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21. 发明授权

US06680312B2 Sulfonamide derivatives, their production and use 失效
标题翻译：磺酰胺衍生物，其生产和使用
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。

22. 发明授权

US4102881A Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US4102881A
公开(公告)日：1978-07-25
申请号：US478823
申请日：1974-06-12
申请人： Hiroyuki Tawada , Hideaki Natsugari , Kanji Meguro , Yutaka Kuwada
发明人： Hiroyuki Tawada , Hideaki Natsugari , Kanji Meguro , Yutaka Kuwada
IPC分类号： C07D243/20 , C07D243/28 , C07D487/04
CPC分类号： C07D487/04 , C07D243/20
摘要： Compounds of the formula ##STR1## wherein R.sub.2 is lower alkyl and each of rings A and B is unsubstituted or substituted by a member selected from the group consisting of nitro, trifluoromethyl, halogen, alkyl and alkoxy, and processes for their preparation.
摘要翻译：其中R 2为低级烷基且环A和B各自为未取代或被选自硝基，三氟甲基，卤素，烷基和烷氧基的成员取代的式IMA化合物及其制备方法。

23. 发明授权

US4044129A 4-Pyridine carbonyl phenyl 1,2,4 triazoles 失效
标题翻译： 4-吡啶羰基苯基1,2,4-三唑
公开(公告)号：US4044129A
公开(公告)日：1977-08-23
申请号：US592889
申请日：1975-07-03
申请人： Yutaka Kuwada , Kanji Meguro , Hideaki Natsugari , Yoshiaki Sato , Hiroyuki Tawada
发明人： Yutaka Kuwada , Kanji Meguro , Hideaki Natsugari , Yoshiaki Sato , Hiroyuki Tawada
IPC分类号： C07D401/04 , A61K31/44 , A61K31/4427 , A61K31/535 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/20 , C07D213/50 , C07D249/08 , C07D401/10 , C07D413/14
CPC分类号： C07D249/08 , C07D213/50
摘要： A novel triazole derivative of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, represent alkyl group or aralkyl group and one of R.sup.1 and R.sup.2 may be hydrogen atom, or R.sup.1 and R.sup.2 form a heterocyclic ring together with the nitrogen atom adjacent thereto; R.sup.3 represents hydrogen atom or a hydrocarbon residue; R.sup.4 represents hydrogen atom or a lower alkyl group; Py represents a pyridyl group; and the ring A is either unsubstituted or substituted by halogen atom, nitro, alkyl, alkoxy or trifluoromethyl group, and pharmaceutically acceptable acid addition salts thereof are found to be useful as medicine in human and animal therapy, as these compounds act on the central nervous as for example, muscle relaxants, anticonvulsants, sedatives, minor tranquilizers, etc.
摘要翻译：通式（I）的新的三唑衍生物：（I）其中R 1和R 2可以相同或不同，表示烷基或芳烷基，R 1和R 2之一可以是氢原子或R 1 R2与邻近的氮原子一起形成杂环; R3表示氢原子或烃残基; R4代表氢原子或低级烷基; Py代表吡啶基; 发现环A是未取代的或被卤素原子取代的硝基，烷基，烷氧基或三氟甲基，其药学上可接受的酸加成盐可用作人和动物治疗中的药物，因为这些化合物作用于中枢神经例如，肌肉松弛剂，抗惊厥药，镇静剂，小镇静剂等

24. 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。

25. 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。

26. 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。

27. 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。

28. 发明申请

US20080146602A1 Thienopyridine Derivatives, Production Method and Use Thereof 审中-公开
标题翻译：噻吩并吡啶衍生物，其生产方法和用途
公开(公告)号：US20080146602A1
公开(公告)日：2008-06-19
申请号：US11596634
申请日：2005-05-13
申请人： Atsuo Baba , Tsuneo Yasuma , Hiroyuki Tawada , Makoto Yamashita
发明人： Atsuo Baba , Tsuneo Yasuma , Hiroyuki Tawada , Makoto Yamashita
IPC分类号： A61K31/4365 , C07D471/04 , A61P19/02
CPC分类号： C07D495/04
摘要： A compound represented by the formula (I) wherein R is a hydrogen atom or a C1-4 alkyl group, and X is CH2, O or S, or a salt thereof. The present invention provides a novel thienopyridine derivative having an anti-inflammatory effect, a bone resorption suppressing effect, an immune cytokine production suppressing effect and the like, and useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of arthritis such as rheumatoid arthritis and the like, and the like, and the like.
摘要翻译：由式（I）表示的化合物，其中R是氢原子或C 1-4烷基，X是CH 2，O或S，或的盐。本发明提供具有抗炎作用，骨吸收抑制作用，免疫细胞因子产生抑制作用等的新颖的噻吩并吡啶衍生物，可用作预防或治疗关节炎的药剂如类风湿关节炎等，类似物等。

29. 发明授权

US07323577B2 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：US07323577B2
公开(公告)日：2008-01-29
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公式：<？in-line-formula description =“In-line Formulas”end =“lead”？> WH <？in-line-formula description =“In-line Formulas”end =“tail”？>其中W 其中环C是任选取代的苯环，环D是任选取代的5-至7-元含氮杂环，R 3是氢原子，含有芳族的脂族烃基基团或酰基，R 4是氢原子，任选取代的烃基或酰基，或其盐，此后，如果需要，将所得产物脱保护，其适用于工业生产。

30. 发明授权

US06359134B1 Sulfonamide derivatives, their production and use 失效
标题翻译：磺酰胺衍生物，其生产和使用
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。

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