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1. 发明授权

US4695580A Phenylserine derivatives and processes for preparing the same 失效
标题翻译：苯基丝氨酸衍生物及其制备方法
公开(公告)号：US4695580A
公开(公告)日：1987-09-22
申请号：US683430
申请日：1984-12-19
申请人： Naohito Ohashi , Shoji Nagata , Masashi Nakatsuka , Kikuo Ishizumi , Junki Katsube , Shunji Aono , Teruo Sakurama
发明人： Naohito Ohashi , Shoji Nagata , Masashi Nakatsuka , Kikuo Ishizumi , Junki Katsube , Shunji Aono , Teruo Sakurama
IPC分类号： A61K31/195 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61P43/00 , C07C67/00 , C07C213/00 , C07C215/30 , C07C215/36 , C07C215/60 , C07C229/36 , C07C231/00 , C07C237/20 , C07C241/00 , C07C251/76 , C07C313/00 , C07C323/25 , C07C323/29 , C07D207/06 , C07D207/08 , C07D207/32 , C07D207/335 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/44 , C07D213/75 , C07D217/06 , C07D257/04 , C07D257/06 , C07D295/12 , C07D295/125 , C07D295/185 , C07D307/52 , C07D317/58 , C07D319/16 , C07F17/02 , C07K5/065 , A61K31/165 , A61K31/215 , C07D295/18
CPC分类号： C07D207/08 , C07C243/00 , C07D207/06 , C07D207/335 , C07D209/08 , C07D209/14 , C07D209/44 , C07D213/75 , C07D217/06 , C07D257/06 , C07D295/125 , C07D295/185 , C07D307/52 , C07D317/58 , C07D319/16 , C07F17/02 , C07K5/06078
摘要： Novel phenylserine derivatives of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions, and a process for preparing the compounds are disclosed. The phenylserine derivatives and pharmaceutically acceptable acid addition salts are capable of inhibiting the biosynthesis of leucotrienes and/or antagonistic activity against SRS-A and hence are useful for prophylaxis and treatment of various allergic diseases (e.g. bronchial asthma, allergic nasitis, urticaria), ischemic heart diseases, ischemic encephalopathy, inflammation, or the like.
摘要翻译：公开了下式的新型苯基丝氨酸衍生物及其药学上可接受的酸加成盐，药物组合物及其制备方法。苯基丝氨酸衍生物和药学上可接受的酸加成盐能够抑制白细胞三烯的生物合成和/或对SRS-A的拮抗活性，因此可用于预防和治疗各种过敏性疾病（例如支气管哮喘，过敏性鼻炎，荨麻疹），缺血性心脏病，缺血性脑病，炎症等。

2. 发明授权

US4230706A Antihypertensive quinazoline compounds 失效
标题翻译：抗高血压喹唑啉化合物
公开(公告)号：US4230706A
公开(公告)日：1980-10-28
申请号：US021776
申请日：1979-03-19
申请人： Isamu Maruyama , Shunji Aono , Junki Katsube
发明人： Isamu Maruyama , Shunji Aono , Junki Katsube
IPC分类号： A61K31/505 , A61K31/517 , A61P9/12 , C07D239/95
CPC分类号： C07D239/95
摘要： Quinazoline compounds of the formula: ##STR1## wherein A is ##STR2## wherein n is an integer of 1 or 2, or ##STR3## wherein X is O or CH.sub.2, and n and m are independently an integer of 1 or 2, and its non-toxic pharmaceutically acceptable salts, having an excellent antihypertensive activity without causing adverse effects such as orthostatic hypotension.
摘要翻译：喹唑啉化合物，其结构式如下：其中A是其中n是1或2的整数，或者其中X是O或CH 2，n和m独立地是1或2的整数，其无毒的药学上可接受的盐，具有优异的抗高血压活性而不引起诸如直立性低血压的不利影响。

3. 发明授权

US4288448A N-Substituted imidazole derivatives, and their use 失效
标题翻译： N-取代的咪唑衍生物及其用途
公开(公告)号：US4288448A
公开(公告)日：1981-09-08
申请号：US210619
申请日：1980-11-26
申请人： Ikutaro Saji , Shunji Aono , Takao Okuda , Hideo Agui
发明人： Ikutaro Saji , Shunji Aono , Takao Okuda , Hideo Agui
IPC分类号： C07D405/04 , A61K31/415 , A61P31/04 , A61P31/10 , C07D521/00 , A61K31/495 , C07D403/00 , C07D405/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： An N-substituted imidazole compound of the formula: ##STR1## wherein R and R' are independently a phenyl group optionally substituted with one or more halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 alkylthio, phenyl, phenoxy, phenylthio, hydroxyl, trifluoromethyl, amino, carbamoyl, di(C.sub.1 -C.sub.8) alkylamino, C.sub.1 -C.sub.8 alkanoylamino, nitro, cyano, carboxy, C.sub.1 -C.sub.8 alkoxycarbonyl, C.sub.1 -C.sub.8 alkylsulfonyloxy or C.sub.1 -C.sub.8 alkanoylpiperazino groups; a C.sub.1 -C.sub.15 alkyl group or a phenyl (C.sub.1 -C.sub.2) alkyl group optionally bearing halogen on the benzene ring, and its acid-addition salts, which is useful as an antifungal agent.
摘要翻译：具有下式的N-取代的咪唑化合物：其中R和R'独立地是任选被一个或多个卤素，C 1 -C 8烷基，C 1 -C 8烷氧基，C 1 -C 8烷硫基，苯基，苯氧基，苯基硫基，羟基，三氟甲基，氨基，氨基甲酰基，二（C1-C8）烷基氨基，C1-C8烷酰基氨基，硝基，氰基，羧基，C1-C8烷氧基羰基，C1-C8烷基磺酰氧基或C1-C8烷酰基哌嗪基; 在苯环上任选带有卤素的C 1 -C 15烷基或苯基（C 1 -C 2）烷基及其酸加成盐，其可用作抗真菌剂。

4. 发明授权

US3959484A Phenoxy carboxylic acid derivatives as anti-atheroslerosis agents 失效
标题翻译：苯氧基羧酸衍生物作为抗动脉粥样硬化剂
公开(公告)号：US3959484A
公开(公告)日：1976-05-25
申请号：US459861
申请日：1974-04-10
申请人： Yasushi Nakamura , Kunio Agatsuma , Yoshihiro Tanaka , Shunji Aono
发明人： Yasushi Nakamura , Kunio Agatsuma , Yoshihiro Tanaka , Shunji Aono
IPC分类号： C07C51/367 , C07C51/41 , C07C59/68 , C07C59/72 , A61K31/235
CPC分类号： C07C59/72 , C07C51/367 , C07C51/412 , C07C59/68 , Y10S514/824
摘要： Novel anti-atheroscelersosis agents having the formula, ##SPC1##Wherein typical examples of R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.8 alkyl, phenyl, benzyl and phenethyl, or R.sup.1 and R.sup.2 may form cycloalkylidene together with a carbon atom bonded therewith; R.sup.3 and R.sup.4 each is hydrogen or C.sub.1 -C.sub.4 alkyl; Y is hydroxyl, C.sub.1 -C.sub.4 alkoxy, phenoxy or an amine residue; A is hydrogen or a group of the formula, ##EQU1## wherein R.sup.3, R.sup.4 and Y have the same meanings as defined above; and D and E each is hydrogen or halogen.These compounds are produced, for example, by reacting a bisphenolic compound of the formula, ##SPC2## with chloroform and a ketone compound of the formula,R.sup.3 --CO--R.sup.4in the presence of an alkali. Alternatively, they are produced by reacting the bisphenolic compound with .alpha.-halogeno- or .alpha.-hydroxycarboxylic acid derivative of the formula, ##EQU2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, d, e and T have the same meanings as definend above; and X is halogen or hydroxyl.
摘要翻译：具有下式的新型抗动脉粥样硬化剂：其中R1和R2的典型实例是氢，C1-C8烷基，苯基，苄基和苯乙基，或R1和R2可以与其键合的碳原子一起形成亚环烷基; R3和R4各自为氢或C1-C4烷基; Y是羟基，C 1 -C 4烷氧基，苯氧基或胺残基; A是氢或下式的基团R3R4 ANGLE -C-COY，其中R3，R4和Y具有与上述相同的含义; D和E各自为氢或卤素。

5. 发明授权

US4461774A Antifungal imidazolylcarboxylic acids and their derivatives 失效
标题翻译：抗真菌咪唑基羧酸及其衍生物
公开(公告)号：US4461774A
公开(公告)日：1984-07-24
申请号：US427558
申请日：1982-09-29
申请人： Ikutaro Saji , Hiroshi Yamazaki , Shunji Aono , Katsuaki Ichise , Takao Okuda
发明人： Ikutaro Saji , Hiroshi Yamazaki , Shunji Aono , Katsuaki Ichise , Takao Okuda
IPC分类号： A01N43/50 , A61K31/415 , A61P31/04 , A61P31/10 , C07D233/60 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： An imidazolylcarboxylic acid compound of the formula: ##STR1## wherein Ph is a phenyl group or a phenyl group substituted with one or two halogen atoms, R is a hydrogen atom or a C.sub.1 -C.sub.8 alkyl group and n is an integer of 1 to 8, which is useful as an antifungal agent.
摘要翻译：下式的咪唑基羧酸化合物：其中Ph是苯基或被一个或两个卤素原子取代的苯基，R是氢原子或C1-C8烷基，n是1至8的整数，其可用作抗真菌剂。

6. 发明授权

US4092324A Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric acid)-cyclohexane).alpha.-methyl substituted 失效
标题翻译： 4-（1,1-双 - （苯氧基 - 丙酸） - 环己烷）（60-甲基取代的）的二杂环酯
公开(公告)号：US4092324A
公开(公告)日：1978-05-30
申请号：US716666
申请日：1976-08-23
申请人： Yoshio Suzuki , Masayoshi Minai , Noritaka Hamma , Eiichi Murayama , Shunji Aono
发明人： Yoshio Suzuki , Masayoshi Minai , Noritaka Hamma , Eiichi Murayama , Shunji Aono
IPC分类号： C07D211/46 , C07D213/30 , C07D213/75 , C07D213/55
CPC分类号： C07D213/30 , C07D211/46 , C07D213/75
摘要： Bisphenoxy carboxylic acid derivatives useful as an antiarteriosclerosis agent with good absorbability and low toxicity, which are novel compounds represented by the general formula, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atoms or lower alkyl groups and A preresents ##STR2## (wherein in case R.sub.3 is a hydrogen atom, R.sub.4 represents an amino-lower-alkyl group, an N-lower-alkylaminoalkyl group, a heterocyclic group, or a heterocyclic group-substituted alkyl group; or R.sub.3 and R.sub.4 may join through an intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent) or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a hydroxyalkyl group or a derivative thereof, and R.sub.6 represents a hydroxyalkyl group or a heterocyclic group; or R.sub.5 and R.sub.6 may join to form a cyclic group, or may join through another intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent).
摘要翻译：作为具有良好吸收性和低毒性的抗动脉硬化剂的双苯氧基羧酸衍生物，它们是由通式表示的新化合物，其中R 1和R 2表示氢原子或低级烷基，并且A表示（其中，在R 3为氢原子的情况下，R 4表示氨基 - 低级烷基，N-低级烷基氨基烷基，杂环基或杂环基取代的烷基;或者，R 3和R 4可以通过中间杂原子原子形成杂环基，如果所述杂原子是氮原子，则该氮原子可以具有作为取代基的低级烷基）或者其中R5表示氢原子，羟烷基或其衍生物，和 R6表示羟基烷基或杂环基;或者R5和R6可以连接形成环状基团，或者可以通过另一个中间杂原子连接形成杂环基，如果所述杂原子是氮原子，该氮原子可以具有低级烷基作为取代基）。

7. 发明授权

US3970694A Cycloalkyl phenoxy carboxylic acid derivatives 失效
标题翻译：环烷基苯氧基羧酸衍生物
公开(公告)号：US3970694A
公开(公告)日：1976-07-20
申请号：US484063
申请日：1974-06-28
申请人： Masayoshi Minai , Yoshio Suzuki , Noritaka Hamma , Eiichi Murayama , Shunji Aono
发明人： Masayoshi Minai , Yoshio Suzuki , Noritaka Hamma , Eiichi Murayama , Shunji Aono
IPC分类号： A61K31/19 , A61K31/215 , A61K31/22 , A61P3/06 , A61P9/10 , C07C51/00 , C07C59/125 , C07C59/68 , C07C59/70 , C07C67/00 , C07C69/712 , C07C63/33
CPC分类号： C07C59/70 , C07C59/68 , C07C69/712 , Y10S514/824
摘要： Novel compounds having the formula, ##SPC1##Wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen or a C.sub.1 -C.sub.4 alkyl; n is an integer of 4-6; and Y is hydrogen or a group of the formula ##EQU1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above. These compounds are produced, for example, by reacting a bisphenolic compound of the formula, ##SPC2##With chloroform and a ketone compound of the formula,R.sub.1 -- CO -- R.sub.2in the presence of an alkali. Alternatively, they are produced by reacting the bisphenolic compound with .alpha.-halogeno- or .alpha.-hydroxycarboxylic acid derivative of the formula, ##EQU2## wherein R.sub.1, R.sub.2, and R.sub.3 are as defined above, and X is a halogen or hydroxyl. The novel compounds are anti-atherosclerosis agents useful for lowering elevated levels of cholesterol or lipids.
摘要翻译：具有式WHEREIN R1，R2和R3的新型化合物各自独立地为氢或C1-C4烷基; n为4-6的整数; 并且Y是氢或式R1R2 ANGLE -C-COOR3的基团，其中R1，R2和R3如上定义。

8. 发明授权

US5106860A Thiazolidin-4-one derivatives and acid addition salts thereof useful for treating PAF mediated diseases 失效
标题翻译：噻唑烷-4-酮衍生物及其适用于治疗PAF介导性疾病的酸添加物
公开(公告)号：US5106860A
公开(公告)日：1992-04-21
申请号：US624566
申请日：1990-12-10
申请人： Masao Enomoto , Atsuyuki Kojima , Yoshihiro Komuro , Shigeaki Morooka , Shunji Aono , Yuzuru Sanemitsu , Masato Mizutani , You Tanabe
发明人： Masao Enomoto , Atsuyuki Kojima , Yoshihiro Komuro , Shigeaki Morooka , Shunji Aono , Yuzuru Sanemitsu , Masato Mizutani , You Tanabe
IPC分类号： C07D417/04
CPC分类号： C07D417/04
摘要： Thiazolidin-4-one derivative represented by the following general formula (I) and acid addition salts thereof ##STR1## wherein; R.sup.1 and R.sup.2 are the same or different and denote each(i) a residue represented by the general formula--A--R.sup.4 wherein, A denotes a single bond, C.sub.1 -C.sub.8 alkylene, C.sub.2 -C.sub.8 alkenylene, or C.sub.2 -C.sub.8 alkynylene and R.sup.4 denotes hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl,or(ii) a residue represented by the general formula ##STR2## wherein, B denotes a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2;R.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, allyl, 2-propynyl,or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR3## (R.sup.10 denotes hydrogen, C.sub.2 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkanoyl and R.sup.11 denotes hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms.Having selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflammation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.

9. 发明授权

US4992455A Thiazolidin-4-one derivatives useful for treating diseases caused by platelet activating factor 失效
标题翻译：可用于治疗血小板活化因子引起的疾病的噻唑烷-4-酮衍生物
公开(公告)号：US4992455A
公开(公告)日：1991-02-12
申请号：US196058
申请日：1988-05-19
申请人： Masao Enomoto , Atsuyuki Kojima , Yoshihiro Komuro , Shigeaki Morooka , Shunji Aono , Yuzuru Sanemitsu , Masato Mizutani , You Tanabe
发明人： Masao Enomoto , Atsuyuki Kojima , Yoshihiro Komuro , Shigeaki Morooka , Shunji Aono , Yuzuru Sanemitsu , Masato Mizutani , You Tanabe
IPC分类号： C07D417/04
CPC分类号： C07D417/04
摘要： Thiazolidin-4-one derivative represented by the folowing general formula (I) and acid addition salts thereof ##STR1## wherein; R.sup.1 and R.sup.2 are the same or different and denote each(i) a residue represented by the general formula--A--R.sup.4 wherein, A denotes a single bond, C.sub.1 -C.sub.8 alkylene, C.sub.2 -C.sub.8 alkenylene, or C.sub.2 -C.sub.8 alkynylene and R.sup.4 denotes hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl, or(ii) a residue represented by the general formula{(CH.sub.2).sub.n O}.sub.m {(CH.sub.2).sub.n' O}B--R.sup.5 wherein, B denotes a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2; andR.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, allyl, 2-propynyl, or a residue represented by(a) the general formula--CH.sub.2).sub.l R.sup.6 wherein, R.sup.6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C.sub.1 -C.sub.4 alkoxy groups, or a residue represented by the general formula --D--R.sup.7 (D denotes oxygen or sulfur and R.sup.7 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkanol) and l denotes an integer of 2 to 4,(b) the general formula--CH.sub.2).sub.k CO--E--R.sup.8 wherein, E denotes oxygen, sulfur, imino, or C.sub.1 -C.sub.4 alkylimino, R.sup.8 denotes hydrogen or C.sub.1 -C.sub.4 alkyl, or --(E--R.sup.8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR2## (R.sup.10 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms), with the proviso that, when R.sup.1 is hydrogen and R.sup.2 is methyl, R.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, 2-propynyl, or a residue represented by(a) the general formula--CH.sub.2).sub.l R.sup.6 wherein, R.sup.6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C.sub.1 -C.sub.4 alkoxy groups, or a residue represented by the general formula --D--R.sup.7 (D denotes oxygen or sulfur and R.sup.7 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkanoyl) and l denotes an integer of 2 to 4,(b) the general formula--CH.sub.2).sub.k CO--E--R.sup.8 wherein, E denotes oxygen, sulfur, imino, or C.sub.1 -C.sub.4 alkylimino, R.sup.8 denotes hydrogen or C.sub.1 -C.sub.4 alkyl, or --(E--R.sup.8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR3## (R.sup.10 denotes hydrogen, C.sub.2 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkanoyl and R.sup.11 denotes hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms.Having selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflammation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.

10. 发明授权

US4228167A Diuretic and vasodilating tricyclic quinazolines 失效
标题翻译：利尿和血管舒张三环喹唑啉
公开(公告)号：US4228167A
公开(公告)日：1980-10-14
申请号：US939869
申请日：1978-09-05
申请人： Michihiro Yamamoto , Masao Koshiba , Shunji Aono
发明人： Michihiro Yamamoto , Masao Koshiba , Shunji Aono
IPC分类号： A61K31/505 , A61P7/10 , C07D487/04 , C07D487/14
CPC分类号： C07D487/04 , Y10S514/869
摘要： Novel imidazo[2,1-b]quinazolines and pyrimido-[2,1-b]quinozolines represented by the formula, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and A are as defined in the specification were prepared. They have prominent pharmacological properties such as diuretic and vasodilating activity.
摘要翻译：由式表示的新型咪唑并[2,1-b]喹唑啉和嘧啶并[2,1-b]喹唑啉，其中R1，R2，R3，R4，R5和A如说明书中所定义。它们具有突出的药理学性质，如利尿和血管扩张活性。

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