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1. 发明授权

EP3092216B1 CARBOCYCLIC SULFONE ROR GAMMA MODULATORS 失效
公开(公告)号：EP3092216B1
公开(公告)日：2018-12-12
申请号：EP15700817.8
申请日：2015-01-05
申请人： Bristol-Myers Squibb Company
发明人： DUAN, Jingwu , DHAR, T. G. Murali , JIANG, Bin , LU, Zhonghui , KARMAKAR, Ananta , GUPTA, Arun Kumar , WEIGELT, Carolyn A.
IPC分类号： C07D213/04 , C07D309/08 , C07D231/14 , C07D401/02 , C07D403/04 , C07D237/06 , C07D405/02 , C07D239/28 , C07C317/00 , C07D241/24 , C07D249/04 , C07D471/04 , C07D205/04 , C07D207/277 , C07D277/60 , C07D295/00 , C07D211/36 , A61K31/33 , A61K31/10 , A61P29/00
CPC分类号： C07C317/14 , C07C317/20 , C07C317/22 , C07C317/30 , C07C317/32 , C07C317/44 , C07C317/46 , C07C317/50 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D205/04 , C07D211/36 , C07D211/62 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D213/85 , C07D231/12 , C07D237/08 , C07D239/38 , C07D241/12 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D285/06 , C07D295/108 , C07D295/155 , C07D295/18 , C07D295/185 , C07D295/20 , C07D295/22 , C07D303/06 , C07D303/34 , C07D305/14 , C07D309/04 , C07D309/14 , C07D317/44 , C07D319/20 , C07D401/04 , C07D471/04 , C07D471/10
摘要： Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

2. 发明授权

EP2424853B1 NON-STEROIDAL COMPOUNDS FOR ANDROGEN RECEPTOR MODULATION, PROCESSES FOR THE PREPARATION AND USES THEREOF 有权
公开(公告)号：EP2424853B1
公开(公告)日：2018-09-19
申请号：EP10716110.1
申请日：2010-04-12
申请人： Istituto Scientifico Romagnolo Per Lo Studio E La Cura Dei Tumori (I.R.S.T.) S.R.L. , Guerrini, Andrea
发明人： VARCHI, Greta , TESEI, Anna , BRIGLIADORI, Giovanni
IPC分类号： C07D333/16 , C07C317/46 , C07C255/60 , C07C323/60 , A61K31/275 , A61P35/00
CPC分类号： C07C317/46 , C07C255/60 , C07C323/60 , C07D333/16
摘要： The present invention concerns compounds of general Formula (I): method of preparation and uses thereof.

3. 发明公开

EP3294706A1 CYCLIC COMPOUNDS 审中-公开
公开(公告)号：EP3294706A1
公开(公告)日：2018-03-21
申请号：EP16729646
申请日：2016-05-06
申请人： TAKEDA PHARMACEUTICALS CO
发明人： KOBAYASHI TOSHITAKE , SAITOH MORIHISA , WADA YASUFUMI , NARA HIROSHI , NEGORO NOBUYUKI , KATOH TAISUKE , YAMASAKI MASASHI , TANAKA TAKAHIRO , KITAMOTO NAOMI
IPC分类号： C07C317/46 , A61K31/216 , A61K31/357 , A61P1/16 , A61P25/02 , C07C317/44 , C07D309/28 , C07D317/72
CPC分类号： C07D317/72 , C07C317/12 , C07C317/44 , C07C317/46 , C07C2601/16 , C07C2602/08 , C07D309/28
摘要： wherein, each symbol is explained in greater detail in the specification.

5. 发明公开

EP3077372A1 ROR GAMMA (RORY) MODULATORS 有权转让
标题翻译： ROR-γ（罗里）-MODULATOREN
公开(公告)号：EP3077372A1
公开(公告)日：2016-10-12
申请号：EP14809794.2
申请日：2014-12-03
申请人： Lead Pharma Cel Models IP B.V.
发明人： CALS, Joseph Maria Gerardus Barbara , NABUURS, Sander Bernardus
IPC分类号： C07C311/16 , C07C311/20 , C07C317/44 , C07C317/46 , C07D213/75 , A61P19/02 , A61P25/28 , A61P29/00 , A61P37/00 , A61K31/18 , A61K31/10 , A61K31/44 , A61K31/167
CPC分类号： C07C317/44 , A61K31/167 , A61K31/18 , A61K31/44 , A61K45/06 , C07C311/16 , C07C311/20 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/75 , Y02A50/409 , A61K2300/00
摘要： The present invention relates to compounds according to Formula I: Wherein: A11 - A14 are N or CR11, CR12, CR13, CR14, respectively, with the proviso that no more than two of the four positions A can be simultaneously N; R1 is C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1 -3)alkyl, (di)C(1-6)alkylamino, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(1 -3)alkyl)amino, with all carbon atoms of alkyl groups optionally substituted with one or more F and all carbon atoms of cycloalkyl groups optionally substituted with one or more F or methyl; R2 and R3 are independently H, F, methyl, ethyl, hydroxy, methoxy or R2 and R3 together is carbonyl, all alkyl groups, if present, optionally being substituted with one or more F; R4 is H or C(1-6)alkyl; R5 is H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1 -9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1 -3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups optionally substituted with one or more F, CI, C(1-2)alkyl, C(1-2)alkoxy or cyano; the sulfonyl group with R1 is represented by one of R7, R8 or R9; the remaining R6-RH are independently H, halogen, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl, all of the alkyl groups optionally being substituted with one or more F; and Ri5 and Ri6 are independently H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups optionally substituted with one or more F, CI, C(1-2)alkyl, C(1-2)alkoxy or cyano. The compounds can be used as inhibitors of RORy and are useful for the treatment of RORy mediated diseases.
摘要翻译：本发明涉及式I化合物：其中：A11-A14分别为N或CR11，CR12，CR13，CR14，条件是四个位置A中不超过两个可以同时为N; R 1是C（1-6）烷基，C（3-6）环烷基，C（3-6）环烷基C（1-3）烷基，（二）C（1-6）烷基氨基，（二）C（3- 6）环烷基氨基或（二）（C（3-6）环烷基C（1-3）烷基）氨基，烷基的所有碳原子任选被一个或多个F取代，并且所有环烷基的碳原子任选被一个或多个更多F或甲基; R2和R3独立地为H，F，甲基，乙基，羟基，甲氧基或R2和R3一起为羰基，所有烷基（如果存在），任选被一个或多个F取代; R4是H或C（1-6）烷基; R5是H，羟乙基，甲氧基乙基，C（1-6）烷基，C（6-10）芳基，C（6-10）芳基C（1-3）烷基，C（1-9）杂芳基， 9）杂芳基C（1-3）烷基，C（3-6）环烷基，C（3-6）环烷基C（1-3）烷基，C（2-5）杂环烷基或C（2-5）杂环烷基C（1- 3）烷基，所有基团任选被一个或多个F，Cl，C（1-2）烷基，C（1-2）烷氧基或氰基取代; 具有R 1的磺酰基由R 7，R 8或R 9中的一个表示; 剩余的R6-RH独立地为H，卤素，C（1-3）烷氧基，（二）C（1-3）烷基氨基或C（1-6）烷基），所有烷基任选被一个或多个 F; （1-6）烷基，C（3-6）环烷基，C（3-6）环烷基C（1-3）烷基，C（6-10）芳基，C（6- C（1-5）杂环烷基或C（2-5）杂环烷基C（1-4）烷基， 3）烷基，所有基团任选被一个或多个F，Cl，C（1-2）烷基，C（1-2）烷氧基或氰基取代。该化合物可用作RORY的抑制剂，可用于治疗RORy介导的疾病。

6. 发明公开

EP2865665A1 AMIDE COMPOUND AND USE THEREOF FOR PEST CONTROL 有权
标题翻译： AMIDVERBINDUNG UND VERWENDUNG DAVON ZURSCHÄDLINGSBEKÄMPFUNG
公开(公告)号：EP2865665A1
公开(公告)日：2015-04-29
申请号：EP13807006.5
申请日：2013-06-05
申请人： Sumitomo Chemical Co., Ltd
发明人： MAEHATA, Ryota , MIZUNO, Hajime , SHIMIZU, Chie , NOKURA, Yoshihiko
IPC分类号： C07C317/44 , A01N41/10 , A01N41/12 , A01N43/40 , A01N43/54 , A01P7/02 , A01P7/04 , A01P17/00 , C07C323/62 , C07D213/56 , C07D239/26
CPC分类号： C07C323/42 , A01N39/00 , A01N41/10 , A01N41/12 , A01N43/40 , A01N43/54 , C07C317/40 , C07C317/44 , C07C317/46 , C07C323/62 , C07C323/63 , C07C2601/02 , C07C2601/14 , C07D213/56 , C07D213/61 , C07D239/26 , C07D277/32
摘要： A fused heterocyclic compound represented by formula (1) has an excellent pest control effect. (In the formula, R 1 represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from group X, or the like; R2, R3, R4 and R5 may be the same or different, and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from group X, or the like; R6 represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from group W, or the like; R7 and R11 may be the same or different, and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from group X, or the like; R8, R9 and R10 may be the same or different, and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from group X, or the like; Q represents an oxygen atom or a sulfur atom; and each of m and n represents 0, 1 or 2.)
摘要翻译：由式（1）表示的稠合杂环化合物具有优异的害虫防治效果。（式中，R 1表示可以具有1个以上选自X等的原子或基团的C1-C6链烃基; R2，R3，R4和R5可以相同或不同，表示可以具有选自X基团的一个或多个原子或基团的C 1 -C 6链烃基; R 6表示可以具有一个或多个选自W组的原子或基团的C 1 -C 6链烃基，或 R 7和R 11可以相同或不同，并且各自表示可以具有一个或多个选自X基团的原子或基团的C 1 -C 6链烃基; R 8，R 9和R 10可以相同或不同，各自表示可以具有一个或多个选自X基团的原子或基团的C1-C6链烃基; Q表示氧原子或硫原子; m和n各自表示0,1或或2.）

8. 发明公开

EP2488489A2 C-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： C-VERLINKTEHYDROXAMINSÄUREDERIVATEALS ANTIBAKTERIELLE WIRKSTOFFE
公开(公告)号：EP2488489A2
公开(公告)日：2012-08-22
申请号：EP10818065.4
申请日：2010-10-04
申请人： Pfizer Inc.
发明人： BROWN, Matthew Frank , MARFAT, Anthony , MELNICK, Michael Joseph , REILLY, Usa
IPC分类号： C07C317/44 , C07D231/56 , C07C317/46 , C07D205/04 , C07D207/08 , C07D209/18 , C07D209/44 , C07D209/46 , C07D211/38 , C07D211/46 , C07D211/48 , A61K31/165 , A61K31/44 , A61P31/04
CPC分类号： C07C317/50 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07C2601/18 , C07D213/30 , C07D213/56 , C07D215/06 , C07D231/12 , C07D231/56 , C07D233/36 , C07D239/26 , C07D261/08 , C07D263/08 , C07D263/20 , C07D295/03 , C07D335/02 , C07F9/09 , C07F9/12
摘要： The present invention is directed to a new class of alpha - alkylsulfonyl hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
摘要翻译：本发明涉及新的式I的异羟肟酸衍生物，其中变量G，T，D，L，A，X，R 1和R 2如上所述，并且它们作为LpxC抑制剂的用途，更具体地它们用于治疗细菌感染。

9. 发明公开

EP2486004A2 SULPHONE COMPOUNDS AND METHODS OF MAKING AND USING SAME 有权
标题翻译：黛ER UNG AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS AS
公开(公告)号：EP2486004A2
公开(公告)日：2012-08-15
申请号：EP10765558.1
申请日：2010-10-08
申请人： Zafgen Corporation
发明人： DYKE, Hazel, Joan , CRAMP, Susan, Mary , PALLIN, Thomas, David , KULAGOWSKI, Janusz, Jozef , MONTANA, John, Gary , ZAHLER, Robert
IPC分类号： C07C317/44 , C07C317/46 , C07D231/10 , C07D263/32 , C07D275/02 , C07D277/30 , C07D307/54 , C07D333/24 , C07D405/12 , A61K31/192 , A61K31/277 , A61K31/341 , A61K31/381 , A61K31/415 , A61K31/421
CPC分类号： A61K31/46 , A61K31/192 , A61K31/195 , A61K31/341 , A61K31/381 , A61K31/397 , A61K31/4025 , A61K31/407 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/4418 , A61K31/443 , A61K31/4525 , C07C317/44 , C07C317/46 , C07C2101/02 , C07C2601/02 , C07D213/55 , C07D231/12 , C07D263/32 , C07D275/02 , C07D277/30 , C07D307/16 , C07D307/54 , C07D333/24 , C07D405/12 , C07D451/02 , C07D487/08
摘要： The invention provides sulphone compounds according to formula (Ia) and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
摘要翻译：本发明提供了砜类化合物及其在治疗医学疾病如肥胖症中的用途。提供制备各种砜类化合物的药物组合物和方法。化合物被认为具有抗甲硫氨酰氨基肽酶2的活性。

10. 发明公开

EP2046322A4 ARYL VINYL SULFIDES, SULFONES, SULFOXIDES AND SULFONAMIDES, DERIVATIVES THEREOF AND THERAPEUTIC USES THEREOF 审中-公开
标题翻译：亚油酰磺隆，-SULFONE，-SULFOXIDE UND -SULFONAMIDE，DERIVATE DAVON UND THERAPEUTISCHE ANWENDUNGEN DAVON
公开(公告)号：EP2046322A4
公开(公告)日：2010-10-06
申请号：EP07811018
申请日：2007-08-01
申请人： UNIV TEMPLE
发明人： REDDY E PREMKUMAR , REDDY M V RAMANA
IPC分类号： A61K31/33
CPC分类号： C07C317/44 , C07C311/12 , C07C311/27 , C07C311/35 , C07C317/18 , C07C317/46 , C07C317/48 , C07C323/65 , C07C323/67

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