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1. 发明申请

US20050038035A1 Heterocyclic amide compounds as apolipoprotein b inhibitors 审中-公开
标题翻译：杂环酰胺化合物作为载脂蛋白b抑制剂
公开(公告)号：US20050038035A1
公开(公告)日：2005-02-17
申请号：US10496967
申请日：2002-10-24
申请人： Hisashi Takasugi , Yoshikazu Inoue , Takeshi Terasawa , Akira Nagayoshi , Yoshiro Furukawa , Masafumi Mikami , Kazumasa Hinoue , Makoto Ohtsubo , Daisuke Fukumoto
发明人： Hisashi Takasugi , Yoshikazu Inoue , Takeshi Terasawa , Akira Nagayoshi , Yoshiro Furukawa , Masafumi Mikami , Kazumasa Hinoue , Makoto Ohtsubo , Daisuke Fukumoto
IPC分类号： A61K31/27 , A61K31/395 , A61K31/4035 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P43/00 , C07C231/02 , C07C233/62 , C07C269/06 , C07C271/24 , C07D207/32 , C07D207/335 , C07D209/44 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/50 , C07D213/53 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/89 , C07D217/04 , C07D217/18 , C07D217/20 , C07D233/54 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/04 , C07D249/08 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/46 , C07D277/48 , C07D295/02 , C07D295/033 , C07D295/12 , C07D295/135 , C07D295/14 , C07D295/15 , C07D295/155 , C07D295/18 , C07D295/192 , C07D295/20 , C07D295/205 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/06 , C07D417/12 , C07D43/02
CPC分类号： C07D207/335 , C07C271/24 , C07C2601/10 , C07C2602/08 , C07D209/44 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/50 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D217/04 , C07D217/18 , C07D217/20 , C07D233/64 , C07D239/26 , C07D239/42 , C07D249/08 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/46 , C07D277/48 , C07D295/033 , C07D295/135 , C07D295/15 , C07D295/155 , C07D295/192 , C07D295/205 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/12 , C07D417/06 , C07D417/12
摘要： The present invention relates to a compound of the formula (I) wherein R1 is optionally substituted aryl; R2 is optionally substituted aryl, optionally substituted heteroaryl, optionally substituted lower cycloalkyl, optionally substituted aryloxy, optionally substituted arylsulfonyl, vinyl, carbamoyl, protected carboxy or protected amino; ring A is bivalent residue derived from optionally substituted aryl or optionally substituted heteroaryl; X is bivalent residue derived from the group consisting of cycloalkene, naphthalene, unsaturated 5 or 6-membered heteromonocyclic group, each of which is optionally substituted, and substituted benzene; Y is -(A1)m1-(A2)m2-; and Z is direct bond or piperazine, or a salt thereof. The compound of the present invention and a salt thereof inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.
摘要翻译：本发明涉及式（I）化合物，其中R 1为任选取代的芳基; R 2是任选取代的芳基，任选取代的杂芳基，任选取代的低级环烷基，任选取代的芳氧基，任选取代的芳基磺酰基，乙烯基，氨基甲酰基，保护的羧基或被保护的氨基; 环A是衍生自任选取代的芳基或任选取代的杂芳基的二价残基; X是衍生自环烯，萘，不饱和5或6元杂单环基团的二价残基，各自任选被取代，取代的苯; Y为 - （A 1）m1-（A 2）m2-; Z是直接键合或哌嗪或其盐。本发明化合物及其盐抑制载脂蛋白B（Apo B）分泌，可用作预防和治疗由ApoB升高的循环水平引起的疾病或病症的药物。

2. 发明授权

US5371097A Thiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same 失效
标题翻译：噻唑衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5371097A
公开(公告)日：1994-12-06
申请号：US80051
申请日：1993-06-22
申请人： Hisashi Takasugi , Yousuke Katsura , Tetsuo Tomishi , Yoshikazu Inoue
发明人： Hisashi Takasugi , Yousuke Katsura , Tetsuo Tomishi , Yoshikazu Inoue
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/44 , A61P1/04 , A61P43/00 , C07D277/48 , C07D417/04 , C07D417/14 , C07D521/00
CPC分类号： C07D417/04 , C07D277/48 , C07D417/14
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is amino, acylamino, cyclo(lower)alkenylamino having amino and oxo, imido, triazolylamino, benzoisothiazolylamino, wherein each of said heterocyclicamino groups may be substituted by one or more substituent(s) selected from the group consisting of lower alkyl, amino and oxo, 2-cyano-3-lower alkylguanidino, 2-acyl-3-lower alkylguanidino, 2-acylguanidino, (1-lower alkylamino-2-nitrovinyl)amino, hydroxy, halogen, cyano, acyl, benzimidazolylthio, triazolyl substituted with amino, or a group of the formula: ##STR2## in which R.sup.4 is hydrogen, cyano, or acyl, andR.sup.5 is amino or lower alkoxy,R.sup.2 and R.sup.3 are each hydrogen, acyl or lower alkyl which may have halogen; orR.sup.2 and R.sup.3 are linked together to form lower alkylene,Y is ##STR3## in which R.sup.6 is hydrogen or halogen, andA is lower alkylene, or pharmaceutically acceptable salt thereof.
摘要翻译：下式的化合物，其中R 1是氨基，酰氨基，具有氨基和氧代的环（低级）烯基氨基，亚氨基，三唑基氨基，苯并异噻唑基氨基，其中每个所述杂环氨基可以被一个或多个被选择的取代基取代由2-烷基氨基和氧代低级烷基，2-氰基-3-低级烷基胍基，2-酰基-3-低级烷基胍基，2-酰基胍基，（1-低级烷基氨基-2-硝基乙烯基）氨基，羟基，卤素，氰基，酰基，苯并咪唑硫基，被氨基取代的三唑基或下式的基团：其中R 4是氢，氰基或酰基，R 5是氨基或低级烷氧基，R 2和R 3各自是氢，酰基或更低级可以具有卤素的烷基; 或R 2和R 3连接在一起形成低级亚烷基，Y是其中R 6是氢或卤素，A是低级亚烷基或其药学上可接受的盐。

3. 发明授权

US07465731B2 HDAC inhibitor 失效
标题翻译： HDAC抑制剂
公开(公告)号：US07465731B2
公开(公告)日：2008-12-16
申请号：US11199453
申请日：2005-08-09
申请人： Naoki Ishibashi , Yuki Sawada , Yasuharu Urano , Shigeki Satoh , Yoshikazu Inoue , Yoshiteru Eikyu , Koichiro Mukoyoshi , Kazunori Kamijo , Fumiyuki Shirai , Hisashi Takasugi
发明人： Naoki Ishibashi , Yuki Sawada , Yasuharu Urano , Shigeki Satoh , Yoshikazu Inoue , Yoshiteru Eikyu , Koichiro Mukoyoshi , Kazunori Kamijo , Fumiyuki Shirai , Hisashi Takasugi
IPC分类号： C07D401/12 , C07D403/12 , A61K31/497 , A61K31/506 , A61K31/501
CPC分类号： C07D213/74 , C07C259/06 , C07D207/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14
摘要： A compound having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is arylene, heterorarylene, cycloalkylene, heterocycloalkylene or aryl-fused cycloalkene, Y is arylene, heteroarylene, which may be substituted with one or more suitable substituent(s), Z lower alenylene, which may be substituted with lower alkyl or halogen, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.
摘要翻译：具有式（I）的化合物：其中R1是氢，低级烷基，低级烯基，低级或高级炔基，环（低级）烷基，环（高级）烷基，环（低级）烷基（低级）烷基，环）（低级）烷基，低级（低级）烷基，芳基稠合环（低级）烷基，低级烷氧基，酰基，芳基，芳（低级）烷氧基，，氨基，杂芳基，杂环基或杂环基（低级）烷基，其可以被一个或多个合适的取代基取代，R 2是氢或低级烷基，X是亚芳基，杂亚芳基，亚环烷基，亚杂环基或芳基稠合的环烯，Y 是亚芳基，可以被一个或多个合适的取代基取代的亚杂芳基，Z可以被低级烷基或卤素取代的低级亚烯基或其盐。该化合物可用作组蛋白脱乙酰酶抑制剂。

4. 发明授权

US4563450A Cephem compounds 失效
公开(公告)号：US4563450A
公开(公告)日：1986-01-07
申请号：US515184
申请日：1983-07-19
申请人： Takao Takaya , Yoshikazu Inoue , Masayoshi Murata , Hisashi Takasugi
发明人： Takao Takaya , Yoshikazu Inoue , Masayoshi Murata , Hisashi Takasugi
IPC分类号： C07D257/04 , C07D501/36 , A61K31/545
CPC分类号： C07D257/04 , Y02P20/55
摘要： This invention relates to a new cephem compound of the formula: ##STR1## wherein R.sup.1 is amino or a substituted amino group;R.sup.2 is carboxy or a protected carboxy group;R.sup.3 is a tetrazolyl group having a lower alkynyl group; andX is --S-- or ##STR2## and pharmaceutically acceptable salts thereof, of high antimicrobial activity.

5. 发明授权

US4639448A 7-amino-3-[substituted vinyl]-3-cephem-4-carboxylates having antimicrobial activity 失效
标题翻译：具有抗菌活性的7-氨基-3- [取代的乙烯基] -3-头孢烯-4-羧酸酯
公开(公告)号：US4639448A
公开(公告)日：1987-01-27
申请号：US741267
申请日：1985-06-04
申请人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka , Kenji Miyai , Yoshikazu Inoue
发明人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka , Kenji Miyai , Yoshikazu Inoue
IPC分类号： A61K20060101 , A61K31/54 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/14 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/48
CPC分类号： C07D501/24 , C07D501/18
摘要： The invention relates to cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or acylamino,R.sup.2 is lower alkyl, andY is CH or N.

6. 发明授权

US4546101A New cephem compounds useful for treating infectious diseases in human being and animals and processes for preparation thereof 失效
标题翻译：用于治疗人和动物中的感染性疾病的新头孢烯化合物及其制备方法
公开(公告)号：US4546101A
公开(公告)日：1985-10-08
申请号：US528796
申请日：1983-09-02
申请人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka , Kenji Miyai , Yoshikazu Inoue
发明人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka , Kenji Miyai , Yoshikazu Inoue
IPC分类号： A61K20060101 , A61K31/54 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/14 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/48
CPC分类号： C07D501/24 , C07D501/18
摘要： The invention relates to cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or acylamino,R.sup.2 is lower alkyl, andY is CH or N.
摘要翻译：本发明涉及具有下式的高抗微生物活性的头孢烯化合物：其中R1是氨基或酰氨基，R2是低级烷基，Y是CH或N.

7. 发明申请

US20060052599A1 HDAC inhibitor 失效
标题翻译： HDAC抑制剂
公开(公告)号：US20060052599A1
公开(公告)日：2006-03-09
申请号：US11199453
申请日：2005-08-09
申请人： Naoki Ishibashi , Yuki Sawada , Yasuharu Urano , Shigeki Satoh , Yoshikazu Inoue , Yoshiteru Eikyu , Koichiro Mukoyoshi , Kazunori Kamijo , Fumiyuki Shirai , Hisashi Takasugi
发明人： Naoki Ishibashi , Yuki Sawada , Yasuharu Urano , Shigeki Satoh , Yoshikazu Inoue , Yoshiteru Eikyu , Koichiro Mukoyoshi , Kazunori Kamijo , Fumiyuki Shirai , Hisashi Takasugi
IPC分类号： C07D237/02 , C07C259/04
CPC分类号： C07D213/74 , C07C259/06 , C07D207/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14
摘要： A compound having the following formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower) alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is arylene, heteroarylene, cycloalkylene, heterocycloalkylene or aryl-fused cycloalkylene, Y is arylene or heteroarylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.
摘要翻译：具有下式（I）的化合物：

8. 发明授权

US5532258A H.sub.2 -receptor antagonist thiazoles 失效
标题翻译： H2受体拮抗剂噻唑
公开(公告)号：US5532258A
公开(公告)日：1996-07-02
申请号：US356967
申请日：1994-12-16
申请人： Yousuke Katsura , Tetsuo Tomishi , Yoshikazu Inoue , Hisashi Takasugi
发明人： Yousuke Katsura , Tetsuo Tomishi , Yoshikazu Inoue , Hisashi Takasugi
IPC分类号： A61K31/425 , A61K31/426 , A61K31/44 , A61P1/00 , A61P1/04 , A61P43/00 , C07D277/20 , C07D277/38 , C07D277/42 , C07D277/48 , C07D417/12 , C07D417/14 , A61K31/125
CPC分类号： C07D277/48
摘要： Thiazole compounds of formula ##STR1## are provided which have antiulcer activity and H.sub.2 -receptor antagonism, wherein R.sup.2 is lower alkyl or lower alkoxy(lower)alkyl, R.sup.3 is hydrogen, A is methylene and R.sup.1 is lower alkyl.
摘要翻译：提供具有抗溃疡活性和H2受体拮抗作用的式“IMAGE”的噻唑化合物，其中R2是低级烷基或低级烷氧基（低级）烷基，R3是氢，A是亚甲基，R1是低级烷基。

9. 发明授权

US5364871A New thiazole derivatives, and pharmaceutical composition comprising the same 失效
标题翻译：新的噻唑衍生物和包含它们的药物组合物
公开(公告)号：US5364871A
公开(公告)日：1994-11-15
申请号：US29359
申请日：1993-03-10
申请人： Hisashi Takasugi , Yousuke Katsura , Tetsuo Tomishi , Yoshikazu Inoue
发明人： Hisashi Takasugi , Yousuke Katsura , Tetsuo Tomishi , Yoshikazu Inoue
IPC分类号： C07D277/48 , C07D417/04 , C07D417/14 , A61K31/44 , C07D417/06
CPC分类号： C07D417/04 , C07D277/48 , C07D417/14
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is amino, ureido, lower alkanoylamino, lower alkoxycarbonylamino, lower alkylsulfonylamino, lower alkoxy(lower)alkanoylamino, mono or di or trihalo(lower)alkanoylamino, hydroxy(lower)alkanoylamino, protected hydroxy(lower)alkanoylamino, or a group of the formula: ##STR2## in which R.sup.4 is hydrogen or sulfamoyl, R.sup.5 is amino or lower alkoxy, R.sup.2 is hydrogen, lower alkyl, lower alkoxy(lower)alkyl, di(lower)alkylamino(lower)alkyl, (C.sub.3 -C.sub.7)-cycloalkyl, lower alkenyl or mono or di or trihalo(lower)alkyl; R.sup.3 is hydrogen or lower alkyl; or R.sup.2 and R.sup.3 are linked together to form lower alkylene,Y is ##STR3## in which R.sup.6 is hydrogen, A is lower alkylene, and W is NH; or R.sup.2 -W is piperidino or morpholino, or pharmaceutically acceptable salt thereof.
摘要翻译：下式的化合物，其中R 1是氨基，脲基，低级烷酰基氨基，低级烷氧基羰基氨基，低级烷基磺酰基氨基，低级烷氧基（低级）烷酰基氨基，一或二或三卤代（低级）烷酰基氨基，羟基（低级）烷酰基氨基，被保护的羟基（低级）烷酰基氨基或下式的基团：其中R 4是氢或氨磺酰基，R 5是氨基或低级烷氧基，R 2是氢，低级烷基，低级烷氧基（低级）烷基，二（低级）烷基氨基低级烷基，（C 3 -C 7） - 环烷基，低级烯基或一或二或三卤代（低级）烷基; R3是氢或低级烷基; 或R 2和R 3连接在一起形成低级亚烷基，Y是其中R 6是氢，A是低级亚烷基，W是NH; 或R 2 -W是哌啶子基或吗啉代，或其药学上可接受的盐。

10. 发明授权

US5308857A Furylthiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same 失效
标题翻译：呋喃噻唑衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5308857A
公开(公告)日：1994-05-03
申请号：US908795
申请日：1992-07-06
申请人： Hisashi Takasugi , Yousuke Katsura , Yoshikazu Inoue , Tetsuo Tomishi
发明人： Hisashi Takasugi , Yousuke Katsura , Yoshikazu Inoue , Tetsuo Tomishi
IPC分类号： C07D417/04 , C07D417/14 , A61K31/425
CPC分类号： C07D417/14 , C07D417/04
摘要： The invention relates to compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and Q are as described, useful in the treatment of ulcers.
摘要翻译：本发明涉及下式的化合物：其中R1，R2，R3，R4，A和Q如上所述，可用于治疗溃疡。

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