公开(公告)号：EP3174853B1

公开(公告)日：2018-12-12

申请号：EP15742253.6

申请日：2015-07-27

申请人： F. Hoffmann-La Roche AG

发明人： CECERE, Giuseppe ,  GALLEY, Guido ,  GOERGLER, Annick ,  NORCROSS, Roger ,  PFLIEGER, Philippe ,  TIRLA, Alina ,  SCHMID, Philipp

IPC分类号： C07D213/81 ,  C07D311/04 ,  C07D231/14 ,  C07D239/28 ,  C07D413/12 ,  C07D261/20 ,  C07C233/80 ,  A61K31/435 ,  A61K31/415 ,  A61K31/505 ,  A61K31/167 ,  A61P25/00 ,  C07D213/73 ,  C07D213/74 ,  C07C255/58 ,  C07C255/60 ,  C07D213/82 ,  C07C211/60 ,  C07D405/04

CPC分类号： C07D417/12 ,  C07C209/78 ,  C07C211/60 ,  C07C217/92 ,  C07C231/12 ,  C07C233/80 ,  C07C237/48 ,  C07C255/42 ,  C07C255/58 ,  C07C255/60 ,  C07C273/1854 ,  C07C275/40 ,  C07C275/42 ,  C07C303/40 ,  C07C311/21 ,  C07C2601/02 ,  C07C2602/10 ,  C07D213/40 ,  C07D213/61 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D231/20 ,  C07D239/28 ,  C07D239/42 ,  C07D241/20 ,  C07D261/18 ,  C07D311/58 ,  C07D405/04 ,  C07D405/12 ,  C07D409/14

摘要： The present invention relates to a compound of formula (I), wherein L is –C(O)NH-, -NHC(O)-, -S(O)2NH-, -NH- or -NHC(O)NH-; Ar is phenyl, benzyl, naphthyl or heteroaryl, selected from the group consisting of pyridinyl, pyrazolyl, pyrimidinyl, isoxazolyl or pyrazinyl, wherein Ar may be optionally substituted by one, two or three R1; R1 is hydrogen, lower alkyl, lower alkoxy, halogen, cyano, cycloalkyl, NHC(O)-lower alkyl, lower alkoxy substituted by halogen, lower alkyl substituted by halogen, or is phenyl optionally substituted by one or two halogen atoms, CF3O or lower alkyl, or is furanyl, thiazolyl or thiophenyl, optionally substituted by halogen or lower alkyl; X is CH or O; R is hydrogen or halogen; or a pharmaceutically suitable acid addition salt thereof, all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.

公开(公告)号：EP2120963B1

公开(公告)日：2018-09-12

申请号：EP07870927.6

申请日：2007-12-21

申请人： Paratek Pharmaceuticals, Inc.

发明人： ASSEFA, Haregewein ,  BHATIA, Beena ,  DRAPER, Michael ,  HONEYMAN, Laura ,  MOLNAR, Dennis P. ,  KIM, Oak, K.

IPC分类号： A61K31/65 ,  A61P17/00 ,  A61P17/06 ,  A61P17/10 ,  A61P43/00 ,  C07C237/26

CPC分类号： C07C237/48 ,  A61K31/65 ,  C07C237/26 ,  C07C2603/46

摘要： Methods and compositions for the treatment of skin disorders (e.g., acne, rosacea) are described.

公开(公告)号：EP3328368A1

公开(公告)日：2018-06-06

申请号：EP16831462.3

申请日：2016-07-30

申请人： Taipei Medical University

发明人： YEN, Yun ,  LIOU, Jing-ping ,  PAN, Shiow-lin

IPC分类号： A61K31/122 ,  C07C50/12

CPC分类号： C07D207/04 ,  A61K31/122 ,  A61K31/166 ,  A61K31/40 ,  A61K31/7048 ,  A61K33/24 ,  A61K45/06 ,  A61P3/10 ,  A61P25/14 ,  A61P25/28 ,  A61P35/00 ,  C07C225/30 ,  C07C235/54 ,  C07C237/34 ,  C07C237/48 ,  C07C255/58 ,  C07C311/29 ,  C07C2602/10 ,  C07D209/08 ,  C07D209/44 ,  C07D213/40 ,  C07D215/38 ,  C07D215/40 ,  C07D295/13 ,  C07D295/135 ,  A61K2300/00

摘要： The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.

公开(公告)号：EP3250552A1

公开(公告)日：2017-12-06

申请号：EP16704983.2

申请日：2016-01-28

申请人： Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

发明人： ALBRECHT, Brian, K. ,  AUDIA, James, Edmund ,  COTE, Alexandre ,  DUPLESSIS, Martin ,  GEHLING, Victor, S. ,  GOOD, Andrew, Charles ,  HARMANGE, Jean-Christophe ,  LEBLANC, Yves ,  NASVESCHUK, Christopher, G. ,  TAYLOR, Alexander, M. ,  VASWANI, Rishi, G.

IPC分类号： C07D231/12 ,  C07D401/12 ,  C07C211/42 ,  C07D405/12 ,  C07D211/78 ,  C07D213/38 ,  A61K31/00 ,  A61P35/00

CPC分类号： C07C211/42 ,  A61K31/135 ,  A61K31/166 ,  A61K31/196 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/4747 ,  A61K31/495 ,  A61K31/517 ,  A61K45/06 ,  C07C217/74 ,  C07C229/50 ,  C07C237/48 ,  C07C255/58 ,  C07C317/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2603/94 ,  C07D205/04 ,  C07D205/12 ,  C07D207/06 ,  C07D211/26 ,  C07D211/46 ,  C07D211/78 ,  C07D213/38 ,  C07D215/08 ,  C07D231/12 ,  C07D295/185 ,  C07D305/08 ,  C07D309/04 ,  C07D401/12 ,  C07D405/12

摘要： and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.

公开(公告)号：EP2456759B1

公开(公告)日：2017-04-19

申请号：EP10732872.6

申请日：2010-07-10

申请人： Bayer CropScience AG

发明人： MIHARA, Jun ,  ARAKI, Koichi ,  MORI, Takuma ,  MURATA, Tetsuya ,  YONETA, Yasushi ,  SHIMOJO, Eiichi ,  ICHIHARA, Teruyuki ,  ATAKA, Masashi ,  SHIBUYA, Katsuhiko ,  GÖRGENS, Ulrich

IPC分类号： C07D215/48 ,  C07D215/60 ,  C07D277/68 ,  A01N43/42 ,  C07C233/67

CPC分类号： C07D215/48 ,  A01N37/34 ,  A01N43/42 ,  A01N43/78 ,  A01N43/82 ,  C07C211/52 ,  C07C217/84 ,  C07C233/66 ,  C07C237/48 ,  C07C255/57 ,  C07C2601/14 ,  C07D215/60 ,  C07D277/68

公开(公告)号：EP2040688B1

公开(公告)日：2014-04-02

申请号：EP07785841.3

申请日：2007-06-25

申请人： SANOFI

发明人： HACHTEL, Stephanie ,  DEDIO, Juergen ,  DEFOSSA, Elisabeth ,  GRUENEBERG, Sven ,  HEITSCH, Holger ,  BOCK, William ,  CHEN, Charlie ,  KOSLEY, Raymond ,  KUNG, Chung-Yi ,  PATEK, Marcel ,  SHER, Rosy ,  SHIMSHOCK, Stephen ,  WEICHSEL, Aleksandra

IPC分类号： C07C235/66 ,  C07C233/83 ,  C07C237/48 ,  C07C311/29 ,  C07D213/65 ,  C07D333/64 ,  C07D215/26 ,  C07D233/60 ,  C07D295/088 ,  C07D307/24 ,  C07D333/16

CPC分类号： C07D333/16 ,  C07C233/83 ,  C07C235/66 ,  C07C237/48 ,  C07C311/29 ,  C07C2601/04 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2602/08 ,  C07D213/65 ,  C07D215/26 ,  C07D233/60 ,  C07D295/088 ,  C07D307/24 ,  C07D333/64

公开(公告)号：EP2231589A2

公开(公告)日：2010-09-29

申请号：EP08859523.6

申请日：2008-12-10

申请人： Theravance, Inc.

发明人： LEADBETTER, Michael R. ,  TRAPP, Sean G. ,  LONG, Daniel D. ,  JACOBSEN, John R. ,  AXT, Sabine

IPC分类号： C07C229/28 ,  C07C229/34 ,  C07C237/06 ,  C07C237/14 ,  C07C237/20 ,  C07C237/48 ,  C07D295/185 ,  A61K31/165 ,  A61K31/166 ,  A61K31/197 ,  A61K31/216 ,  A61K31/45 ,  A61K31/495 ,  A61P1/00

CPC分类号： C07C237/48 ,  A61K9/0019 ,  A61K9/0075 ,  A61K9/10 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/12 ,  A61K47/14 ,  A61K47/26 ,  C07C229/28 ,  C07C229/34 ,  C07C237/06 ,  C07C237/14 ,  C07C237/20 ,  C07C2601/14 ,  C07C2602/10 ,  C07D295/185

摘要： The invention provides aminotetralin compounds of formula (I): (I) wherein R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

公开(公告)号：EP1285651B1

公开(公告)日：2010-09-01

申请号：EP01925947.2

申请日：2001-04-26

申请人： Takeda Pharmaceutical Company Limited

发明人： ISHIHARA, Yuji ,  SUZUKI, Nobuhiro ,  TAKEKAWA, Shiro

IPC分类号： A61K31/167 ,  A61K31/40 ,  A61K31/4453 ,  A61K31/4709 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4725 ,  C07C233/80 ,  C07C237/48 ,  C07D211/16 ,  C07D211/14 ,  C07D211/18 ,  C07D295/135 ,  C07D405/12 ,  C07D401/06 ,  C07D417/06 ,  C07D401/12 ,  C07D211/22 ,  C07D471/04

CPC分类号： C07D295/096 ,  C07C233/80 ,  C07C235/66 ,  C07C237/48 ,  C07C271/30 ,  C07D207/06 ,  C07D209/12 ,  C07D215/38 ,  C07D295/135 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06 ,  C07D471/04

摘要： Melanin concentrating hormone antagonists containing compounds of the general formula (I) or salts thereof are useful as preventive or therapeutic drugs for obesity and so on wherein Ar1 is an optionally substituted cyclic group; X and Y are each independently a spacer having a C¿1-6? main chain; Ar is an optionally substituted fused polycyclic aromatic ring; R?1 and R2¿ are each independently hydrogen or an optionally substituted hydrocarbon group, or alternatively R?1 and R2¿ together with the nitrogen atom adjacent thereto may form a nitrogenous heterocycle, or R2 together with the nitrogen atom adjacent thereto and Y may form an optionally substituted nitrogenous heterocycle, or R2 together with the nitrogen atom adjacent thereto, Y, and Ar may form a fused ring.

公开(公告)号：EP1868985A4

公开(公告)日：2010-05-05

申请号：EP06739372

申请日：2006-03-24

申请人： MERCK SHARP & DOHME

发明人： LIANG RUI ,  PARMEE EMMA R

IPC分类号： C07C229/34 ,  A61K31/195 ,  A61K31/35 ,  A61K31/41 ,  C07D257/06 ,  C07D311/74

CPC分类号： C07C323/44 ,  C07C237/48 ,  C07C275/30 ,  C07C275/34 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D257/06 ,  C07D311/68 ,  C07D317/60 ,  C07D319/08 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12

公开(公告)号：EP1846375A1

公开(公告)日：2007-10-24

申请号：EP05820407.4

申请日：2005-12-21

申请人： GLAXO GROUP LIMITED

发明人： BOZZOLI, Andrea, GlaxoSmithKline SpA ,  BRANCH, Clive Leslie, GlaxoSmithKline ,  MACRITCHIE, Jacqueline A., BioFocus Discovery Ltd ,  MARSHALL, Howard Robert, GlaxoSmithKline ,  PORTER, Roderick Alan, GlaxoSmithKline ,  SPADA, Simone, GlaxoSmithKline SpA

IPC分类号： C07D215/48 ,  C07C233/80 ,  A61K31/166 ,  A61K31/47 ,  C07D215/50 ,  A61P25/00

CPC分类号： C07C255/57 ,  C07C233/78 ,  C07C235/66 ,  C07C237/48 ,  C07C2601/08 ,  C07C2602/08 ,  C07D215/50 ,  C07D295/135 ,  C07D405/12

摘要： The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof. Formula (I) wherein R1 is a group selected from: Formulas (A), (B), (C)

摘要翻译： 本发明涉及式（I）化合物或其盐或溶剂化物，其在制备用于治疗神经病学和神经精神病学障碍，特别是精神病，痴呆或注意力缺陷障碍的药物中的用途。 本发明还包括制备这些化合物及其药物制剂的方法。 式（I）其中R 1是选自以下的基团：式（A），（B），（C）