group and n is an integer of 2 to 6; R.sup.2 is a lower alkyl group, a lower cycloalkyl group or a lower alkoxyalkyl group and R.sup.3 is a lower alkyl group, formyl group, dimethoxymethyl group, cyano group or amino group, when X is oxygen atom and R.sup.1 is hydrogen atom or magnesium atom, R.sup.3 is methyl group, when X is nitrogen atom, R.sup.3 is methyl group, or a pharmaceutically acceptable salt thereof, some processes for preparing the same and a pharmaceutical composition containing the same. According to the present invention, a superior cerebral function improver can be provided.

2. 再颁专利

USRE34918E Azaazulene compounds which are useful as antiallergic and antiinflammatory agents 失效
公开(公告)号：USRE34918E
公开(公告)日：1995-04-25
申请号：US225761
申请日：1994-04-05
申请人： Michiko Nagahara , Chikara Ieda , Mitsuo Mimura , Katsuhiro Uchida , Soichiro Sato , Makoto Okumura
发明人： Michiko Nagahara , Chikara Ieda , Mitsuo Mimura , Katsuhiro Uchida , Soichiro Sato , Makoto Okumura
IPC分类号： A61K31/40 , A61K31/403 , A61K31/41 , A61K31/47 , A61K31/495 , A61P29/00 , A61P37/08 , C07D209/52 , C07D401/06 , C07D401/14 , C07D403/04 , C07D409/06 , C07D409/14 , C07D209/02
CPC分类号： C07D401/06 , C07D209/52 , C07D401/14 , C07D403/04 , C07D409/06 , C07D409/14
摘要： An azaazulene derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond or double bond; when the bond C N is single bond, R.sup.2 is 5-tetrazolyl group, R.sup.3 is taken together with carbon atom to form carbonyl group at the 2-position, and R.sup.4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: ##STR2## in which W is single bond or carbonyl group, oxygen atom, sulfur atom or --CH.dbd.CH--, n is an integer of 1 to 6, and R.sup.1', R.sup.2' and R.sup.3' are the same or different and each is hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, trifluoromethyl group, hydroxyl group, a lower alkoxycarbonyl group, carboxyl group, acetyl group or cyano group; when the bond C N is double bond, N at the 1-position has no substituent R.sup.4, R.sup.2 is cyano group, and R.sup.3 is amino group or a salt thereof, azido group, a diphenyl lower alkyl amino group, a substituted phenyl amino group, a substituted piperazinyl group, a substituted homopiperazinyl group, an amino acid residue bonded by N terminal group in which C terminal group is carboxyl group or a lower alkyl ester thereof, or a lower alkyl amino group which may have an alkyl amino group that may be cyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agent and an antiinflammatory agent and has also an inhibitory activity against histamine release, 5-lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealis and inhibitory activity against carrageenin edema, and further, is useful as medicine for prevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis, urticaria, atopic dermatitis, other inflammatory diseases or the like.

3. 发明授权

US5013736A Azaazulene compounds which are useful as antiallergic and antiinflammatory agents 失效
标题翻译：可用作抗过敏和抗炎剂的氮杂薁化合物
公开(公告)号：US5013736A
公开(公告)日：1991-05-07
申请号：US457125
申请日：1989-12-26
申请人： Michiko Nagahara , Chikara Ieda , Mitsuo Mimura , Katsuhiro Uchida , Soichiro Sato , Makoto Okumura
发明人： Michiko Nagahara , Chikara Ieda , Mitsuo Mimura , Katsuhiro Uchida , Soichiro Sato , Makoto Okumura
IPC分类号： A61K31/40 , A61K31/403 , A61K31/41 , A61K31/47 , A61K31/495 , A61P29/00 , A61P37/08 , C07D209/52 , C07D401/06 , C07D401/14 , C07D403/04 , C07D409/06 , C07D409/14
CPC分类号： C07D401/06 , C07D209/52 , C07D401/14 , C07D403/04 , C07D409/06 , C07D409/14
摘要： An azaazulene derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond or double bond; when the bond C N is single bond, R.sup.2 is 5-tetrazolyl group, R.sup.3 is taken together with carbon atom to form carbonyl group at the 2-position, and R.sup.4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: ##STR2## in which W is single bond or carbonyl group, oxygen atom, sulfur atom or --CH.dbd.CH--, n is an integer of 1 to 6, and R.sup.1', R.sup.2' and R.sup.3' are the same or different and each is hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, trifluoromethyl group, hydroxyl group, a lower alkoxycarbonyl group, carboxyl group, acetyl group or cyano group; when the bond C N is double bond, N at the 1-position has no substituent R.sup.4, R.sup.2 is cyano group, and R.sup.3 is amino group or a salt thereof, azido group, a diphenyl lower alkyl amino group, a substituted phenyl amino group, a substituted piperazinyl group, a substituted homopiperazinyl group, an amino acid residue bonded by N terminal group in which C terminal group is carboxyl group or a lower alkyl ester thereof, or a lower alkyl amino group which may have an alkyl amino group that may be cyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agent and an antiinflammatory agent and has also an inhibitory activity against histamine release, 5-lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealis and inhibitory activity against carrageenin edema, and further, is useful as medicine for prevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis, urticaria, atopic dermatitis, other inflammatory diseases or the like.

4. 发明授权

US4652566A Benzofuran derivatives, processes for preparing the same and antihypertensive agents containing the same 失效
标题翻译：苯并呋喃衍生物，其制备方法和含有它们的抗高血压药
公开(公告)号：US4652566A
公开(公告)日：1987-03-24
申请号：US713662
申请日：1985-03-19
申请人： Jun Nakano , Michiko Nagahara , Mitsuo Hayashida , Yuji Suzuki , Yohichi Maruyama
发明人： Jun Nakano , Michiko Nagahara , Mitsuo Hayashida , Yuji Suzuki , Yohichi Maruyama
IPC分类号： A61K31/34 , A61K31/343 , A61K31/495 , A61P9/12 , C07D307/80 , C07D307/85 , C07D307/86 , C07D407/12 , A61K31/395 , C07D405/12
CPC分类号： C07D407/12 , C07D307/80 , C07D307/85 , C07D307/86
摘要： A [2-hydroxy-3-(4-phenylpiperazinyl)propoxy]benzofuran derivative having the formula (I): ##STR1## wherein X is acetyl, carbamoyl, cyano, a lower alkoxycarbonyl, carboxyl or 1-hydroxyethyl group, R is hydrogen atom, a lower alkoxy group, a lower alkyl group or a halogen atom; R is attached to an arbitrary position of ortho-position, meta-position and para-position to N-phenyl group, and a group having the formula: ##STR2## is attached to an arbitrary position of 4, 5, 6 and 7 positions to benzofuran ring or the salt thereof, a process for preparing the same and an antihypertensive agent containing the same as an effective component. The benzofuran derivative has a strong .alpha.-adrenergic blockade effect and calcium antagonistic effect with a more decreased side-effect.
摘要翻译：具有式（I）的[2-羟基-3-（4-苯基哌嗪基）丙氧基]苯并呋喃衍生物：其中X是乙酰基，氨基甲酰基，氰基，低级烷氧基羰基，羧基或1-羟基乙基， R是氢原子，低级烷氧基，低级烷基或卤原子; R连接到N-苯基的邻位，间位和对位的任意位置，具有下式的基团：附着在4,5,6和7位的任意位置至苯并呋喃环或其盐，其制备方法和含有该有效成分的抗高血压药。苯并呋喃衍生物具有强的α-肾上腺素能阻断作用和钙拮抗作用，副作用降低。

5. 发明授权

US4666931A Benzofuran derivatives useful in treating diabetic complications 失效
标题翻译：可用于治疗糖尿病并发症的苯并呋喃衍生物
公开(公告)号：US4666931A
公开(公告)日：1987-05-19
申请号：US814135
申请日：1985-12-27
申请人： Yoshitaka Ohishi , Michiko Nagahara , Norio Kajikawa , Motoyuki Yajima , Katsumi Nogimori , Shigeki Kurokawa
发明人： Yoshitaka Ohishi , Michiko Nagahara , Norio Kajikawa , Motoyuki Yajima , Katsumi Nogimori , Shigeki Kurokawa
IPC分类号： C07D337/00 , A61K31/34 , A61K31/343 , A61K31/36 , A61K31/415 , A61P3/08 , A61P3/10 , A61P7/02 , C07D307/79 , C07D307/80 , C07D307/82 , C07D307/85 , C07D307/86 , C07D405/04 , C07D493/04
CPC分类号： C07D307/82 , C07D307/80 , C07D307/85 , C07D307/86 , C07D405/04 , C07D493/04
摘要： A benzofuran derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a benzyl group, unsubstituted or substituted with a halogen atom or an alkyloxy group, or an alkyl group having 1 to 3 carbon atoms, R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R.sup.3 is acetyl group, ethyl group, carboxyl group or 4-methyl-2,5-dioxoimidazolidine-4-yl group, R.sup.4 is hydrogen atom, hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 9 carbon atoms, carboxymethoxy group, nitro group, acetoamino group, a benzylozy group unsubstituted or substituted with a halogen atom, nitro group or an alkyloxy group or a group having the formula: --OR.sup.6, wherein R.sup.6 is an alkenyl group having 2 to 4 carbon atoms or an alkyl group having 2 to 3 carbon atoms having a halogen atom, cyano group or oxo group, R.sup.5 is hydrogen atom or methylenedioxy group together with R.sup.4 group, n is 1 or 2, and the unsubstituted or substituted N-carboxymethylsulfamoyl group, R.sup.4 and R.sup.5 are attached at 3-position, 4-position, 5-position, 6-position or 7-position of the benzofuran ring, or a nontoxic salt thereof, process for preparing the same and a pharmaceutical composition containing the same.The compounds of the present invention have powerful aldose reductase inhibiting activity, platelet aggregation inhibiting activity and arachidonic acid metabolism inhibiting activity and are useful for a remedy for treatment of diabetic complications.
摘要翻译：具有通式（I）的苯并呋喃衍生物：其中R1是氢原子，未被取代或被卤素原子或烷氧基取代的苄基或具有1至3个碳原子的烷基的苄基， R2是氢原子或碳原子数1〜3的烷基，R3是乙酰基，乙基，羧基或4-甲基-2,5-二氧代咪唑烷-4-基，R4是氢原子，羟基，具有1至6个碳原子的烷基，具有1至9个碳原子的烷氧基，羧甲氧基，硝基，乙酰氨基，未被取代或被卤素原子取代的苄氧基，硝基或烷氧基或具有式：-OR6，其中R6是具有2至4个碳原子的烯基或具有2至3个碳原子的具有卤素原子的烷基，氰基或氧代基，R5是氢原子或亚甲二氧基以及R4基团， n为1或2，未取代或取代的N-羧甲基氨磺酰基基团，R4和R5连接在苯并呋喃环的3-位，4-位，5-位，6-位或7-位上，或其无毒盐，其制备方法和含有它们的药物组合物。本发明化合物具有强大的醛糖还原酶抑制活性，血小板聚集抑制活性和花生四烯酸代谢抑制活性，可用于治疗糖尿病并发症的治疗方法。

6. 发明授权

US4609736A Rhodanines useful as a therapeutic agent for diabetic complications 失效
标题翻译：用作糖尿病并发症治疗剂的红豆杉素
公开(公告)号：US4609736A
公开(公告)日：1986-09-02
申请号：US675579
申请日：1984-11-28
申请人： Yoshitaka Ohishi , Michiko Nagahara , Yoshitaka Takehisa , Motoyuki Yajima , Shigeki Kurokawa , Norio Kajikawa , Akira Itoh
发明人： Yoshitaka Ohishi , Michiko Nagahara , Yoshitaka Takehisa , Motoyuki Yajima , Shigeki Kurokawa , Norio Kajikawa , Akira Itoh
IPC分类号： A61K31/425 , A61K31/426 , A61P3/08 , A61P3/10 , A61P7/02 , A61P9/10 , A61P43/00 , C07D277/20 , C07D277/36 , C07D417/06 , C12N9/99
CPC分类号： C07D277/20 , C07D417/06
摘要： A rhodanine derivative having the following general formula (I): ##STR1## wherein R is an acyclic alkyl group having 2 to 10 carbon atoms which may be substituted by a halogen atom or an acyclic alkenyl group having 2 to 19 carbon atoms which may be substituted by a halogen atom; or a nontoxic salt thereof. The rhodanine derivative has potent platelet aggregation inhibiting activity and aldose reductase inhibiting activity and therefore is useful as a therapeutic agent for diabetic complications.
摘要翻译：具有以下通式（I）的绕丹宁衍生物：其中R是可被卤素原子取代的具有2至10个碳原子的无环烷基或具有2至19个碳原子的无环烯基其可以被卤素原子取代; 或其无毒盐。罗丹明衍生物具有有效的血小板聚集抑制活性和醛糖还原酶抑制活性，因此可用作糖尿病并发症的治疗剂。

7. 发明授权

US4606860A Rhodanines useful as a therapeutic agent for diabetic complications 失效
标题翻译：用作糖尿病并发症治疗剂的红豆杉素
公开(公告)号：US4606860A
公开(公告)日：1986-08-19
申请号：US675580
申请日：1984-11-28
申请人： Michiko Nagahara , Yoshitaka Ohishi , Motoyuki Yajima , Katsumi Nogimori , Shigeki Kurokawa , Norio Kajikawa
发明人： Michiko Nagahara , Yoshitaka Ohishi , Motoyuki Yajima , Katsumi Nogimori , Shigeki Kurokawa , Norio Kajikawa
IPC分类号： A61K31/425 , A61K31/426 , A61K31/495 , A61K31/535 , A61K31/55 , A61P3/08 , A61P3/10 , A61P7/02 , A61P13/02 , A61P15/00 , A61P25/02 , A61P27/02 , C07D243/00 , C07D277/20 , C07D277/36 , C07D417/06 , C07D421/04 , A61K31/33
CPC分类号： C07D277/20 , C07D417/06
摘要： A rhodanine derivative having the following general formula (I): ##STR1## wherein R is a mono- or di-alkylamino group having 1 to 6 carbon atoms which may be substituted by a hydroxyl group; an alkenylamino group having 3 to 6 carbon atoms; a phenylamino group, the benzene ring of which may be substituted by a lower alkyl group, a lower alkoxyl group, phenyl group or a halogen atom; or a cyclic amino group which may contain in the ring an oxygen atom or a nitrogen atom to which a lower alkyl group is attached; or a nontoxic salt thereof. The rhodanine derivative has potent platelet aggregation inhibiting activity and aldose reductase inhibiting activity and therefore is useful as a therapeutic agent for diabetic complications.
摘要翻译：具有以下通式（I）的绕丹宁衍生物：其中R是可以被羟基取代的具有1至6个碳原子的单或二烷基氨基; 具有3至6个碳原子的链烯基氨基; 苯基氨基，其苯环可以被低级烷基，低级烷氧基，苯基或卤素原子取代; 或在环中可以含有低级烷基的氧原子或氮原子的环状氨基; 或其无毒盐。罗丹明衍生物具有有效的血小板聚集抑制活性和醛糖还原酶抑制活性，因此可用作糖尿病并发症的治疗剂。

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