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1. 发明公开

EP3187488A1 NOVEL AMINO-PHENYL-SULFONYL-ACETATE DERIVATIVE AND USE THEREOF 有权转让
标题翻译：新的氨基 - 苯基 - 磺酰基乙酸酯衍生物及其用途
公开(公告)号：EP3187488A1
公开(公告)日：2017-07-05
申请号：EP15835298.9
申请日：2015-07-14
申请人： CJ Healthcare Corporation
发明人： YOO, Jae Ho , KIM, Seung Chan , JUNG, Soo Yeon , BAK, Hyoung Rok , CHUNG, Young Mee , KIM, Sung Jun , PARK, Sook Kyung , SONG, Seog Beom , RYU, Shin-Young , YOON, Mi Young , KO, Dong Hyun , PARK, Sun Young , PARK, Chi Hye , CHOI, Nak Hyun
IPC分类号： C07C317/44 , C07C317/48 , C07C317/14 , A61K31/18 , A61P3/00
CPC分类号： C07C317/14 , A61K31/192 , A61K31/196 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/44 , A61K31/4406 , A61K31/4409 , C07C317/44 , C07C2603/26 , C07D213/36 , C07D213/64 , C07D307/52 , C07D307/79 , C07D307/81 , C07D317/46 , C07D317/58 , C07D317/62 , C07D319/16 , C07D319/18
摘要： The present invention relates to a novel amino-phenyl-sulfonyl-acetate derivative or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating diabetes comprising the same as an active ingredient.
摘要翻译：本发明涉及新的氨基 - 苯基 - 磺酰基 - 乙酸酯衍生物或其药学上可接受的盐; 以及包含其作为活性成分的用于预防或治疗糖尿病的药物组合物。

2. 发明公开

EP2361243A4 HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS 有权
标题翻译：胆碱酯酶维生素A
公开(公告)号：EP2361243A4
公开(公告)日：2012-04-25
申请号：EP09826761
申请日：2009-11-12
申请人： VIROBAY INC
发明人： HART BARRY , GREEN MICHAEL , SETTI EDUARDO , ROEPEL MICHAEL
IPC分类号： C07C237/04 , A61K31/277 , A61P11/06 , A61P19/02 , C07C255/46 , C07C317/48 , C07C323/60 , C07D213/32
CPC分类号： C07C317/48 , C07C237/04 , C07C255/46 , C07C323/60 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/32

3. 发明公开

EP2288615A1 SELECTIVE CASPASE INHIBITORS AND USES THEREOF 有权转让
标题翻译：选择性CASPASEHEMMER及其用途
公开(公告)号：EP2288615A1
公开(公告)日：2011-03-02
申请号：EP09749369.6
申请日：2009-05-21
申请人： New World Laboratories Inc.
发明人： AHLFORS, Jan-Eric , MEKOUAR, Khalid
IPC分类号： C07K7/06 , A61K31/223 , A61K31/47 , A61K31/5375 , A61K31/662 , A61K38/00 , C07C237/12 , C07C237/20 , C07C317/48 , C07D215/14 , C07D295/26 , C07F9/40 , C07K5/08 , C07K5/10 , C07K14/81 , C12N9/64
CPC分类号： C07K5/0819 , A61K38/00 , A61K38/005 , C07C271/22 , C07C317/50 , C07C2602/08 , C07D209/16 , C07D213/81 , C07D215/12 , C07D295/26 , C07F9/4006 , C07F9/6533 , C07K5/0202 , C07K5/06034 , C07K5/06052 , C07K5/06078 , C07K5/06104 , C07K5/06139 , C07K5/081 , C07K5/0812 , C07K5/1013 , C07K14/8139
摘要： The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).

4. 发明公开

EP1791811A1 AMINOALCOHOL DERIVATIVES 有权
标题翻译： AMINOALKOHOLDERIVATE
公开(公告)号：EP1791811A1
公开(公告)日：2007-06-06
申请号：EP05787773.0
申请日：2005-09-20
申请人： Astellas Pharma Inc.
发明人： HATTORI, Kouji, c/o Astellas Pharma Inc. , TODA, Susumu, c/o Astellas Pharma Inc. , WASHIZUKA, Kenichi, c/o Astellas Pharma Inc. , ITO, Shinji, c/o Astellas Pharma Inc. , TANABE, Daisuke, c/o Astellas Pharma Inc. , ARAKI, Takanobu, c/o Astellas Pharma Inc. , SAKURAI, Minoru, c/o Astellas Pharma Inc.
IPC分类号： C07C317/46 , C07C317/48 , C07D213/38
CPC分类号： C07D213/70 , C07C311/51 , C07C323/63 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07D209/42 , C07D213/38 , Y02P20/55
摘要： The present invention relates to a compound of the formula [I]: wherein (a), in which -Y-, R4, R5 and R6 are4 R5 each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20 R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, -Z-R9 or (b), in which -Z- is -0-, -S-, R9 -SO- or -SO2-, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R10, in which -D- is -CONHSO2- or -S02NHCO-, E is bond or lower alkylene, and R10 is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.
摘要翻译：本发明涉及式[I]化合物：其中（a）其中-Y-，R4，R5和R6各自如说明书中所定义的R 4等，R 1是氢，卤素，低级烷基，羟基等，R2是氢，低级烷基或羟基（低级）烷基，R3是氢或氨基保护基，20R7是氢，低级烷基，环（低级）烷基，低级R9链烯基，-Z-R9或（b）中，-Z-为-O - ， - S - ，R 9 -SO-或-SO 2 - ，各R 9为氢，低级烷基，环（低级）烷基等， DE-R10，其中-D-是-CONHSO2-或-SO 2 NHCO-，E是键或低级亚烷基，R 10是卤素，氰基，羧基等，或其前药或其盐。本发明的化合物[I]及其药学上可接受的盐可用于溃疡，膀胱过度活动症等的预防和/或治疗性治疗。

5. 发明公开

EP1781602A1 4-SULFONYL-SUBSTITUTED BENZOYLALANINE DERIVATIVES USEFUL AS KYNURENINE-AMINOTRANSFERASE INHIBITORS 审中-公开
标题翻译： -4-磺酰BENZOYLALANINDERIVATE所产生作为适合KYNURENINAMINOTRANSFERASE抑制剂的
公开(公告)号：EP1781602A1
公开(公告)日：2007-05-09
申请号：EP05775813.8
申请日：2005-08-02
申请人： PELLICCIARI, Roberto , Schwarcz, Robert , Guidetti, Paolo
发明人： PELLICCIARI, Roberto , Schwarcz, Robert , Guidetti, Paolo
IPC分类号： C07C317/48 , A61K31/198 , A61P25/00
CPC分类号： C07C317/48
摘要： The invention relates to compounds of formula (I), in which R, R' and R' are as defined in the disclosure and the pharmaceutically acceptable esters thereof. The compounds of the invention reduce the synthesis of kynurenic acid thus inhibiting the enzyme kynurenine aminotransferase and can be used for the preparation of medicaments for the treatment of those psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as depression, bipolar illness, anxiety, Alzheimer's disease. Furthemore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly.

6. 发明公开

EP1680394A4 NOVEL NITROPHENYL MUSTARD AND NITROPHENYLAZIRIDINE ALCOHOLS AND THEIR CORRESPONDING PHOSPHATES AND THEIR USE AS TARGETED CYTOTOXIC AGENTS 审中-公开
标题翻译：新NITROPHENYLLOST-及其各自的NITROPHENYLAZIRIDINALKOHOLE和磷酸盐及其作为特异性结合细胞毒性药物
公开(公告)号：EP1680394A4
公开(公告)日：2006-10-11
申请号：EP04817434
申请日：2004-10-29
申请人： AUCKLAND UNISERVICES LTD
发明人： DENNY WILLIAM ALEXANDER , ATWELL GRAHAM JOHN , YANG SHANGJIN , WILSON WILLIAM ROBERT , PATTERSON ADAM VORN , HELSBY NUALA ANN
IPC分类号： C07C233/67 , A61K31/166 , A61K31/396 , A61K31/661 , A61P35/00 , C07C237/32 , C07C301/00 , C07C309/66 , C07C317/36 , C07C317/48 , C07D203/14 , C07F9/09
CPC分类号： C07F9/091 , C07C237/32 , C07C309/66 , C07C317/48 , C07D203/14

7. 发明公开

EP1701695A1 MEROCYANINE DERIVATIVES FOR COSMETIC USE 有权
标题翻译：花青化妆品用
公开(公告)号：EP1701695A1
公开(公告)日：2006-09-20
申请号：EP04820463.0
申请日：2004-12-08
申请人： CIBA SPECIALTY CHEMICALS HOLDING INC. Patent Departement
发明人： WAGNER, Barbara , EHLIS, Thomas , MÜLLER, Stefan
IPC分类号： A61K8/40 , A61Q17/04 , C07C255/31 , C07C229/46 , C07C317/48 , C07C225/20 , C07D295/155 , C07D295/116 , C07D319/06 , C07D295/185
CPC分类号： C07D295/116 , A61K8/41 , A61K8/44 , A61K8/46 , A61K8/494 , A61K8/81 , A61Q17/00 , A61Q17/02 , C07C225/20 , C07C229/46 , C07C255/31 , C07C317/48 , C07C2601/14 , C07C2601/16 , C07D295/155
摘要： Described are merocyanine derivatives of formula (1a) or (1b) wherein n and o are integers from 2 to 4 and aminocyclohexenone intermediates. They are used in protecting human and animal hair and skin from UV radiation.

8. 发明公开

EP1515947A1 FLUORIERTE CYCLOALKYL-DERIVATISIERTE BENZOYLGUANIDINE UND IHRE VERWENDUNG ALS MEDIKAMENT 有权
标题翻译：氟利昂环丙基衍生物苯甲酰胺在IHRE VERWENDUNG ALS MEDIKAMENT
公开(公告)号：EP1515947A1
公开(公告)日：2005-03-23
申请号：EP03759904.0
申请日：2003-06-02
申请人： Aventis Pharma Deutschland GmbH
发明人： KLEEMANN, Heinz-Werner
IPC分类号： C07C317/46 , C07C317/48 , C07C317/44 , A61K31/155 , A61P9/10
CPC分类号： C07C317/48 , C07C317/46 , C07C2601/04
摘要： Fluorinated cycloalkyl-derivatised benzoylguanidines of formula (I) are suitable for use as anti-arrhythmic medicaments comprising cardioprotective components for the prophylaxis and treatment of infarcts and also for the treatment of angina pectoris. They also preventatively inhibit the pathophysiological processes during the occurrence of ischaemically induced damage, in particular during the triggering of ischaemically induced cardiac arrhythmia and cardiac failure.
摘要翻译： N - （（4-多氟环烷基 - 氧基 - 硫代或 - 氨基） - 苯甲酰基） - 胍衍生物（I）是新的。式（I）的苯甲酰基胍衍生物及其盐是新的。 [图像] X：O，S或NR 6; R 6H，1-4C烷基或 - （CH 2）k-CF 3; k，l，m，n，p，r：0-3; q = 0-3，条件是m + n + p + q + r =至少2; R 1，C 1-4烷基，F，Cl，OR 7，NR 8 R 9或1-4C全氟烷基; R 7 -R 9，C 1-4烷基或 - （CH 2）t-CF 3; t：0-4; R 2H，F，Cl，1-4C烷基或CF 3; R 3H，F，Cl，1-4C烷基，CF 3或SO uR 10; 你：0-2; R 1 01-4C烷基或NR 1 1R 1 2; R 11，R 1 2H或1-4C烷基; R 4H，F，Cl，1-4C烷基，OR 13，NR 1 4R 15或1-4C全氟烷基; R 1 3 -R 1 5H，1-4C烷基或 - （CH 2）w-CF 3; w：0-4; 活性：Vasotropic; 抗心律不整; Cardiant; 抗心绞痛; 脑保护; 抑制细胞生长; 抗动脉硬化; 降血脂; 低血压; 镇惊; 安神; 抗抑郁药; 抗精神病药; 降血糖; 溶栓; 抗凝血剂; 嗜肝; Nephrotropic; 抗炎; 抗原虫; 抗疟药; 抗甲状腺。作用机制：细胞钠 - 质子反转录酶（NHE）抑制剂。 N-（4-（3,3-二氟 - 环丁氧基）-5-甲磺酰基-2-甲基 - 苯甲酰基） - 胍（Ia）具有抑制NHE1的IC5.0±5.9nM。

9. 发明公开

EP1144366A3 USE OF ANDROGEN RECEPTOR SUPPRESSORS 有权
标题翻译： VERWENDUNG VON ANDROGEN REZEPTOR SUPPRESSOREN
公开(公告)号：EP1144366A3
公开(公告)日：2003-06-04
申请号：EP99958948.4
申请日：1999-11-12
申请人： BIOPHYSICA, INC.
发明人： SOVAK, Milos , SELIGSON, Allen, L. , DOUGLAS, James, Gordon, III , CAMPION, Brian , BROWN, Jason, W.
IPC分类号： C07C237/04 , A61K31/16 , A61K31/40 , A61K31/415 , C07C237/22 , C07C323/60 , C07C317/48 , C07D207/40 , C07D207/26 , C07D233/88 , C07D233/86 , C07C335/22 , C07C335/16 , C07C335/08 , C07C255/56
CPC分类号： C07D207/408 , A61K31/165 , C07C237/04 , C07C255/56 , C07C255/60 , C07C275/30 , C07C317/46 , C07C323/60 , C07C335/08 , C07C335/16 , C07C335/22 , C07C2601/14 , C07D233/86 , C07D233/88

10. 发明公开

EP1174028A4 SULFONAMIDE DERIVATIVES 有权
标题翻译：磺酰胺衍
公开(公告)号：EP1174028A4
公开(公告)日：2002-11-06
申请号：EP00922891
申请日：2000-04-27
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： TABUCHI TAKANORI , YAMAMOTO TETSUHIRO , NAKAYAMA MASAHARU
IPC分类号： A01N41/06 , A01N43/10 , A01N43/40 , A01N43/42 , A01N43/50 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/80 , A01N43/82 , A01N43/90 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/44 , C07C311/46 , C07C311/48 , C07C311/49 , C07C311/51 , C07C317/36 , C07C317/48 , C07C323/49 , C07C323/63 , C07C327/48 , C07C327/58 , A01N47/04 , A01N47/24 , A01N47/48 , C07C303/40
CPC分类号： C07C327/58 , A01N41/06 , A01N43/10 , A01N43/40 , A01N43/42 , A01N43/50 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/653 , A01N43/80 , A01N43/82 , A01N43/90 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/44 , C07C311/46 , C07C311/48 , C07C311/49 , C07C311/51 , C07C317/36 , C07C317/48 , C07C323/49 , C07C323/63 , C07C327/48 , C07C2601/02 , A01N2300/00
摘要： Microbicides for agricultural and horticultural use, containing sulfonamide derivatives such as compounds of general formula (I) or salts thereof; some of the derivatives; and processes for the preparation of the same. In said formula, A1 is optionally substituted aryl or a heterocyclic group; X1 is a chemical bond, optionally substituted methylene, or vinylene; B1 is a five-membered heterocycle or fused-heterocycle group which contains nitrogen or sulfur as the ring-constituent heteroatom and may be substituted; and Z1 is optionally substituted hydrocarbyl, acyl, formyl, amino, -N=CR1R2, cyclic amino, -OR3, or -S (O)¿nR?4 (wherein n is 0 to 2). The compounds and the salts exhibit microbicidal effects, are safe by virtue of their little influence on human beings, farm animals, natural enemies, or the environment, and exert excellent control effects even on resistant microbes.
摘要翻译：本发明涉及用于农业或园艺用途的杀微生物剂，其包含例如式（I）的磺酰胺衍生物：其中A 1为（1）可以被取代的芳基或（2）可以被取代的杂环基，X 1是（1）化学键，（2）可以被取代的亚甲基，或（3）可被取代的亚乙烯基，B 1，是包含氮原子或硫原子的五元杂环基，作为除了碳原子以外的环构成原子，可以被取代，或可以被取代的稠合杂环基，Z 1是（1）可以是取代的（2）可被取代的酰基，（3）甲酰基，（4）可被取代的氨基，（5）由-N = CR 1 R 2表示的基团（其中 R 1和R 2各自为氢原子或可被取代的烃基），（6）环状氨基，（7）-OR 3表示的基团，（其中R 3为氢原子，可被取代的烃基，可被取代的酰基，甲酰基或可被取代的烷基磺酰基）或（8）-S（O）nR 4 >（其中n表示0至2的整数，R 4表示氢原子或可被取代的烃基）。所述化合物或其盐是具有杀微生物作用的磺酰胺衍生物，因为它们是安全的，并且对人类，农场动物，天敌或环境几乎没有影响，因此可用作农业或园艺用途的优良杀微生物剂，以及即使对抗性微生物也具有优异的防治效果。

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