公开(公告)号：US06359134B1

公开(公告)日：2002-03-19

申请号：US09424892

申请日：1999-11-30

申请人： Hiroyuki Tawada ,  Fumio Ito ,  Norihiko Moriya ,  Zen-ichi Terashita

发明人： Hiroyuki Tawada ,  Fumio Ito ,  Norihiko Moriya ,  Zen-ichi Terashita

IPC分类号： C07D29518

CPC分类号： C07D213/30 ,  C07D211/34 ,  C07D213/56 ,  C07D213/82 ,  C07D231/12 ,  C07D233/56 ,  C07D233/88 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D277/56 ,  C07D295/26 ,  C07D307/82 ,  C07D311/58 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D417/14

摘要： The present invention provides compounds which specifically inhibit FXa, which are effective when orally administered and which are useful as a safe medicine for the prevention or treatment of diseases caused by thrombus or infarction. Compounds of this invention are piperazinones of the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, in addition to being substituted by the group of the formula: and the group of the formula: Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent heterocyclic group; X is a direct bond or an optionally substituted alkylene chain; Z is (1) an amino group substituted with an optionally substituted hydrocarbon group, (2) an optionally substituted imino group or (3) an optionally substituted nitrogen-containing heterocyclic group; provided that when X is a direct bond and Z is an optionally substituted 6-membered nitrogen-containing aromatic heterocyclic group, Y is an optionally substituted divalent hydrocarbon group or an optionally substituted divalent unsaturated heterocyclic group; or a salt thereof.

摘要翻译： 本发明提供特异性抑制FXa的化合物，其在口服给药时是有效的，并且其可用作预防或治疗由血栓或梗塞引起的疾病的安全药物。本发明的化合物是下式的哌嗪酮：其中R1是 任选取代的烃基或任选取代的杂环基; 环A是任选取代的二价含氮杂环基，除了被下式所示的基团取代：下式基团：Y是任选取代的二价烃基或任选取代的二价杂环基; X是直接键或任选取代的亚烷基链; Z是（1）被任选取代的烃基取代的氨基，（2）任选取代的亚氨基或（3）任选取代的含氮杂环基; 条件是当X是直接键，Z是任选取代的6元含氮芳族杂环基时，Y是任选取代的二价烃基或任选取代的二价不饱和杂环基; 或其盐。

公开(公告)号：US06403595B1

公开(公告)日：2002-06-11

申请号：US09601660

申请日：2000-08-03

申请人： Hiroyuki Tawada ,  Fumio Itoh ,  Hiroshi Banno ,  Zen-ichi Terashita

发明人： Hiroyuki Tawada ,  Fumio Itoh ,  Hiroshi Banno ,  Zen-ichi Terashita

IPC分类号： A61K31495

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D241/08 ,  C07D243/08 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/12

摘要： The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which have activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.

摘要翻译： 本发明提供由下式表示的化合物或其盐：其中R1是任选取代的烃基或任选取代的杂环基，环A是任选取代的二价含氮杂环基，X'是 任选取代的亚烷基链，Y是任选取代的二价环基，X是化学键或任选取代的亚烷基链，Z是（1）任选取代的氨基，（2）任选取代的亚氨基或（3） 任选取代的含氮杂环基或其前体药物，其具有活化的凝血因子X抑制活性并且可用作抗凝血剂。

公开(公告)号：US06680312B2

公开(公告)日：2004-01-20

申请号：US10128809

申请日：2002-04-24

申请人： Hiroyuki Tawada ,  Fumio Itoh ,  Hiroshi Banno ,  Zen-ichi Terashita

发明人： Hiroyuki Tawada ,  Fumio Itoh ,  Hiroshi Banno ,  Zen-ichi Terashita

IPC分类号： A61K3133

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D241/08 ,  C07D243/08 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/12

摘要： The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which has activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.

摘要翻译： 本发明提供由下式表示的化合物或其盐：其中R 1是任选取代的烃基或任选取代的杂环基，环A是任选取代的二价含氮杂环基，X '是任选取代的亚烷基链，Y是任选取代的二价环状基团，X是化学键或任选取代的亚烷基链，Z是（1）任选取代的氨基，（2）任选取代的亚氨基或 （3）具有活化凝血因子X抑制活性的任选取代的含氮杂环基或其前药，可用作抗凝血剂。

公开(公告)号：US07541478B2

公开(公告)日：2009-06-02

申请号：US10591561

申请日：2005-03-01

申请人： Shogo Marui ,  Masaki Ogino ,  Hiroyuki Tawada ,  Osamu Yabe

发明人： Shogo Marui ,  Masaki Ogino ,  Hiroyuki Tawada ,  Osamu Yabe

IPC分类号： C07D311/02

CPC分类号： C07D311/16

摘要： The present invention relates to an alkaline earth metal salt or an organic amine salt of a compound represented by the formula [I]: wherein R1 and R2 are each a hydrogen atom, a halogen atom, or an optionally substituted linear hydrocarbon group; ring A is an optionally further substituted benzene ring; B is an optionally substituted benzene ring; R is a carboxyl group or a linear hydrocarbon group substituted with a carboxyl group and the like.

摘要翻译： 本发明涉及由式[I]表示的化合物的碱土金属盐或有机胺盐：其中R1和R2各自为氢原子，卤素原子或任选取代的直链烃基; 环A是任选进一步取代的苯环; B是任选取代的苯环; R是羧基或被羧基等取代的直链烃基。

公开(公告)号：US07034039B2

公开(公告)日：2006-04-25

申请号：US10470805

申请日：2002-02-01

申请人： Satoru Oi ,  Koji Ikedou ,  Koji Takeuchi ,  Masaki Ogino ,  Yoshihiro Banno ,  Hiroyuki Tawada ,  Taihei Yamane

发明人： Satoru Oi ,  Koji Ikedou ,  Koji Takeuchi ,  Masaki Ogino ,  Yoshihiro Banno ,  Hiroyuki Tawada ,  Taihei Yamane

IPC分类号： C07D217/02 ,  A61K31/47

CPC分类号： C07D401/04 ,  C07D217/24 ,  C07D217/26 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/04 ,  C07D417/04 ,  C07D417/06 ,  C07D495/04

摘要： The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

摘要翻译： 本发明提供下式的化合物：其中环A是任选取代的5至10元芳环; R 1和R 2相同或不同，并且各自为任选取代的烃基或任选取代的杂环基; X是一个键等; 和L是二价烃基及其盐，除了3-（氨基甲基）-2,6,7-三甲基-4-苯基-1（2H） - 异喹啉酮，3-（氨基甲基）-2-甲基-4 - 苯基-1（2H） - 异喹啉酮，3-（氨基甲基）-6-氯-2-甲基-4-苯基-1（2H） - 异喹啉酮和3-（氨基甲基）-2-异丙基-4-苯基-1 （2H） - 异喹啉酮。 该化合物显示出优异的肽酶抑制活性，并且可用作预防或治疗糖尿病等的药剂。

公开(公告)号：US20050107606A1

公开(公告)日：2005-05-19

申请号：US10506955

申请日：2003-03-11

申请人： Hiroyuki Tawada ,  Tomomi Ikemoto ,  Atsuko Nishiguchi ,  Tatsuya Ito ,  Mari Adachi

发明人： Hiroyuki Tawada ,  Tomomi Ikemoto ,  Atsuko Nishiguchi ,  Tatsuya Ito ,  Mari Adachi

IPC分类号： C07D233/64 ,  A61K31/4164 ,  A61K31/55 ,  A61P43/00 ,  C07D225/06 ,  C07D233/54 ,  C07D403/12 ,  C07D43/02

CPC分类号： C07D233/64 ,  C07D225/06 ,  C07D403/12 ,  Y02P20/582

摘要： A process for preparing an optically active sulfoxide derivative (I) having CCR5 antagonism without causing side reactions such as racemization and Pummerer rearrangement, which comprises reacting a compound (II) with a compound (III) as shown by the following scheme: wherein R1 represents hydrogen, an aliphatic hydrocarbon group or an aromatic group; R2 represents halogeno, alkyl, hydroxyl, amino, an aromatic group, etc.; R3 represents a 5- or 6-membered ring; R4 represents hydrogen, alkyl, alkoxy or halogeno; R5 represents hydrogen, a hydrocarbon group, a heterocyclic group, acyl, etc.; ring A represents an optionally substituted benzene ring; X represents a bond or divalent group comprising a linear part constituted of 1 to 4 atoms; m represents an integer of 1 to 5; n represents an integer of 0 to 3; p represents an integer of 0 to 2; and *1 represents an asymmetric center.

摘要翻译： 一种制备具有CCR5拮抗作用的光学活性亚砜衍生物（I）的方法，不会引起副反应，例如外消旋化和Pummerer重排，其包括使化合物（II）与化合物（III）反应，如下列方案所示：其中R SUP> 1表示氢，脂族烃基或芳基; R 2表示卤代，烷基，羟基，氨基，芳基等; R 3表示5或6元环; R 4表示氢，烷基，烷氧基或卤代; R 5表示氢，烃基，杂环基，酰基等; 环A表示任选取代的苯环; X表示包含由1至4个原子构成的直链部分的键或二价基团; m表示1〜5的整数， n表示0〜3的整数， p表示0〜2的整数， 和* 1 表示不对称中心。

公开(公告)号：US4150139A

公开(公告)日：1979-04-17

申请号：US821623

申请日：1977-08-03

申请人： Yutaka Kuwada ,  Hiroyuki Tawada

发明人： Yutaka Kuwada ,  Hiroyuki Tawada

IPC分类号： C07D249/12 ,  C07D487/04 ,  A61K31/55

CPC分类号： C07D487/04 ,  C07D249/12

摘要： Novel triazolobenzazepine derivatives of the formula ##STR1## (wherein R.sup.1 and R.sup.2 are hydrogen or alkyl, X is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen, alkyl, aryl or aralkyl, and R.sup.5 is hydrogen or alkyl), Z is --SR.sup.6, --S(O).sub.n R.sup.6 or --OR.sup.7 (wherein R.sup.6 and R.sup.7 are alkyl or aralkyl, and n is 1 or 2), and Ring A is unsubstituted or substituted with at least one of halogen, lower alkyl, lower alkoxy and trifluoromethyl, and their physiologically acceptable salts have excellent pharmacological activities and are useful as medicines such as muscle-relaxants, analgesics and antiinflammatory drugs.

摘要翻译： 式（IMA）的新型三唑并苯并吖庚因衍生物（其中R 1和R 2是氢或烷基，X是其中R 3和R 4是氢，烷基，芳基或芳烷基，R 5是氢或烷基），Z是-SR 6， -S（O）n R 6或-OR 7（其中R 6和R 7为烷基或芳烷基，n为1或2），环A为未取代的或被至少一个卤素，低级烷基，低级烷氧基和三氟甲基取代，以及 其生理上可接受的盐具有优异的药理活性，并且可用作药物如肌肉松弛剂，止痛剂和抗炎药。

公开(公告)号：US20060142598A1

公开(公告)日：2006-06-29

申请号：US11359023

申请日：2006-02-22

申请人： Hiroyuki Tawada ,  Makoto Yamashita ,  Yujiro Ono

发明人： Hiroyuki Tawada ,  Makoto Yamashita ,  Yujiro Ono

IPC分类号： C07D493/00

CPC分类号： C07D307/79 ,  Y02P20/55

摘要： A novel process for efficiently and easily producing a compound represented by the formula: wherein ring A is a benzene ring that may be optionally further substituted in addition to the group represented by W, or a salt thereof; which comprises reacting a compound represented by the formula: wherein R1 and R2 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, Y is a halogen atom, ring A is a benzene ring that may be optionally further substituted in addition to the group represented by Y and ring B is an optionally substituted benzene ring, or a salt thereof, with a compound represented by the formula: WH wherein W is wherein ring C is an optionally substituted benzene ring, ring D is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, R3 is a hydrogen atom, an aliphatic hydrocarbon group containing an aromatic group or an acyl group, and R4 is a hydrogen atom, an optionally substituted hydrocarbon group or an acyl group, or a salt thereof and thereafter, if necessary, deprotecting the resultant product, which is suitable for industrial production.

摘要翻译： 一种用于有效且容易地制备由下式表示的化合物的新方法：其中环A是可以任选进一步被W代表的基团进一步取代的苯环或其盐; 其包括使下式表示的化合物：其中R 1和R 2彼此相同或不同，并且各自为氢原子，任选取代的烃基或任选地 取代的杂环基，Y是卤素原子，环A是可以任选地进一步被Y代表的基团进一步取代的苯环，并且环B是任选取代的苯环或其盐与由 式中W为W，其中环C为任选取代的苯环，环D为任选取代的5至7元含氮杂环，R 3为氢原子， 含有芳基或酰基的脂族烃基，R 4为氢原子，任选取代的烃基或酰基，或其盐，然后如果需要，将所得物 产品，适用于工业产品 说明。

公开(公告)号：US20050171184A1

公开(公告)日：2005-08-04

申请号：US11054371

申请日：2005-02-09

申请人： Isao Aoki ,  Mari Adachi ,  Hiroyuki Tawada ,  Makoto Yamashita ,  Misayo Sera

发明人： Isao Aoki ,  Mari Adachi ,  Hiroyuki Tawada ,  Makoto Yamashita ,  Misayo Sera

IPC分类号： C07D307/79 ,  C07D405/04 ,  C07F9/6574 ,  A61K31/4035 ,  C07D45/02

CPC分类号： C07D307/79 ,  C07B2200/07 ,  C07D405/04 ,  C07F9/65742

摘要： A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

摘要翻译： 一种制备光学活性2,3-二氢苯并呋喃化合物的方法，其包括用光学活性酸化合物对其进行光学拆分的2,3-二氢苯并呋喃化合物或其盐进行光学拆分：其中R 1， SUP>和R 2各自为氢或任选取代的烃基; R 3是任选取代的芳族基团; 并且C是除了氨基之外还可以具有取代基的苯环]。 该方法可以在工业上有利地生产用于合成可用作神经变性疾病等的预防和/或治疗药物的光学活性2,3-二氢苯并呋喃化合物的中间体。

公开(公告)号：US06414003B1

公开(公告)日：2002-07-02

申请号：US09708542

申请日：2000-11-09

申请人： Tsuneo Kanamaru ,  Masafumi Nakao ,  Hiroyuki Tawada ,  Keiji Kamiyama

发明人： Tsuneo Kanamaru ,  Masafumi Nakao ,  Hiroyuki Tawada ,  Keiji Kamiyama

IPC分类号： A61K31422

CPC分类号： C07D413/06 ,  C07D263/48 ,  C07D413/14 ,  C07D471/04 ,  C12P17/16

摘要： An anti-Helicobacter pylori agent comprising a compound represented by the formula: wherein A represents an aromatic ring group which may be substituted; R1 and R2, whether identical or not, each represent a hydrogen atom or a hydrocarbon group which may be substituted; R3 and R4, whether identical or not, each represent a hydrogen atom, a hydrocarbon group which may be substituted, an acyl group, a carbamoyl group which may be substituted, or a carboxyl group which may be esterified; or a salt thereof.

摘要翻译： 一种抗幽门螺杆菌药物，其包含由下式表示的化合物：其中A表示可被取代的芳族环基团; R1和R2各自表示氢原子或可被取代的烃基; R 3和R 4各自表示氢原子，可被取代的烃基，酰基，可被取代的氨基甲酰基或可被酯化的羧基; 或其盐。