公开(公告)号：EP4406939A1

公开(公告)日：2024-07-31

申请号：EP23305100.2

申请日：2023-01-26

申请人： Université Grenoble Alpes ,  Université Libre de Bruxelles ,  Centre National de la Recherche Scientifique ,  Institut National de la Santé et de la Recherche Médicale ,  Centre Hospitalier Régional de Grenoble ,  COMMISSARIAT À L'ÉNERGIE ATOMIQUE ET AUX ÉNERGIES ALTERNATIVES

发明人： BUSSER, Benoît ,  DENIAUD, Aurélien ,  LELIEVRE, Pierre ,  SANCEY GALLIOT, Lucie ,  RENIER, Nathan ,  VALKENIER-VAN DIJK, Elisabeth H. ,  JABIN, Ivan

IPC分类号： C07D233/64 ,  C07D235/12 ,  C07D263/32 ,  C07D277/24 ,  A61P35/00 ,  A61K31/4164

CPC分类号： C07D233/64 ,  C07D235/12 ,  C07D263/32 ,  C07D277/24 ,  A61P35/00

摘要： The present invention relates to calix[4]arenes of the formula (1),

in which:
Y1, Y2, Y3 and Y4 are selected from the group consisting of hydrogen, NO2, amine, azide, halogen, triazole and C1-C8-alkyl group, X1, X2, X3 and X4 are selected from the group consisting of CH2 and S, Z is a heterocyclic moiety which is selected from the group consisting of imidazole, benzimidazole, benzothiazole, benzoxazole, purine, oxazole, triazole, pyrazole and thiazole, R1, R2 and R3 are selected from the group consisting -(CH2)nZ, hydrogen and C1-C8-alkyl group, n being an integer comprised between 1 and 4. They exhibit high cytotoxicity against cancer cells.

公开(公告)号：EP2608671B1

公开(公告)日：2018-12-12

申请号：EP11820603.6

申请日：2011-08-24

申请人： Gtx, Inc. ,  University of Tennessee Research Foundation

发明人： DALTON, James, T. ,  MILLER, Duane, D. ,  LI, Chien-Ming ,  AHN, Sunjoo ,  LU, Yan ,  WANG, Zhao ,  CHEN, Jianjun ,  LI, Wei ,  DUKE, Charles

IPC分类号： A61K31/415 ,  C07D233/60 ,  C07D403/04 ,  C07D417/12 ,  C07D417/14 ,  C07D263/32 ,  C07D277/24 ,  C07D277/42 ,  A61P35/00 ,  C07D403/12 ,  C07D417/04

CPC分类号： A61K31/415 ,  C07D233/60 ,  C07D263/32 ,  C07D277/24 ,  C07D277/42 ,  C07D403/04 ,  C07D403/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

公开(公告)号：EP3055314B1

公开(公告)日：2018-09-12

申请号：EP14790899.0

申请日：2014-10-06

申请人： Merck Sharp & Dohme Corp.

发明人： STACHEL, Shawn ,  PAONE, Daniel V. ,  LI, Jing ,  NANDA, Kausik

IPC分类号： C07D495/08 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/14 ,  C07D263/34 ,  C07D513/08 ,  A61P19/10 ,  A61K31/5377 ,  A61K31/547 ,  A61K31/541 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/496

CPC分类号： C07F7/0807 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/547 ,  A61K31/695 ,  A61K45/06 ,  C07D263/32 ,  C07D263/34 ,  C07D277/30 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/14 ,  C07D495/08 ,  C07D513/08

摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

公开(公告)号：EP2743256B1

公开(公告)日：2018-06-27

申请号：EP12821416

申请日：2012-08-08

申请人： TAKEDA PHARMACEUTICALS CO

发明人： TOMITA NAOKI ,  KAJII SHIGEO ,  CARY DOUGLAS ROBERT ,  TOMITA DAISUKE ,  IMAMURA SHINICHI ,  TSUCHIDA KEN ,  MATSUDA SATORU ,  HARA RYUJIRO

IPC分类号： C07C233/80 ,  A61K31/167 ,  A61K31/36 ,  A61K31/366 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/428 ,  A61K31/429 ,  A61K31/433 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4453 ,  A61K31/4468 ,  A61K31/451

CPC分类号： C07C233/80 ,  A61K31/167 ,  A61K31/36 ,  A61K31/366 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/428 ,  A61K31/429 ,  A61K31/433 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4453 ,  A61K31/4468 ,  A61K31/451 ,  A61K31/495 ,  A61K31/55 ,  C07C235/56 ,  C07C237/40 ,  C07C237/42 ,  C07C271/20 ,  C07C271/22 ,  C07C2601/02 ,  C07C2601/18 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/337 ,  C07D209/08 ,  C07D209/42 ,  C07D209/46 ,  C07D209/48 ,  C07D211/40 ,  C07D211/56 ,  C07D211/58 ,  C07D211/76 ,  C07D211/98 ,  C07D213/04 ,  C07D213/38 ,  C07D213/56 ,  C07D223/16 ,  C07D231/14 ,  C07D231/20 ,  C07D231/22 ,  C07D231/26 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D239/36 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D263/34 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D277/62 ,  C07D285/06 ,  C07D295/135 ,  C07D295/14 ,  C07D295/155 ,  C07D309/14 ,  C07D317/58 ,  C07D333/20 ,  C07D335/02 ,  C07D405/04 ,  C07D409/04 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula wherein A is a hydrocarbon group or heterocyclic group optionally having substituent(s); R is H, a hydrocarbon group or heterocyclic group optionally having substituent(s); A and R are optionally bonded to each other to form a ring optionally having substituent(s); Q 1 , Q 2 , Q 3 and Q 4 are each a hydrogen atom or a substituent; Q 1 and Q 2 , and Q 3 and Q 4 , are each optionally bonded to each other to form a ring optionally having substituent(s); X is H, an acyclic hydrocarbon group or saturated cyclic group optionally having substituent(s); Y 1 , Y 2 and Y 3 are each H, a hydrocarbon group or heterocyclic group optionally having substituent(s); X and Y 1 , and Y 1 and Y 2 , are each optionally bonded to each other to form a ring optionally having substituent(s); and Z 1 , Z 2 and Z 3 are each H or a substituent, or a salt thereof.

公开(公告)号：EP3201174A4

公开(公告)日：2018-06-06

申请号：EP15847016

申请日：2015-10-02

申请人： THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING / MCGILL UNIV

发明人： WU JIAN HUI ,  TIAN XIAOHONG ,  LIU WEIGUO

IPC分类号： C07C275/40 ,  A61K31/17 ,  A61K31/341 ,  A61K31/36 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5375 ,  A61P35/00 ,  C07D209/08 ,  C07D213/75

CPC分类号： A61K31/17 ,  A61K31/192 ,  A61K31/277 ,  A61K31/341 ,  A61K31/36 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5375 ,  A61K45/06 ,  C07C275/24 ,  C07C275/30 ,  C07C275/34 ,  C07C275/40 ,  C07C275/42 ,  C07D209/08 ,  C07D213/75 ,  C07D215/38 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D263/32 ,  C07D263/48 ,  C07D295/104 ,  C07D295/135 ,  C07D307/52 ,  C07D317/66 ,  C07D333/20 ,  C07D401/12 ,  C07D413/12 ,  A61K2300/00

摘要： Urea-based and bis-urea based compounds and analogues thereof are disclosed. These compounds are useful in the treatment of androgen-dependent diseases or disorders and androgen receptor-mediated diseases or disorders. Specifically, the compounds are useful in the treatment of diseases or disorders that are AR negative.

公开(公告)号：EP3325473A1

公开(公告)日：2018-05-30

申请号：EP16826974.4

申请日：2016-07-22

申请人： The Royal Institution for the Advancement of Learning / McGill University

发明人： WU, Jian Hui ,  TIAN, Xiaohong ,  YI, Qianhui

IPC分类号： C07D413/06 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/451 ,  A61K31/454 ,  A61P35/00 ,  C07D211/16 ,  C07D211/42 ,  C07D211/52 ,  C07D233/64 ,  C07D263/32 ,  C07D295/192 ,  C07D307/68 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14

CPC分类号： C07D413/04 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/422 ,  A61K31/451 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/42 ,  C07D211/44 ,  C07D211/52 ,  C07D233/64 ,  C07D263/32 ,  C07D295/192 ,  C07D307/68 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14

摘要： There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders.

公开(公告)号：EP2794556B1

公开(公告)日：2018-04-18

申请号：EP12860412.1

申请日：2012-12-20

申请人： Gleason, James L. ,  White, John H. ,  Kaldre, Dainis ,  Fischer, Joshua

发明人： Gleason, James L. ,  White, John H. ,  Kaldre, Dainis ,  Fischer, Joshua

IPC分类号： C07C259/06 ,  A61K31/16 ,  A61K31/381 ,  A61K31/404 ,  A61K31/421 ,  A61P35/00 ,  C07D209/18 ,  C07D263/32 ,  C07D333/06 ,  C07D333/16 ,  C07D333/24 ,  C07D209/12

CPC分类号： C07C259/06 ,  C07D209/12 ,  C07D209/18 ,  C07D263/32 ,  C07D333/16 ,  C07D333/24

摘要： The present disclosure relates to novel compounds having vitamin D receptor agonist and histone deacetylase inhibitory efficacy as well as methods for reducing or inhibiting the proliferation of cancer cells or for treating cancer.

公开(公告)号：EP3284738A1

公开(公告)日：2018-02-21

申请号：EP16779633.3

申请日：2016-04-15

申请人： Shanghai Institute Of Materia Medica Chinese Academy of Sciences

发明人： LIU, Hong ,  ZHOU, Yu ,  ZHANG, Dong ,  LI, Jian ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D213/56 ,  C07D401/12 ,  C07D277/30 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D417/06 ,  C07D213/82 ,  C07D213/75 ,  C07D239/26

CPC分类号： C07D487/04 ,  C07D213/56 ,  C07D213/75 ,  C07D213/82 ,  C07D231/56 ,  C07D239/26 ,  C07D261/08 ,  C07D263/32 ,  C07D277/30 ,  C07D277/32 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D491/10

摘要： The present invention relates to the fields of pharmaceutical chemistry and drug therapy, and particularly relates to a compound of formula I, and a preparation method and use thereof as a negative allosteric modulator of a metabotropic glutamate receptor (mG1uR) subtype 5.

摘要翻译： 本发明涉及药物化学和药物治疗领域，具体涉及作为代谢型谷氨酸受体（mG1uR）亚型5的负变构调节剂的式I化合物及其制备方法和用途。

公开(公告)号：EP2498611B1

公开(公告)日：2018-01-10

申请号：EP10830877.6

申请日：2010-11-15

申请人： Celgene International II Sàrl

发明人： MARTINBOROUGH, Esther ,  BOEHM, Marcus, F. ,  YEAGER, Adam, Richard ,  TAMIYA, Junko ,  HUANG, Liming ,  BRAHMACHARY, Enugurthi ,  MOORJANI, Manisha

IPC分类号： A01N43/82 ,  A61K31/41

CPC分类号： C07D271/06 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D263/32 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12

摘要： Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

公开(公告)号：EP2882724B1

公开(公告)日：2017-11-01

申请号：EP13745671.1

申请日：2013-08-07

申请人： IRBM - Science Park S.p.A. ,  C.N.C.C.S. Scarl Collezione Nazionale Dei Composti Chimici e Centro Screening

发明人： ALTAMURA, Sergio ,  BRESCIANI, Alberto ,  BREVEGLIERI, Giulia ,  FABBRINI, Danilo ,  GAMBARI, Roberto ,  HARPER, Steven ,  LAUFER, Ralph ,  MONTEAGUDO, Edith ,  NIZI, Emanuela ,  PACE, Paola ,  SUMMA, Vincenzo

IPC分类号： C07D263/32 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/421 ,  A61P35/00 ,  A61P7/00

CPC分类号： C07D263/32 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14