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公开(公告)号：EP2774926A1
公开(公告)日：2014-09-10
申请号：EP12829693.6
申请日：2012-09-07
IPC分类号： C07D491/18 , A61K31/485 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5375 , A61K31/541 , A61K31/55 , A61P25/04 , A61P43/00 , C07D471/08
CPC分类号： C07D491/18 , C07D471/08 , C07D471/22 , C07D487/08 , C07D491/22 , C07F7/1856
摘要： A morphinan derivative represented by the following general formula (I):
(in the formula, R 1 represents hydrogen, C 1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,
R 2 represents hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, C 6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,
R 3 , R 4 and R 5 represent hydrogen, hydroxy, carbamoyl, C 1-6 alkoxy, C 6-10 aryloxy and the like,
R 6a , R 6b , R 7 , R 8 , R 9 , and R 10 represent hydrogen and the like,
X represents O or CH 2 , and
Y represents C=O, SO 2 , an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.摘要翻译： 由以下通式（I）表示的吗啡喃衍生物：（式中，R 1表示氢，C 1-6烷基，环烷基烷基（环烷基部分具有3〜6个碳原子，亚烷基部分具有1〜5个碳原子 原子），芳烷基（芳基部分具有6〜10个碳原子，亚烷基部分具有1〜5个碳原子）等，R 2表示氢，C 1-6烷基，C 3-6环烷基， 10芳基，芳烷基（芳基部分具有6至10个碳原子，亚烷基部分具有1至5个碳原子）等，R 3，R 4和R 5表示氢，羟基，氨基甲酰基，C 1-6烷氧基 ，C 6-10芳氧基等，R 6a，R 6b，R 7，R 8，R 9和R 10表示氢等，X表示O或CH 2，Y表示C = O，SO 2 ，原子键等）或其酸加成盐用作止痛剂。
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2.发明公开SALT OF (2S,3S)-3- (1S)-1-ISOBUTOXYMETHYL-3-METHYLBUTYL CARBAMOYLOXIRANE-2-CARBOXYLIC ACID 有权SALZE VON（2S，3S）-3 - [[（1S）-1-异丙氧基甲基-3-甲基丁基]羰基]氧基-2-碳
公开(公告)号：EP1619190A1
公开(公告)日：2006-01-25
申请号：EP04728921.0
申请日：2004-04-22
IPC分类号： C07D303/48
CPC分类号： C07D303/48
摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics:
DSC: exothermic peak observed at a temperature in the range of 170 to 175°C with weight decrease; and
characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm -1 .摘要翻译： 本发明涉及（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-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。 本发明还涉及提供羧酸的结晶钠盐。 钠盐可用作制备药物的材料并提高储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱的特征吸收带（KBr片剂）：3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm -1。
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公开(公告)号：EP2397480A1
公开(公告)日：2011-12-21
申请号：EP10741334.6
申请日：2010-02-15
IPC分类号： C07D403/10 , A61K31/5513 , A61P25/04 , A61P43/00 , C07D413/10 , C07D417/10
CPC分类号： C07D243/10 , C07D403/10 , C07D413/10
摘要： A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X 4 receptor antagonist:
wherein R 1 represents a hydrogen atom, an alkyl group having' 1 to 8 carbon atoms, or the like, R 2 and R 3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R 4 and R 5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.摘要翻译： 作为P2X 4受体拮抗剂，使用式（I）所示的二氮杂二酮衍生物或其药理学上可接受的盐作为P2X 4受体拮抗剂，式中，R 1表示氢原子，碳原子数1〜8的烷基等，R 2和R 3表示 氢原子，具有1至8个碳原子的烷基，卤素原子等，R 4和R 5表示氢原子，具有1至8个碳原子的烷基等，并且W表示四唑或 喜欢。
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公开(公告)号：EP1310494A1
公开(公告)日：2003-05-14
申请号：EP01955606.7
申请日：2001-08-09
发明人： SAKUMA, Shogo , ENDO, Tsuyoshi , TENDO, Atsushi , TAKAHASHI, Toshihiro , YOSHIDA, Shinichi , KOBAYASHI, Kunio , MOCHIZUKI, Nobutaka , YAMAKAWA, Tomio , KANDA, Takashi , MASUI, Seiichiro
IPC分类号： C07D263/32 , C07D277/24 , C07D413/04 , C07D263/48 , C07D263/34 , C07D277/28 , C07D417/04 , C07D233/64 , C07D233/70 , C07D233/88 , C07D233/90 , A61K31/421 , A61K31/4439 , A61K31/426 , A61K31/4164 , A61K31/4709 , A61K31/506 , A61K31/422 , A61K31/427
CPC分类号： C07D413/04 , C07D263/32 , C07D277/24
摘要： Compounds of the general formula (I) or salts thereof and activators of PPARδ (peroxisome proliferator activated receptor δ) containing the compounds or the salts as the active ingredient: wherein R 1 and R 2 each are hydrogen, C 1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X 1 and X 2 are each a free valency, oxygen, S(O) p (wherein p is an integer of 0 to 2), C(=O), C(=O)NH, NHC(=O), CH=CH, or the like; Y is optionally substituted C 1-8 alkylene; Z is oxygen or sulfur; R 3 and R 4 are each optionally substituted C 1-8 alkyl; and R 8 is hydrogen or C 1-8 alkyl, with the proviso that when X 1 is a free valency, X 2 is not O or S(O) p , while when X 1 is C(=O)NH, X 2 is not a free valency.
摘要翻译： 通式（I）化合物或其盐和含有化合物或其盐作为活性成分的PPARδ（过氧化物酶体增殖物激活受体δ）的活化剂：其中R 1和R 2各自为氢，C1- 8烷基，可被取代的芳基或杂环基等; A是氧，硫等; X 1和X 2各自为自由价，氧，S（O）p（其中p为0至2的整数），C（= O），C（= O）NH，NHC O），CH = CH等; Y为任选取代的C 1-8亚烷基; Z是氧或硫; R 3和R 4各自为任选取代的C 1-8烷基; 并且R 8是氢或C 1-8烷基，条件是当X 1是自由价时，X 2不是O或S（O）p，而当X 1是C（O） = O）NH，X 2不是自由价。
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公开(公告)号：EP0794178A1
公开(公告)日：1997-09-10
申请号：EP95932948.3
申请日：1995-09-29
IPC分类号： C07D239/95 , A61K31/505
CPC分类号： C07D239/95
摘要： The present invention provides a new compound which shows slow and continuous blood pressure reducing action and is useful as an antihypertensive agent.
The invention resides in a quinazoline derivative of the following formula (I) and its pharmaceutically acceptable salt:
in which, each of R 1 and R 2 is H or an alkyl group of 1 to 6 carbon atoms, or R 1 and R 2 are combined to form an ethylene group; each of R 3 and R 4 is an alkyl group of 1 to 6 carbon atoms; R 5 is a hydrogen atom, a hydroxyl group, an alkyl group of 1 to 6 carbon atoms, or an alkoxy group of 1 to 6 carbon atoms; each of R 6 and R 7 is a hydrogen atom or an alkyl group of 1 to 6 carbon atoms; and n is 2 or 3. The invention further resides in an antihypertensive agent containing the above compound.摘要翻译： 本发明提供了一种新的化合物，其显示缓慢且持续的减压作用，并且可用作抗高血压药。 本发明涉及下式（I）的喹唑啉衍生物及其药学上可接受的盐：其中R 1和R 2各自为H或1至6个碳原子的烷基， 或R 1和R 2结合形成亚乙基; R 3和R 4各自为1至6个碳原子的烷基; R 5为氢原子，羟基，碳原子数为1〜6的烷基或碳原子数1〜6的烷氧基。 R 6和R 7各自为氢原子或1〜6个碳原子的烷基; 并且n为2或3.本发明还涉及含有上述化合物的抗高血压药。
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公开(公告)号：EP1310494B1
公开(公告)日：2012-01-25
申请号：EP01955606.7
申请日：2001-08-09
发明人： SAKUMA, Shogo , ENDO, Tsuyoshi , TENDO, Atsushi , TAKAHASHI, Toshihiro , YOSHIDA, Shinichi , KOBAYASHI, Kunio , MOCHIZUKI, Nobutaka , YAMAKAWA, Tomio , KANDA, Takashi , MASUI, Seiichiro
IPC分类号： C07D263/32 , C07D277/24 , C07D413/04 , C07D263/48 , C07D263/34 , C07D277/28 , C07D417/04 , C07D233/64 , C07D233/70 , C07D233/88 , C07D233/90 , A61P3/10 , A61P3/06 , A61P3/04 , A61P9/10 , A61P9/00 , C07D263/40 , C07D277/26 , A61K31/4164 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/4725 , A61K31/506
CPC分类号： C07D413/04 , C07D263/32 , C07D277/24
摘要： Compounds of the general formula (|) or salts thereof; and activators of PPARδ (peroxisome proliferator activated receptor δ) containing the compounds or the salts as the active ingredient: (I) wherein R?1 and R2¿ are each hydrogen, C¿1-8? alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X?1 and X2¿ are each a free valency, oxygen, S(O)¿p? (wherein p is an integer of 0 to 2), C(=O), C(=O)NH, NHC(=O), CH=CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R?3 and R4¿ are each optionally substituted C¿1-8? alkyl; and R?8¿ is hydrogen or C¿1-8? alkyl, with the proviso that when X?1¿ is a free valency, X2 is not O or S(O)¿p?, while when X?1¿ is C(=O)NH, X2 is not a free valency.
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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
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。
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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
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]。
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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
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。
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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
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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