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1. 发明公开

EP1778629A1 PROCESS FOR THE SYNTHESIS C-2, C-3 SUBSTITUTED N-ALKYLATED INDOLES USEFUL AS CPLA2 INHIBITORS 有权
标题翻译：用于合成的C-2，方法C-3取代的N-烷基化的吲哚核ALS的cPLA 2抑制剂
公开(公告)号：EP1778629A1
公开(公告)日：2007-05-02
申请号：EP05788529.5
申请日：2005-08-18
申请人： Wyeth
发明人： MICHALAK, Ronald, S. , LEVENT, Mahmut , VYVERBERG, Frederick, J. , BOYAJIAN, Ara, R. , RAVEENDRANATH, Panolil , CANTIN, Michel , STOCKTON, Alan , WINKLEY, Michael, W. , GHOSH, Mousumi , DEHNHARDT, Christoph , GUINOSSO, Charles
IPC分类号： C07C303/38 , C07C303/40 , C07C311/12 , C07D209/14
CPC分类号： C07C311/14 , C07C303/38 , C07C303/40 , C07C311/13 , C07D209/14
摘要： The present invention provides method for making a compound of formula (1) comprising the steps of reacting compounds of formulas (2) and (3) to produce a compound of formula (4) wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula (4) is then converted to the compound of formula (1). The invention further comprises compounds of formula (3) and (4) and methods for making compounds of formulae (3) and (4).

2. 发明公开

EP2865664A1 NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT 有权
标题翻译：需要有能力对抑制酶11B-HSD1或其药学上可接受的盐，过程的新颖的组合用于生产和药物组合物，其作为活性
公开(公告)号：EP2865664A1
公开(公告)日：2015-04-29
申请号：EP13806654.3
申请日：2013-06-04
申请人： BAMICHEM CO., LTD , Ahn-Gook Pharmaceutical Co., Ltd. , Incheon University Industry Academic Cooperation Foundation
发明人： HAN, Cheol Kyu , AUH, Jin , CHOI, Nam Song , HAN, Chang Kyun , KIM, Tae-Jeong , PAE, Kamsa , SHIN, Young June , HAN, Dong-Oh , AHN, Soon Kil
IPC分类号： C07C311/12 , A61K31/18 , A61P3/10
CPC分类号： C07C311/21 , C07C237/24 , C07C275/28 , C07C311/08 , C07C311/14 , C07C311/19 , C07C311/29 , C07C2601/02 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D209/08 , C07D213/70 , C07D213/82 , C07D215/08 , C07D217/06 , C07D231/18 , C07D239/42 , C07D241/42 , C07D275/06 , C07D277/36 , C07D277/56 , C07D295/215 , C07D307/64 , C07D333/34 , C07D417/12
摘要： The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.
摘要翻译：本发明涉及一种新颖的化合物或其药学上可接受的盐抑制11²-HSD1的酶活性，同样的制备方法，和包含其作为上活性成分的药物组合物。由于本发明的化合物选择性地抑制11²-HSD1（11²羟基类固醇脱氢酶1型）的活性，本发明的化合物可以有效地用作用于疾病由11²过度活化引起的治疗的治疗剂 HSD1：如非胰岛素依赖性II型糖尿病，胰岛素抵抗，肥胖症，脂质紊乱，代谢综合症，和其它疾病或病症由糖皮质激素的过度活性介导。

3. 发明公开

EP1086063A4 NOVEL POTASSIUM CHANNEL DRUGS AND THEIR USES 审中-公开
标题翻译：镓通道活性物质及其使用
公开(公告)号：EP1086063A4
公开(公告)日：2001-03-28
申请号：EP99927330
申请日：1999-06-07
申请人： ADVANCED MEDICINE INC
发明人： JACOBSEN JOHN R , EASTMAN DONNA , GRIFFIN JOHN H
IPC分类号： G01N33/50 , A61K9/06 , A61K31/18 , A61K31/343 , A61K31/395 , A61K31/407 , A61K31/4178 , A61K31/4427 , A61K31/443 , A61K31/4545 , A61K45/00 , A61K47/48 , A61P9/00 , A61P43/00 , C07C311/08 , C07C311/10 , C07C311/12 , C07C311/22 , C07C311/30 , C07D257/02 , C07D307/80 , C07D401/06 , C07D405/12 , C07D487/04 , C07D487/08 , C07K5/09 , C07K5/11 , C07K7/06 , C07K7/08 , G01N33/15 , G01N33/566 , G01N33/68 , C07B61/00 , A61K38/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00 , G01N33/53 , G01N33/543
CPC分类号： G01N33/6872 , A61K47/55 , A61K47/65

4. 发明授权

EP1778629B1 PROCESS FOR THE SYNTHESIS C-2, C-3 SUBSTITUTED N-ALKYLATED INDOLES USEFUL AS CPLA2 INHIBITORS 有权
标题翻译：用于合成的C-2，方法C-3取代的N-烷基化的吲哚核ALS的cPLA 2抑制剂
公开(公告)号：EP1778629B1
公开(公告)日：2011-07-20
申请号：EP05788529.5
申请日：2005-08-18
申请人： Wyeth LLC
发明人： MICHALAK, Ronald, S. , LEVENT, Mahmut , VYVERBERG, Frederick, J. , BOYAJIAN, Ara, R. , RAVEENDRANATH, Panolil , CANTIN, Michel , STOCKTON, Alan , WINKLEY, Michael, W. , GHOSH, Mousumi , DEHNHARDT, Christoph , GUINOSSO, Charles
IPC分类号： C07C303/38 , C07C303/40 , C07C311/12 , C07D209/14
CPC分类号： C07C311/14 , C07C303/38 , C07C303/40 , C07C311/13 , C07D209/14
摘要： The present invention provides method for making a compound of formula (1) comprising the steps of reacting compounds of formulas (2) and (3) to produce a compound of formula (4) wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula (4) is then converted to the compound of formula (1). The invention further comprises compounds of formula (3) and (4) and methods for making compounds of formulae (3) and (4).

5. 发明授权

EP1278718B1 NOUVEAUY DERIVES D'AMINOACIDES, LEUR PROCEDE DE PREPARATION, COMPOSITIONS LES CONTENANT ET LEURS UTILISATIONS COMME FILTRES SOLAIRES 有权
标题翻译： NOUVEAUY DERIVES D'AMINOACIDES，LEUR程序DE制剂，组合物LES含量ET LEURS应用COMME FILTRES SOLAIRES
公开(公告)号：EP1278718B1
公开(公告)日：2003-12-17
申请号：EP01925635.3
申请日：2001-04-12
申请人： L'OREAL
发明人： BORDIER, Thierry , PHILIPPE, Michel
IPC分类号： C07C233/51 , C07C311/12 , C07C231/02 , A61K7/42
CPC分类号： C07C235/34 , A61K8/44 , A61K8/447 , A61Q17/04 , C07C233/51 , C07C311/13 , C07C311/21 , C07C311/29 , C07C2602/42
摘要： The invention concerns novel amino acid derivatives, the method for preparing them and their uses as UV filters, in particular in cosmetics. The invention concerns in particular the use of said novel compounds for skin and/or hair protection against ultraviolet radiation, or for protecting any other UV-sensitive material (mineral or organic glasses, plastics, food products, paint and the like).
摘要翻译：本发明涉及新型氨基酸衍生物，制备它们的方法以及它们作为紫外线过滤剂的用途，特别是在化妆品中。本发明特别涉及所述新化合物用于抗紫外线辐射的皮肤和/或头发护理，或用于保护任何其他UV敏感材料（矿物或有机玻璃，塑料，食品，涂料等）的用途。

7. 发明授权

EP0608847B1 Carbocyclic sulfonamides as agonists or antagonists of PGEZ 失效
标题翻译：碳磺胺作为Agoniste或antagoniste PGE的
公开(公告)号：EP0608847B1
公开(公告)日：1996-12-04
申请号：EP94101085.2
申请日：1994-01-25
申请人： ONO PHARMACEUTICAL CO., LTD.
发明人： Hamanaka, Nobuyuki, c/o Minase Res. Inst. , Miyamoto, Tsumoru
IPC分类号： C07C311/13 , C07C311/20 , C07C311/07 , C07C311/12 , C07C311/27 , C07C311/29 , C07C311/10 , C07C311/11 , A61K31/18
CPC分类号： C07C311/19 , C07C311/07 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/20 , C07C311/27 , C07C311/29

8. 发明公开

EP0516181A1 Novel sulfonamide derivatives 失效
标题翻译：新型磺酰胺衍生物
公开(公告)号：EP0516181A1
公开(公告)日：1992-12-02
申请号：EP92112113.3
申请日：1988-10-12
申请人： ONO PHARMACEUTICAL CO., LTD.
发明人： Arai, Yoshinobu , Hamanaka, Nobuyuki , Miyazaki, Tohru, Dai 2 Minase Haitsu 501
IPC分类号： C07C405/00 , C07C311/20 , C07C311/10 , C07C311/12 , C07D303/02 , C07D493/08 , C07D331/02 , A61K31/557
CPC分类号： C07C405/0091 , C07C311/20 , C07C2601/08 , C07C2602/42
摘要： A sulfonamide derivative of the general formula:

wherein, R¹ represents

(i) COOR¹¹,
(ii) CH₂OR¹² or
(iii) CONR¹³R¹⁴,
wherein
R¹¹ represents a carbocyclic ring unsubstituted or substituted by an alkyl or alkoxy group of from 1 to 4 carbon atom(s) or halogen atom, or steroid,
R¹² represents a hydrogen atom or COR¹⁵,
R¹³ and R¹⁴ each represent a hydrogen atom or alkyl group of form 1 to 4 carbon atom(s) or NR¹³R¹⁴ represents an amino acid residue or heterocyclic ring, or
R¹⁵ represents an alkyl group of from 1 to 4 carbon atom(s) or phenyl group,

wherein

represents

Ba represents

(i) -CH₂-CH₂-(CH₂)m- (Ba-1),
(ii) cis-CH=CH-(CH₂)m- (Ba-2),
(iii) -CH₂-O-(CH₂)m- (Ba-3),
(iV) -S-(CH₂)m- (Ba-4) or
(V)
wherein m represents an integer of from 1 to 6, and the configuration of a double bond is E, Z or EZ and a phenylene group represetns an o-, m- or p-phenylene group in the formula (Ba-5),
R 2a represents a bond or an alkylene group of from 1 to 4 carbon atom(s),
R 3a represents a carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of an alkyl group of from 1 to 4 carbon atom(s), alkoxy group of from 1 to 4 carbon atom(s), hydroxy group, carboxyl group, ciano group, halogen atom or nitro group, or
R 2a represents an alkyl group of from 1 to 12 carbon atom(s) together with R 3a,
cyclodextrin clathrates thereof, or non-toxic salts thereof in case that NR¹³R¹⁴ represents an amino acid residue, possess an antagonistic activity on TXA₂, in particular, inhibit blood platelet aggregation and contraction of artery, and are, therefore, useful for prevention and/or treatment of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, cardiac infarction, angina pectoris, cerebral infarction and death by aucte cardiac diseases in mammales, in particular in humans, which are induced by thromboxane A₂.
摘要翻译：具有下列通式的磺酰胺衍生物：其中R 1代表（ⅰ）COOR 11，（ⅱ）CH 2 OR 12或（ⅲ）CONR 13 R 14，其中R 11代表未取代的或被1-4个碳原子的烷基或烷氧基取代的碳环 s）或卤原子或甾族化合物，R 12代表氢原子或COR 15，R 13和R 14各代表氢原子或1-4个碳原子的烷基或NR 13 R 14代表氨基酸残基或杂环，或（ⅰ）-CH 2 -CH 2 - （CH 2）m - （Ba-1），（ⅱ）顺式-CH = CH - （CH 2）m-（Ba-2），（iii）-CH 2 -O-（CH 2）m-（Ba-3），（Ⅳ）-S-（CH 2）m- ）（式中，m表示1〜6的整数，双键的构型为E，Z或EZ，亚苯基表示式（Ba-5）中的邻，间或对亚苯基） R 2a代表1至4个碳的键或亚烷基原子，R3a表示未取代的或被1至3个1至4个碳原子的烷基，1至4个碳原子的烷氧基，羟基取代的碳环或杂环，羧基，噌基，卤素原子或硝基，或者R2a代表1至12个碳原子的烷基连同R3a，环糊精包合物或其无毒盐，在NR 13 R 14代表氨基酸残基，对TXA 2具有拮抗活性，特别是抑制血小板凝集和动脉收缩，因此可用于预防和/或治疗炎症，高血压，血栓，脑卒中，哮喘，心肌梗塞，心绞痛心肌梗塞和由于血栓素A 2诱导的乳房中尤其是人类中的心脏病引起的死亡。

9. 发明公开

EP3189032A1 NEUE 2,2' -DIAMINOBIARYLE MIT ZWEI SEKUNDÄREN AMINEN UND DEREN HERSTELLUNG DURCH ELEKTROCHEMISCHE KUPPLUNG 审中-公开
标题翻译：具有二级胺的新型2,2'-二氨基二苯甲酮及其电化学偶联制备
公开(公告)号：EP3189032A1
公开(公告)日：2017-07-12
申请号：EP15741996.1
申请日：2015-07-23
申请人： Evonik Degussa GmbH
发明人： DYBALLA, Katrin Marie , FRANKE, Robert , FRIDAG, Dirk , WALDVOGEL, Siegfried R. , ELSLER, Bernd , ENDERS, Mathias
IPC分类号： C07C303/40 , C07C231/12 , C25B3/10 , C07C233/43 , C07C311/12
CPC分类号： C25B3/10 , C07C233/43 , C07C233/44 , C07C311/21 , C25B9/06 , C25B15/02
摘要： Novel 2,2'-diamino biaryls of formula (I), (II) and (III), wherein R1-R10, R1'-R10' and X1-X3 are defined in claim 1. The invention also relates to an electrochemical method for the production thereof.
摘要翻译：式（I），（II）和新型2,2-二氨基二芳基（III），worin R1-R10，R10 R1'和X1-X3在claimsoft 1限定的本发明因此涉及在电化学方法用于其生产。

10. 发明公开

EP1278718A1 NOUVEAUY DERIVES D'AMINOACIDES, LEUR PROCEDE DE PREPARATION, COMPOSITIONS LES CONTENANT ET LEURS UTILISATIONS COMME FILTRES SOLAIRES 有权
标题翻译：新AMIN酸衍生物，PROCESS其产生，其成分及其作为防晒
公开(公告)号：EP1278718A1
公开(公告)日：2003-01-29
申请号：EP01925635.3
申请日：2001-04-12
申请人： L'OREAL
发明人： BORDIER, Thierry , PHILIPPE, Michel
IPC分类号： C07C233/51 , C07C311/12 , C07C231/02 , A61K7/42
CPC分类号： C07C235/34 , A61K8/44 , A61K8/447 , A61Q17/04 , C07C233/51 , C07C311/13 , C07C311/21 , C07C311/29 , C07C2602/42
摘要： The invention concerns novel amino acid derivatives, the method for preparing them and their uses as UV filters, in particular in cosmetics. The invention concerns in particular the use of said novel compounds for skin and/or hair protection against ultraviolet radiation, or for protecting any other UV-sensitive material (mineral or organic glasses, plastics, food products, paint and the like).
摘要翻译：具有式（I）的氨基酸化合物：非常适合于人的皮肤和/或头发的紫外光光保护，以及用于各种各样的感光工业材料/底物，例如，塑料，玻璃的UV-光保护，纺织等

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