公开(公告)号：EP1874755A2

公开(公告)日：2008-01-09

申请号：EP06750201.3

申请日：2006-04-14

申请人： Merck & Co., Inc.

发明人： HUBBS, Jed Lee ,  KATTAR, Sam ,  METHOT, Joey ,  MILLER, Thomas ,  SILIPHAIVANH, Phieng ,  STANTON, Matthew ,  WILSON, Kevin ,  WITTER, David, J.

IPC分类号： C07D333/56 ,  C07D271/10 ,  A61K31/38 ,  A61K31/41

CPC分类号： C07D333/70 ,  A61K31/38 ,  A61K31/381 ,  A61K31/41

摘要： The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

公开(公告)号：EP1863787A1

公开(公告)日：2007-12-12

申请号：EP06727679.0

申请日：2006-03-20

申请人： Actelion Pharmaceuticals Ltd.

发明人： BOLLI, Martin ,  LEHMANN, David ,  MATHYS, Boris ,  MUELLER, Claus ,  NAYLER, Oliver ,  VELKER, Jörg ,  WELLER, Thomas

IPC分类号： C07D333/72 ,  C07D333/78 ,  C07D413/04 ,  C07D409/12 ,  C07D413/14 ,  A61K31/38 ,  A61K31/41 ,  A61P37/00

CPC分类号： C07D409/12 ,  C07D333/72 ,  C07D333/78 ,  C07D413/04 ,  C07D413/14

摘要： The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.

公开(公告)号：EP1863782A1

公开(公告)日：2007-12-12

申请号：EP06839054.1

申请日：2006-12-05

申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD.

发明人： INI, Sanriago ,  PLOUTNO, Alexei ,  LIBERMAN, Anita ,  ABROMOV, Mili ,  BEREZOVSKY, Dina ,  PORTER-KLERKS, Osnat

IPC分类号： C07D307/52 ,  A61K31/38 ,  A61P13/00 ,  A61P25/24 ,  A61P29/00

CPC分类号： C07D333/20

摘要： The invention encompasses 2-(N-methyl-propanamine)-3-(2-naphthol) thiophene, a duloxetine hydrochloride impurity, as well as its use as a reference marker and reference standard.

公开(公告)号：EP1758879B1

公开(公告)日：2007-12-12

申请号：EP05793945.6

申请日：2005-10-21

申请人： Zentiva, a.s.

发明人： RIDVAN, Ludek ,  HRUBY, Petr ,  PLACEK, Lukas ,  KUCHAR, Miroslav

IPC分类号： C07D333/20 ,  A61K31/38

CPC分类号： C07D333/20

摘要： A method of preparation of (S)-N-methyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (I) or its pharmaceutically acceptable salt, in which (RS)-N,N-dimethyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (III) is reacted with an optically active acid, after which a crystallization is made of that diastereoisomer which yields, by reaction with an inorganic or organic base, (S)-N,N-dimethyl-3-(l-naphthyloxy)-3-(2-thienyl)propylamine of formula (S)-III, which is then demethylated using alkylchloroformates, followed by a hydrolysis and optional conversion of the compound of formula (I) to its salt.

公开(公告)号：EP1846415A1

公开(公告)日：2007-10-24

申请号：EP06704282.0

申请日：2006-01-25

申请人： JANSSEN PHARMACEUTICA N.V.

发明人： CID-NÚÑEZ, José, Maria ,  MEGENS, Antonius, Adrianus, Hendrikus, Petrus ,  TRABANCO-SUÁREZ, Andrés, Avelino

IPC分类号： C07D495/14 ,  C07D495/04 ,  C07D491/14 ,  A61K31/55 ,  A61K31/381 ,  A61K31/38 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  A61P3/04

CPC分类号： C07D495/04 ,  C07D491/14 ,  C07D495/14

摘要： This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivat ives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5- HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) , and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

公开(公告)号：EP1831227A2

公开(公告)日：2007-09-12

申请号：EP05826587.7

申请日：2005-12-15

申请人： Glenmark Pharmaceuticals S.A.

发明人： GHARAT, Laxmikant Atmaram, Parvati Apt., A-2 ,  GOPALAN, Balasubramanian, Flat No. 54 Block B-3 ,  KHAIRATKAR-JOSHI, Neelima C101, Dev. Prayag Co-op.H.S

IPC分类号： C07D491/04 ,  C07D471/04 ,  C07D495/04 ,  A61K31/343 ,  A61K31/38 ,  A61K31/407 ,  A61P29/00

CPC分类号： C07D491/048 ,  A61K31/4355 ,  A61K31/5025 ,  C07D471/04 ,  C07D495/04

摘要： The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjuctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome.

公开(公告)号：EP1748046A3

公开(公告)日：2007-08-22

申请号：EP06011600.1

申请日：2000-11-22

申请人： Methylgene, Inc.

发明人： Delorme, Daniel ,  Ruel, Rejean ,  Lavoie, Rico ,  Thibault, Carl ,  Abou-Khalil, Elie

IPC分类号： C07D333/38 ,  C07C311/21 ,  C07D333/62 ,  C07C259/10 ,  C07C321/28 ,  C07D285/135 ,  A61K31/38 ,  A61K31/18 ,  A61K31/165 ,  A61K31/41

CPC分类号： C07D213/76 ,  C07C259/06 ,  C07C259/10 ,  C07C275/42 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07C317/44 ,  C07D213/71 ,  C07D215/36 ,  C07D285/135 ,  C07D307/46 ,  C07D307/54 ,  C07D307/91 ,  C07D333/34 ,  C07D333/62

摘要： The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

摘要翻译： 本发明涉及组蛋白脱乙酰酶的抑制。 本发明提供了用于抑制组蛋白脱乙酰酶酶活性的化合物和方法。 本发明还提供了用于治疗细胞增殖性疾病和病症的组合物和方法。

公开(公告)号：EP1804786A2

公开(公告)日：2007-07-11

申请号：EP05802540.4

申请日：2005-09-29

申请人： Cytovia, Inc.

发明人： KEMNITZER, Wiliam, E. ,  CAI, Sui Xiong ,  DREWE, John, A. ,  SIRISOMA, Nilantha, Sudath

IPC分类号： A61K31/34 ,  A61K31/38 ,  A61K31/40 ,  A61K31/165

CPC分类号： C07D209/88 ,  A61K31/165 ,  A61K31/167 ,  A61K31/343 ,  A61K31/381 ,  A61K31/403

摘要： The present invention is directed to substituted N-aryl-9-oxo-9H-fluorene-1-carboxamides and analogs thereof, represented by the general Formula I: (I) wherein R1-R8, X and Ar are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

公开(公告)号：EP1442032B1

公开(公告)日：2007-04-18

申请号：EP02802300.0

申请日：2002-10-21

申请人： F. HOFFMANN-LA ROCHE AG

发明人： KLAUS, Michael ,  LAPIERRE, Jean-Marc

IPC分类号： C07D311/58 ,  C07D335/06 ,  C07D215/12 ,  C07D409/04 ,  C07D409/12 ,  A61K31/38 ,  A61P17/00

CPC分类号： C07D335/06 ,  C07D215/12 ,  C07D311/58 ,  C07D409/04 ,  C07D409/12

摘要： The current invention provides novel heterocyclic retinoid compounds of formula (I), wherein R1 to R5, A,B,Z and n are as defined in the description and claims. The compounds of the present invention are useful for the treatment and/or prevention of diseases such as chronic obstructive pulmonary disease, cancer and dermatological disorders.

公开(公告)号：EP1761485A1

公开(公告)日：2007-03-14

申请号：EP04776274.5

申请日：2004-06-04

申请人： Schering AG

发明人： PATTERSON, John, W. ,  Woo, Soon, H.

IPC分类号： C07C311/18 ,  C07C311/54 ,  A61K31/41 ,  A61K31/18 ,  A61K31/38 ,  A61P29/02 ,  A61P25/28 ,  A61P37/02 ,  A61P35/00 ,  A61P9/10 ,  C07D263/56 ,  C07D335/02 ,  A61P17/06

CPC分类号： C07D335/02 ,  C07C311/51 ,  C07C317/50 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/54 ,  C07D263/56 ,  C07D271/06 ,  C07D271/10 ,  C07D417/12

摘要： The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

摘要翻译： 本发明涉及半胱氨酸蛋白酶，特别是组织蛋白酶B，K，L，F和S的抑制剂的化合物，因此可用于治疗由这些蛋白酶介导的疾病。 本发明涉及包含这些化合物的药物组合物及其制备方法。