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1. 发明授权

US08211919B2 Amide derivatives as rock inhibitors 失效
标题翻译：酰胺衍生物作为岩石抑制剂
公开(公告)号：US08211919B2
公开(公告)日：2012-07-03
申请号：US12065043
申请日：2006-08-29
申请人： Kouzo Sawada , Tatsuya Zenkoh , Takeshi Terasawa , Yoshimasa Imamura , Hiroki Fukudome , Satoru Kuroda , Jun Maeda , Junko Watanabe , Hiroshi Inami , Nobuaki Takeshita
发明人： Kouzo Sawada , Tatsuya Zenkoh , Takeshi Terasawa , Yoshimasa Imamura , Hiroki Fukudome , Satoru Kuroda , Jun Maeda , Junko Watanabe , Hiroshi Inami , Nobuaki Takeshita
IPC分类号： A61K31/44 , A61K31/47 , A61K31/505 , A61K31/54 , C07D239/02 , C07D413/00 , C07D499/48
CPC分类号： C07D213/40 , C07D213/61 , C07D213/75 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
摘要翻译：本发明涉及新颖的酰胺衍生物及其盐。更具体地说，本发明涉及作为ROCK抑制剂的新型酰胺衍生物及其盐，涉及包含该酰胺衍生物及其盐的治疗和/或预防ROCK相关疾病的方法。

2. 发明申请

US20090105231A1 AMIDE DERIVATIVES AS ROCK INHIBITORS 失效
标题翻译：酰胺衍生物作为岩石抑制剂
公开(公告)号：US20090105231A1
公开(公告)日：2009-04-23
申请号：US12065043
申请日：2006-08-29
申请人： Kouzo Sawada , Tatsuya Zenkoh , Takeshi Terasawa , Yoshimasa Imamura , Hiroki Fukudome , Satoru Kuroda , Jun Maeda , Junko Watanabe , Hiroshi Inami , Nobuaki Takeshita
发明人： Kouzo Sawada , Tatsuya Zenkoh , Takeshi Terasawa , Yoshimasa Imamura , Hiroki Fukudome , Satoru Kuroda , Jun Maeda , Junko Watanabe , Hiroshi Inami , Nobuaki Takeshita
IPC分类号： A61K31/541 , C07D213/56 , A61K31/4409 , A61K31/4725 , C07D409/12 , A61P25/28 , A61K31/506 , C07D401/12 , C07D417/12
CPC分类号： C07D213/40 , C07D213/61 , C07D213/75 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention relates to novel amide derivatives and salts thereof. More particularly, it relates to novel amide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
摘要翻译：本发明涉及新颖的酰胺衍生物及其盐。更具体地说，本发明涉及作为ROCK抑制剂的新型酰胺衍生物及其盐，涉及包含该酰胺衍生物及其盐的治疗和/或预防ROCK相关疾病的方法。

3. 发明申请

US20110166161A1 HETEROCYCLIC CARBOXAMIDE COMPOUNDS 审中-公开
标题翻译：杂环羧酰胺化合物
公开(公告)号：US20110166161A1
公开(公告)日：2011-07-07
申请号：US13061855
申请日：2009-09-17
申请人： Takeshi Terasawa , Shinji Shigenaga , Shinji Itoh , Jun Maeda , Hideyuki Watanabe , Satoshi Kubo , Noe Iahii
发明人： Takeshi Terasawa , Shinji Shigenaga , Shinji Itoh , Jun Maeda , Hideyuki Watanabe , Satoshi Kubo , Noe Iahii
IPC分类号： A61K31/4965 , C07D213/72 , A61K31/44 , C07D409/02 , A61K31/4436 , C07D401/02 , A61K31/4545 , C07D241/10 , C07D239/02 , A61K31/505 , A61P19/02 , A61P9/00 , A61P11/00 , A61P27/02
CPC分类号： C07D213/82 , C07D239/48 , C07D241/26 , C07D401/12 , C07D409/12
摘要： This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
摘要翻译：本发明涉及新型杂环羧酰胺衍生物及其盐。更具体地说，本发明涉及作为ROCK抑制剂的新型杂环羧酰胺衍生物及其盐，涉及包含其的药物组合物以及在治疗和/或预防ROCK相关疾病中使用该化合物的方法。

4. 发明授权

US5401734A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US5401734A
公开(公告)日：1995-03-28
申请号：US63982
申请日：1993-05-20
申请人： Hideaki Yamanaka , Yoshiki Yoshida , Jiro Goto , Takeshi Terasawa , Shinya Okuda , Kazuo Sakane
发明人： Hideaki Yamanaka , Yoshiki Yoshida , Jiro Goto , Takeshi Terasawa , Shinya Okuda , Kazuo Sakane
IPC分类号： A61K31/545 , C07D501/18 , C07D501/36 , C07D501/46
CPC分类号： C07D501/46
摘要： Cephem compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,Z is N or CH,R.sup.2 is lower alkyl, mono(or di or tri)halo(lower)alkyl, lower alkenyl, lower alkynyl, phenyl, naphthyl, phenyl(lower)alkyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl, andR is a group of the formula: ##STR2## in which R.sup.3 and R.sup.4 are each lower alkyl,A is lower alkylene, andR.sup.5 is hydroxy or a protected hydroxy group; or pharmaceutically acceptable salts thereof show antimicrobial activities and are useful in the treatment of microbial infections.
摘要翻译：下式化合物：其中R 1为氨基或被保护的氨基，Z为N或CH，R 2为低级烷基，单（或二或三）卤代（低级）烷基，低级烯基，低级炔基，苯基，萘基，苯基（低级）烷基，羧基（低级）烷基或保护的羧基（低级）烷基，R是下式的基团：其中R 3和R 4各自为低级烷基，A为低级亚烷基， R5是羟基或被保护的羟基; 或其药学上可接受的盐显示抗微生物活性，并且可用于治疗微生物感染。

5. 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。

6. 发明授权

US06468995B1 Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US06468995B1
公开(公告)日：2002-10-22
申请号：US08781924
申请日：1996-12-30
申请人： Kohji Kawabata , Takeshi Terasawa , Ayako Ohki , Fumiyuki Shirai , Hirofumi Yamamoto
发明人： Kohji Kawabata , Takeshi Terasawa , Ayako Ohki , Fumiyuki Shirai , Hirofumi Yamamoto
IPC分类号： C07D50134
CPC分类号： C07D501/00 , Y02P20/55
摘要： A compound of the formula: wherein R1 is amino or protected amino; R2 is hydrogen, lower alkyl or hydroxy protective group; R3 is carboxy or protected carboxy; R4 is an unsubstituted 5, 6 or 7-membered heteromonocyclic group containing two nitrogen atoms as heteroatoms, and which optionally further contains one oxygen or sulfur atom; or R4 is said 5, 6 or 7-membered heteromonocyclic group substituted by 1 to 4 groups selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, cyclo(lower)alkyl, cyclo(lower)alkenyl, halogen, amino, protected amino, protected hydroxy, cyano, nitro, carboxy, hydroxy(lower)alkyl, amino(lower)alkyl, and carbamoyloxy; and n is 1 or 2.
摘要翻译：下式的化合物：其中R 1是氨基或被保护的氨基; R 2是氢，低级烷基或羟基保护基; R 3是羧基或被保护的羧基; R 4是未取代的5,6或7元杂单环基，杂原子，并且任选地还含有一个氧或硫原子; 或R4是由1-4个选自低级烷基，低级烷氧基，低级烷硫基，低级烷基氨基，环（低级）烷基，环（低级）烯基，卤素，氨基，保护的氨基，保护的羟基，氰基，硝基，羧基，羟基（低级）烷基，氨基（低级）烷基和氨基甲酰氧基; andn是1或2。

7. 发明授权

US4842816A High toughness steel 失效
标题翻译：高韧性钢
公开(公告)号：US4842816A
公开(公告)日：1989-06-27
申请号：US77976
申请日：1987-07-27
申请人： Akihiro Miyasaka , Hiroyo Haga , Takeshi Terasawa
发明人： Akihiro Miyasaka , Hiroyo Haga , Takeshi Terasawa
IPC分类号： C22C38/00 , C22C38/14 , C22C38/50 , C22C38/58
CPC分类号： C22C38/14
摘要： A steel composition particularly suitable for the manufacture of electric resistance welded pipes for use in most hostile environments and able to display excellent sour resistance and high toughness. The aluminum content of the steel composition is reduced to not more than 0.005%, while from 0.006 to 0.2% in total of one or both of titanium and zirconium is used instead for steel containing 0.0005 to 0.008% Ca. The steel, apart from iron and unavoidable impurities further contains:0.01 to 0.35% C0.02 to 0.5% Si0.1 to 1.8% Mnnot more than 0.015% P, andnot more than 0.003% SCu, Ni, Cr, Mo, Nb and V may be added in appropriate amounts to enhance the steel performance.
摘要翻译：一种钢组合物，特别适用于制造用于大多数恶劣环境的电阻焊管，能够显示出优异的耐酸性和高韧性。钢组合物的铝含量降低到不超过0.005％，而代替含有0.0005至0.008％Ca.a的钢代替钛和锆中的一种或两种，从0.006至0.2％。除了铁和不可避免的杂质之外，钢还含有：0.01〜0.35％的C 0.02〜0.5％的Si 0.1〜1.8％的Mn不大于0.015％的P，不超过0.003％的S Cu，Ni，Cr，Mo，Nb 并且可以以适当的量添加V以提高钢的性能。

8. 发明授权

US5532354A Intermediates for cephem compounds 失效
标题翻译：头孢烯化合物的中间体
公开(公告)号：US5532354A
公开(公告)日：1996-07-02
申请号：US350065
申请日：1994-11-29
申请人： Hideaki Yamanaka , Yoshiki Yoshida , Jiro Goto , Takeshi Terasawa , Shinya Okuda , Kazuo Sakane
发明人： Hideaki Yamanaka , Yoshiki Yoshida , Jiro Goto , Takeshi Terasawa , Shinya Okuda , Kazuo Sakane
IPC分类号： A61K31/545 , C07D501/18 , C07D501/36 , C07D501/46
CPC分类号： C07D501/46
摘要： Compounds of the formula: ##STR1## wherein R is a group of the formula: ##STR2## in which R.sup.3 and R.sup.4 are each lower alkyl or R.sup.3 and R.sup.4 are linked together to form C.sub.3 -C.sub.6 alkylene, A is lower alkylene, and R.sup.5 is hydroxy or a protected hydroxy group;or a group of the formula: ##STR3## in which R.sup.6 is lower alkyl, R.sup.7 and R.sup.8 are each hydroxy or a protected hydroxy group, and Y is N or CH, and salts thereof are intermediates for cephem compounds which show antimicrobial activities and which are useful in the treatment of microbial infections.
摘要翻译：其中R是下式的基团：其中R 3和R 4各自为低级烷基或R 3和R 4连接在一起形成C 3 -C 6亚烷基，A为低级亚烷基，R 5为是羟基或被保护的羟基; 或下式的基团：其中R 6为低级烷基，R 7和R 8各自为羟基或被保护的羟基，Y为N或CH，并且其盐为显示抗微生物活性的头孢烯化合物的中间体，可用于治疗微生物感染。

9. 发明授权

US5359066A Certain tricyclic pyrido[3,2,1-ij]cinnoline-8-carboxylates, useful as antimicrobial agents 失效
标题翻译：某些三环吡啶并[3,2,1-ij]噌啉-8-羧酸盐，可用作抗微生物剂
公开(公告)号：US5359066A
公开(公告)日：1994-10-25
申请号：US938249
申请日：1993-06-15
申请人： Hideo Tsutsumi , Takeshi Terasawa , David Barrett , Masayoshi Murata , Kazuo Sakane , Akira Yazaki , Satoshi Inoue
发明人： Hideo Tsutsumi , Takeshi Terasawa , David Barrett , Masayoshi Murata , Kazuo Sakane , Akira Yazaki , Satoshi Inoue
IPC分类号： C07D471/06 , C07D519/00 , A61K31/50 , C07D487/06
CPC分类号： C07D471/06 , Y02P20/55
摘要： A compound represented by the following general formula: ##STR1## which is useful as an intermediate for production of a clinically excellent synthetic antibacterial, a salt thereof, and a process for producing the same.In said formula,R.sup.1 is a hydrogen atom or a carboxyl-protecting group;R.sup.2 is a hydrogen atom or a lower alkyl group;X.sup.1 is a hydrogen atom or a halogen atom;X.sup.2 is a halogen atom;X.sub.a.sup.5 is a hydrogen atom or a halogen atom;A is a methylene group; a group of >CH--COOR.sup.4, etc.,in which R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom or a carboxyl-protecting group;B is a methylene group or a carbonyl group;provided that both A and B must not be methylene groups at the same time.
摘要翻译： PCT No.PCT / JP92 / 00215 Sec。 371日期：1993年6月15日 102（e）日期1993年6月15日PCT提交1992年2月27日PCT公布。第WO92 / 15584号公报日期：1992年9月17日，由以下通式表示的化合物：作为制备临床上优异的合成抗菌剂的中间体及其制备方法可以使用的化合物（A）。在所述式中，R 1为氢原子或羧基保护基; R2是氢原子或低级烷基; X1是氢原子或卤素原子; X2是卤原子; Xa5是氢原子或卤素原子; A是亚甲基; 一组> CH-COOR4等，其中R4，R5和R6各自为氢原子或羧基保护基; B是亚甲基或羰基; 条件是A和B不能同时为亚甲基。

10. 发明授权

US5244890A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US5244890A
公开(公告)日：1993-09-14
申请号：US885252
申请日：1992-05-20
申请人： Hideaki Yamanaka , Yoshiki Yoshida , Jiro Goto , Takeshi Terasawa , Shinya Okuda , Kazuo Sakane
发明人： Hideaki Yamanaka , Yoshiki Yoshida , Jiro Goto , Takeshi Terasawa , Shinya Okuda , Kazuo Sakane
IPC分类号： A61K31/545 , C07D501/18 , C07D501/36 , C07D501/46
CPC分类号： C07D501/46
摘要： Cephem compounds having the following formula are disclosed: ##STR1## R.sup.1 =amino or protected amino R.sup.2 =an organic group ##STR2## R.sup.6 =lower alkyl R.sup.7, R.sup.8 .dbd.OH or protected OHY.dbd.N or CHThe compounds are useful as antimicrobial agents.
摘要翻译：公开了具有下式的头孢烯化合物：R1 =氨基或被保护的氨基R2 =有机基团R6 =低级烷基R7，R8 = OH或受保护的OH Y = N或CH该化合物可用作抗微生物剂。

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