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1. 发明授权

US4997943A Quinoline-3-carboxylic acid derivatives 失效
标题翻译：喹啉-3-羧酸衍生物
公开(公告)号：US4997943A
公开(公告)日：1991-03-05
申请号：US33066
申请日：1987-03-31
申请人： Masayuki Iwata , Tomio Kimura , Yoshimi Fujihara , Tetsushi Katsube
发明人： Masayuki Iwata , Tomio Kimura , Yoshimi Fujihara , Tetsushi Katsube
IPC分类号： A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61P31/04 , C07D215/56 , C07D215/58 , C07D401/04 , C07D521/00
CPC分类号： C07D215/56 , C07D215/58 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： Compounds of formula (I): ##STR1## (in which R.sup.1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.
摘要翻译：式（I）化合物：其中R 1为烷氧基，R为烷基，卤代烷基，烷基氨基，环烷基或任意取代的苯基，X为氯或氟，Y为某些特定杂环）抗菌活性。它们可以通过将由Y表示的基团引入到其中Y被卤素原子代替的相应化合物中来制备。

2. 发明授权

US5073556A 4-oxoquinoline-3-carboxylic acid derivatives and their use 失效
标题翻译： 4-氧杂环辛烷-3-羧酸衍生物及其用途
公开(公告)号：US5073556A
公开(公告)日：1991-12-17
申请号：US659829
申请日：1991-02-22
申请人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
发明人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
IPC分类号： C07D215/56 , C07D401/04 , C07D521/00
CPC分类号： C07D231/12 , C07D215/56 , C07D233/56 , C07D249/08 , C07D401/04 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy; R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.

3. 发明授权

US5436367A Intermediates for certain 4-oxoquinoline-3-carboxylic acid derivatives 失效
标题翻译：某些4-氧代喹啉-3-羧酸衍生物的中间体
公开(公告)号：US5436367A
公开(公告)日：1995-07-25
申请号：US227678
申请日：1994-04-14
申请人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
发明人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
IPC分类号： C07D215/56 , C07D401/04 , C07D521/00 , C07C65/21
CPC分类号： C07D231/12 , C07D215/56 , C07D233/56 , C07D249/08 , C07D401/04 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy; R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.
摘要翻译：式（I）的化合物：其中：R1表示氟化甲氧基; R2表示含氮杂环基，R3表示氢或氨基），其药学上可接受的盐，酯和酰胺是有价值的抗菌剂其可以通过使类似于式（I）的化合物与其中R 2被卤素原子替换的化合物与提供所需基团R2的化合物反应来制备。

4. 发明授权

US5496951A 4-oxoquinoline-3-carboxylic acid derivatives their preparation and their use 失效
标题翻译： 4-氧代喹啉-3-羧酸衍生物的制备及其用途
公开(公告)号：US5496951A
公开(公告)日：1996-03-05
申请号：US379975
申请日：1995-01-27
申请人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
发明人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
IPC分类号： C07D215/56 , C07D401/04 , C07D521/00
CPC分类号： C07D231/12 , C07D215/56 , C07D233/56 , C07D249/08 , C07D401/04 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy: R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.
摘要翻译：式（I）化合物：其中：R1表示氟化甲氧基：R2表示含氮杂环基，R3表示氢或氨基），其药学上可接受的盐，酯和酰胺是有价值的抗菌剂其可以通过使类似于式（I）的化合物与其中R 2被卤素原子替换的化合物与提供所需基团R2的化合物反应来制备。

5. 发明授权

US5348961A 4-oxoquinoline-3-carboxylic acid derivatives and their use 失效
标题翻译： 4-氧代喹啉-3-羧酸衍生物及其用途
公开(公告)号：US5348961A
公开(公告)日：1994-09-20
申请号：US594283
申请日：1990-10-09
申请人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
发明人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
IPC分类号： C07D215/56 , C07D401/04 , C07D521/00 , A61K31/47
CPC分类号： C07D231/12 , C07D215/56 , C07D233/56 , C07D249/08 , C07D401/04 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy; R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.
摘要翻译：式（I）的化合物：其中：R1表示氟化甲氧基; R2表示含氮杂环基，R3表示氢或氨基），其药学上可接受的盐，酯和酰胺是有价值的抗菌剂其可以通过使类似于式（I）的化合物与其中R 2被卤素原子替换的化合物与提供所需基团R2的化合物反应来制备。

6. 发明授权

US5688791A Aryl group-or aromatic heterocyclic group-substituted aminoquinolone derivatives and anti-hiv agent 失效
标题翻译：芳基或芳族杂环基取代的氨基喹诺酮衍生物和抗-Hiv剂
公开(公告)号：US5688791A
公开(公告)日：1997-11-18
申请号：US526225
申请日：1995-09-11
申请人： Tomio Kimura , Tetsushi Katsube
发明人： Tomio Kimura , Tetsushi Katsube
IPC分类号： C07D487/04 , A61K31/4375 , A61K31/47 , A61K31/535 , A61P31/18 , C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/14 , C07D498/06 , C07D513/04 , C07D513/06 , A61K31/54 , C07D401/02 , C07D403/02
CPC分类号： C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D471/06 , C07D513/04 , C07D513/06 , Y10S514/934
摘要： Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS curing agent containing the same as an effective ingredient.
摘要翻译：公开了由式（Ia），（Ib）或（Ic）表示的芳基或杂环基取代的氨基喹诺酮化合物：（Ia）取代基在说明书中定义，或化合物的盐，和含有该有效成分的AIDS固化剂。

7. 发明授权

US06034086A Trifluoromethylquinolinecarboxylic acid derivative 失效
标题翻译：三氟甲基喹啉羧酸衍生物
公开(公告)号：US06034086A
公开(公告)日：2000-03-07
申请号：US154464
申请日：1998-09-16
申请人： Tomio Kimura , Tetsushi Katsube , Takashi Nishigaki
发明人： Tomio Kimura , Tetsushi Katsube , Takashi Nishigaki
IPC分类号： C07D401/04 , A61K31/4709 , A61P31/18 , C07D215/56 , C07D295/00 , A61K31/495 , A61K31/50 , C07D401/00 , C07D403/00
CPC分类号： C07D215/56
摘要： This invention relates to a 8-trifluoromethylquinolinecaboxylic acid derivative represented by the following formula (I): ##STR1## (wherein R.sup.1 represents a lower alkyl group, a halogeno-lower alkyl group or a cycloalkyl group, R.sup.2 represents a phenyl group which may be substituted by R.sup.0, a 5-membered or 6-membered aromatic heteromonocyclic ring group containing 1 or 2 hetero atoms selected from N, O and S, which may be substituted by R.sup.0, or an aromatic heterocyclic fused ring group in which the said aromatic heteromonocyclic ring group and a benzene ring are fused, R.sup.0 represents a group selected from a halogen, a lower alkyl, a fluorine-substituted lower alkyl, a lower alkoxy or a lower alkylthio, R.sup.3 represents hydrogen or a lower alkyl group, and m represents an integer of 2 or 3.) or a pharmaceutically acceptable salt thereof or an ester thereof.
摘要翻译：本发明涉及由下式（I）表示的8-三氟甲基喹啉代羧酸衍生物：其中R1表示低级烷基，卤代低级烷基或环烷基，R2表示可被R0取代的苯基含有可被R 0取代的选自N，O和S的1或2个杂原子的5元或6元芳族杂单环环基或芳族杂环稠合环基，其中所述芳族杂单环环基和苯环稠合，R 0表示选自卤素，低级烷基，氟取代的低级烷基，低级烷氧基或低级烷硫基，R 3表示氢或低级烷基，m表示2的整数或3.）或其药学上可接受的盐或其酯。

8. 发明授权

US5519016A Aryl group- or aromatic heterocyclic group-substituted aminoquinolone derivatives and anti-HIV agent 失效
标题翻译：芳基或芳族杂环基取代的氨基喹诺酮衍生物和抗HIV剂
公开(公告)号：US5519016A
公开(公告)日：1996-05-21
申请号：US341295
申请日：1994-11-15
申请人： Tomio Kimura , Tetsushi Katsube
发明人： Tomio Kimura , Tetsushi Katsube
IPC分类号： C07D487/04 , A61K31/4375 , A61K31/47 , A61K31/535 , A61P31/18 , C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/14 , C07D498/06 , C07D513/04 , C07D513/06 , A61K31/495 , C07D215/227 , C07D215/233
CPC分类号： C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D471/06 , C07D513/04 , C07D513/06 , Y10S514/934
摘要： Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS curing agent containing the same as an effective ingredient.
摘要翻译：公开了由式（Ia），（Ib）或（Ic）表示的芳基或杂环基取代的氨基喹诺酮化合物：（Ia）取代基在说明书中定义，或化合物的盐，和含有该有效成分的AIDS固化剂。

9. 发明授权

US06063782A Pyrrolopyridazine derivatives 失效
标题翻译：吡咯并哒嗪衍生物
公开(公告)号：US06063782A
公开(公告)日：2000-05-16
申请号：US676375
申请日：1996-07-17
申请人： Tomio Kimura , Nobuhiko Shibakawa , Hiroshi Fujiwara , Etsuro Itoh , Keiji Matsunobu , Keiichi Tabata , Hiroshi Yasuda , Yoshimi Fujihara, deceased
发明人： Tomio Kimura , Nobuhiko Shibakawa , Hiroshi Fujiwara , Etsuro Itoh , Keiji Matsunobu , Keiichi Tabata , Hiroshi Yasuda , Yoshimi Fujihara, deceased
IPC分类号： E04F13/08 , A61K31/5025 , A61P1/04 , C07D487/04 , E04F13/073 , E04F13/26 , E04F19/02
CPC分类号： C07D487/04
摘要： Pyrrolopyridazine derivatives having the general formula. ##STR1## In the above formula, R.sup.1 represents a C.sub.2 -C.sub.6 alkenyl-group, a halogeno-C.sub.2 -C.sub.6 -alkenyl group, a C.sub.6 -C.sub.10 aryl-C.sub.2 -C.sub.6 -alkenyl group, a C.sub.2 -C.sub.6 alkynyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.6 -alkyl group, a C.sub.5 -C.sub.7 cycloalkenyl-C.sub.1 -C.sub.6 -alkyl group or a halogeno-C.sub.1 -C.sub.6 -alkyl group; R.sup.2 and R.sup.3 are the same or different and each represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.6 -C.sub.10 aryl group; R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.5 represents a C.sub.6 -C.sub.10 aryl group or a 5-10 membered heteroaryl group comtaining heteroatom(s) selected from nitrogen, oxygen and sulfur;
摘要翻译：具有通式的吡咯并哒嗪衍生物。在上式中，R 1表示C 2 -C 6链烯基，卤代-C 2 -C 6 - 烯基，C 6 -C 10芳基-C 2 -C 6 - 烯基，C 2 -C 6炔基，C 3 -C 7环烷基 C 3 -C 7环烷基-C 1 -C 6烷基，C 5 -C 7环烯基-C 1 -C 6烷基或卤代-C 1 -C 6烷基; R2和R3相同或不同，各自表示氢原子，C1-C6烷基或C6-C10芳基; R4表示氢原子或C1-C6烷基; R5表示C6-C10芳基或含有选自氮，氧和硫的杂原子的5-10元杂芳基;

10. 发明授权

US07829580B2 Cyclic amine derivative having heteroaryl ring 失效
标题翻译：具有杂芳基环的环胺衍生物
公开(公告)号：US07829580B2
公开(公告)日：2010-11-09
申请号：US11442429
申请日：2006-05-26
申请人： Tomio Kimura , Naoki Tanaka , Atsuhiro Sugidachi , Toshiyuki Konosu
发明人： Tomio Kimura , Naoki Tanaka , Atsuhiro Sugidachi , Toshiyuki Konosu
IPC分类号： A61K31/445 , C07D211/54
CPC分类号： C07D211/72 , C07D401/06 , C07D401/14 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： A compound having the general formula (I) wherein R1 represents C1-C6 alkyl, etc., R2 represents hydrogen, C2-C7 alkanoyl, C7-C11 arylcarbonyl, the formula R4—(CH2)l—, etc., R3 represents C6-C10 aryl, etc., X1, X2, X3, X4 and X5 each independently represents hydrogen, halogen, etc., and n represents an integer of 0 to 2, pharmacologically acceptable salts thereof or prodrugs thereof. They have excellent inhibition of platelet activation, etc. and are useful as a prophylactic or therapeutic agents for diseases related to thrombus or embolus formation.
摘要翻译：具有通式（I）的化合物，其中R1表示C1-C6烷基等，R2表示氢，C2-C7烷酰基，C7-C11芳基羰基，式R4-（CH2）-1-等，R3表示C6 -C 10芳基等，X 1，X 2，X 3，X 4和X 5各自独立地表示氢，卤素等，n表示0〜2的整数，其药理学上可接受的盐或其前药。它们具有优异的血小板活化抑制等，并且可用作与血栓或栓塞形成有关的疾病的预防或治疗剂。

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