公开(公告)号：US4960883A

公开(公告)日：1990-10-02

申请号：US310683

申请日：1989-02-15

申请人： Sohei Tanabe ,  Seiichi Sato ,  Yoshinori Kyotani ,  Tomio Ohta ,  Yasumi Uchida

发明人： Sohei Tanabe ,  Seiichi Sato ,  Yoshinori Kyotani ,  Tomio Ohta ,  Yasumi Uchida

IPC分类号： C07D295/18 ,  A61K31/47 ,  A61K31/472 ,  A61K31/495 ,  A61K31/55 ,  A61P9/00 ,  C07D217/02 ,  C07D243/08 ,  C07D295/192 ,  C07D295/22 ,  C07D295/26

CPC分类号： C07D295/192 ,  C07D217/02 ,  C07D295/26

摘要： A propane derivative represented by the following formula ##STR1## wherein R represents a lower alkyl group; one of A and B represents a group of the formula ##STR2## and the other represents a group of the formula ##STR3## in which R.sup.1 and R.sup.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, R.sup.3 represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group, and X represents a sulfonyl group or a carbonyl group,and an acid addition salt thereof. The compounds provided by this invention have useful biological activities such as the spasmolytic activity on the vascular smooth muscles and anti-platelet aggregatory activity and are useful as drugs for treating cardiovascular diseases such as angina pectoris, cerebral circulation disorder and thrombosis.

公开(公告)号：US4948892A

公开(公告)日：1990-08-14

申请号：US310684

申请日：1989-02-15

申请人： Sohei Tanabe ,  Seiichi Sato ,  Yoshinori Kyotani ,  Tomio Ohta ,  Yasumi Uchida

发明人： Sohei Tanabe ,  Seiichi Sato ,  Yoshinori Kyotani ,  Tomio Ohta ,  Yasumi Uchida

IPC分类号： C07D295/12 ,  A61K31/495 ,  A61P9/00 ,  C07D213/74 ,  C07D213/75 ,  C07D241/04 ,  C07D295/13

CPC分类号： C07D213/74 ,  C07D295/13

摘要： A sulfonamide compound represented by the following formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are identical or different, and each represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; R.sup.4 represents a hydrogen atom, a lower alkyl group, or a substituted or unsubstituted aralykyl group; R.sup.5 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted aralkyl group; R.sup.6 and R.sup.7 are identical or different and each represents a hydrogen atom, a lower alkyl group or a lower alkoxy group; and n is an integer of 1 to 8,and an acid addition salt thereof. The compounds of formula (I) provided by this invention have some useful biological activities such as the spasmolytic activity on the vascular smooth muscles and anti-platelet aggregatory activity and are useful as drugs for treating cardiovascular disorders such as angina pectoris, cerebral circulation disorder and thrombosis.

公开(公告)号：US5576324A

公开(公告)日：1996-11-19

申请号：US325270

申请日：1994-10-27

申请人： Yoshinori Kyotani ,  Tadaaki Ohgiya ,  Tsutomu Toma ,  Yuji Kurihara ,  Takahiro Kitamura ,  Takashi Yamaguchi ,  Kazuhiro Onogi ,  Seiichi Sato ,  Hiromichi Shigyo ,  Tomio Ohta ,  Mitsuo Kawada ,  Yasumi Uchida

发明人： Yoshinori Kyotani ,  Tadaaki Ohgiya ,  Tsutomu Toma ,  Yuji Kurihara ,  Takahiro Kitamura ,  Takashi Yamaguchi ,  Kazuhiro Onogi ,  Seiichi Sato ,  Hiromichi Shigyo ,  Tomio Ohta ,  Mitsuo Kawada ,  Yasumi Uchida

IPC分类号： C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  A61K31/44

CPC分类号： C07D491/04

摘要： A quinoline derivative represented by general formula (1), a medicinally acceptable salt thereof, and a remedy for cardiac diseases containing the same: ##STR1## [wherein ring A represents a furan, dihydrofuran or dioxolane ring, and R.sup.1 represents an aminoalkyl group].The compound (1) has a positively inotropic effect on myocardia and an antiarrhythmic effect, and can dilate blood vessels without extremely increasing the heart rate. Therefore, a remedy for cardiac diseases containing the same as the active ingredient is remarkably useful for treating cardiac insufficiency, arrhythmia, and so forth.

摘要翻译： PCT No.PCT / JP93 / 00566 Sec。 371日期：1994年10月27日 102（e）日期1994年10月27日PCT提交1993年4月28日PCT公布。 公开号WO93 / 22317 日本特公昭日1993年11月11日由通式（1）表示的喹啉衍生物及其药学上可接受的盐以及含有该喹啉衍生物的心脏病的药物：其中环A表示呋喃，二氢呋喃或二氧戊环 ，R1表示氨基烷基]。 化合物（1）对心肌具有正性变力作用，具有抗心律失常作用，能够扩张血管而不会极大地提高心率。 因此，含有与活性成分相同的心脏病的治疗对于治疗心功能不全，心律失常等是非常有用的。

公开(公告)号：US5510366A

公开(公告)日：1996-04-23

申请号：US330670

申请日：1994-10-28

申请人： Yoshinori Kyotani ,  Katsumi Kawamine ,  Tsutomu Toma ,  Tadaaki Ohgiya ,  Takashi Yamaguchi ,  Kazuhiro Onogi ,  Seiichi Sato ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Tomio Ohta ,  Toshiaki Oda ,  Yukihiro Okuno ,  Kimiyuki Shibuya ,  Yoshio Takahashi ,  Mikio Fujii ,  Yasumi Uchida

发明人： Yoshinori Kyotani ,  Katsumi Kawamine ,  Tsutomu Toma ,  Tadaaki Ohgiya ,  Takashi Yamaguchi ,  Kazuhiro Onogi ,  Seiichi Sato ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Tomio Ohta ,  Toshiaki Oda ,  Yukihiro Okuno ,  Kimiyuki Shibuya ,  Yoshio Takahashi ,  Mikio Fujii ,  Yasumi Uchida

IPC分类号： C07D491/04 ,  C07D491/048 ,  A61K31/40 ,  C07D491/056

CPC分类号： C07D491/04

摘要： An indole derivative represented by formula (1), ##STR1## wherein A is a group ##STR2## wherein R.sup.10 is hydrogen or lower alkyl, dotted lines may optionally be present, and R.sup.1 -R.sup.9 represents various substitutional groups. The compound (1) exhibits a positive inotropic action on cardiac muscle, an anti-arrhythmic action, and a vasodilation action without increasing the heart rate. A heart affection therapeutic agent comprising this compound as an effective component is extremely effective for treating heart failures and arrhythmia.

摘要翻译： 由式（1）表示的吲哚衍生物，本文R10为氢或低级烷基，虚线可以任选存在，R 1 -R 9表示各种取代基。 化合物（1）对心肌呈现正性肌力作用，抗心律失常作用和血管舒张作用而不增加心率。 包含该化合物作为有效成分的心脏治疗剂对于治疗心力衰竭和心律失常是非常有效的。

公开(公告)号：US4394382A

公开(公告)日：1983-07-19

申请号：US271927

申请日：1981-06-09

申请人： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

发明人： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

IPC分类号： C07D311/04 ,  A61K31/353 ,  A61P9/02 ,  A61P9/04 ,  A61P21/02 ,  C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D311/66 ,  A61K31/35

CPC分类号： C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D311/66 ,  Y10S514/821

摘要： A benzopyran compound represented by the following ##STR1## wherein A represents a direct bond or the bond --CH.sub.2 --O--,R.sub.1 represents a member selected from the group consisting of a C.sub.3 -C.sub.5 alkyl group, a hydroxy-(C.sub.3 -C.sub.5 alkyl) group, a lower alkylamino-lower alkyl group, a nitrato-(C.sub.3 -C.sub.5 alkyl) group and a phenyl-(C.sub.1 -C.sub.5) alkyl group, provided that the phenyl may be substituted by a lower alkoxy group, R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, NO.sub.2, a carbamoyl group, a lower alkyl group, a lower alkoxy group, a lower alkyleneoxy group and acetyl group,R.sub.3 represents hydrogen or NO.sub.2,B represents a direct bond, a C.sub.1 -C.sub.7 alkylene group, a --O-lower alkylene group or a --CONH-lower alkylene group, andn represents 1 or 2;and an acid addition salt thereof and a pharmaceutical composition comprising aforesaid compound.

摘要翻译： 由下式（I）表示的苯并吡喃化合物，其中A表示直接键或键-CH2-O-，R1表示选自C3-C5烷基，羟基 - （C3 -C 5烷基）基，低级烷基氨基 - 低级烷基，硝基 - （C 3 -C 5烷基）基和苯基 - （C 1 -C 5）烷基，条件是苯基可以被低级烷氧基取代，R 2 表示选自氢，卤素，OH，NO 2，氨基甲酰基，低级烷基，低级烷氧基，低级亚烷基氧基和乙酰基的成员，R 3表示氢或NO 2，B表示直接键 ，C 1 -C 7亚烷基，-O-低级亚烷基或-CONH-低级亚烷基，n表示1或2; 及其酸加成盐和包含上述化合物的药物组合物。

公开(公告)号：US4482562A

公开(公告)日：1984-11-13

申请号：US414819

申请日：1982-09-03

申请人： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

发明人： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

IPC分类号： A61K31/21 ,  A61K31/135 ,  A61K31/165 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61P9/00 ,  A61P9/12 ,  A61P25/02 ,  A61P25/28 ,  C07C67/00 ,  C07C203/04 ,  C07C213/00 ,  C07C217/32 ,  C07C217/70 ,  C07C219/16 ,  C07C219/34 ,  C07C225/16 ,  C07C231/00 ,  C07C231/12 ,  C07C235/42 ,  C07C235/46 ,  C07C237/30 ,  C07C301/00 ,  C07C303/40 ,  C07C311/17 ,  C07C311/29 ,  C07C313/00 ,  C07C315/04 ,  C07C317/22 ,  C07C317/24 ,  C07C317/32 ,  C07C319/20 ,  C07C323/25 ,  C07D213/30 ,  C07D213/60 ,  C07D213/64 ,  C07D213/69 ,  C07D303/24 ,  C07D303/26 ,  C07D309/12 ,  C07D213/74

CPC分类号： C07D213/64 ,  C07C203/04 ,  C07D213/69 ,  C07D303/24 ,  C07D303/26 ,  C07D309/12

摘要： A compound represented by the following formula ##STR1## wherein A represents a direct bond or the bond --O--CH.sub.2 --,B represents a C.sub.1 -C.sub.11 alkylene group bonded to a carbon atom of the aromatic ring D either directly or through --O--, --S--, --SO-- or --NH--,W represents a carbon or nitrogen atom,R.sub.1 represents a C.sub.3 -C.sub.7 alkyl group, a hydroxy-C.sub.1 -C.sub.6 alkyl group, or a phenyl- or diphenyl-alkyl group with the alkyl group having 1 to 4 carbon atoms,R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, C.sub.1 -C.sub.4 alkyl, NO.sub.2, C.sub.1 -C.sub.4 alkoxy, acetyl, allyloxy, carbamoyl and sulfamoyl, and when two or more R.sub.2 groups exist, they may be identical or different, andn represents 1, 2 or 3 and m represents 1 or 2, provided that n+m.gtoreq.4;and an acid addition salt thereof; a process for producing the same; and a pharmaceutical composition comprising aforesaid compound.

公开(公告)号：US4374840A

公开(公告)日：1983-02-22

申请号：US233643

申请日：1981-02-11

申请人： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

发明人： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

IPC分类号： A61K31/21 ,  A61K31/135 ,  A61K31/165 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61P9/00 ,  A61P9/12 ,  A61P25/02 ,  A61P25/28 ,  C07C67/00 ,  C07C203/04 ,  C07C213/00 ,  C07C217/32 ,  C07C217/70 ,  C07C219/16 ,  C07C219/34 ,  C07C225/16 ,  C07C231/00 ,  C07C231/12 ,  C07C235/42 ,  C07C235/46 ,  C07C237/30 ,  C07C301/00 ,  C07C303/40 ,  C07C311/17 ,  C07C311/29 ,  C07C313/00 ,  C07C315/04 ,  C07C317/22 ,  C07C317/24 ,  C07C317/32 ,  C07C319/20 ,  C07C323/25 ,  C07D213/30 ,  C07D213/60 ,  C07D213/64 ,  C07D213/69 ,  C07D303/24 ,  C07D303/26 ,  C07D309/12 ,  C07D213/74

CPC分类号： C07D213/64 ,  C07C203/04 ,  C07D213/69 ,  C07D303/24 ,  C07D303/26 ,  C07D309/12

摘要： A compound represented by the following formula ##STR1## wherein A represents a direct bond or the bond --0--CH.sub.2--,B represents a C.sub.1 -C.sub.11 alkylene group bonded to a carbon atom of the aromatic ring D either directly or through --O--, --S--, --SO-- or --NH--,W represents a carbon or nitrogen atom,R.sub.1 represents a C.sub.3 -C.sub.7 alkyl group, a hydroxy-C.sub.1 -C.sub.6 alkyl group, or a phenyl- or diphenyl-alkyl group with the alkyl group having 1 to 4 carbon atoms,R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, C.sub.1 -C.sub.4 alkyl, NO.sub.2, C.sub.1 -C.sub.4 alkoxy, acetyl, allyloxy, carbamoyl and sulfamoyl, and when two or more R.sub.2 groups exist, they may be identical or different, andn represents 1, 2 or 3 and m represents 1 or 2, provided that n+m.gtoreq.4;and an acid addition salt thereof; a process for producing the same; and a pharmaceutical composition comprising aforesaid compound.

摘要翻译： 由下式表示的化合物：其中A表示直接键或-O-CH 2 - 键，B表示与芳环D的碳原子键合的C1-C11亚烷基直接或-O- ，-S-，-SO-或-NH-，W表示碳原子或氮原子，R1表示C3-C7烷基，羟基-C1-C6烷基或苯基或二苯基 - 烷基，其中 具有1至4个碳原子的烷基，R 2表示选自氢，卤素，OH，C 1 -C 4烷基，NO 2，C 1 -C 4烷氧基，乙酰基，烯丙氧基，氨基甲酰基和氨磺酰基的成员，当两个或更多个 R2基团存在，它们可以相同或不同，n表示1,2或3，m表示1或2，条件是n + m> = 4; 及其酸加成盐; 其制造方法; 和包含上述化合物的药物组合物。

公开(公告)号：US06861428B2

公开(公告)日：2005-03-01

申请号：US10396726

申请日：2003-03-26

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D237/14 ,  C07D237/24 ,  A61K31/51 ,  C07D237/04 ,  C07D403/06

CPC分类号： A61K31/50 ,  A61K31/501 ,  C07D237/14 ,  C07D237/24

摘要： Compounds having the formula (1): wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represents a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represents a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to pharmaceutical compositions containing them. These compounds have inhibitory activity against IL-1β production, high water solubility and good oral absorbability.

摘要翻译： 具有式（1）的化合物：其中R 1表示烷基或烯基，R 2和R 3各自独立地表示氢原子或烷基，羟基烷基，二羟基烷基或炔基，或R 2 >和R 3可以与相邻的氮原子一起形成取代或未取代的含氮饱和杂环基，X，Y和Z各自独立地表示氢原子，烷基，卤素原子或 n，n表示1〜5的整数， 以及含有它们的药物组合物。 这些化合物对IL-1β生产具有抑制活性，水溶性高，口服吸收性好。

公开(公告)号：US20050085480A1

公开(公告)日：2005-04-21

申请号：US10960993

申请日：2004-10-12

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  A61P1/04 ,  A61P9/00 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P37/02 ,  A61P43/00 ,  C07D237/24 ,  C07D43/02

CPC分类号： C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  C07D237/24

摘要： Compounds having the formula (1): wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1β production, high water solubility and good oral absorbability.

摘要翻译： 具有式（1）的化合物：其中R 1表示烷基或烯基，R 2和R 3各自独立地表示氢原子 或烷基，羟基烷基，二羟基烷基或炔基或R 2和R 3可以与相邻的氮原子一起形成取代或未取代的含氮的 饱和杂环基，X，Y和Z各自独立地表示氢原子，烷基，卤素原子等，n表示1〜5的整数， 以及含有它们的药物组合物。 这些化合物对IL-1β生产具有抑制活性，水溶性高，口服吸收性好。

公开(公告)号：US07211577B2

公开(公告)日：2007-05-01

申请号：US10544881

申请日：2004-03-16

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： C07D237/04 ,  C07D403/06 ,  A61K31/50 ,  A61K31/51

CPC分类号： A61K31/501 ,  A61K31/50 ,  C07D237/14

摘要： A phenylpyridazine derivative represented by the formula (1): Wherein, R1, R2, R3, X, Y, Z and n have the same meaning as defined in the specification; or a salt thereof, or a medicine containing the compound. The present invention provides water-soluble phenylpyridazine derivatives and medicines containing them, which have excellent inhibitory activity against interleukin-β production, high water solubility and high oral absorbability.

摘要翻译： 由式（1）表示的苯基哒嗪衍生物：其中R1，R2，R3，X，Y，Z和n与说明书中定义相同; 或其盐，或含有该化合物的药物。 本发明提供水溶性苯基哒嗪衍生物和含有它们的药物，其对白细胞介素-β产生具有优异的抑制活性，高水溶性和高口服吸收性。