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11. 发明授权

US5300646A Heterocyclic amine derivatives, their production and use 失效
标题翻译：杂环胺衍生物，其生产和使用
公开(公告)号：US5300646A
公开(公告)日：1994-04-05
申请号：US995016
申请日：1992-12-22
申请人： Hideaki Natsugari , Hiroyuki Tawada , Hitoshi Ikeda
发明人： Hideaki Natsugari , Hiroyuki Tawada , Hitoshi Ikeda
IPC分类号： C07D217/24 , C07D311/76 , C07D335/06 , C07D217/22 , C07D311/04 , C07D311/78
CPC分类号： C07D335/06 , C07D217/24 , C07D311/76
摘要： A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.sup.o stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.
摘要翻译：一种新颖的通式如下的杂环胺衍生物：其中环A和环B独立地代表任选取代的苯环，Z代表O或S，或者表示-CH 2 - ，X 代表O，S或NR1，其中R1表示氢原子或烷基，Y表示NH，O或（CH2）n，其中n表示0至2，R2表示任选取代的烃基或其盐。

12. 发明授权

US5198462A Heterocyclic amine, derivatives, their production and use 失效
标题翻译：杂环胺，衍生物，生产和使用
公开(公告)号：US5198462A
公开(公告)日：1993-03-30
申请号：US777169
申请日：1991-10-16
申请人： Hideaki Natsugari , Hiroyuki Tawada , Hitoshi Ikeda
发明人： Hideaki Natsugari , Hiroyuki Tawada , Hitoshi Ikeda
IPC分类号： C07D217/24 , C07D311/76 , C07D335/06
CPC分类号： C07D335/06 , C07D217/24 , C07D311/76
摘要： A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.degree. stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.

13. 发明授权

US4046772A Benzodiazepine derivative and process for producing the same 失效
标题翻译：苯并二氮杂衍生物及其制备方法
公开(公告)号：US4046772A
公开(公告)日：1977-09-06
申请号：US566434
申请日：1975-04-09
申请人： Yutaka Kuwada , Hiroyuki Tawada , Kanji Meguro
发明人： Yutaka Kuwada , Hiroyuki Tawada , Kanji Meguro
IPC分类号： A61K31/55 , A61P21/02 , A61P25/08 , A61P25/20 , B23B33/00 , C07D487/04 , C07D487/14
CPC分类号： C07D487/04 , B23B33/005 , Y10S514/906 , Y10S514/96
摘要： A benzodiazepine derivative of the general formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group or a carboxyl group which may be esterified or amidated; R represents a hydrogen atom, an acyl group or a lower alkyl group, and each of the rings A and B is unsubstituted or substituted by halogen atom, nitro, lower alkyl, trifluoromethyl or lower alkoxy group, or its pharmaceutically acceptable acid addition salt is found to be useful as medicine in human and animal therapy, which acts on the central nervous system, e.g. muscle relaxants, anticonvulsants, sedatives, tranquilizers etc.
摘要翻译：一种通式如下的苯并二氮杂衍生物：其中R 1表示氢原子，烷基或可被酯化或酰胺化的羧基; R表示氢原子，酰基或低级烷基，环A和B各自未被取代或被卤素原子，硝基，低级烷基，三氟甲基或低级烷氧基取代，或其药学上可接受的酸加成盐是被发现在人和动物治疗中用作中枢神经系统的药物，例如肌肉松弛剂，抗惊厥药，镇静剂，止痛药等。

14. 发明授权

US4017620A Thienodiazepine derivatives 失效
标题翻译：噻吩并二氮杂衍生物
公开(公告)号：US4017620A
公开(公告)日：1977-04-12
申请号：US575727
申请日：1975-05-08
申请人： Yutaka Kuwada , Kanji Meguro , Hiroyuki Tawada , Takashi Sohda , Hideaki Natsugari , Yoshiaki Sato
发明人： Yutaka Kuwada , Kanji Meguro , Hiroyuki Tawada , Takashi Sohda , Hideaki Natsugari , Yoshiaki Sato
IPC分类号： A61K31/55 , A61P25/00 , A61P25/20 , C07D495/14
CPC分类号： C07D495/14
摘要： There is disclosed new thienodiazepine derivatives of the general formula: ##STR1## wherein R.sup.1 represents a carboxyl group which may be esterified or amidated; each of R.sup.2 and R.sup.3 represents hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 may bond to each other to form an alkylene group; R.sup.4 represents a phenyl group which may have substituent; and R represents hydrogen atom, an acyl group or an alkyl group, or its pharmaceutically acceptable acid addition salts. The above compounds are useful as medicine in human and animal therapy, which act on the central nervous system, for example, as muscle relaxants, anticonvulsants, sedatives, minor tranquilizers, etc.
摘要翻译：公开了以下通式的新的噻吩并二氮杂衍生物：其中R 1表示可被酯化或酰胺化的羧基; R 2和R 3各自表示氢原子或低级烷基，或者R 2和R 3可以彼此键合形成亚烷基; R4表示可以具有取代基的苯基; R表示氢原子，酰基或烷基，或其药学上可接受的酸加成盐。上述化合物可用作人和动物治疗中的药物，其作用于中枢神经系统，例如肌肉松弛剂，抗惊厥药，镇静剂，微量镇静剂等。

15. 发明授权

US4013763A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US4013763A
公开(公告)日：1977-03-22
申请号：US592814
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： C07D213/50 , C07D249/08 , C07D487/14 , C07D498/14 , C07D491/22
CPC分类号： C07D249/08 , C07D213/50 , C07D487/14
摘要： A novel heterocyclic compound of the general formula: ##STR1## wherein R.sup.1 represents hydrogen atom or a hydrocarbon residue; R.sup.2 represents hydrogen atom or a lower alkyl group; Py represents a pyridyl group; Y represents an ethylene or a trimethylene group which may have lower alkyl group as substituent; Z represents oxygen atom, sulfur atom or --NH-- groups; and the ring A is either unsubstituted or substituted by a halogen atom, nitro, alkyl, alkoxy or trifluoromethyl group, is found to be useful as medicine in human and animal therapy, as these compounds act on the central nervous system, as, for example, muscle relaxants, anticonvulsants, sedatives, minor tranquilizers, etc.

16. 发明授权

US3947417A Triazolobenzodiazepine derivatives 失效
标题翻译：三唑并苯并二氮杂衍生物
公开(公告)号：US3947417A
公开(公告)日：1976-03-30
申请号：US443528
申请日：1974-02-19
申请人： Yutaka Kuwada , Hiroyuki Tawada , Kanji Meguro
发明人： Yutaka Kuwada , Hiroyuki Tawada , Kanji Meguro
IPC分类号： A61K31/55 , A61P21/02 , A61P25/08 , A61P25/20 , C07D249/08 , C07D249/10 , C07D487/14 , C07D498/14 , C07D513/14
CPC分类号： C07D487/14 , C07C251/72 , C07D249/10 , C07D513/14
摘要： Compounds of the formula: ##SPC1##Wherein R.sup.1 and R.sup.2 are the same or different and each stands for hydrogen atom or alkyl group which may be substituted by hydroxy or/and alkoxy group; R.sup.1 and R.sup.2 may, taken together with the adjacent nitrogen atom, form a heterocyclic ring; R.sup.3 stands for hydrogen atom or lower alkyl group; Q stands for ethylene or trimethylene group which may be substituted by lower alkyl group; Y stands for --O--, --S-- or --NH--; and rings A and B are unsubstituted or substituted by halogen atom, nitro, alkyl, trifluoromethyl or/and alkoxy group, and pharmaceutically acceptable salts thereof, are useful as tranquilizers, muscle relaxants, sedatives, anticonvulsants, sleep inducers, etc.
摘要翻译：下式的化合物：

17. 发明授权

US07420070B2 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：US07420070B2
公开(公告)日：2008-09-02
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： C07D405/00 , C07D307/00
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

US07034166B2 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：US07034166B2
公开(公告)日：2006-04-25
申请号：US10483089
申请日：2002-07-11
申请人： Hiroyuki Tawada , Makoto Yamashita , Yujiro Ono
发明人： Hiroyuki Tawada , Makoto Yamashita , Yujiro Ono
IPC分类号： C07D307/79 , C07C49/76 , C07C43/23
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。

19. 发明授权

US06878831B2 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：US06878831B2
公开(公告)日：2005-04-12
申请号：US10451723
申请日：2001-12-27
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 , C07D307/78
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使其由通式或其盐表示的2,3-二氢苯并呋喃化合物进行光学拆分：[其中R 1和R 2' 2>各自为氢或任选取代的烃基; R 3是任选取代的芳基; 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。

20. 发明申请

US20050014813A1 Process for production of pyrazole compounds 审中-公开
标题翻译：吡唑化合物的制备方法
公开(公告)号：US20050014813A1
公开(公告)日：2005-01-20
申请号：US10495173
申请日：2002-11-12
申请人： Hiroyuki Tawada , Makoto Yamashita , Tomomi Ikemoto , Atsuko Nishiguchi
发明人： Hiroyuki Tawada , Makoto Yamashita , Tomomi Ikemoto , Atsuko Nishiguchi
IPC分类号： C07D231/20 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D231/04 , A61K31/4152
CPC分类号： C07D401/12 , C07D231/20 , C07D413/12 , C07D413/14 , C07D417/12
摘要： As a method capable of conveniently producing a pyrazole compound in a high yield, which is useful as a synthetic intermediate for a pharmaceutical agent such as a therapeutic agent for diabetes and the like, a production method of a compound represented by the formula (I) wherein n is an integer of 1 to 4 and R1 is a. hydrocarbon group optionally having substituents, or a salt thereof, is provided, which includes reacting a compound represented by the formula, (II) wherein Q is a hydroxy group optionally having substituents or an amino group optionally having substituents, R is a hydrocarbon group optionally having substituents and other symbols are as defined above, or a salt thereof, with hydrazine or a salt thereof.
摘要翻译：作为能够以高收率制备吡唑化合物的方法，作为糖尿病治疗剂等药剂的合成中间体是有用的，由式（I）表示的化合物的制造方法，其中n为1〜4的整数，R 1为a。提供任选具有取代基的烃基或其盐，其包括使式（II）表示的化合物，其中Q是任选具有取代基的羟基或任选具有取代基的氨基，R是任选的烃基具有取代基和其它符号如上所定义，或其盐与肼或其盐反应。

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