Nitrogen Attached Directly Or Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/550)
-
Patent number: 7563912Abstract: The present invention relates to an improved process for the preparation of (S)-(?)-?-ethyl-2-oxo-1-pyrrolidine acetamide and analogues thereof. The invention also relates to compounds of the general formula (6) wherein R1 is methyl or ethyl; and R2 is C?2#191 -C?4#191 alkyl, C?2#191-C?4#191 alkenyl or C?2#191-C?4#191 alkynyl, optionally substituted by one or more halogen, and their preparation processes.Type: GrantFiled: July 18, 2006Date of Patent: July 21, 2009Assignee: UCB Pharma, S.A.Inventors: Celal Ates, John Surtees, Anne-Catherine Burteau, Violeta Marmon, Emile Cavoy
-
Patent number: 7560572Abstract: The present invention provides analogues of autoinducer molecules that are derivatized to allow their attachment to other molecules and surfaces. Libraries of the autoinducer analogues are also contemplated. Also provided are methods for using the compounds of the invention to produce compositions, such as immunoconjugates, antibodies and vaccines, which are useful for treating and preventing disease states in a subject. The compositions of the invention are also useful in various assays, including assessing the autoinducer load in a subject.Type: GrantFiled: January 13, 2004Date of Patent: July 14, 2009Assignee: K-Quay Enterprises, LLCInventor: Steven C. Quay
-
Patent number: 7550453Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.Type: GrantFiled: May 24, 2007Date of Patent: June 23, 2009Assignee: Aventis Pharma SAInventors: Jidong Zhang, Neerja Bhatnagar, Jean-Marie Ruxer
-
Publication number: 20090124668Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: ApplicationFiled: January 15, 2009Publication date: May 14, 2009Inventors: Percy H. Carter, Robert J. Cherney, Douglas G. Batt, John V. Duncia, Daniel S. Gardner, Soo S. Ko, Anurag S. Srivastava, Michael G. Yang
-
Patent number: 7531673Abstract: A process for making amino acid amides, comprising reacting an amino acid, or acid salt of an amino acid, with a halogenating agent, or with a substance that reacts with carboxylic acids to form a leaving group, to form an intermediate, then reacting the intermediate with ammonia. When the amino acid or acid salt is enantiomerically pure, the amide will be a stereoisomer. An amide made by the process can be used to form levetiracetam.Type: GrantFiled: February 16, 2005Date of Patent: May 12, 2009Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Palle V. R. Acharyulu, C. M. Haricharan Raju
-
Publication number: 20090118335Abstract: The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.Type: ApplicationFiled: March 30, 2007Publication date: May 7, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Atsushi Hasuoka, Terufumi Takagi, Masahiro Kajino, Haruyuki Nishida
-
Publication number: 20090082422Abstract: The present application describes deuterium-enriched levetiracetam, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
-
Patent number: 7501528Abstract: The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are as defined in the description and claims and to intermediates useful in the method of the invention as well as salts thereof.Type: GrantFiled: March 8, 2006Date of Patent: March 10, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Stefan Hildbrand, Bruno Lohri, Wolfgang Wostl
-
Patent number: 7485731Abstract: The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are as defined the description and claims and to intermediates and salts thereof useful in the method of the invention.Type: GrantFiled: March 8, 2006Date of Patent: February 3, 2009Assignee: Hoffmann-La Roche Inc.Inventor: Bruno Lohri
-
Patent number: 7482374Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.Type: GrantFiled: July 17, 2004Date of Patent: January 27, 2009Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Henry Anderson Kelly, Nigel Stephen Watson, Robert John Young
-
Publication number: 20090012313Abstract: The present invention relates to 3-carboxy-2-oxo-1-pyrrolidine derivatives of formula (I), geometrical isomers, enantiomers, diastereoisomers, pharmaceutically acceptable salts and all possible mixtures thereof, and processes using them.Type: ApplicationFiled: December 5, 2006Publication date: January 8, 2009Applicant: UCB PHARMA, S.A.Inventors: Celal Ates, Arnaud Schule
-
Publication number: 20080194840Abstract: Process for the preparation of (S)-(?)-?-ethyl-2-oxo-1-pyrrolidineacetamide of Formula (I), comprising the steps of (i) resolution of racemic 2-amino butynamide with L-(+)-tartaric acid either in alcoholic solvents like methanol, isopropanol, ethanol or in water or mixture of water-alcohol to provide (S)-(+)-2-amino butynamide tartarate salt; and ii) direct conversion of (S)-(+)-2-amino butynamide tartarate salt and 4-halobutryl chloride in presence of inorganic or organic base in suitable solvent and drying agents yielded the desired (S)-(?)-?-ethyl-2-oxo-1-pyrrolidineacetamide (I). Further (S)-(+)-2-amino butynamide tartarate salt is converted to (S)-(+)-2-amino butynamide hydrochloride salt, by reacting with an inorganic or organic base in a suitable solvent followed by reaction with HCl gas in an appropriate solvent.Type: ApplicationFiled: January 20, 2006Publication date: August 14, 2008Applicant: Rubamin Laboratories LimitedInventors: Arun Kanti Mandal, Satish Wasudeo Mahajan, Pintoo Ganguly, Apurba Chetia, Nitesh Dolatram Chauhan, Nilay Dilipkumar Bhatt, Reenaben Ratansing Baria
-
Patent number: 7396846Abstract: This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.Type: GrantFiled: March 31, 2003Date of Patent: July 8, 2008Assignee: Eli Lilly and CompanyInventors: Britta Evers, Ruehter Gerd, Eva Maria Martin De La Nava, Mark Joseph Tebbe
-
Publication number: 20080146819Abstract: Process for the preparation of (S)-(?)-?-ethyl-2-oxo-1-pyrrolidineacetamide of Formula (I) by the steps of condensation of (S)-2-amino butanol of Formula (II) and 4-halobutryl chloride, where halo group can be chloro, bromo or iodo in solvents to form ?-ethyl-2-oxo pyrrolidine ethanol of Formula (III); oxidation of (S)-?-ethyl-2-oxo pyrrolidine ethanol to yield (S)-?-ethyl-2-oxo pyrrolidine acetic acid having the formula (IV); esterification of (S)-?-ethyl-2-oxo pyrrolidine acetic acid (IV) with an alcohol to provide alkyl ester of Formula (V) wherein, R is 14 Carbon atom; ammonolysis of alkyl esters of formula (V) with ammonia to provide (S)-(?)—?-ethyl-2-oxo-1-pyrrolidine acetamide of formula (1).Type: ApplicationFiled: January 20, 2006Publication date: June 19, 2008Applicant: RUBAMIN LIMITEDInventors: Arun Kanti Mandal, Satish Wasudeo Mahajan, Madan Kumar Sharma, Apurba Chetia, Nitesh Dolatram Chauhan
-
Patent number: 7338975Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.Type: GrantFiled: February 11, 2004Date of Patent: March 4, 2008Assignee: Bristol-Myers Squibb Co.Inventors: Percy H. Carter, Matthew E. Voss
-
Publication number: 20080039517Abstract: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a combination thereof, wherein R1, R2, and X are as defined herein. Compounds of the present invention are useful as progesterone receptor modulators.Type: ApplicationFiled: August 7, 2007Publication date: February 14, 2008Inventors: David G. WASHBURN, Tram H. HOANG
-
Patent number: 7304088Abstract: This invention relates to treating an infection with a virus using protease inhibitors. Examples of the protease inhibitors include compounds of formula (I).Type: GrantFiled: December 29, 2004Date of Patent: December 4, 2007Assignee: TaiGen BiotechnologyInventors: Syaulan Yang, Jen-Dar Wu, Feng-Yih Su, Chun-Wei Kuo, Wen-Chang Chen, Yibin Xiang, Ching-Cheng Wang, Shao-Ying Liao
-
Patent number: 7291620Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: June 25, 2004Date of Patent: November 6, 2007Assignee: Merck + Co., Inc.Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca, Harold G. Selnick
-
Patent number: 7279582Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: October 25, 2002Date of Patent: October 9, 2007Assignee: Abbott LaboratoriesInventors: Eric J. Stoner, Arthur J. Cooper, Lawrence Kolaczkowski, Ketan M. Patel, Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Daniel A. Dickman, Patricia A. Oliver, Jien-Heh J. Tien
-
Patent number: 7235581Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, e.g. which are mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.Type: GrantFiled: September 18, 2003Date of Patent: June 26, 2007Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
-
Patent number: 7214803Abstract: The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.Type: GrantFiled: March 31, 2005Date of Patent: May 8, 2007Assignee: Eastman Chemical CompanyInventors: Neil Warren Boaz, Sheryl Davis Debenham
-
Patent number: 7199242Abstract: The invention provides a process for the production of a compound of formula (I): wherein P1 and P2, which may be the same or different, are amino protecting groups, which comprises protection of a compound of formula (II) in solution phase continuous operation mode. This confers advantages over batch mode operation. The process is usually conducted in reaction equipment adapted for use in continuous processing mode, for example comprising one or more static mixers or a plug flow reactor. Preferably, the plug flow reactor comprises a jacketed tubular reactor fitted inside with internal mixing elements which continually split and remix the reaction streams promoting mass and heat transfer, whereby a uniform plug flow profile with turbulent fluid flow is achieved. The invention also provides a process for production of the antibacterial compound gemifloxacin or a pharmaceutically acceptable salt and/or hydrate thereof, comprising converting a compound of formula (I).Type: GrantFiled: August 2, 2002Date of Patent: April 3, 2007Assignee: LG Life Sciences LimitedInventors: Clemens Michael Helmut Brechtelsbauer, Stephen Thomas Carpenter, Trevor John Grinter, Michael Anthony Harris, Yeongdae Kim, Youngwoon Kwon, Dongchul Lee, François Xavier Ricard, Richard Neville Saunders
-
Patent number: 7196113Abstract: The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: May 23, 2005Date of Patent: March 27, 2007Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills
-
Patent number: 7151111Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer's disease and senile dementia.Type: GrantFiled: September 18, 2003Date of Patent: December 19, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Hans Iding, Synese Jolidon, Daniela Krummenacher, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Beat Wirz, Wolfgang Wostl, Rene Wyler
-
Patent number: 7132552Abstract: The invention relates to a method of making optically and chemically pure levetiracetam and to the levetiracetam produced by such process.Type: GrantFiled: February 3, 2004Date of Patent: November 7, 2006Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Ben-Zion Dolitzky, Jean Hildesheim, Serguei Finogueev
-
Patent number: 7122682Abstract: The present invention relates to an improved process for the preparation of (S)-(?)-?-ethyl-2-oxo-1-pyrrolidine acetamide and analogues thereof.Type: GrantFiled: August 5, 2002Date of Patent: October 17, 2006Assignee: UCB, S.A.Inventors: Celal Ates, John Surtees, Anne-Catherine Burteau, Violeta Marmon, Emile Cavoy
-
Patent number: 7037935Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.Type: GrantFiled: September 18, 2003Date of Patent: May 2, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Hans Iding, Synese Jolidon, Daniela Krummenacher, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Beat Wirz, Wolfgang Wostl, Rene Wyler
-
Patent number: 7038061Abstract: A process for preparing an anhydrous benzoate salt in crystalline form having the formula I: and the corresponding benzoate monohydrate in crystalline form. The benzoate salts and pharmaceutical compositions thereof are selective kappa-receptor agonists, and are useful as analgesics, anesthetics, anti-inflammatory or neuroprotective agents, or in the treatment of arthritis, stroke or functional bowel disease.Type: GrantFiled: April 23, 2003Date of Patent: May 2, 2006Assignee: Pfizer IncInventors: George J. Quallich, Michael J. Castaldi
-
Patent number: 7001905Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: GrantFiled: March 12, 2001Date of Patent: February 21, 2006Assignee: Warner-Lambert CompanyInventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
-
Patent number: 6992103Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (?-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.Type: GrantFiled: November 29, 2002Date of Patent: January 31, 2006Assignee: SmithKline Beecham P.L.C.Inventors: Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Steven James Stanway, Leontine Saskia Trouw
-
Patent number: 6989384Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: July 23, 2003Date of Patent: January 24, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Ye Hua, Hiep The Luu, Fora P. Chan, Theodore O. Johnson, Jr., Siegfried Heinz Reich, Donald James Skalitzky, Yi Yang, Thomas F. Hendrickson, Shao Song Chu, Brian Walter Eastman
-
Patent number: 6977303Abstract: The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.Type: GrantFiled: November 25, 2003Date of Patent: December 20, 2005Assignee: Eastman Chemical CompanyInventors: Neil Warren Boaz, Sheryl Davis Debenham
-
Patent number: 6969770Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing ?-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particularly the invention concerns novel intermediates and their use in methods for the preparation of S-?-ethyl-2-oxo-1-pyrrolidine acetamide.Type: GrantFiled: April 15, 2004Date of Patent: November 29, 2005Assignee: U.C.B. Farchim S.A.Inventors: John Surtees, Violeta Marmon, Edmond Differding, Vincent Zimmermann
-
Patent number: 6965019Abstract: Mono- and Bis-Azo/Hydrazone Pyrrole Pigments and Methods for preparing same.Type: GrantFiled: April 3, 2001Date of Patent: November 15, 2005Assignee: Sun Chemical CorporationInventors: Terence Chamberlain, Norman W. Smith, Donald T. DeRussy
-
Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
-
Patent number: 6906097Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.Type: GrantFiled: April 9, 2003Date of Patent: June 14, 2005Assignee: Allergan, Inc.Inventors: David W. Old, Danny Thang Dinh, Robert M. Burk
-
Patent number: 6900213Abstract: The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.Type: GrantFiled: July 21, 2003Date of Patent: May 31, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
-
Patent number: 6897323Abstract: The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.Type: GrantFiled: November 25, 2003Date of Patent: May 24, 2005Assignee: Eastman Chemical CompanyInventors: Neil Warren Boaz, Sheryl Davis Debenham
-
Patent number: 6897233Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: March 1, 2002Date of Patent: May 24, 2005Assignee: SmithKline Beecham CorporationInventors: Jia-Ning Xiang, Siegfried B. Christensen, IV, Xiangmin Liao, Maxwell D. Cummings
-
Patent number: 6872745Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: May 12, 2003Date of Patent: March 29, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Theodore O. Johnson, Jr., Ye Hua, Hiep T. Luu, Peter S. Dragovich
-
Patent number: 6858740Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing ?-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particularly the invention concerns novel intermediates and their use in methods for the preparation of S-?-ethyl-2-oxo-1-pyrrolidine acetamide.Type: GrantFiled: July 1, 2003Date of Patent: February 22, 2005Assignee: UCB Farchim S.A.Inventors: John Surtees, Violeta Marmon, Edmond Differding, Vincent Zimmermann
-
Patent number: 6849657Abstract: This invention relates to 8-aza prostanoid analogs which are generally EP4 receptor agonists and are represented by Formula I: wherein Q, B, X, J, Z, A and R1-R6 are as defined, their synthesis and use for treatment of osteoporosis and increasing bone density.Type: GrantFiled: July 16, 2002Date of Patent: February 1, 2005Assignee: Syntex (U.S.A.) LLCInventors: Todd Richard Elworthy, Michael Garret Roepel, David Bernard Smith
-
Patent number: 6849639Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a ?v?3, ?v?5, ?v?6, ?5?1 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 8, 2000Date of Patent: February 1, 2005Assignee: Amgen Inc.Inventors: Celia Dominguez, Guoqing Chen, Ning Xi, Shimin Xu, Nianhe Han, Qingyian Liu, Qi Huang, Aaron Siegmund, Michael Handley, Longbin Liu, Alexander Kiselyov
-
Patent number: 6831039Abstract: The invention relates to 3-(heterocyclyl)-substituted benzoylpyrazois of formula (I), wherein the variables have the following meanings: X is O, NH or N-alkyl; R1 is alkyl; R2, R3, R4, R5 are hydrogen, alkyl or alkyl halide; R6 is halogen, nitro, alkyl halide, alkoxy, halogenalkoxy, alkylthio, halogenalkylthio, alkylsulfonyl or halogenalkylsulfonyl; R7 is hydroxy, alkoxy, alkenyloxy, alkylsulfonyloxy, alkylcarboyloxy, alkylthiocarbonyloxy, phenylsulfonyloxy or phenylcarbonyloxy, and the phenyl radical can be substituted; R8, R9 are alkyl; R10 is hydrogen or alkyl; and R11 is hydrogen or alkyl; and to their agriculturally useable salts. The invention also relates to intermediate products and methods for producing the inventive compounds and to the use of these compounds or products containing them for combating undesirable plants.Type: GrantFiled: May 21, 2001Date of Patent: December 14, 2004Assignee: BASF AktiengesellschaftInventors: Ulf Neidlein, Norbert Götz, Ernst Baumann, Wolfgang von Deyn, Steffen Kudis, Klaus Langemann, Guido Mayer, Ulf Misslitz, Matthias Witschel, Martina Otten, Karl-Otto Westphalen, Helmut Walter
-
Publication number: 20040235906Abstract: This invention relates to novel substituted amine derivatives. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: January 30, 2004Publication date: November 25, 2004Inventors: Alex Haahr Gouliaev, Dan Peters
-
Publication number: 20040220222Abstract: The invention relates to malonamide derivatives of formula 1Type: ApplicationFiled: January 29, 2004Publication date: November 4, 2004Inventors: Guido Galley, Annick Goergler, Helmut Jacobsen, Eric Argirios Kitas, Jens-Uwe Peters
-
Publication number: 20040186143Abstract: The present application describes modulators of MCP-1 of formula (I): 1Type: ApplicationFiled: February 11, 2004Publication date: September 23, 2004Inventors: Percy H. Carter, Matthew E. Voss
-
Patent number: 6780998Abstract: The oxidation hair dye precursor composition contains from 0.005 to 20.0 percent by weight of one or more coupler compounds and from 0.005 to 20.0 percent by weight of one or more developer compounds. The one or more developer compounds include at least one substituted 2-aminoalkyl-1,4-diaminobenzene compound of the formula (I): New substituted 2-aminoalkyl-1,4-diaminobenzene compounds of formula (I) are described.Type: GrantFiled: April 17, 2002Date of Patent: August 24, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
-
Patent number: 6774243Abstract: Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: October 30, 2001Date of Patent: August 10, 2004Assignee: Agouron Pharmaceuticals, Inc.Inventors: Qingping Tian, Naresh K. Nayyar, Srinivasan Babu, Junhua Tao, Terence Jarold Moran, Raymond Dagnino, Jr., Lennert J. Mitchell, Jr., Travis Paul Remarchuk, Michael Joseph Melnick, Steven Lee Bender
-
Publication number: 20040152697Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: ApplicationFiled: December 3, 2003Publication date: August 5, 2004Inventors: Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young