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1. 发明授权

US4443443A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4443443A
公开(公告)日：1984-04-17
申请号：US213232
申请日：1980-12-05
申请人： Ikuo Ueda , Masaaki Matsuo , Kiyoshi Tsuji , Masayuki Kato
发明人： Ikuo Ueda , Masaaki Matsuo , Kiyoshi Tsuji , Masayuki Kato
IPC分类号： C07D209/48 , C07D257/04 , C07D277/20 , C07D295/13 , C07D295/205 , C07D501/36 , A61K31/545
CPC分类号： C07D209/48 , C07D257/04 , C07D277/587 , C07D295/13 , C07D295/205 , Y02P20/55
摘要： This invention relates to novel cephem compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is carboxy or a protected carboxy group;A is lower alkylene which may have an oxo group;R.sup.3 is carboxy, a protected carboxy group, lower alkyl, lower alkenyl, hydroxy (lower) alkyl, phenyl (lower) alkyl, phenyl, tolyl, xylyl, cumenyl, or naphthyl; andR.sup.4 is hydrogen or lower alkoxy, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及高抗微生物活性的新型头孢烯化合物，其具有下式：其中R 1是氨基或被保护的氨基; R2是羧基或被保护的羧基; A是可以具有氧代基的低级亚烷基; R3是羧基，被保护的羧基，低级烷基，低级烯基，羟基（低级）烷基，苯基（低级）烷基，苯基，甲苯基，二甲苯基，枯烯基或萘基; 和R4是氢或低级烷氧基，及其药学上可接受的盐。

2. 发明授权

US4563524A Cephem compounds and processes for preparation thereof 失效
标题翻译：头孢烯化合物及其制备方法
公开(公告)号：US4563524A
公开(公告)日：1986-01-07
申请号：US570297
申请日：1984-01-13
申请人： Ikuo Ueda , Masaaki Matsuo , Kiyoshi Tsuji , Masayuki Kato
发明人： Ikuo Ueda , Masaaki Matsuo , Kiyoshi Tsuji , Masayuki Kato
IPC分类号： C07D209/48 , C07D257/04 , C07D277/20 , C07D295/13 , C07D295/205 , C07D501/36 , C07D403/06
CPC分类号： C07D209/48 , C07D257/04 , C07D277/587 , C07D295/13 , C07D295/205 , Y02P20/55
摘要： The invention relates to novel intermediates for preparing novel cephem compounds of high antimicrobial activity, the intermediates being of the formula: ##STR1## wherein A is lower alkylene which may have an oxo group;R.sup.3 is carboxy, protected carboxy, lower alkyl, lower alkenyl, hydroxy(lower)alkyl, phenyl(lower)alkyl or aryl; andR.sup.7a is hydrogen or a mercapto-protective group, or a salt thereof.
摘要翻译：本发明涉及用于制备高抗微生物活性的新型头孢烯化合物的新型中间体，其中间体具有下式：其中A是可具有氧代基团的低级亚烷基; R3是羧基，被保护的羧基，低级烷基，低级烯基，羟基（低级）烷基，苯基（低级）烷基或芳基; 和R7a是氢或巯基保护基，或其盐。

3. 发明授权

US4797399A Piperazine compounds and antithrombotic pharmaceutical composition comprising the same 失效
标题翻译：哌嗪化合物和包含其的抗血栓药物组合物
公开(公告)号：US4797399A
公开(公告)日：1989-01-10
申请号：US945853
申请日：1986-12-23
申请人： Ikuo Ueda , Masaaki Matsuo , Kiyoshi Tsuji , Hiroyuki Okumura , Osamu Nakaguchi
发明人： Ikuo Ueda , Masaaki Matsuo , Kiyoshi Tsuji , Hiroyuki Okumura , Osamu Nakaguchi
IPC分类号： C07D209/34 , A61K31/495 , A61K31/496 , A61P7/02 , A61P29/00 , A61P37/08 , C07D209/36 , C07D209/38 , C07D209/40 , C07D263/58 , C07D277/68 , C07D277/82 , C07D417/06 , C07D513/04 , A61K31/44 , C07D513/00 , C07D513/06
CPC分类号： C07D263/58 , C07D209/38 , C07D209/40 , C07D277/68 , C07D277/82 , C07D417/06 , C07D513/04
摘要： The present invention relates to N-containing fused heterocyclic compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, halogen, aryl, lower alkyl, halo (lower) alkyl or nitro,R.sub.3 is lower alkylene,R.sub.4 and R.sub.5 are each lower alkylene,X is CH or N,Y is S, O, NH, C.dbd.N--OH or CO,Z is O or NH, andA is hydrogen, nitroso, amidino, a group of ##STR2## wherein R.sub.6 and R.sub.7 are each hydrogen, lower alkyl, acyl, or lower alkaneimidoyl which may be substituted with esterified carboxy, or a group of the formula:--N.dbd.R.sub.8,wherein R.sub.8 is lower alkylidene which may be substituted with aryl optionally substituted with suitable substituent(s).The compounds are useful for treatment of thrombosis, inflammation, or allergic disease.
摘要翻译：本发明涉及下式的含N的稠合杂环化合物：其中R 1和R 2各自为氢，卤素，芳基，低级烷基，卤代（低级）烷基或硝基，R 3为低级亚烷基，R 4和R 5为每个低级亚烷基，X是CH或N，Y是S，O，NH，C = N-OH或CO，Z是O或NH，A是氢，亚硝基，脒基，一组 R 7各自为可被酯化羧基取代的氢，低级烷基，酰基或低级亚烷基亚氨基，或下式-N = R 8的基团，其中R 8为可被任选被适当取代基取代的芳基取代的低级亚烷基 s）。该化合物可用于治疗血栓形成，炎症或过敏性疾病。

4. 发明授权

US4742057A Antiallergic thiazole compounds 失效
标题翻译：抗过敏型噻唑化合物
公开(公告)号：US4742057A
公开(公告)日：1988-05-03
申请号：US932592
申请日：1986-11-20
申请人： Ikuo Ueda , Masaaki Matsuo , Takashi Manabe , Hiroshi Matsuda
发明人： Ikuo Ueda , Masaaki Matsuo , Takashi Manabe , Hiroshi Matsuda
IPC分类号： C07D417/12 , A61K31/40 , A61K31/404 , A61K31/425 , A61K31/427 , A61K31/44 , A61K31/445 , A61K31/4523 , A61P11/00 , A61P27/16 , A61P37/08 , C07D401/04 , C07D401/14 , C07D417/14 , A61K31/535
CPC分类号： C07D401/04 , C07D417/14
摘要： A thiazole compound of allergically activity of the formula: ##STR1## wherein R.sup.1 is amino optionally having suitable substituent(s),R.sup.2 is hydrogen, lower alkyl or aryl,R.sup.3 is hydrogen, nitro, amino optionally having suitable substituent(s), hydroxy or lower alkoxy,A is lower alkylene,Q is hydrogen or halogen, anda heavy solid line means a single or double bond,or a pharmaceutically acceptable salt thereof, processes for the preparation thereof and pharmaceutical composition comprising the same.
摘要翻译：下式的具有过敏活性的噻唑化合物：其中R 1为任选具有适当取代基的氨基，R 2为氢，低级烷基或芳基，R 3为氢，硝基，任选具有合适取代基的氨基，羟基或低级烷氧基，A为低级亚烷基，Q为氢或卤素，重实线表示单键或双键或其药学上可接受的盐，其制备方法和包含其的药物组合物。

5. 发明授权

US4001280A Chromone derivatives 失效
标题翻译：色酮衍生物
公开(公告)号：US4001280A
公开(公告)日：1977-01-04
申请号：US371852
申请日：1973-06-20
申请人： Suminori Umio , Ikuo Ueda , Masaaki Matsuo , Masakazu Kobayashi , Osamu Nakaguti , Yoshinari Sato
发明人： Suminori Umio , Ikuo Ueda , Masaaki Matsuo , Masakazu Kobayashi , Osamu Nakaguti , Yoshinari Sato
IPC分类号： C07D311/24
CPC分类号： C07D311/24
摘要： Chromone derivatives of the formula: ##STR1## wherein R.sup.1 is alkoxy, an N,S-containing heterocyclic group or aryloxy in which heterocyclic group may be substituted with halogen or acyl, and aryl may be substituted with amino, alkylamino, acylamino, nitro or alkylenedioxy; R.sup.2 is alkylene; R.sup.3 is hydroxy, alkoxy or a group of the formula ##STR2## in which R.sup.4 is hydrogen, R.sup.5 is hydroxy or amino or R.sup.4 and R.sup.5 means taken together with the adjacent nitrogen atom, piperazinyl substituted with alkyl or hydroxyalkyl; provided that when R.sup.3 is hydroxy or alkoxy, R.sup.1 is an N,S-containing heterocyclic group or aryloxy in which heterocyclic group is substituted with halogen or acyl, and aryl is substituted with amino, alkylamino, acylamino, nitro or alkylenedioxy, and nontoxic, pharmaceutically acceptable salt thereof. These compounds are useful as anti-allergic agents.

6. 发明授权

US3965122A Chromone compounds and preparation thereof 失效
标题翻译：色酮化合物及其制备方法
公开(公告)号：US3965122A
公开(公告)日：1976-06-22
申请号：US213180
申请日：1971-12-28
申请人： Suminori Umio , Shizuo Maeno , Ikuo Ueda , Yoshinari Sato , Masaaki Matsuo
发明人： Suminori Umio , Shizuo Maeno , Ikuo Ueda , Yoshinari Sato , Masaaki Matsuo
IPC分类号： C07D311/30 , C07D407/12 , C07D311/28
CPC分类号： C07D407/12 , C07D311/30 , Y02P20/55 , Y10S514/826
摘要： Chromone compounds having the structure ##SPC1##Wherein R is aryl, substituted aryl, thienyl, furyl or pyridyl, Y is hydroxy(lower)alkylene, R.sub.1 is hydrogen, lower alkyl, aryl, substituted aryl or a heterocyclic group, R.sub.2 is hydrogen or lower alkoxy, Y.sub.1 is lower alkylene or hydroxyl(lower)alkylene, Z is oxygen or sulfur and R.sub.3 is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl have anti-allergic activity and are useful in the treatment of asthma. Compounds of the structure [I] are prepared by reacting ##SPC2##Wherein Y' is hydroxy(lower)alkylene whose hydroxy group is optimally protected or a reactive derivative of [II] with a carboxylic acid of the formula R--COOH in the presence of a basic catalyst. The resulting compound is then reacted with an acid. Compounds of the structure [I'] are prepared by reacting the compound ##SPC3##With the compound X--Y.sub.1 '--Z--R.sub.3 ' wherein X is an acid residue, Y' is lower alkylene or hydroxy(lower)alkylene whose hydroxy group is optionally protected by a protective group, R.sub.3 ' is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl and Z is as defined above. When R.sub.3 ' is hydrogen, --Z--R.sub.3 ' is optionally protected by a protective group. The resultant compound is subjected to an elimination reaction when Y' is a protected group or when --Z--R.sub.3 ' is protected to split off the protective group.
摘要翻译：具有下式结构的色酮化合物是芳基，取代的芳基，噻吩基，呋喃基或吡啶基，Y是羟基（低级）亚烷基，R1是氢，低级烷基，芳基，取代的芳基或杂环基，R2是氢或低级烷氧基， Y1是低级亚烷基或羟基（低级）亚烷基，Z是氧或硫，R3是氢，低级烷基，芳基，取代芳基或芳（低级）烷基具有抗过敏活性，可用于治疗哮喘。结构[I]的化合物通过在碱存在下使WHEREIN Y'为羟基被最佳保护的羟基（低级）亚烷基或[II]的反应性衍生物与式R-COOH的羧酸反应来制备催化剂。然后将所得化合物与酸反应。通过使化合物与化合物X-Y1'-Z-R3'反应制备化合物，其中X是酸残基，Y'是羟基被任选保护的低级亚烷基或羟基（低级）亚烷基通过保护基团，R 3'是氢，低级烷基，芳基，取代的芳基或芳（低级）烷基，Z如上所定义。当R3'为氢时，-Z-R3'任选被保护基保护。当Y'为受保护基团时或当-Z-R3'被保护以分离保护基团时，所得化合物进行消除反应。

7. 发明授权

US4735952A Arylthio piperidinamide of (4-quinolinylamino)benzoic acid and S-oxidized derivatives 失效
标题翻译：（4-喹啉基氨基）苯甲酸和S-氧化衍生物的芳硫基哌啶酰胺
公开(公告)号：US4735952A
公开(公告)日：1988-04-05
申请号：US821974
申请日：1986-01-24
申请人： Ikuo Ueda , Masaaki Matsuo , Kiyoshi Taniguchi , Takatomo Ogahara
发明人： Ikuo Ueda , Masaaki Matsuo , Kiyoshi Taniguchi , Takatomo Ogahara
IPC分类号： C07D211/16 , A61K31/435 , A61K31/445 , A61K31/4545 , A61K31/47 , A61P9/12 , C07D20060101 , C07D211/22 , C07D211/30 , C07D211/38 , C07D211/46 , C07D211/54 , C07D215/44 , C07D215/54 , C07D333/00 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D215/46 , C07D403/12
CPC分类号： C07D401/12 , C07D211/22 , C07D211/30 , C07D211/38 , C07D211/46 , C07D211/54 , C07D215/54 , C07D401/14 , C07D409/12 , C07D409/14
摘要： This invention provides a piperidine compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or trihalomethyl,R.sup.2 is hydrogen or protected carboxy,R.sup.3 is heterocyclic group or aryl which may be halogen substituted, andX is --S--, ##STR2## --O--, --NH-- or lower alkylene which may be hydroxy substituted, and pharmaceutically acceptable salt thereof, These compounds possess hypotensive activity and are useful as anti-hypertensive agents. The invention further relates to processes for the preparation of these compounds and pharmaceutical compositions comprising compounds of the above formula.
摘要翻译：本发明提供下式的哌啶化合物：其中R 1是氢或三卤甲基，R 2是氢或被保护的羧基，R 3是杂环基或可被卤素取代的芳基，X是-S-， O-，-NH-或可被羟基取代的低级亚烷基及其药学上可接受的盐。这些化合物具有低血压活性，可用作抗高血压药。本发明还涉及制备这些化合物的方法和包含上式化合物的药物组合物。

8. 发明授权

US4438126A Lower alkanoic acid derivatives of 2-oxo-benzoxazolines and aldose reductase inhibiting compositions thereof 失效
标题翻译： 2-氧代 - 苯并恶唑啉的低级链烷酸衍生物及其醛糖还原酶抑制组合物
公开(公告)号：US4438126A
公开(公告)日：1984-03-20
申请号：US409089
申请日：1982-08-18
申请人： Ikuo Ueda , Masaaki Matsuo , Susumu Satoh , Takao Watanabe
发明人： Ikuo Ueda , Masaaki Matsuo , Susumu Satoh , Takao Watanabe
IPC分类号： A61K31/495 , A61P25/04 , A61P29/00 , A61P37/08 , C07C17/26 , C07C205/12 , C07C335/18 , C07C335/26 , C07D209/34 , C07D263/58 , C07D277/68 , C07D277/82 , A61K31/42
CPC分类号： C07D277/82 , C07C205/12 , C07C323/00 , C07C335/18 , C07C335/26 , C07D209/34 , C07D263/58 , C07D277/68 , Y10S514/866
摘要： The invention is directed to compounds of the formula ##STR1## wherein R.sub.a.sup.1 is phenyl,R.sup.2 is halogen,R.sup.3 is carboxy or lower alkoxycarbonyl,Y.sub.a is oxygen,A is C.sub.1 -C.sub.6 alkylene,pharmaceutically acceptable salts thereof, and aldose reductase inhibiting pharmaceutical compositions thereof.
摘要翻译：本发明涉及下式的化合物，其中R 1a是苯基，R 2是卤素，R 3是羧基或低级烷氧基羰基，Ya是氧，A是C 1 -C 6亚烷基，其药学上可接受的盐和醛糖还原酶抑制药物组合物其中。

9. 发明授权

US4367238A Phenyl-alkanoic acid derivative and preparation thereof 失效
标题翻译：苯基 - 链烷酸衍生物及其制备
公开(公告)号：US4367238A
公开(公告)日：1983-01-04
申请号：US226908
申请日：1981-01-21
申请人： Ikuo Ueda , Yoshihiko Kitaura , Masaaki Matsuo , Nobukiyo Konishi
发明人： Ikuo Ueda , Yoshihiko Kitaura , Masaaki Matsuo , Nobukiyo Konishi
IPC分类号： A61K31/095 , C07C45/40 , C07C45/71 , C07C47/575 , C07C51/09 , C07C59/52 , C07C59/56 , C07C59/64 , C07C59/68 , C07C317/00 , C07D307/83 , C07D307/86 , C07D311/18 , A61K31/365
CPC分类号： C07D311/18 , C07C255/00 , C07C317/00 , C07C323/00 , C07C45/40 , C07C45/71 , C07C47/575 , C07C59/68 , C07D307/83 , C07D307/86
摘要： This invention relates to new phenyl-alkanoic acids, their derivatives at the carboxy group, and pharmaceutically acceptable salts thereof, which have anti-inflammatory, analgesic and antipyretic activities.
摘要翻译：本发明涉及具有抗炎，止痛和解热活性的新的苯基 - 链烷酸，它们在羧基上的衍生物及其药学上可接受的盐。

10. 发明授权

US4094870A 2-Substituted thio-1,4-benzodiazepine derivatives 失效
标题翻译： 2-取代的硫代-1,4-苯并二氮杂衍生物
公开(公告)号：US4094870A
公开(公告)日：1978-06-13
申请号：US732929
申请日：1976-10-15
申请人： Ikuo Ueda , Masaaki Matsuo
发明人： Ikuo Ueda , Masaaki Matsuo
IPC分类号： C07D243/22 , A61K31/395
CPC分类号： C07D243/22
摘要： 2-substituted thio-1,4-benzodiazepine derivatives having medicinal use of the general formula ##STR1## wherein R.sub.1 and R.sub.2 individually signify hydrogen atom or a halogen atom, or a nitro, amino, hydroxy, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, alkanoylamino or dialkylamino group, R.sub.3 signifies an alkylene group, and R.sub.4 and R.sub.5 individually signify hydrogen atom or an alkyl group and, when R.sub.4 and R.sub.5 are both alkyl groups, said alkyl groups together may form a ring with or without oxygen atom or an imino group, said ring optionally having a substituent or substituents, and its non-toxic pharmaceutically acceptable salts.
摘要翻译：其中R1和R2各自表示氢原子或卤素原子，或硝基，氨基，羟基，氰基，烷基，卤代烷基，烷氧基，苯基，烷硫基，链烷亚磺酰基，烷磺酰基，烷酰基氨基或二烷基氨基，R3表示亚烷基，R4和R5分别表示氢原子或烷基，当R4和R5均为烷基时，所述烷基一起可以与无氧原子或亚氨基，所述环任选具有取代基，及其无毒的药学上可接受的盐。

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