公开(公告)号：EP3353170A1

公开(公告)日：2018-08-01

申请号：EP16847688.5

申请日：2016-09-22

申请人： Pharmascience Inc.

发明人： LAURENT, Alain ,  ROSE, Yannick ,  MORRIS, Stephen J.

IPC分类号： C07D409/12 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/425 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  C07D235/30 ,  C07D401/12 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

CPC分类号： C07D409/12 ,  A61K45/06 ,  A61K47/02 ,  A61K47/16 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/00 ,  C07D235/32 ,  C07D409/14

摘要： The present invention relates to a novel family of covalent kinases inhibitors. Compounds of this class have been found to have inhibitory activity against members of the Tec kinase family, particularly ITK, BTK, BMX, Tec and/or RLK. The present invention is directed to a compound of Formula I or pharmaceutically acceptable salt, solvate, solvate of salt, stereoisomer, tautomer, isotope, prodrug, complex or biologically active metabolite thereof, and its use in therapy.

公开(公告)号：EP2872252A1

公开(公告)日：2015-05-20

申请号：EP13816862.0

申请日：2013-07-11

申请人： STC.UNM

发明人： SEROV, Alexey ,  ATANASSOV, Plamen B

IPC分类号： B01J37/08 ,  B01J23/745 ,  C07D235/30

CPC分类号： H01M4/9075 ,  B01J23/745 ,  B01J37/084 ,  C07D235/30 ,  C07D235/32 ,  H01M4/90 ,  H01M4/9041 ,  H01M2008/1095 ,  Y02E60/50

摘要： A method of preparation of M-N-C catalytic material utilizing a sacrificial support approach and using inexpensive and readily available metal precursors and carbendazim (CBDZ) as the carbon source is described.

公开(公告)号：EP2736334A1

公开(公告)日：2014-06-04

申请号：EP12820152.2

申请日：2012-07-27

申请人： MediciNova, Inc.

发明人： RUBY, Kale

IPC分类号： A01N43/40

CPC分类号： C07D235/32 ,  A61K31/4184 ,  A61K45/06

摘要： MN-029 di-hydrochloride (MN-029.2HC1, Formula 2) is a potent vascular targeting agent. The present invention focuses on the synthesis and characterization of the di-hydrochloride salt MN-029 and the preparation of pharmaceutically acceptable formulations thereof. Methods are disclosed of using the compound and formulations thereof in the treatment of diseases that rely on the generation of neovasculature by angiogenesis for disease progression.

公开(公告)号：EP2643304A2

公开(公告)日：2013-10-02

申请号：EP11843289.7

申请日：2011-11-23

申请人： Sequent Scientific Ltd. ,  Arulmoli, Thangavel

发明人： RANE, Ramkrishna Appaji ,  NAITHANI, Sushil ,  NATIKAR, Rajendra Devendra ,  VERMA, Sudhakar

IPC分类号： C07D235/30

CPC分类号： C07D235/32 ,  C07D235/30

摘要： The present invention discloses a novel, cost-effective process for preparation of a benzimidazole carbamates compound. Specifically, it relates to the process for the preparation of anti-parasite bulk drug albendazole. The process comprises a) thiocyanating 2-nitroaniline of formula VI with ammonium thiocyanated in presence of a halogen to obtain 2-nitro-4-thiocyanoaniline of formula V; b)propylating 2-nitro-4-thiocyanoaniline of formula V with propylbromide in presence of n-propanol and a base in absence of a phase transfer catalyst to obtain 4-propylthio-2-nitroaniline of formula III; C) reducing the nitro group of 4- propylthio-2-nitroaniline prepared in step b) by reacting an aqueous alkali metal sulphide or an alkaline metal sulphide to obtain 4-propylthio-o-phenylenediamine of formula II; and d)condensing 4-propylthio-o-phenylenediamine of formula II with alkali or alkaline earth metal salt of methylcyano carbamate in presence of an acid to form Albendazole of formula I.

摘要翻译： 本发明公开了一种制备苯并咪唑氨基甲酸酯化合物的新型成本有效的方法。 具体而言，涉及制备抗寄生虫药物阿苯达唑的方法。 该方法包括a）在卤素存在下硫氰酸化式VI的2-硝基苯胺与硫氰酸铵反应，得到式Ⅴ的2-硝基-4-硫代氰胺; b）在不存在相转移催化剂的情况下，在正丙醇和碱的存在下，用丙基溴将式V的2-硝基-4-氰基氰胺丙基化，得到式III的4-丙硫基-2-硝基苯胺; C）通过使碱金属硫化物水溶液或碱金属硫化物水溶液还原步骤b）中制备的4-丙基硫代-2-硝基苯胺的硝基，得到式II的4-丙硫基 - 邻苯二胺; 和d）将式II的4-丙硫基 - 邻苯二胺与甲基氰基氨基甲酸酯的碱金属或碱土金属盐在酸存在下缩合形成式I的阿苯达唑。

公开(公告)号：EP2407459A1

公开(公告)日：2012-01-18

申请号：EP11008295.5

申请日：2006-09-25

申请人： Shionogi & Co., Ltd.

发明人： Kugimiya, Akira ,  Fujioka, Masahiko ,  Tachibana, Yuki ,  Murashi, Takami ,  Onodera, Naohiro

IPC分类号： C07D233/64 ,  C07D263/32 ,  C07D271/10 ,  C07D277/24 ,  C07D295/096 ,  C07D307/42 ,  C07D333/16

CPC分类号： C07D295/26 ,  C07D207/14 ,  C07D207/48 ,  C07D211/58 ,  C07D211/70 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/74 ,  C07D231/12 ,  C07D231/40 ,  C07D235/08 ,  C07D235/30 ,  C07D235/32 ,  C07D243/08 ,  C07D261/08 ,  C07D261/18 ,  C07D263/32 ,  C07D263/58 ,  C07D265/36 ,  C07D271/10 ,  C07D277/24 ,  C07D277/28 ,  C07D285/12 ,  C07D285/135 ,  C07D295/096 ,  C07D295/155 ,  C07D307/42 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D333/36 ,  C07D401/12 ,  C07D413/12

摘要： The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.
A compound of the general formula (V):

wherein the ring D is a benzene ring etc.; R 1 is hydroxyalkyl etc.; R 2 is independently a hydrogen atoms etc.; R 8 is a halogen atom etc.; L 3 is independently a single bond etc.; R 7 is independently a hydrogen atom etc.; and p is 1, 2, 3 or 4; provided that the substituting position of the piperidino group and L 3 each other is not an ortho-position in the ring D when the ring D is a benzene ring and -L 3 - is -(O-alkylene)-;
a pharmaceutically acceptable salt or hydrate thereof.

摘要翻译： 本发明提供了到磺酰胺衍生物具有DP受体拮抗活性和包含所述化合物作为活性成分的药物组合物，和另外的治疗剂用于治疗过敏性疾病。 通式（V）的化合物：worin环D为苯环等; R 1为羟烷基等; R 2为独立地为氢原子等; R 8为卤原子等; L 3是单键unabhängig等; R 7为独立地为氢原子等; 且p是1，2，3或4; 提供，DASS模具代哌啶子基基团，L的位置3海誓山盟不在环D邻位当环D为苯环和-L 3 - 是 - （O-亚烷基） - ; 药学上可接受的盐或水合物。

公开(公告)号：EP2407453A1

公开(公告)日：2012-01-18

申请号：EP11008294.8

申请日：2006-09-25

申请人： Shionogi & Co., Ltd.

发明人： Kugimiya, Akira ,  Fujioka, Masahiko ,  Tachibana, Yuki ,  Murashi, Takami ,  Onodera, Naohiro

IPC分类号： C07D207/48 ,  C07D207/14 ,  A61K31/40 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61P11/06 ,  A61P37/08 ,  A61P43/00

CPC分类号： C07D295/26 ,  C07D207/14 ,  C07D207/48 ,  C07D211/58 ,  C07D211/70 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/74 ,  C07D231/12 ,  C07D231/40 ,  C07D235/08 ,  C07D235/30 ,  C07D235/32 ,  C07D243/08 ,  C07D261/08 ,  C07D261/18 ,  C07D263/32 ,  C07D263/58 ,  C07D265/36 ,  C07D271/10 ,  C07D277/24 ,  C07D277/28 ,  C07D285/12 ,  C07D285/135 ,  C07D295/096 ,  C07D295/155 ,  C07D307/42 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D333/36 ,  C07D401/12 ,  C07D413/12

摘要： A compound of the general formula (I) for use in the treatment of diseases associated with a PGD2 receptor:

wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R 1 is hydroxyalkyl etc.; R 2 is independently a halogen atom etc.; R 3 is a hydrogen atom etc.; R 4 is independently a halogen atom etc.; R 5 is independently a halogen atom etc.; M is carbonyl etc.; Y is a single bond etc.; L 1 , L 2 and L 3 are independently a single bond etc.; R 6 and R 7 are independently a hydrogen atom etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s), and the ring C is a benzene ring, b) the ring C is not an indole ring or an azaindole ring, c) R 1 is not carboxy when the ring C is a benzene ring, -L3- is - (O-alkylene)-, and the substituting position of L 3 and Y is an ortho-position each other in the ring C, and d) the substituting position of L 3 and Y is not a para-position in the ring C when the ring B is a thiazolidine ring and the ring C is a benzene ring;
a pharmaceutically acceptable salt or solvate thereof.

摘要翻译： 用于治疗与PGD2受体有关的疾病的通式（I）的化合物：其中环A为芳族碳环等; 环B为含氮非芳族杂环等; 环C是芳族碳环等; R 1是羟烷基等; R 2独立地为卤素原子等; R 3为氢原子等。 R 4独立地为卤素原子等; R 5独立地为卤素原子等; M是羰基等。 Y是单键等; L 1，L 2和L 3独立地为单键等; R 6和R 7独立地为氢原子等; k为0，1，2，3或4; n为0,1或2; q为0,1,2或3; 条件是当环B是含有一个或两个氮原子的6元含氮杂环时a）k不为0，并且环C是苯环，b）环C不是吲哚 环或氮杂环，c）当环C为苯环时，R 1不为羧基，-L 3为 - （O-亚烷基） - ，并且L 3和Y的取代位置为彼此的邻位 在环C中，d）当环B为噻唑烷环且环C为苯环时，L 3和Y的取代位置不在环C中的对位; 其药学上可接受的盐或溶剂化物。

公开(公告)号：EP2107052B1

公开(公告)日：2011-10-12

申请号：EP07860141.6

申请日：2007-12-26

申请人： Santen Pharmaceutical Co., Ltd

发明人： MOGI, Hiroyuki ,  TAJIMA, Hisashi ,  MISHINA, Noriko ,  YAMAZAKI, Yusuke ,  YONEDA, Shinji ,  WATANABE, Katsuhiko ,  FUJIKAWA, Junko ,  YAMAMOTO, Minoru

IPC分类号： C07C275/28 ,  C07D207/09 ,  C07D211/26 ,  C07D213/40 ,  C07D213/75 ,  C07D215/38 ,  C07D235/32 ,  C07D261/14 ,  C07D277/46 ,  C07D277/82 ,  C07D295/12 ,  C07D307/79 ,  A61K31/17 ,  A61K31/197 ,  A61K31/245 ,  A61K31/277 ,  A61K31/36 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61P27/02 ,  C07D317/50 ,  C07D319/18 ,  C07D333/36 ,  C07D405/12

CPC分类号： C07D207/09 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C275/40 ,  C07C275/42 ,  C07C2601/08 ,  C07C2602/08 ,  C07C2602/10 ,  C07D207/27 ,  C07D211/26 ,  C07D213/40 ,  C07D213/75 ,  C07D215/38 ,  C07D235/32 ,  C07D261/14 ,  C07D277/46 ,  C07D277/82 ,  C07D295/12 ,  C07D307/79 ,  C07D317/50 ,  C07D319/18 ,  C07D333/36 ,  C07D405/12

摘要： Disclosed are: a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of the pharmacological activity of the derivative. A compound represented by the general formula (1) or a salt thereof has an activity of changing the morphology of a trabecular cell and therefore is effective for the prevention and/or treatment of a disease associated with an ocular tension. In the formula, R1 and R2 independently represents a hydrogen atom, a lower alkyl group or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group or the like; R4 and R5 independently represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group or the like; l and m independently represent a number of 0, 1, 2 or the like.

公开(公告)号：EP2205568A1

公开(公告)日：2010-07-14

申请号：EP08869645.5

申请日：2008-10-16

申请人： Sanofi-Aventis

发明人： NEMECEK, Conception ,  WENTZLER, Sylvie

IPC分类号： C07D235/30 ,  C07D277/82 ,  C07D417/12 ,  A61K31/4184 ,  A61K31/428 ,  A61P35/00 ,  A61P25/00

CPC分类号： C07D235/30 ,  C07D235/32 ,  C07D277/82 ,  C07D417/12

摘要： The invention relates to novel products of the formula (I) in which : R is H, HaI or AIk; A is NH or S; R5 is H or Alk optionally substituted by one or more HaI; R6 is an optionally substituted aryl or heteroaryl; W is H or COR7 in which R7 is a cycloalkyl, an optionally substituted alkyl, an optionally substituted alkoxy or NR1 R2 with one of R1 and R2 being H or alk while the other of R1 and R2 is a cycloakyl or an optionally substituted alkyl; or R1 and R2 form together with N to which they are bonded; a cyclic radical optionally including one or more optionally substituted O, S, N and NH; the invention also relates to said products in any of their isomer forms or as salts, and they can be used as drugs, in particular as c-Met inhibitors.

公开(公告)号：EP1939175A4

公开(公告)日：2009-07-22

申请号：EP06810485

申请日：2006-09-25

申请人： SHIONOGI & CO

发明人： KUGIMIYA AKIRA ,  FUJIOKA MASAHIKO ,  TACHIBANA YUKI ,  MURASHI TAKAMI ,  ONODERA NAOHIRO

IPC分类号： C07D207/48 ,  A61K31/40 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61P11/06 ,  A61P37/08 ,  A61P43/00 ,  C07D207/14

CPC分类号： C07D295/26 ,  C07D207/14 ,  C07D207/48 ,  C07D211/58 ,  C07D211/70 ,  C07D211/96 ,  C07D213/38 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/74 ,  C07D231/12 ,  C07D231/40 ,  C07D235/08 ,  C07D235/30 ,  C07D235/32 ,  C07D243/08 ,  C07D261/08 ,  C07D261/18 ,  C07D263/32 ,  C07D263/58 ,  C07D265/36 ,  C07D271/10 ,  C07D277/24 ,  C07D277/28 ,  C07D285/12 ,  C07D285/135 ,  C07D295/096 ,  C07D295/155 ,  C07D307/42 ,  C07D307/52 ,  C07D307/56 ,  C07D307/68 ,  C07D333/36 ,  C07D401/12 ,  C07D413/12

摘要： A sulfonamide derivative having DP receptor antagonistic activity; and a medicinal composition and a therapeutic agent for allergic diseases which each contains the compound as an active ingredient. The derivative is a compound represented by the general formula (II): (II) (wherein ring A is an aromatic carbocycle, etc.; ring B is a nitrogenous nonaromatic heterocycle, etc.; ring C is an aromatic carbocycle, etc.; R1 is carboxy, etc.; R2's each independently is halogeno, etc.; R3 is optionally substituted alkyloxy, etc.; R4's each independently is halogeno, etc.; R5's each independently is optionally substituted alkyl, etc.; M is sulfonyl, etc.; Y is a single bond, etc.; L1 is a single bond, etc.; L2 is a single bond, etc.; k is 0, 1, 2, 3, or 4; n is 0, 1, or 2; and q is 0, 1, 2, or 3, provided that, for example, a) when ring B is a 6-membered nitrogenous heterocycle containing one or two nitrogen atoms and ring C is a benzene ring, then k is not 0), a pharmaceutically acceptable salt of the compound, or a hydrate of either.

公开(公告)号：EP1052250B1

公开(公告)日：2004-07-14

申请号：EP00114155.5

申请日：1996-03-07

申请人： G.D. SEARLE & CO.

发明人： Getman, Daniel P. ,  Decrescenzo, Gary A. ,  Freskos, John N. ,  Vazquez, Michael L. ,  Sikorski, James A. ,  Devadas, Balkudru ,  Nagarajan, Srinivasan ,  McDonald, Joseph J.

IPC分类号： C07C311/00 ,  C07D317/62 ,  C07D319/18 ,  C07D277/64 ,  C07D307/82 ,  C07D235/32 ,  C07D277/82 ,  A61K31/34 ,  A61K31/36 ,  A61K31/415 ,  A61K31/425

CPC分类号： C07D235/06 ,  C07C311/29 ,  C07C311/41 ,  C07C317/44 ,  C07D215/36 ,  C07D217/04 ,  C07D235/30 ,  C07D235/32 ,  C07D249/18 ,  C07D249/20 ,  C07D263/56 ,  C07D277/62 ,  C07D277/82 ,  C07D303/36 ,  C07D307/79 ,  C07D317/62 ,  C07D319/18