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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
161 Antibacterial agents EP10179798.3 2004-01-08 EP2295402A3 2011-08-03 Andersen, Neils H.; Bowman, Jason; Erwin, Alice; Harwood, Eric; Kline, Toni; Mdluli, Khisimuzi; Ng, Simon; Pfister, Keith B.; Shawar, Ribhi; Wagman, Allan; Yabannavar, Asha

Antibacterial compounds of formula (I) are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

162 ANTI-VIRAL COMPOUNDS TO TREAT HCV INFECTION EP10724656.3 2010-06-10 EP2337781A2 2011-06-29 RANDOLPH, John T.; DEGOEY, David A.; KATI, Warren M.; HUTCHINS, Charles W.; DONNER, Pamela L.; KRUEGER, Allan C.; MOTTER, Christopher E.; NELSON, Lissa T.; PATEL, Sachin V.; MATULENKO, Mark A.; KEDDY, Ryan G.; JINKERSON, Tammie K.; SOLTWEDEL, Todd N.; HUTCHINSON, Douglas K.; FLENTGE, Charles A.; WAGNER, Rolf; MARING, Clarence J.; TUFANO, Michael D.; BETEBENNER, David A.; ROCKWAY, Todd W.; LIU, Dachun; PRATT, John K.; LAVIN, Michael J.; SARRIS, Kathy; WOLLER, Kevin R.; WAGAW, Seble H.; CALIFANO, Jean C.; LI, Wenke; CASPI, Daniel.D.; BELLIZZI, Mary, E.
Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
163 ANTIBACTERIAL AGENTS EP04700887 2004-01-08 EP1618087A4 2007-01-31 ANDERSON NIELS H; BOWMAN JASON; ERWIN ALICE; HARWOOD ERIC; KLINE TONI; MDLULI KHISIMUZI; NG SIMON; PFISTER KEITH B; SHAWAR RIBHI; WAGMAN ALLAN; YABANNAVAR ASHA
164 Verfahren zur Herstellung von optisch aktivem 3-Chinuclidinol EP96120280.1 1996-12-17 EP0785198A1 1997-07-23 Brieden, Walter Dr.

Optisch aktives 3-Chinuclidinol wird durch asymmetrische Hydrierung von 3-Chinuclidinon, dessen Lewis-Säure-Addukten oder dessen tertiären oder quartären Salzen wie beispielsweise 1-(Diphenylmethyl)-3-oxochinuclidiniumbromid erhalten. Als Katalysatoren werden vorzugsweise Rhodiumkomplexe mit chiralen Diphosphinen mit Metallocenstruktur eingesetzt. Das optisch aktive 3-Chinuclidinol ist ein Synthesebaustein für pharmazeutische Wirkstoffe (M1-Rezeptor-Agonisten).

165 PHENYLETHYLPYRIDINE DERIVATIVES AS PDE4-INHIBITORS AND MUSCARINIC RECEPTOR ANTAGONISTS EP13811821.1 2013-12-04 EP2928879B1 2018-02-28 AMARI, Gabriele; ARMANI, Elisabetta; RICCABONI, Mauro; BAKER-GLENN, Charles
Compounds of formula (I) defined herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of a disease of the respiratory tract characterized by airway obstruction.
166 PHENYLETHYLPYRIDINE DERIVATIVES AS PDE4-INHIBITORS AND MUSCARINIC RECEPTOR ANTAGONISTS EP13811823.7 2013-12-04 EP2928883B1 2018-02-14 AMARI, Gabriele; ARMANI, Elisabetta; RICCABONI, Mauro; BAKER-GLENN, Charles
Compounds of formula (I) described herein are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
167 PHENYLETHYLPYRIDINE DERIVATIVES AS PDE4-INHIBITORS AND MUSCARINIC RECEPTOR ANTAGONISTS EP13811822.9 2013-12-04 EP2928880B1 2018-02-14 AMARI, Gabriele; ARMANI, Elisabetta; RICCABONI, Mauro; RIZZI, Andrea; BAKER-GLENN, Charles; BLACKABY, Wesley; VAN DE PÖEL, Hervé; WHITTAKER, Ben
Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of diseases of the respiratory tract characterized by airway obstruction.
168 3,5-DICHLORO,4-(3,4-(CYCLO-)ALKOXYPHENYL)- 2-CARBONYLOXY)ETHYL)PYRIDINE DERIVATIVES AS PDE-4 INHIBITORS EP14731175.7 2014-06-04 EP3152203A1 2017-04-12 AMARI, Gabriele; ARMANI, Elisabetta; RICCABONI, Mauro; BAKER-GLENN, Charles
The invention relates to novel 3,5-dichloro,4-(3,4-(cyclo-) alkoxyphenyl)-2-carbonyloxy)ethyl)pyridine compounds which are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
169 BENZOPYRROLIDONE DERIVATIVES POSSESSING ANTIVIRAL AND ANTICANCER PROPERTIES EP15155298.1 2015-02-16 EP3056202A1 2016-08-17 Kéri, György; Örfi, László; Horváth, Zoltán; Szokol, Bálint; Dobos, Judit; Nemes, Zoltán; Szàntay Kis, Csaba; Erös, Dánilel; Breza, Nóra; Baska, Ferenc; Karlas, Alexander; Gödert, Sigrid; Meyer, Thomas F.

The present invention relates to benzopyrrolidone derivatives and/or pharmaceutically acceptable salts thereof for the use in the treatment of infectious diseases or cancer, and pharmaceutical compositions containing at least one of said benzopyrrolidone derivatives and/or pharmaceutically acceptable salts thereof for the use in the treatment of infectious diseases or cancer.

170 Antibacterial agents EP10179798.3 2004-01-08 EP2295402B1 2015-08-12 Andersen, Niels H.; Bowman, Jason; Erwin, Alice; Harwood, Eric; Kline, Toni; Mdluli, Khisimuzi; Ng, Simon; Pfister, Keith B.; Shawar, Ribhi; Wagman, Allan; Yabannavar, Asha
171 GLUCOSYLCERAMIDE SYNTHASE INHIBITORS EP12760259 2012-03-16 EP2685986A4 2015-03-04 BOURQUE ELYSE; CELATKA CASSANDRA; HIRTH BRADFORD; METZ MARKUS; ZHAO ZHONG; SKERLJ RENATO; XIANG YIBIN; JANCISICS KATHERINE; MARSHALL JOHN; CHENG SENG; SCHEULE RONALD; CABRERA-SALAZAR MARIO; GOOD ANDREW
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
172 COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE EP12772843.4 2012-09-21 EP2758395A1 2014-07-30 EVERITT, Simon; KNEGTEL, Ronald; MORTIMORE, Michael; Rutherford, Alistair
The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
173 Anti-viral compounds EP13191049.9 2011-10-12 EP2692726A1 2014-02-05 Degoey, David A.; Kati, Warren M.; Hutchins, Charles W.; Donner, Pamela L; Krueger, Allan C.; Randolph, John T.; Motter, Christopher E.; Nelson, Lissa T.; Patel, Sachel V.; Matulenko, Mark A.; Keddy, Ryan G.; Jinkerson, Tammie K.; Gao, Yi; Liu, Dachun; Pratt, John K.; Rockway, Todd W.; Maring, Clarence J.; Hutchinson, Douglas K.; Flentge, Charles A.; Wagner, Rolf; Tufano, Michael D.; Betebenner, David A.; Sarris, Kathy; Woller, Kevin R.; Wagaw, Sebel H.; Califano, Jean C.; Li, Wenke; Caspi, Daniel D.; Bellizzi, Mary E.; Carroll, William A.

Compounds effective in inhibiting replication of Hepatitis C virus (HCV) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

174 Trisubstituted heterocycles as replication inhibitors of hepatitis C virus HCV EP13167828.6 2010-06-10 EP2628481A1 2013-08-21 Randolph, John T.; Degoey, David A.; Kati, Warren M.; Hutchins, Charles W.; Donner, Pamela L.; Krueger Allan C.; Motter, Christopher E.; Nelson, Lissa T.; Patel, Sachin V.; Matulenko, Mark A.; Keddy, Ryan G.; Jinkerson, Tammie K.; Hutchinson Douglas K.; Flentge, Charles A.; Wagner, Rolf; Maring, Clarence J.; Tufano, Michael D.; Betebenner, David A.; Rockway, Todd W.; Liu, Dachun; Pratt, John K.; Sarris, Kathy; Woller, Kevin R.; Wagaw, Seble H.; Califano, Jean C.; Li, Wenke; Caspi, Daniel.D.; Bellizzi, Mary, E.; Gao, Yi

Compounds effective in inhibiting replication of Hepatitis C virus ("HCV") are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

175 ANTIBACTERIAL AGENTS EP04700887.5 2004-01-08 EP1618087B1 2012-06-13 ANDERSON, Niels H.; BOWMAN, Jason; ERWIN, Alice; HARWOOD, Eric; KLINE, Toni; MDLULI, Khisimuzi; NG, Simon; PFISTER, Keith B.; SHAWAR, Ribhi; WAGMAN, Allan; YABANNAVAR, Asha
Antibacterial compounds of formula (I) are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
176 Antibacterial agents EP10179798.3 2004-01-08 EP2295402A2 2011-03-16 Andersen, Neils H.; Bowman, Jason; Erwin, Alice; Harwood, Eric; Kline, Toni; Mdluli, Khisimuzi; Ng, Simon; Pfister, Keith B.; Shawar, Ribhi; Wagman, Allan; Yabannavar, Asha

Antibacterial compounds of formula (I) are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

177 NOUVEAUX DERIVES DE CARBAZOLE INHIBITEURS D' HSP90, COMPOSITIONS LES CONTENANT ET UTILISATION EP09728587.8 2009-03-13 EP2265598A2 2010-12-29 ALASIA, Marcel; BERTIN, Luc; CERTAL, Victor; HALLEY, Frank; MAILLIET, Patrick; MENDEZ PEREZ, Maria; MINOUX, Hervé; RUXER, Jean-Marie
The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R'1; R is selected from the group comprising Formula (II) with R1 and/or R'1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkythio, or carboxy that is free or esterified by an alkyl, carboxamide, CO-NH(alkyl), CON(alkyl)2, NH-CO-alkyl, sulfonamide, NH-SO2-alkyl, S(O)2-NHalkyl, or S(O2)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is O, S, NR2, C(O), S(O), or S(O)2; Z is optionally substituted H, HaI, -O-R2 or –NH-R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.
178 A METHOD FOR THE PREPARATION OF SOLIFENACIN EP07855994.5 2007-12-21 EP2094693A2 2009-09-02 JIRMAN, Josef; JUNEK, Richard
A method of preparing (lS)-(3R)-l-azabicyclo[2.2.2]oct-3-yl 3,4-dihydro-l-phenyl-2(lH)- isoquinoline carboxylate (solifenacin) or its pharmaceutically acceptable salts with high optic purity, wherein the crude solifenacin base is transformed to the hydrogen tartrate, which is then optionally transformed to another pharmaceutically acceptable salt or the base of solifenacin. A crystalline salt of solifenacin hydrogen tartrate.
179 PYRIDONE/HYDROXYPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS EP07812540.8 2007-07-02 EP2046753A2 2009-04-15 ROBL, Jeffrey A.; WU, Shung C.; YOON, David S.
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure formula (I) enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.
180 Nouveaux dérivés peptidiques, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent EP90401877.7 1990-06-29 EP0406119B1 1994-01-19 Vincent, Michel; Remond, Georges; Portevin, Bernard; Hervé, Yolande; Lepagnol, Jean; Biton, Catherine
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