Five-membered Hetero Ring Consisting Of One Nitrogen And Four Carbons Patents (Class 544/372)
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Patent number: 7514438Abstract: Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.Type: GrantFiled: August 11, 2004Date of Patent: April 7, 2009Assignee: Amgen, Inc.Inventors: Christopher Hulme, Paul A. Tempest, Vu Van Ma, Thomas Nixey, Guity Balow
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Publication number: 20090076020Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: ApplicationFiled: August 21, 2008Publication date: March 19, 2009Applicant: ASTRAZENECA ABInventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
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Publication number: 20090069326Abstract: The present invention discloses novel compounds of Formula I: (I) possessing 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 23, 2007Publication date: March 12, 2009Inventors: John Gordon Allen, Alexei Pavlovych Krasutsky, Owen Brendan Wallace, Yanping Xu, Jeremy Schulenburg York
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Publication number: 20090054644Abstract: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: August 21, 2008Publication date: February 26, 2009Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
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Publication number: 20090036441Abstract: 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.Type: ApplicationFiled: December 22, 2005Publication date: February 5, 2009Applicant: Cell Therapeutics Europe S.R.L.Inventors: Mario Grugni, Mara Cassin, Gennaro Colella, Sergio De Munari, Gianluca Pardi, Paolo Pavesi
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Patent number: 7482335Abstract: 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: GrantFiled: October 10, 2006Date of Patent: January 27, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Robert J. Cherney, Douglas G. Batt, John V. Duncia, Daniel S. Gardner, Soo S. Ko, Anurag S. Srivastava, Michael G. Yang
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Publication number: 20090023708Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.Type: ApplicationFiled: October 25, 2006Publication date: January 22, 2009Applicant: UCB PHARMA, S.A.Inventors: Sylvain Celanire, Luc Quere, Frederic Denonne, Laurent Provins
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Patent number: 7479559Abstract: The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.Type: GrantFiled: March 17, 2005Date of Patent: January 20, 2009Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Stephane Caron, Christopher John Helal, Jeffrey W. Raggon, Yong Tao, Nga M. Do
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Publication number: 20080317712Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: December 25, 2008Inventors: Deqiang Niu, Yat Sun Or, Zhe Wang
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Patent number: 7468369Abstract: The invention relates to substituted sulfonylpyrrolidines of the formula I and to the physiologically tolerated salts thereof, as well as to their use as medicaments.Type: GrantFiled: June 20, 2007Date of Patent: December 23, 2008Assignee: Sanofi-AventisInventors: Stefanie Keil, Hans-Ludwig Schaefer, Maike Glien, Stefan Guessregen, Wolfgang Wendler, Marion Schneider
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Publication number: 20080306086Abstract: The present invention relates to a compound of formula I wherein R2 R3, R4, R5, X, n, and o are as defined herein and to a pharmaceutically acceptable acid addition salt thereof which are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: May 30, 2008Publication date: December 11, 2008Inventors: Bo Han, Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
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Publication number: 20080293699Abstract: Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.Type: ApplicationFiled: May 23, 2008Publication date: November 27, 2008Applicant: BURNHAM INSTITUTE FOR MEDICAL RESEARCHInventors: John C. Reed, In-Ki Kim
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Publication number: 20080287419Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: ApplicationFiled: May 15, 2008Publication date: November 20, 2008Applicant: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Publication number: 20080280903Abstract: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.Type: ApplicationFiled: March 10, 2006Publication date: November 13, 2008Inventors: Dennis A. Carson, Howard B. Cottam, Sylvie Barchechath, Mary Patricia Corr
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Publication number: 20080281102Abstract: A method of forming a CBI CC-1065 analog utilizes NH2 as a starting material, where R3 is H or alkyl and R6 is H, substituted or unsubstituted lower alkyl, cyano, or alkoxy. Intermediates (I) are used and are claimed.Type: ApplicationFiled: October 18, 2006Publication date: November 13, 2008Applicant: MEDAREX, INC.Inventors: Sanjeev Gangwar, Qian Zhang
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Publication number: 20080275021Abstract: The invention relates to pyrrolidine derivatives of formula wherein R1, R2, R3, n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.Type: ApplicationFiled: April 14, 2008Publication date: November 6, 2008Inventors: Caterina Bissantz, Torsten Hoffmann, Philippe Jablonski, Henner Knust, Mathias Nettekoven, Hasane Ratni, Xihan Wu
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Publication number: 20080275027Abstract: The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: wherein R1 and R2 are as defined in the specification.Type: ApplicationFiled: July 17, 2006Publication date: November 6, 2008Inventors: Rachael Ann Ancliff, Mark James Bamford, Simon Teanby Hodgson, Christopher Allan Parr, Panayiotic Alexandrou Procopiou, David Matthew Wilson, Michael Woodrow
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Publication number: 20080275043Abstract: The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.Type: ApplicationFiled: October 26, 2005Publication date: November 6, 2008Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace, John Gordon Allen, Zhaogen Chen, Thomas Edward Mabry, Jefferson Ray McCowan, Nancy June Snyder, Leonard Larry Winneroski
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Publication number: 20080269489Abstract: The present invention relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylic acid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide-(R)-pyrrolidone-5-carboxylic salt. The present invention relates also to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl) piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.Type: ApplicationFiled: February 23, 2006Publication date: October 30, 2008Applicant: UCB PHARMA, S.A.Inventors: Magali Palacio, Celal Ates
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Publication number: 20080261987Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: July 21, 2006Publication date: October 23, 2008Applicant: ChemoCentryx, Inc.Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
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Publication number: 20080242676Abstract: Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).Type: ApplicationFiled: June 11, 2008Publication date: October 2, 2008Applicant: Lupin LimitedInventors: Sudershan Kumar Arora, Neelima Sinha, Sanjay Jain, Ram Shankar Upadhayaya, Gourhari Jana, Shankar Ajay, Rakesh Kumar Sinha
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Publication number: 20080241077Abstract: 4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine hydrochloride and its hydrates, processes for preparing this benzoylguanidine salt and its hydrates, pharmaceutical compositions containing this benzoylguanidine salt and its hydrates, and its use in treating diseases, particularly those in which inhibition of the cellular Na+/H+ exchange is of therapeutic benefit.Type: ApplicationFiled: June 6, 2008Publication date: October 2, 2008Inventors: Christian Eickmeier, Peter Sieger, Werner Rall, Volkmar Koerner, Rolf Herter
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Patent number: 7427612Abstract: A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: GrantFiled: September 2, 2004Date of Patent: September 23, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
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Publication number: 20080206137Abstract: The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radiopharmaceutical for positron emission tomography.Type: ApplicationFiled: January 11, 2006Publication date: August 28, 2008Inventors: Christopher John Helal, Gunnar Antoni, Bengt Langstrom, Jia Zhi Sheng, Susan Beth Jaynes-Sobolov, Timothy John McCarthy
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Patent number: 7414047Abstract: Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: October 21, 2003Date of Patent: August 19, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Richard L. Apodaca, Jill A. Jablonowski, Kiev S. Ly, Chandravadan R. Shah, Devin M. Swanson, Wei Xiao
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Publication number: 20080194581Abstract: The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds including the intermediates therefor and their therapeutic use.Type: ApplicationFiled: April 14, 2008Publication date: August 14, 2008Applicant: SANOFI-AVENTISInventors: Francis BARTH, Christian CONGY, Laurent HORTALA, Murielle RINALDI-CARMONA
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Publication number: 20080188652Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hypedlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.Type: ApplicationFiled: February 14, 2008Publication date: August 7, 2008Inventors: Anthony Michael Campeta, Joseph F. Krzyzaniak, Jason Albert Leonard
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Publication number: 20080176854Abstract: The present invention relates to nitro-substituted phenyl-piperazine compounds of general formula I, a process for their preparation, medicaments comprising said nitro-substituted phenyl-piperazine compounds as well as the use of said nitro-substituted phenylpiperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.Type: ApplicationFiled: December 29, 2005Publication date: July 24, 2008Applicant: Laboratorios Del Dr. Esteve S.AInventors: Andrea Aschenbrenner, Juergen Kraus, Stefan Tasler, Andreas Wuzik, Jordi-Ramon Quintana-Ruiz
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Publication number: 20080171872Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.Type: ApplicationFiled: April 25, 2005Publication date: July 17, 2008Inventors: Anthony Michael Campeta, Joseph E. Kryzaniak, Jason A. Leonard
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Publication number: 20080167318Abstract: The present invention is related to pyrrolidine derivatives of formula I. Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula I are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation.Type: ApplicationFiled: April 9, 2007Publication date: July 10, 2008Applicant: APPLIED RESEARCH SYSTEM ARS HOLDING N.V.Inventors: Serge Halazy, Anna Quattropani, Alexander Scheer, Matthias Schwarz, Russell J. Thomas, Anthony Baxter
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Patent number: 7396834Abstract: Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: GrantFiled: November 5, 2003Date of Patent: July 8, 2008Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin, Niklas Plobeck, Christopher Walpole
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Publication number: 20080146556Abstract: The present invention relates to a method of treating cancer using PARP inhibitors as radio-sensitization agents of tumors. Specifically the present invention relates to a method of radio-sensitization of tumors using a compound of Formula (I) or a pharmaceutically acceptable salt form thereof. The present invention also relates to a pharmaceutical compositions of PARP inhibitors for radiosensitizing tumors.Type: ApplicationFiled: November 20, 2007Publication date: June 19, 2008Applicant: Cephalon, Inc.Inventors: James L. Diebold, Robert L. Hudkins, Sheila J. Miknyoczki, Bruce Ruggeri
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Patent number: 7381727Abstract: The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds and their therapeutic use.Type: GrantFiled: January 22, 2007Date of Patent: June 3, 2008Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
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Publication number: 20080119477Abstract: The present invention relates to certain biarylz and arylheteroaryl piperazine derivatives of Formula (Ia) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.Type: ApplicationFiled: December 9, 2005Publication date: May 22, 2008Inventors: Brian M. Smith, Vincent J. Santora, Rena Hayashi, Jason B. Ibarra, Jeffrey A. Schultz, Scott A. Estrada
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Publication number: 20080113968Abstract: A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.Type: ApplicationFiled: April 10, 2007Publication date: May 15, 2008Applicant: Novo Nordisk A/SInventors: Florencio Zaragoza Dorwald, Knud Erik Andersen, Jan Lindy Sorensen
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7348440Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 12, 2003Date of Patent: March 25, 2008Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman, Edward S. Tasber
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Patent number: 7348425Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: GrantFiled: February 3, 2006Date of Patent: March 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7338947Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma, processes for preparing and intermediates thereof.Type: GrantFiled: October 10, 2006Date of Patent: March 4, 2008Assignee: Bristol-Myers Squibb Co.Inventors: Robert J. Cherney, Percy H. Carter, John V. Duncia, Daniel S. Gardner, Joseph B. Santella
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Patent number: 7335660Abstract: This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the treatment of central nervous system disorders, such as depression, bipolar disorder, and anxiety.Type: GrantFiled: December 6, 2002Date of Patent: February 26, 2008Assignee: Eli Lilly and CompanyInventors: Javier Agejas-Chicharro, Graham Henry Timms, Andrew Caerwyn Williams, Nicholas Paul Camp, Jeremy Gilmore, Ana Belen Bueno Melendo, Carlos Lamas-Peteira
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Patent number: 7297711Abstract: The present invention relates to novel tetracyclic arylalkyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel tetracyclic arylalkyl of the general formula (I), their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention also relates to process/es for preparing such compound/s of general formula (I), composition/s containing effective amount/s of such a compound and the use of such a compound/composition in therapy.Type: GrantFiled: June 19, 2003Date of Patent: November 20, 2007Assignee: Suven Life Sciences LimitedInventors: Venkateswarlu Jasti, Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Srinivasa Reddy Battula, Venkata Satya Veerabhadra Vadlamudi Rao
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Patent number: 7294628Abstract: The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4) alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents the aromatic group 1,3-thiazol-2-yl of formula: Preparation process and therapeutic application.Type: GrantFiled: June 5, 2003Date of Patent: November 13, 2007Assignee: Sanofi-AventisInventors: Françoise Bono, Michaël Bosch, Victor Dos Santos, Jean-Marc Herbert, Dino Nisato, Bernard Tonnerre, Jean Wagnon
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Patent number: 7253205Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent a variety of substituents, ring A is a phenyl or pyridyl ring; d is zero, 1 or 2; and pharmaceutically acceptable salts and N-oxides thereof.Type: GrantFiled: June 10, 2002Date of Patent: August 7, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
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Patent number: 7250414Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: July 31, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, Yan Chen, Craig Husfeld
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Patent number: 7241764Abstract: Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared.Type: GrantFiled: November 5, 2003Date of Patent: July 10, 2007Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin
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Patent number: 7238688Abstract: Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H1 receptor antagonist.Type: GrantFiled: October 27, 2004Date of Patent: July 3, 2007Assignee: Schering CorporationInventors: Stuart B. Rosenblum, Qingbei Zeng, Mwangi Wa Mutahi, Robert G. Aslanian, Pauline C. Ting, Neng-Yang Shih, Daniel M. Solomon, Jianhua Cao, Henry A. Vaccaro, Kevin D. McCormick, John J. Baldwin, Ge Li
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Patent number: 7229994Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is independently selected from hydrogen and fluoro; R4 is independently selected from —OH, —NH2 and —NHSO2R5; and R5 is independently selected from hydrogen, —CF3 and C1–C6 alkyl, or salts thereof or separate enantiomers and salts thereof; where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6 alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo.Type: GrantFiled: May 16, 2002Date of Patent: June 12, 2007Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Niklas Plobeck
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Patent number: 7223751Abstract: The present invention relates to a novel sulfonamide derivatives and novel intermediates thereof, preparation thereof, and a pharmaceutical composition comprising the same, and more particularly, to novel sulfonamide derivatives and intermediates thereof that are used as angiogenesis controlling material and that can inhibit overexpression of matrix metalloproteinase that decomposes protein constituents in extracellular and basement membranes of connective tissues, and preparation methods thereof, and a pharmaceutical composition comprising the same.Type: GrantFiled: April 24, 2002Date of Patent: May 29, 2007Assignee: Kolon Ind. Inc.Inventors: Yong-Jun Chung, Kyeong-Ho Lee, Youn-Chul Kim, Ho-Jin Park
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Patent number: 7214714Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.Type: GrantFiled: April 26, 2002Date of Patent: May 8, 2007Assignee: Taisho Pharmaceutical Co. Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Patent number: 7214679Abstract: Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase.Type: GrantFiled: January 13, 2004Date of Patent: May 8, 2007Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sundeep Dugar, Gregory R. Luedtke, Xuefei Tan, Glen McEnroe