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1. 发明授权

US5670498A 8-substituted styryl xanthine derivatives 失效
标题翻译： 8-取代的苯乙烯基黄嘌呤衍生物
公开(公告)号：US5670498A
公开(公告)日：1997-09-23
申请号：US527497
申请日：1995-09-13
申请人： Fumio Suzuki , Junichi Shimada , Nobuaki Koike , Hiroshi Kase , Joji Nakamura , Shizuo Shiozaki , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Nobuaki Koike , Hiroshi Kase , Joji Nakamura , Shizuo Shiozaki , Hiromi Nonaka
IPC分类号： C07D473/06 , C07D473/12 , A61K31/52 , C07D473/10
CPC分类号： C07D473/06
摘要： Disclosed are xanthine derivatives represented by the following Formula (I): ##STR1## in which R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen or lower alkyl; Q.sup.1, Q.sup.2, and Q.sup.3 independently represent hydrogen, lower alkyl, lower alkoxy, or halogen; and X represents --COR.sup.4 (in which R.sup.4 represents hydrogen, hydroxy, lower alkyl, or lower alkoxy) or --SO.sub.2 R.sub.5 {in which R.sup.5 represents hydroxy, lower alkoxy, trifluoromethyl, ##STR2## in which R.sup.6 and R.sup.7 independently represent hydrogen, hydroxy-substituted or unsubstituted lower alkyl, aryl, or ##STR3## (in which m represents an integer of 1 to 3; and R.sup.8 and R.sup.9 independently represent hydrogen or lower alkyl), or ##STR4## (in which Y represents a single bond, oxygen, or N--R.sup.10 in which R.sup.10 represents hydrogen or lower alkyl; and n1 and n2 independently represent an integer of 1 to 3)}, and pharmaceutically acceptable salts thereof.
摘要翻译：公开了由下式（I）表示的黄嘌呤衍生物：其中R 1，R 2和R 3独立地表示氢或低级烷基; Q1，Q2和Q3独立地表示氢，低级烷基，低级烷氧基或卤素; 或其中R 4表示氢，羟基，低级烷基或低级烷氧基）或-SO 2 R 5（其中R 5表示羟基，低级烷氧基，三氟甲基，取代或未取代的低级烷基，芳基或者（其中m表示1〜3的整数; R 8和R 9分别表示氢或低级烷基），或者（其中Y表示单键，氧，或其中R 10表示氢或低级烷基的N-R 10，n1和n2独立地表示1〜3的整数）}及其药学上可接受的盐。

2. 发明授权

US5703085A Xanthine derivatives 失效
标题翻译：黄嘌呤衍生物
公开(公告)号：US5703085A
公开(公告)日：1997-12-30
申请号：US537770
申请日：1995-10-20
申请人： Fumio Suzuki , Nobuaki Koike , Junichi Shimada , Joji Nakamura , Shizuo Shiozaki , Shigeto Kitamura , Shunji Ichikawa , Hiroshi Kase , Hiromi Nonaka
发明人： Fumio Suzuki , Nobuaki Koike , Junichi Shimada , Joji Nakamura , Shizuo Shiozaki , Shigeto Kitamura , Shunji Ichikawa , Hiroshi Kase , Hiromi Nonaka
IPC分类号： C07D473/06 , A61K31/52 , C07D473/10 , C07D473/12
CPC分类号： C07D473/06
摘要： The present invention relates to novel xanthine derivatives and pharmaceutically acceptable salts thereof, represented by Formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, R.sup.4 represents lower alkyl, or substituted or unsubstituted aryl, R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, and lower alkoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--(CH.sub.2)p--O-- (p is an integer of 1 to 3), n represents 0, 1, or 2, and m represents 1 or 2. The compounds of the present invention have an adenosine A.sub.2 receptor antagonistic activity, and are useful for the treatment or prevention of various kinds of diseases caused by hyperergasia of adenosine A.sub.2 receptors (for example, Parkinson's disease, senile dementia, depression, asthma, and osteoporosis).
摘要翻译： PCT No.PCT / JP95 / 00267 Sec。 371 1995年10月20日第 102（e）1995年10月20日日期PCT提交1995年2月23日PCT公布。公开号WO95 / 23148 日期：1995年8月31日本发明涉及由式（I）表示的新颖的黄嘌呤衍生物及其药学上可接受的盐：其中R1，R2和R3独立地表示氢，低级烷基，低级链烯基或低级炔基，R 4表示低级烷基或取代或未取代的芳基，R 5和R 6独立地表示氢，低级烷基和低级烷氧基，或者R 5和R 6结合在一起代表-O-（CH 2）p O-（p是整数 1〜3），n表示0,1或2，m表示1或2.本发明化合物具有腺苷A2受体拮抗活性，可用于治疗或预防各种疾病腺苷A2受体（例如帕金森病，老年性痴呆，抑郁症，哮喘和骨质疏松症）的过度高血症。

3. 发明授权

US5587378A Therapeutic agent for Parkinson's disease 失效
标题翻译：帕金森病治疗剂
公开(公告)号：US5587378A
公开(公告)日：1996-12-24
申请号：US447885
申请日：1995-05-23
申请人： Fumio Suzuki , Junichi Shimada , Nobuaki Koike , Joji Nakamura , Shizuo Shiozaki , Shunji Ichikawa , Akio Ishii , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Nobuaki Koike , Joji Nakamura , Shizuo Shiozaki , Shunji Ichikawa , Akio Ishii , Hiromi Nonaka
IPC分类号： C07D473/06 , C07D473/08 , C07D473/12 , A61K31/52
CPC分类号： C07D473/08 , C07D473/06 , C07D473/12
摘要： Methods for the treatment of Parkinson's disease comprising administering to a patient an agent which contains, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 is cycloalkyl, --(CH.sub.2).sub.n --R.sup.5, wherein R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4, or ##STR2## wherein Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z is substituted or unsubstituted aryl, ##STR3## wherein R.sup.6 is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m is an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 are independently O or S.
摘要翻译：用于治疗帕金森病的方法包括向患者施用含有作为活性成分的黄嘌呤衍生物或其药学上可接受的盐的试剂。黄嘌呤衍生物由下式表示：其中R 1，R 2和R 3独立地是氢，低级烷基，低级链烯基或低级炔基; 并且R 4是环烷基， - （CH 2）n -R 5，其中R 5表示取代或未取代的芳基或取代或未取代的杂环基; n为0〜4的整数，或者，其中Y1和Y2独立地表示氢，卤素或低级烷基; Z是取代或未取代的芳基，其中R6是氢，羟基，低级烷基，低级烷氧基，卤素，硝基或氨基; m为1〜4的整数，或取代或未取代的杂环基; X1和X2独立地为O或S.

4. 发明授权

US5484920A Therapeutic agent for Parkinson's disease 失效
标题翻译：帕金森病治疗剂
公开(公告)号：US5484920A
公开(公告)日：1996-01-16
申请号：US133510
申请日：1993-10-07
申请人： Fumio Suzuki , Junichi Shimada , Nobuaki Koike , Joji Nakamura , Shizuo Shioazaki , Shunji Ichikawa , Akio Ishii , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Nobuaki Koike , Joji Nakamura , Shizuo Shioazaki , Shunji Ichikawa , Akio Ishii , Hiromi Nonaka
IPC分类号： C07D473/06 , C07D473/08 , C07D473/12 , A61K31/52
CPC分类号： C07D473/08 , C07D473/06 , C07D473/12
摘要： Agents for the treatment of Parkinson's disease contain, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## in which R.sup.1, R.sup.2 are R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 represents cycloalkyl, --(CH.sub.2).sub.n --R.sup.5 (in which R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4), or ##STR2## in which Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z represents substituted or unsubstituted aryl, ##STR3## in which R.sup.6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m represents an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 represent independently O or S.
摘要翻译：用于治疗帕金森病的药物含有作为活性成分的黄嘌呤衍生物或其药学上可接受的盐。黄嘌呤衍生物由下式表示：其中R 1，R 2为R 3独立地为氢，低级烷基，低级烯基或低级炔基; 并且R 4表示环烷基， - （CH 2）n -R 5（其中R 5表示取代或未取代的芳基或取代或未取代的杂环基; n为0至4的整数）或其中Y 1和Y 2表示独立地是氢，卤素或低级烷基; Z表示取代或未取代的芳基，其中R 6表示氢，羟基，低级烷基，低级烷氧基，卤素，硝基或氨基; m表示1〜4的整数，或取代或未取代的杂环基; X1和X2独立地表示O或S.

5. 发明授权

US06222035B1 [1,2,4] triazolo [1,5-C] pyrimidine derivatives 失效
标题翻译： [1,2,4]三唑并[1,5-C]嘧啶衍生物
公开(公告)号：US06222035B1
公开(公告)日：2001-04-24
申请号：US09401984
申请日：1999-09-23
申请人： Hiroshi Tsumuki , Junichi Shimada , Hironori Imma , Akiko Nakamura , Hiromi Nonaka , Shizuo Shiozaki , Shunji Ichikawa , Tomoyuki Kanda , Yoshihisa Kuwana , Michio Ichimura , Fumio Suzuki
发明人： Hiroshi Tsumuki , Junichi Shimada , Hironori Imma , Akiko Nakamura , Hiromi Nonaka , Shizuo Shiozaki , Shunji Ichikawa , Tomoyuki Kanda , Yoshihisa Kuwana , Michio Ichimura , Fumio Suzuki
IPC分类号： C07D48700
CPC分类号： C07D487/04
摘要： [1,2,4]Triazolo[1,5-c]pyrimidine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof are provided, which have adenosine A2A receptor antagonism and are useful for the treatment or prevention of various diseases induced by hyperactivity of adenosine A2A receptors (for example, Parkinson's disease or senile dementia): wherein R1 represents substituted or unsubstituted aryl, or the like; R2 represents hydrogen, halogen, lower alkyl, substituted or unsubstituted aryl, or the like; R3 represents hydrogen, halogen, XR10 (wherein X represents O or S; and R10 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic ring, substituted or unsubstituted aralkyl, lower alkyl, or hydroxy lower alkyl), or the like; and Q represents hydrogen or 3,4-dimethoxybenzyl.
摘要翻译： [1,2,4]具有式（I）表示的三唑并[1,5-c]嘧啶衍生物或其药学上可接受的盐，其具有腺苷A2A受体拮抗作用，可用于治疗或预防由腺苷A2A受体（例如帕金森病或老年性痴呆）的多动症：其中R1表示取代或未取代的芳基等; R 2表示氢，卤素，低级烷基，取代或未取代的芳基等; R3表示氢，卤素，XR10（其中X表示O或S; R10表示取代或未取代的芳基，取代或未取代的芳族杂环，取代或未取代的芳烷基，低级烷基或羟基低级烷基）等; Q表示氢或3,4-二甲氧基苄基。

6. 发明授权

US5342841A Xanthine derivatives 失效
标题翻译：黄嘌呤衍生物
公开(公告)号：US5342841A
公开(公告)日：1994-08-30
申请号：US29069
申请日：1993-03-10
申请人： Fumio Suzuki , Junichi Shimada , Akira Karasawa , Hideaki Mizumoto , Hiroshi Kase , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Akira Karasawa , Hideaki Mizumoto , Hiroshi Kase , Hiromi Nonaka
IPC分类号： C07D473/06 , A61K31/52 , C07D473/02
CPC分类号： C07D473/06
摘要： A xanthine derivative of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are substituted or unsubstituted alicyclic alkyl; m1 and m2 are the same or different and represent an integer of 0 to 2; and Q represents ##STR2## (in which R.sup.3 and R.sup.4 are the same or different and are substituted or unsubstituted alicyclic alkyl) or ##STR3## (in which n is 0 or 1, and Y is a single bond or alkylene); or a pharmaceutically acceptable salt thereof is disclosed.This derivative has diuretic activity and renal protecting activity.
摘要翻译：式（I）的黄嘌呤衍生物：其中R1和R2相同或不同，为取代或未取代的脂环族烷基; m1和m2相同或不同，表示0〜2的整数。和Q表示（其中R 3和R 4相同或不同，是取代或未取代的脂环族烷基）或（其中n为0或1，Y为单键或亚烷基）。或其药学上可接受的盐。该衍生物具有利尿活性和肾脏保护活性。

7. 发明授权

US5525607A Xanthine compounds 失效
标题翻译：黄嘌呤化合物
公开(公告)号：US5525607A
公开(公告)日：1996-06-11
申请号：US63684
申请日：1993-05-20
申请人： Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka , Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka , Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka
IPC分类号： C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22 , A61K31/52 , C07D473/00
CPC分类号： C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22
摘要： Novel xanthine compounds represented by the following formula: ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen or lower alkyl;each of X.sup.1 and X.sup.2 independently represents oxygen or sulfur; and Q represents: ##STR2## The compounds are useful as a diuretic, a renal-protecting agent and bronchodilator.
摘要翻译：由下式表示的新型黄嘌呤化合物：其中R 1，R 2和R 3各自独立地表示氢或低级烷基; X1和X2各自独立地表示氧或硫; Q表示：该化合物可用作利尿剂，肾保护剂和支气管扩张剂。

8. 发明授权

US6107064A Process for producing xanthine derivatives with bacteria and fungi 失效
标题翻译：用细菌和真菌生产黄嘌呤衍生物的方法
公开(公告)号：US6107064A
公开(公告)日：2000-08-22
申请号：US581533
申请日：1996-01-17
申请人： Junichi Shimada , Tamotsu Eguchi , Kenichi Mochida , Akira Horiguchi , Tohru Yasuzawa , Hideaki Kusaka , Hiromi Nonaka , Fumio Suzuki
发明人： Junichi Shimada , Tamotsu Eguchi , Kenichi Mochida , Akira Horiguchi , Tohru Yasuzawa , Hideaki Kusaka , Hiromi Nonaka , Fumio Suzuki
IPC分类号： C07D473/04 , C07D473/06 , C12P17/18 , C12P17/16
CPC分类号： C07D473/04 , C07D473/06 , C12P17/18
摘要： The present invention relates to a process for producing a xanthine derivative represented by formula (II), comprising converting a xanthine derivative represented by formula (I) {hereinafter, referred to as Compound (I)}: ##STR1## (wherein R.sup.1 and R.sup.2 independently represent hydrogen, or hydroxy-substituted, oxo-substituted, or unsubstituted lower alkyl) into a xanthine derivative represented by formula (II) {hereinafter, referred to as Compound (II)}: ##STR2## (wherein R.sup.3 and R.sup.4 independently represent hydrogen, or hydroxy-substituted, oxo-substituted, or unsubstituted lower alkyl; R.sup.5 and R.sup.6 independently represent hydrogen, hydroxy, or oxo; with the proviso that R.sup.5 and R.sup.6 are both hydrogen, at least one of R.sup.3 and R.sup.4 is hydroxy-substituted or oxo-substituted lower alkyl; and X and Y both represent hydrogen or are combined with each other to form a single bond) in the presence of an enzyme source for catalyzing hydroxylation or carbonylation of Compound (I) into Compound (II), and collecting the produced Compound (II).
摘要翻译： PCT No.PCT / JP95 / 00929 Sec。 371日期1996年1月17日 102（e）日期1996年1月17日PCT提交1995年5月16日PCT公布。公开号WO95 / 31460 日本特开平9-1252号公报发明内容本发明涉及由式（II）表示的黄嘌呤衍生物的制造方法，其特征在于，将由式（I）表示的黄嘌呤衍生物{以下称为化合物（I）} 和R2独立地表示氢或羟基取代的，取代或未取代的低级烷基）转化为由式（II）表示的黄嘌呤衍生物（以下称为化合物（II）}：（其中R 3和R 4独立地表示氢或羟基取代的，取代或未取代的低级烷基; R 5和R 6独立地表示氢，羟基或氧代;条件是R 5和R 6都是氢，R 3和R 4中的至少一个是羟基取代的或氧代取代的低级烷基; X和Y均表示氢或彼此结合形成单键）在用于催化化合物（I）羟化或羰基化成化合物（II）的酶源的存在下，以及大学将所制备的化合物（II）。

9. 发明授权

US5068236A Xanthine derivatives 失效
标题翻译： XANTHINE DERIVATIVES
公开(公告)号：US5068236A
公开(公告)日：1991-11-26
申请号：US486831
申请日：1990-03-01
申请人： Fumio Suzuki , Junichi Shimada , Kazuhiro Kubo , Tetsuji Ohno , Akira Karasawa , Akio Ishii , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Kazuhiro Kubo , Tetsuji Ohno , Akira Karasawa , Akio Ishii , Hiromi Nonaka
IPC分类号： A61K31/52 , A61K31/522 , A61P7/10 , A61P9/08 , A61P9/12 , A61P13/02 , A61P15/00 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/10 , C07D473/12 , C07D473/20 , C07D473/22
CPC分类号： C07D473/04 , C07D473/06 , C07D473/22
摘要： Novel xanthine compounds represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof have a diuretic action, a renal-protecting action and a vasodilative action.The compounds are useful as a diuretic, a renal-protecting agent and an antihypertensive agent.

10. 发明授权

US06306847B1 Condensed purine derivatives 失效
标题翻译：凝血嘌呤衍生物
公开(公告)号：US06306847B1
公开(公告)日：2001-10-23
申请号：US09090936
申请日：1998-06-05
申请人： Hiroshi Tsumuki , Mayumi Saki , Hiromi Nonaka , Michio Ichimura , Junichi Shimada , Fumio Suzuki , Shunji Ichikawa , Nobuo Kosaka
发明人： Hiroshi Tsumuki , Mayumi Saki , Hiromi Nonaka , Michio Ichimura , Junichi Shimada , Fumio Suzuki , Shunji Ichikawa , Nobuo Kosaka
IPC分类号： C07D48714
CPC分类号： C07D487/14
摘要： The present invention provides condensed purine derivatives or pharmacologically acceptable salts thereof exhibiting adenosine A3 acceptor antagonising activity, and having an antiasthmatic action, a bronchodilator action, an antiantiitching action, etc., and represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; R3 represents hydrogen, lower alkyl, or substituted or unsubstituted aralkyl; X1 and X2 are the same or different and each represents hydrogen, lower alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted aryl; and n represents an integer of 0 to 3).
摘要翻译：本发明提供具有腺苷A3受体拮抗活性的缩合嘌呤衍生物或其药理学上可接受的盐，并具有抗哮喘作用，支气管扩张剂作用，抗脱除作用等，并由下式（I）表示:(其中R1表示取代或未取代的芳基或取代或未取代的芳族杂环基; R 2表示氢，低级烷基，脂环族烷基，取代或未取代的芳烷基，取代或未取代的芳基或取代或未取代的芳族杂环基; R 3表示氢，低级烷基或取代或未取代的芳烷基; X 1和X 2相同或不同，各自表示氢，低级烷基，取代或未取代的芳烷基或取代或未取代的芳基; n表示0〜3的整数。

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