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1. 发明授权

EP2834248B1 NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF 有权
标题翻译：新型噻吩并嘧啶衍生物，方法其制造和治疗应用程序
公开(公告)号：EP2834248B1
公开(公告)日：2016-03-16
申请号：EP13716241.8
申请日：2013-04-02
申请人： SANOFI
发明人： CARRY, Jean-Christophe , CHATREAUX, Fabienne , DEPRETS, Stéphanie , DUCLOS, Olivier , LEROY, Vincent , MALLART, Sergio , MELON-MANGUER, Dominique , MENDEZ-PEREZ, Maria , VERGNE, Fabrice
IPC分类号： C07D495/04 , A61P35/00 , A61K31/505
CPC分类号： A61K31/553 , A61K31/519 , A61K31/55 , A61K31/551 , C07D495/04

2. 发明公开

EP2432766A1 COMPOSE ANTICANCÉREUX ET COMPOSITION PHARMACEUTIQUE LE CONTENANT 有权
标题翻译：抗癌化合物和药物组合物包含此
公开(公告)号：EP2432766A1
公开(公告)日：2012-03-28
申请号：EP10728768.2
申请日：2010-05-17
申请人： SANOFI
发明人： CARRY, Jean-Christophe , CHEVE, Michel , CLERC, François , COMBEAU, Cécile , GONTIER, Sylvie , KRICK, Alain , LACHAUD, Sylvette , SCHIO, Laurent
IPC分类号： C07D235/26 , C07D471/04 , A61K31/4745 , A61P35/00
CPC分类号： C07D471/04 , C07D235/26
摘要： The invention relates to a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [α]D= -38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a base or an acid addition salt, in particular a pharmaceutically acceptable acid. The compound is a selective Aurora A and B kinase inhibitor and can be used as an anticancer drug.

3. 发明公开

EP2834248A1 NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF 有权
标题翻译：新型噻吩并嘧啶衍生物，方法其制造和治疗应用程序
公开(公告)号：EP2834248A1
公开(公告)日：2015-02-11
申请号：EP13716241.8
申请日：2013-04-02
申请人： SANOFI
发明人： CARRY, Jean-Christophe , CHATREAUX, Fabienne , DEPRETS, Stéphanie , DUCLOS, Olivier , LEROY, Vincent , MALLART, Sergio , MELON-MANGUER, Dominique , MENDEZ-PEREZ, Maria , VERGNE, Fabrice
IPC分类号： C07D495/04 , A61P35/00 , A61K31/505
CPC分类号： A61K31/553 , A61K31/519 , A61K31/55 , A61K31/551 , C07D495/04
摘要： The present invention relates to compounds of formula (I): wherein R6 is -CONH
2 or a -C(Rα)(R
β )(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.

4. 发明公开

EP2758399A1 N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： N- [4-（1H-吡唑并[3,4-B]哒嗪-6-基） - 苯基] - 磺酰胺在DEREN VERWENDUNG ALS ARZNEIMITTEL
公开(公告)号：EP2758399A1
公开(公告)日：2014-07-30
申请号：EP12759725.0
申请日：2012-09-18
申请人： SANOFI
发明人： NAZARE, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin , CARRY, Jean-Christophe
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04
摘要： The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺，其中Ar，R 1，R 2和n具有如索赔。式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶异构体1（SGK-1，SGK1）的活性的有价值的药理学活性化合物，并且是适用于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。本发明还涉及制备式I化合物，其作为药物的用途以及包含它们的药物组合物的方法。

5. 发明公开

EP2408762A1 DERIVES D'INDAZOLE INHIBITEURS D'HSP90, COMPOSITIONS LES CONTENANT ET UTILISATION 审中-公开
标题翻译： HSP90抑制吲唑，包括成分及其用途
公开(公告)号：EP2408762A1
公开(公告)日：2012-01-25
申请号：EP10715951.9
申请日：2010-03-18
申请人： SANOFI
发明人： BERTIN, Luc , CARRY, Jean-Christophe , MAILLIET, Patrick , MINOUX, Hervé , PILORGE, Fabienne , RUXER, Jean-Marie
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D407/14 , C07D493/08 , A61K31/4709 , A61K31/4184 , A61P35/00
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D407/14 , C07D493/08
摘要： The invention relates to novel products having formula (I), wherein: R4 represents H, CH3, CH2CH3, CF3, F, Cl, Br, I; Het represents a heterocycle optionally substituted by one or more R1 or R'1 radicals selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalkoxy, alkylthio, carboxy that is free or sterified with an alkyl radical, carboxamide, CO-NH(alkyl), CON(alkyl)2, NH-CO-alkyl, sulfonamide, NH-SO2-alkyl, S(O)2-NHalkyl, S(O2)-N(alkyl)2, all of the alkyl, alkoxy and alkylthio radicals being optionally substituted; R being selected from the group comprising (A'), (B), (C), (D) and (E), wherein W1, W2, W3 represent independently CH or N, X represents O, S, NR2, C(O), S(O) or S(O)2; V represents H, HaI, -O-R2 or -NH-R2 with R2 representing H, alkyl, cycloalkyl or heterocycloalkyl, optionally substituted; said products being in all isomer forms, as well as the salts and intended for use as drugs.

6. 发明授权

EP2758399B1 N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： N- [4-（1H-吡唑并[3,4-B]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途
公开(公告)号：EP2758399B1
公开(公告)日：2017-11-15
申请号：EP12759725.0
申请日：2012-09-18
申请人： SANOFI
发明人： NAZARE, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin , CARRY, Jean-Christophe
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04

7. 发明授权

EP2570415B1 N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals 失效
标题翻译： N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺和它们作为药物的用途
公开(公告)号：EP2570415B1
公开(公告)日：2015-08-26
申请号：EP11306179.0
申请日：2011-09-19
申请人： SANOFI
发明人： Nazaré, Marc , Halland, Nis , Schmidt, Friedemann , Weiss, Tilo , Dietz, Uwe , Hofmeister, Armin , CARRY, Jean-Christophe
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04

8. 发明授权

EP2448927B1 NOUVEAUX DERIVES DE (6-OXO-1,6-DIHYDRO-PYRIMIDIN-2-YL)-AMIDE, LEUR PREPARATION ET LEUR UTILISATION PHARMACEUTIQUE COMME INHIBITEURS DE PHOSPHORYLATION D'AKT 有权
标题翻译： NEW（6-氧代-1,6-二氢 - 嘧啶-2-基）-AMIDDERIVATE，它们的制备和制药用AS AKT-PHOSPHORYLIERUNGSHEMMER
公开(公告)号：EP2448927B1
公开(公告)日：2014-03-12
申请号：EP10742014.3
申请日：2010-07-01
申请人： SANOFI
发明人： CARRY, Jean-Christophe , CERTAL, Victor , HALLEY, Frank , KARLSSON, Karl Andreas , SCHIO, Laurent , THOMPSON, Fabienne
IPC分类号： C07D239/36 , C07D403/12 , C07D409/12 , C07D413/12 , A61K31/513 , A61P35/00 , A61K31/5377 , C07D239/47 , C07D403/06 , C07D403/10 , C07D413/06
CPC分类号： C07D239/22 , C07D239/47 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D471/04

9. 发明公开

EP2448927A1 NOUVEAUX DERIVES DE (6-OXO-1,6-DIHYDRO-PYRIMIDIN-2-YL)-AMIDE, LEUR PREPARATION ET LEUR UTILISATION PHARMACEUTIQUE COMME INHIBITEURS DE PHOSPHORYLATION D'AKT(PKB) 有权
标题翻译： NEW（6-氧代-1,6-二氢 - 嘧啶-2-基）-AMIDDERIVATE，它们的制备和制药用AS AKT-PHOSPHORYLIERUNGSHEMMER
公开(公告)号：EP2448927A1
公开(公告)日：2012-05-09
申请号：EP10742014.3
申请日：2010-07-01
申请人： SANOFI
发明人： CARRY, Jean-Christophe , CERTAL, Victor , HALLEY, Frank , KARLSSON, Karl Andreas , SCHIO, Laurent , THOMPSON, Fabienne
IPC分类号： C07D239/36 , C07D403/12 , C07D409/12 , C07D413/12 , A61K31/513 , A61P35/00 , A61K31/5377 , C07D239/47 , C07D403/06 , C07D403/10 , C07D413/06
CPC分类号： C07D239/22 , C07D239/47 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D471/04
摘要： The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted aryl or heteroaryl; R is an H or, when formed with R1, a 5- or 6-member ring fused with an aryl or heretoaryl group optionally containing one or more of O, S, N, NH, and Nalk, being optionally substituted; R2 and R3 are, independently, an H, Hal, or alkyl optionally substituted by one or more Hal; R4 is H; and R5 is an H or alkyl optionally substituted by one or more halogen atoms. Said materials being in any isomeric form and the salts thereof, and are intended for drugs, particularly AKT(PKB) phosphorylation inhibitors.

10. 发明公开

EP1641791A1 3-(GUANIDINOCARBONYL)HETEROCYCLE DERIVATIVES, PREPARATION PROCESS AND INTERMEDIATES OF THIS PROCESS, THEIR USE AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM 有权
标题翻译： 3-（GUANIDINOCARBONYL）HETEROCYCLUSDERIVATIVE，HERSETLLUNGSVERFAHREN和用于该方法的中间产物，其使用AS药品和药物组合物含
公开(公告)号：EP1641791A1
公开(公告)日：2006-04-05
申请号：EP04739421.8
申请日：2004-05-28
申请人： Sanofi-Aventis Deutschland GmbH
发明人： CARRY, Jean-Christophe , DOERFLINGER, Gilles, 2 avenue du Berry , GENEVOIS-BORELLA, Arielle , EVERS, Michel , LE BRUN, Alain , MARTIN, Jean-Paul , DESMAZEAU, Pascal , MIGNANI, Serge , KLEEMANN, Heinz-Werner
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The present invention relates to the novel compounds of the formula (I) and their pharmaceutically acceptable salts. The inventive compounds are suitable, for example, as antiarrhythmic medicaments with a cardioprotective component for infarction prophylaxis and infarction treatment and for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiologicaI processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure.

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