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11. 发明授权

US5143919A Thienopyridine derivatives and their pharmaceutical use 失效
标题翻译：噻吩吡啶衍生物及其药物用途
公开(公告)号：US5143919A
公开(公告)日：1992-09-01
申请号：US744492
申请日：1991-08-13
申请人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
发明人： Kanji Meguro , Hiroyuki Tawada , Hitoshi Ikeda
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Thienopyridine derivatives of the formula (I): ##STR1## wherein the ring A is an optionally substituted benzene ring; the ring B is an optionally substituted thiophene ring: X is a group of the formula: ##STR2## (wherein R.sup.1 is hydrogen, alkyl or alkoxy; and n is 0 or 1) or a group of the formula: ##STR3## (wherein R.sup.2 is hydrogen or alkyl); Y is a single bond, --NH--, alkylene having 1 or 2 carbon atoms or --CH.dbd.CH--; and R.sup.3 is an optionally substituted hydrocarbon group, or their salts are disclosed. They show strong ACAT inhibitory activities.

12. 发明授权

US07541478B2 Coumarin derivative and use thereof 失效
标题翻译：香豆素衍生物及其用途
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。

13. 发明授权

US07034039B2 Fused heterocyclic compounds 失效
标题翻译：稠合杂环化合物
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。

14. 发明申请

US20050107606A1 Process for producing optically active sulfoxide derivative 审中-公开
标题翻译：光学活性亚砜衍生物的制备方法
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。

15. 发明授权

US4150139A Triazolobenzazepine derivatives 失效
标题翻译：三唑并苯并吖嗪衍生物
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。

16. 发明申请

US20060142598A1 Process for producing benzofuran derivative 失效
标题翻译：苯并呋喃衍生物的制备方法
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。

17. 发明申请

US20050171184A1 Process for preparing optically active 2,3-dihydrobenzofuran compounds 失效
标题翻译：光学活性2,3-二氢苯并呋喃化合物的制备方法
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。

18. 发明授权

US06414003B1 Oxazolone derivatives and their use as anti-helicobacter pylori agents 失效
标题翻译：恶唑酮衍生物及其作为幽门螺杆菌药物的用途
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。

19. 发明授权

US06403595B1 Sulfonamide derivatives, processes for producing the same and utilization thereof 失效
标题翻译：磺酰胺衍生物，其制备方法及其利用
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。

20. 发明授权

US4082764A Methods for the production of 4H-s-triazolo[4,3-a][1,4]benzodiazepine 5N-oxides 失效
标题翻译：生产4H-S-三唑（4,3-A）+8,1,4）苯并咪唑5N-氧化物的方法
公开(公告)号：US4082764A
公开(公告)日：1978-04-04
申请号：US612745
申请日：1975-09-12
申请人： Yutaka Kuwada , Kanji Meguro , Hiroyuki Tawada
发明人： Yutaka Kuwada , Kanji Meguro , Hiroyuki Tawada
IPC分类号： A61K20060101 , A61K31/55 , C07D20060101 , C07D239/92 , C07D243/00 , C07D249/00 , C07D249/08 , C07D487/04
CPC分类号： C07D239/92 , C07D249/08 , C07D487/04
摘要： The title compounds are prepared by reacting a 3-amino-3,4-dihydro-4-hydroxy-4-phenylquinazoline with a reactive derivative of a halogenoacetic acid, reacting the resultant halogenoacetyl derivative with a weak acid, reacting the resultant 2-(3-halomethyl-s-triazol-4-yl)benzophenone with hydroxylamine and subjecting the resultant 2-(3-hydroxyamino-methyl-s-triazol-4-yl)benzophenone to dehydration to effect ring closure.

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