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41. 发明授权

EP1757610B1 CONDENSED PYRIMIDINE DERIVATIVE AND XANTHINE OXIDASE INHIBITOR 有权
标题翻译：稠合嘧啶衍生物和黄嘌呤氧化酶抑制剂
公开(公告)号：EP1757610B1
公开(公告)日：2011-06-08
申请号：EP05751417.6
申请日：2005-06-13
申请人： Nippon Chemiphar Co., Ltd.
发明人： YOSHIDA, Shinichi , KOBAYASHI, Kunio , MOCHIDUKI, Nobutaka , YAMAKAWA, Tomio , KOBAYASHI, Tadashi , SHINOHARA, Yoriko
IPC分类号： C07D498/04 , A61K31/519 , A61P19/06 , A61P43/00 , C07D513/04
CPC分类号： C07D513/04 , C07D498/04
摘要： Disclosed is a compound represented by the following general formula (I) (wherein R1 represents an aryl group having 6-10 carbon atoms or a heteroaryl group which may have, as a substituent, a group selected from an alkyl group having 1-8 carbon atoms, an alkyl group having 1-8 carbon atoms which is substituted with a halogen atom, an alkoxy group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms which is substituted with an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, a formyl group, a carboxyl group, a halogen atom, a hydroxyl group, a nitro group, a cyano group, an amino group, an aryl group having 6-10 carbon atoms and an aryloxy group having 6-10 carbon atoms; R2 represents a cyano group, a nitro group or the like; R3 represents an hydroxyl group or the like; X represents an oxygen atom, a sulfur atom or the like; and Y represents an oxygen atom or a sulfur atom). Also disclosed is a xanthine oxidase inhibitor containing such a compound.

42. 发明公开

EP1911760A1 XANTHINE OXIDASE INHIBITOR 审中-公开
标题翻译： XANTHINOXIDASEINHIBITOR
公开(公告)号：EP1911760A1
公开(公告)日：2008-04-16
申请号：EP06780819.6
申请日：2006-06-29
申请人： Nippon Chemiphar Co., Ltd.
发明人： NISHINO, Takeshi , YOSHIDA, Shinichi , TENDO, Atsushi , YAMAKAWA, Tomio , KOBAYASHI, Tadashi , SHINOHARA, Yoriko
IPC分类号： C07D473/00 , A61K31/519 , A61K31/52 , A61K31/5377 , A61K31/541 , A61P19/06 , A61P43/00 , C07D498/04 , C07D513/04
CPC分类号： C07D473/00 , C07D498/04 , C07D513/04
摘要： A compound represented by the following formula (I) is used as a xanthine oxidase inhibitor:

in which R 1 is phenyl or pyridyl each optionally having, as a substituent, C 1-8 alkyl, C 1-8 haloalkyl, C 1-8 alkoxy, carboxyl, halogeno, hydroxyl, nitro, cyano, amino, etc.; R 2 is cyano, nitro, etc.; X is oxygen, sulfur, etc.; and Y is sulfur, NH, etc.
摘要翻译：将下式（I）表示的化合物用作黄嘌呤氧化酶抑制剂：其中R 1为苯基或吡啶基，每个任选具有C 1-8烷基，C 1-8卤代烷基，C 1-8烷基烷氧基，羧基，卤代，羟基，硝基，氰基，氨基等; R 2是氰基，硝基等; X是氧，硫等; Y为硫，NH等

43. 发明公开

EP1795526A1 N-SUBSTITUTED N-(4-PIPERIDINYL)AMIDE DERIVATIVE 审中-公开
标题翻译： N-取代的N-（4-哌啶子基）氨基甲酸酯
公开(公告)号：EP1795526A1
公开(公告)日：2007-06-13
申请号：EP05785892.0
申请日：2005-09-13
申请人： Nippon Chemiphar Co., Ltd.
发明人： TAKAHASHI, Toshihiro , ENDO, Tsuyoshi , USHIODA, Masatoshi , KOBAYASHI, Kunio , YAMAKAWA, Tomio , SHIKA, Kiichi , KAWASAKI, Toru , IMAI, Toshiyasu ,
IPC分类号： C07D211/58 , A61K31/4468 , A61K31/4525 , A61K31/4535 , A61P25/02 , A61P25/04 , C07D405/12 , C07D409/12
CPC分类号： C07D211/58 , C07D405/12 , C07D409/12
摘要： An N-substituted N-(4-piperininyl)amide derivative represented by the following formula (I): (wherein R 1 represents C 1-6 alkyl, furyl, etc.; R 2 represents amino, acetylamino, ureido, etc.; R 3 represents hydrogen, C 2-8 alkoxycarbonyl, etc.; R 4 represents optionally substituted phenyl, etc.; R 5 represents hydroxyl, benzyloxy, etc.; R 6 represents hydrogen or methyl; and m is 1 or 2) or a salt of the derivative, and an analgesic containing the derivative or salt.
摘要翻译：由下式（I）表示的N-取代的N-（4-哌啶基）酰胺衍生物：其中R 1表示C 1-6烷基，呋喃基等; R 2表示氨基，乙酰氨基，脲基等; R 3表示氢，C 2-8烷氧基羰基等; R 4表示任意取代的苯基等; R 5表示羟基，苄氧基等; R 6表示氢或甲基; m表示1或2）或衍生物的盐和含有衍生物或盐的止痛剂。

44. 发明公开

EP1757610A1 CONDENSED PYRIMIDINE DERIVATIVE AND XANTHINE OXIDASE INHIBITOR 有权
标题翻译：新戊酰氧化酶抑制剂的邻苯二酚
公开(公告)号：EP1757610A1
公开(公告)日：2007-02-28
申请号：EP05751417.6
申请日：2005-06-13
申请人： Nippon Chemiphar Co., Ltd.
发明人： YOSHIDA, Shinichi , KOBAYASHI, Kunio , MOCHIDUKI, Nobutaka , YAMAKAWA, Tomio , KOBAYASHI, Tadashi , SHINOHARA, Yoriko
IPC分类号： C07D498/04 , A61K31/519 , A61P19/06 , A61P43/00 , C07D513/04
CPC分类号： C07D513/04 , C07D498/04
摘要： The invention relates to compounds of the following formula (I) or their salts:

in which R 1 is a group of phenyl, naphthyl, pyridyl or the like which may have a substituent such as an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, carboxyl, halogen, hydroxyl, nitro, or cyano; R 2 is cyano, nitro, or the like; R 3 is hydroxyl or the like; X is oxygen, sulfur, or the like; and Y is oxygen or sulfur, and a xanthine oxidase inhibitor containing the compound.
摘要翻译：本发明涉及下式（I）的化合物或其盐：其中R 1是可具有取代基的苯基，萘基，吡啶基等基团，例如具有1-8个碳原子的烷基，具有1-8个碳原子的烷氧基，具有2-8个碳原子的烷氧基羰基，羧基，卤素，羟基，硝基或氰基; R 2是氰基，硝基等; R 3是羟基等; X是氧，硫等; Y为氧或硫，含有该化合物的黄嘌呤氧化酶抑制剂。

45. 发明公开

EP1717314A1 Receptor for modified low-density lipoprotein 失效
标题翻译： Rezeptorfürmodifizierte Lipoprotein niedriges Molekulargewichtes
公开(公告)号：EP1717314A1
公开(公告)日：2006-11-02
申请号：EP06012158.9
申请日：1995-11-30
申请人： NIPPON CHEMIPHAR CO., LTD.
发明人： Sawamura, Tatsuya, Rose Vira Kitashirakawa 208 , Masaki, Tomoo
IPC分类号： C12N15/12 , C12P21/02 , C07K14/705
CPC分类号： C07K14/705 , A61K38/00
摘要： The present invention provides a DNA sequence essentially encoding a mammalian vascular endothelial receptor for modified low-density lipoprotein. The sequence is set forth in the Sequence No. 1, 2 or 3.
摘要翻译：本发明提供了基本上编码修饰的低密度脂蛋白的哺乳动物血管内皮受体的DNA序列。该顺序列于序列号1,2或3中。

46. 发明公开

EP1538142A1 AMINE DERIVATIVE 审中-公开
标题翻译：胺衍生物
公开(公告)号：EP1538142A1
公开(公告)日：2005-06-08
申请号：EP03795320.5
申请日：2003-09-09
申请人： NIPPON CHEMIPHAR CO., LTD.
发明人： TENDO, Atsushi , TAKAHASHI, Toshihiro , YAMAKAWA, Tomio
IPC分类号： C07C213/08 , C07C217/08
CPC分类号： C07C217/08
摘要： The invention relates to (1S)-1-isobutoxymethyl-3-methylbutylamine useful as an intermediate in the synthesis of sodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate and a process for production thereof. The process comprises reacting L-leucinol with a compound represented by the following formula in the presence of a base and reducing the obtained (1S)-1-(2-methyl-2-propenoxymethyl)-3-methylbutylamine:
[in which X is a leaving group].
摘要翻译：本发明涉及用作（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-1-羧酸钠合成中间体的（1S）-1-异丁氧基甲基-3-甲基丁胺。 2-羧酸乙酯及其制备方法。该方法包括在碱存在下使L-亮氨醇与由下式表示的化合物反应并还原所得（1S）-1-（2-甲基-2-丙烯氧基甲基）-3-甲基丁胺：[其中X是离开组]。

47. 发明公开

EP1342720A3 Epoxysuccinamide derivatives 审中-公开
标题翻译：环氧琥珀衍生品
公开(公告)号：EP1342720A3
公开(公告)日：2004-02-11
申请号：EP03011154.6
申请日：1998-09-04
申请人： NIPPON CHEMIPHAR CO., LTD.
发明人： Nomura, Yutaka , Takahashi, Toshihiro , Yoshino, Yasushi , Nishioka, Koichiro
IPC分类号： C07D303/48 , C07D405/12 , C07D409/12 , A61K31/335 , A61K31/495 , A61K31/38 , A61K31/415 , A61K31/44 , A61P19/00
CPC分类号： C07D405/12 , C07D303/48
摘要： Novel epoxysuccinamide derivatives represented by the general formula (1) or physiologically acceptable salts thereof, which are useful particularly as remedies for bone diseases and arthritis, wherein R 1 and R 3 are each hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; R 2 is alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a hetericyclic -alkyl group; X is -O- or -NR 4 - (wherein R 4 is hydrogen, alkyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; Y 1 is OR 5 , SR 6 , or NR 7 R 8 (wherein each of R 5 , R 6 and R 7 is hydrogen, alkyl, aryl, aralkyl, acyl, a heterocyclic group, or a heterocyclic-alkyl group, and R 8 is the same as defined for R 4 ); and Y 2 is hydrogen or alkyl, or alternatively Y 1 and Y 2 can be combined to form =O, =S, =N-R 9 , or =N-OR 10 (wherein each of R 9 and R 10 is the same as defined for R 4 ), provided that each of the alkyl, aryl and heterocyclic groups defined for R 5 to R 10 can have one or more specific substituents and that each of the group defined for R 1 to R 10 and Y 2 is specificed in the number of carbon atoms.

48. 发明公开

EP1022276A1 EPOXYSUCCINAMIDE DERIVATIVES 有权
标题翻译： EPOXYBERNSTEINSÄUREAMID衍
公开(公告)号：EP1022276A1
公开(公告)日：2000-07-26
申请号：EP98941728.2
申请日：1998-09-04
申请人： NIPPON CHEMIPHAR CO., LTD.
发明人： NOMURA, Yutaka , TAKAHASHI, Toshihiro , YOSHINO, Yasushi , NISHIOKA, Koichiro
IPC分类号： C07D303/48 , C07D405/12 , C07D409/12 , A61K31/335 , A61K31/495 , A61K31/38 , A61K31/415 , A61K31/44
CPC分类号： C07D405/12 , C07D303/48
摘要： Novel epoxysuccinamide derivatives represented by the general formula (1) or physiologically acceptable salts thereof, which are useful particularly as remedies for bone diseases and arthritis, wherein R 1 and R 3 are each hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; R 2 is alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a hetericyclic -alkyl group; X is -O- or -NR 4 -(wherein R 4 is hydrogen, alkyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; Y 1 is OR 5 , SR 6 , or NR 7 R 8 (wherein each of R 5 , R 6 and R 7 is hydrogen, alkyl, aryl, aralkyl, acyl, a heterocyclic group, or a heterocyclic-alkyl group, and R 8 is the same as defined for R 4 ); and Y 2 is hydrogen or alkyl, or alternatively Y 1 and Y 2 can be combined to form =O, =S, =N-R 9 , or =N-OR 10 (wherein each of R 9 and R 10 is the same as defined for R 4 ), provided that each of the alkyl, aryl and heterocyclic groups defined for R 5 to R 10 can have one or more specific substituents and that each of the group defined for R 1 to R 10 and Y 2 is specificed in the number of carbon atoms.
摘要翻译：由通式（1）表示的新型环氧琥珀酰胺衍生物或其生理上可接受的盐，其特别用作骨疾病和关节炎的治疗剂，其中R 1和R 3各自为氢，烷基，烯基，炔基，芳基芳烷基，杂环基或杂环烷基; R 2是烷基，烯基，炔基，芳基，芳烷基，杂环基或杂环烷基; X是-O-或-NR 4 - （其中R 4是氢，烷基，芳基，芳烷基，杂环基或杂环烷基; Y 1是OR 5，或其中R 5，R 6和R 7各自为氢，烷基，芳基，芳烷基，酰基，杂环基或杂环烷基基团，R 8与R 4中定义的相同）; Y 2是氢或烷基，或者Y 1和Y 2可以组合形成= O，= S ，= NR 9或= N-OR 10（其中R 9和R 10各自与R 4中定义的相同），条件是每个烷基，芳基和杂环对R 5至R 10定义的基团可以具有一个或多个特定取代基，并且对于R 1至R 10和Y 2定义的基团中的每一个以碳原子数为特定。

49. 发明公开

EP0877614A1 METHOD FOR INDUCING DEATH OF NEOPLASTIC CELLS USING PIPERAZINE OXIRANE DERIVATIVES 失效
标题翻译：一种杀灭肿瘤细胞的方法的装置哌嗪衍生物环氧乙烷
公开(公告)号：EP0877614A1
公开(公告)日：1998-11-18
申请号：EP97903981.0
申请日：1997-01-24
申请人： HITACHI CHEMICAL COMPANY, LTD. , HITACHI CHEMICAL RESEARCH CENTER, INC. , NIPPON CHEMIPHAR CO., LTD.
发明人： EILON, Gabriel, F. , JACOBS, John, W.
IPC分类号： C07D303 , A61K31 , A61P35 , C07D405 , C07D407
CPC分类号： A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/70 , A61K2300/00
摘要： Use of a piperazine compound of formula (I) or a pharmaceutically acceptable salt thereof in the preparation of a medicament for inducing cell death in neoplastic cells as a primary chemotherapeutic agent, or for potentiating chemotherapy to treat multidrug-resistant neoplastic cells, where R1 is hydroxyl, C1-4 alkoxyl, C1-4 alkylcarbonyloxymethoxyl, phenyl C1-2 alkylamino group, 2,5-pyrrolidinedione-1-alkoxyl(C1-4), or formula (II) wherein X1 is a chemical bond or C1-2 alkylene, X2 is hydrogen or carboxyl forming a 5-membered ring with X?1 when X1¿ is methylene, X3 is hydrogen or C1-2 alkyl, X4 is hydrogen or C1-2 alkyl, or X?3 and X4¿ together form a 5-membered ring, in which at least one of X?2, X3, and X4¿ is hydrogen, R2 is C3-4 alkyl, R3 is C1-4 alkyl, formulae (III), (IV) or (V) in which n is an integer of 0 to 3.

50. 发明公开

EP0826681A1 EPOXYSUCCINIC ACID DERIVATIVES 失效
标题翻译： DERIVATE DEREPOXYBERNSTEINSÄURE
公开(公告)号：EP0826681A1
公开(公告)日：1998-03-04
申请号：EP96907747.8
申请日：1996-04-01
申请人： NIPPON CHEMIPHAR CO., LTD.
发明人： NOMURA, Yutaka , TAKAHASHI, Toshihiro , HARA, Kaoru , YOSHINO, Yasushi , MASAKI, Mitsuo
IPC分类号： C07D303/48 , A61K31/335
CPC分类号： C07D303/48
摘要： Epoxysuccinic acid derivatives having general formula (I) (wherein R 1 represents hydrogen, alkyl, aryl or aralkyl; R 2 and R 3 independently represent each aryl, aralkyl or alkyl; and X represents -O-or NR 4 - wherein R 4 represents hydrogen, alkyl or aralkyl) which is useful in the prevention or treatment of bone diseases such as osteoporosis, malignant hypercalcemia, and bone Behcet's disease, in the treatment of osteoarthritis and rheumatoid arthritis in association with the abnormal hyperergasia of cathepsin L activity, and as a remedy for diseases in which cathepsins L and B participate such as muscular dystrophy and amyotrophy.
摘要翻译：具有通式（I）（其中R 1表示氢，烷基，芳基或芳烷基; R 2和R 3）的环氧琥珀酸衍生物独立地表示各芳基，芳烷基或烷基; X表示-O - 或NR 4 - 其中R 4表示氢，烷基或芳烷基），其可用于预防或治疗骨疾病如骨质疏松症，恶性高钙血症和骨白塞病，用于治疗骨关节炎和类风湿性关节炎与组织蛋白酶L活性的异常高血压有关，并且作为组织蛋白酶L和B参与的疾病如肌营养不良和肌萎缩的补救措施。

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