Plural Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/217.05)
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Patent number: 7304051Abstract: Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I) are CCK2 modulators useful in the treatment of CCK2 mediated diseases.Type: GrantFiled: August 4, 2004Date of Patent: December 4, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Brett D. Allison, Michael D. Hack, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen
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Patent number: 7304052Abstract: The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- represents a saturated or an unsaturated homopiperidinyl having one double bond, and wherein said bivalent radical -{circle around (A)}- is substituted with R2 being hydrogen, hydroxy, C1-4alkyl, or C1-4alkyloxy; -a1=a2-a3=a4- represents an optionally substituted bivalent radical; R1 is hydrogen, C1-6alkyl, aryl1, C1-6alkyl substituted with aryl1, C1-4alkyloxycarbonyl, aryl1carbonyl, aryl1C1-6alkylarbonyl C1-4alkylcarbonyl, trifluoromethyl, trifluoromethylcarbonyl, C1-6alkylsulfonyl, aryl1sulfonyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl; X represents O, S or NR3, wherein R3 is hydrogen, C1-6alkyl, methanesulfonyl, benzenesulfonyl, trifluoromethanesulfonyl, dimethylsulfamoyl, C1-4alkyl substituted with aryl2 and optionally with hydroxy, C1-4alkylcarbonylC1-4alkyl suType: GrantFiled: December 14, 2000Date of Patent: December 4, 2007Assignee: Janssen Pharmaceuitca N.V.Inventors: Frans Eduard Janssens, Jérôme Emile Georges Guillemont, François Maria Sommen
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Publication number: 20070249579Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: ApplicationFiled: April 10, 2007Publication date: October 25, 2007Inventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini
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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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Publication number: 20070141147Abstract: A mixed-release tablet or capsule formulation including vehicles for the delivery of a plurality of drugs in various combinations of immediate release, extended release, and/or delayed release modes over a predetermined time period have been developed, which provide for controlled release not just of the drugs, but controlled release that is designed to create more effective coordination between the drugs being delivered. The drugs can be any medically and/or physiologically appropriate combination of drugs and active ingredients, preferably decongestant drugs, antihistamines, expectorants, antitussives, cough suppressants, and drying agents.Type: ApplicationFiled: July 31, 2006Publication date: June 21, 2007Inventors: Matthew F. Heil, Glynn Wilson
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Patent number: 7196087Abstract: Compounds of the formula I: and pharmaceutically acceptable salts thereof, wherein X is CH or N, Y is C or S, Z is —(CRaRb)r— or —SO2—, A is —NR3— or —O—, R2 is optionally substituted aryl or optionally substituted heteroaryl, n is 1 or 2, m is 1 when Y is C and m is 2 when Y is S, and p, q, r, R1, R3, R4, R5, R6, R7, R8, R9, R10, Ra and Rb are as defined herein. The compounds are useful in the treatment of 5-HT6 and 5-HT2A mediated diseases.Type: GrantFiled: January 14, 2005Date of Patent: March 27, 2007Assignee: Roche Palo Alto LLCInventors: Nancy Elisabeth Krauss, Meng Sui, Shu-Hai Zhao
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Patent number: 7179803Abstract: The present invention relates generally to a method of retarding, reducing or otherwise inhibiting viral functional activity and, more particularly, to a method of reducing, retarding or otherwise inhibiting viral functional activity by down-regulating Vpu ion channel functional activity. Even more particularly, the present invention provides a method of treating HIV infection or AIDS by inhibiting Vpu ion channel mediated HIV replication.Type: GrantFiled: October 12, 1999Date of Patent: February 20, 2007Assignee: Australian National UniversityInventors: Graeme Cox, Gary Ewart, Peter Gage
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Patent number: 7173032Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: March 17, 2003Date of Patent: February 6, 2007Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Karen A. Campbell
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Patent number: 7141562Abstract: Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R2 is aryl or heteroaryl, and R1, R3, R4, R5, R6, R7, R8, R9, Ra, Rb, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.Type: GrantFiled: November 6, 2003Date of Patent: November 28, 2006Assignee: Roche Palo Alto LLCInventors: Hans Maag, Meng Sui, Shu-Hai Zhao
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Patent number: 7074798Abstract: The present invention provides novel compounds exhibiting an excellent DPPIV inhibition effect. The compounds are represented by the formula: wherein, m is 0 or 1; n is 0; R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, and R42 each represent a hydrogen atom; X represents an alkynyl group, an aryl group, and such, which group may be substituted; and, R1 and R2 each independently represents a hydrogen atom, an alkyl group, an alkoxyl group, or such, or salts or hydrates thereof.Type: GrantFiled: February 24, 2003Date of Patent: July 11, 2006Assignee: Eisai Co., LtdInventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki, Mika Aoki
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Patent number: 7071184Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: March 7, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: 7022687Abstract: The present invention relates to a novel combination of a soft steroid, in particular loteprednol, and at least one antihistamine, such as, for example, azelastine and/or levocabastine, for simultaneous, sequential or separate administration in the local treatment of allergies and airway disorders, for example of allergic rhinitis (rhinoconjunctivitis).Type: GrantFiled: September 26, 2000Date of Patent: April 4, 2006Assignee: Asta Medica AGInventors: Istvan Szelenyl, Degenhard Marx, Sabine Heer, Juergen Engel
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Patent number: 6960575Abstract: A compound having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine 4-tetrahydropyrazine as a main skeleton. The compound is a chymase inhibitor and is represented by the following formula [I] and salts thereof: In the formula [I], X is S; R1 and R2 are H, alkyl, cycloalkyl or aryl; R3 and R4 are H, alkyl, cycloalkyl, aryl or an aromatic heterocycle; R5 is H, alkyl, cycloalkyl, aryl or -A3-A4-R7; R6 is H, alkyl, cycloalkyl, hydroxy, alkoxy, aryl, aryloxy or an aromatic heterocycle; R7 is H, alkyl, hydroxy, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle; A1 is alkylene; A2 is carbonyl or sulfonyl; A3 is alkylene; A4 is carbonyl or oxalyl; and n is 0 or 1.Type: GrantFiled: November 13, 2003Date of Patent: November 1, 2005Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Takahiro Honda, Eiko Matsumoto, Junzo Matsumoto
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Patent number: 6951851Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: October 4, 2005Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6936603Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: August 30, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Hui Cai, James P. Edwards, Steven P Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6906057Abstract: Methods for modulating the activity of the mammalian FXR receptor. The methods include methods of treating a hyper- or hypocholesterolemic mammal comprising contacting the mammal with synthetic compounds having FXR receptor activity.Type: GrantFiled: June 9, 2000Date of Patent: June 14, 2005Assignees: Allergan, Inc., City of Hope National Medical CenterInventors: Barry M. Forman, Richard L. Beard, Roshantha A. Chandraratna
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Patent number: 6890517Abstract: A liquid, propellant-free pharmaceutical preparation comprising: (a) a first active substance comprising a tiotropium salt, in a concentration based on tiotropium of between 0.0005% and 5% by weight; (b) a second active substance selected from the group consisting of: an antiallergic, antihistamine, steroid, and leukotriene antagonist; (c) a solvent selected from water or a water/ethanol mixture; and (d) a pharmacologically acceptable preservative, wherein the pH of the preparation is adjusted to between 2.0 and 4.5 with an acid and the tiotropium salt is dissolved in the solvent, optionally including a pharmacologically acceptable complexing agent, stabilizer, a pharmacologically acceptable cosolvent, or other pharmacologically acceptable adjuvants and additives; a method for administering a pharmaceutical preparation by nebulizing the pharmaceutical preparation in an inhaler, and a method of treating asthma or COPD in a patient using the pharmaceutical preparation.Type: GrantFiled: March 24, 2003Date of Patent: May 10, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Karin Drechsel, Barbara Niklaus-Humke, Christel Schmelzer, Petra Barth
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Patent number: 6890921Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the ?-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: March 15, 2000Date of Patent: May 10, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allen Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
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Patent number: 6887864Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.Type: GrantFiled: March 6, 2003Date of Patent: May 3, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Birgit Masjost, Ralf Schumacher
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Patent number: 6867204Abstract: Compounds of the formula: or pharmaceutically acceptable salts or prodrugs thereof, where each of n and p independently is 2 or 3, Y is —SO2— or —SO2—N(R10)—, Z1 is CH or N, and R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined herein. The compounds have selective 5-HT6 affinity and are useful in the treatment of certain CNS disorders. Also provided are compositions comprising, methods for using, and methods for preparing Compounds of Formula I.Type: GrantFiled: May 9, 2003Date of Patent: March 15, 2005Assignee: Roche Palo Alto LLCInventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
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Publication number: 20040254162Abstract: The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharma-ceutical compositions containing the compounds of the present invention as anti-microbials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: ApplicationFiled: July 13, 2004Publication date: December 16, 2004Inventors: Anita Mehta, Sudershan R Arora, Bisjawit Das, Abhijit Ray, Sonali Rudra, Ashok Rattan
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Publication number: 20040253311Abstract: The present invention is directed to a pharmaceutical composition and method for treatment of rhinitis and cold like symptoms, the composition includes a non-steroidal anti-inflammatory drug (NSAID), a decongestant and an antihistamine preferably in a multi-layer tablet comprising an immediate release layer and an extended release layer to optimize the delivery profile and match the duration of biological action of the multiple active agents.Type: ApplicationFiled: June 2, 2004Publication date: December 16, 2004Inventors: Roger Berlin, Peter Ramsey, Arunya Usayapant, Josephine Fubara, Scott Poxon, Bill Bubnis, David Giamalva, John Strode, John Bachert, Michael Williams
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Publication number: 20040248881Abstract: Compounds of Formula (I) or (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.Type: ApplicationFiled: May 25, 2004Publication date: December 9, 2004Applicant: Pfizer IncInventors: Philip A. Carpino, Subas M. Sakya
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Publication number: 20040248897Abstract: Substituted N-acylaniline derivatives of general formula 1Type: ApplicationFiled: December 22, 2003Publication date: December 9, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Henning Priepke, Norbert Hauel, Armin Heckel, Uwe Ries, Klaus Binder, Rainer Zimmermann, Jean-Marie Stassen, Wolfgang Wienen
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Patent number: 6821951Abstract: A fluid bed spray process is described where one or more carbohydrates are incorporated into an echinocandin formulation to provide a significant improvement in thermal stability. The carbohydrate is solubilized with an echinocandin compound or echinocandin/carbohydrate complex in a solvent(s) to form a pharmaceutical solution which is sprayed onto the surface of a granular diluent or carrier. The resulting granular oral formulations and medicaments derived therefrom are also described.Type: GrantFiled: August 29, 2001Date of Patent: November 23, 2004Assignee: Eli Lilly and CompanyInventors: John Richard Schwier, Jerry Taylor
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Patent number: 6821966Abstract: The invention is directed to methods to inhibit p38-&agr; kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; B is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; each R3 is independently a noninterfering substituent, where n is 0-3; Z3 is NR7 or O; wherein R7 is H or a noninterfering substituent; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; wherein A is: such that Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0-2 wherein the sum of l and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfeType: GrantFiled: November 20, 2001Date of Patent: November 23, 2004Assignee: Scios, Inc.Inventors: Sundeep Dugar, John Perumattam, Gregory Luedtke, Xuefei Tan, Qing Lu
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Patent number: 6821965Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)alklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-2(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseaseType: GrantFiled: February 2, 2001Date of Patent: November 23, 2004Assignee: AsterZeneca ABInventors: Dearg S Brown, George R Brown
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Publication number: 20040204399Abstract: Pharmaceutical compositions contain a surfactant and one or more active ingredients selected from among anti-infective agents, anti-inflammatory agents, anti-mucolytic agents, antihistamines, antiseptics, combinations of antibiotics and combinations of these agents. The compositions are formulated for aerosol administration to treat chronic sinusitis or nasal polyps.Type: ApplicationFiled: April 29, 2004Publication date: October 14, 2004Inventors: Robert S. Osbakken, Mary Anne Hale, Frederick T. Leivo, James D. Munk
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Publication number: 20040204371Abstract: The present invention provides methods of treating and preventing mortality associated with heart failure in an African American patient with hypertension and improving oxygen consumption, quality of life and exercise tolerance by administering a therapeutically effective amount of at least one hydralazine compound and at least one of isosorbide dinitrate and isosorbide mononitrate, and, optionally, one or more compounds, such as, for example, a digitalis, a diuretic compound, or a compound used to treat cardiovascular diseases. In the present invention, the hydralazine compound is preferably hydralazine or a pharmaceutically acceptable salt thereof. Preferred methods of the invention comprise administering hydralazine or a pharmaceutically acceptable salt thereof and isosorbide dinitrate.Type: ApplicationFiled: April 15, 2004Publication date: October 14, 2004Applicant: NitroMed, Inc.Inventors: Jay N. Cohn, Peter Carson
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Patent number: 6800636Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.Type: GrantFiled: December 20, 2001Date of Patent: October 5, 2004Assignee: Schering CorporationInventors: Timothy Guzi, Dinanath F. Rane, Alan K. Mallams, Alan B. Cooper, Ronald J. Doll, Viyyoor M. Girijavallabhan, Arthur G. Taveras, Corey Strickland, Joseph M. Kelly, Jianping Chao
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Publication number: 20040192675Abstract: A pharmaceutical composition comprising a tiotropium salt; and an antihistamine, optionally together with a pharmaceutically acceptable excipient, the tiotropium salt and the antihistamine optionally in the form of their enantiomers, mixtures of their enantiomers, their racemates, their solvates, or their hydrates, processes for preparing them, and their use in the treatment of respiratory tract diseases.Type: ApplicationFiled: April 14, 2004Publication date: September 30, 2004Applicant: Boehringer Ingelheim Pharma KGInventors: Michel Pairet, Michael P. Pieper, Christopher John Montague Meade, Christel Schmelzer
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Publication number: 20040192674Abstract: The present invention provides methods which uses certain 4-amino-azepan-3-ones to inhibit cathepsin L. Consequently they are useful for preventing or treating diseases in which cathepsin L is implicated, such as rheumatoid arthritis or inhibition of positive selection of CD4+T-cells by cortical thymic epithelial cells.Type: ApplicationFiled: February 5, 2004Publication date: September 30, 2004Inventor: Robert W. Marquis
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Patent number: 6794382Abstract: The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group, and, when X represents a carbon atom: R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3+, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH, R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group.Type: GrantFiled: January 30, 2003Date of Patent: September 21, 2004Assignee: Sanofi-SynthelaboInventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
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Publication number: 20040147508Abstract: The present invention relates to a phenothiazinium compound of Formula (I): 1Type: ApplicationFiled: November 26, 2003Publication date: July 29, 2004Applicant: PHOTOPHARMICA LIMITEDInventors: Stanley Beames Brown, Cassandra Claire O'Grady, John Griffiths, Kirste Joanne Mellish, Richard George Tunstall, David John Howard Roberts, David Ian Vernon
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Patent number: 6767912Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.Type: GrantFiled: December 20, 2001Date of Patent: July 27, 2004Assignee: WyethInventors: Ping Zhou, Derek Cecil Cole, Michael Gerard Kelly, William Joseph Lennox
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Publication number: 20040142925Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: 1Type: ApplicationFiled: March 9, 2004Publication date: July 22, 2004Inventors: Mervyn Thompson, Paul Adrian Wyman
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Publication number: 20040132719Abstract: Phenothiazine derivatives of formula (I) are disclosed. The compounds are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: ApplicationFiled: February 17, 2004Publication date: July 8, 2004Inventors: Jeffrey T Finer, John C Chabala
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Publication number: 20040132720Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: in which Ra is a group of formula (i) wherein P1 is phenyl, naphthyl or heteroaryl; R1 is halogen, C1-6alkyl, C3-6cycloalkyl, COC1-6alkyl, C1-6alkoxy, hydroxy, hydroxyC1-6alkyl, nitro, haloC1-6alkyl, cyano, SR6, SOR6, SO2R6, SO2NR6R7, CO2R6, CONR6R7, OCONR6COR7, NR6r7, NR6COR7, NR6CO2R7, NR6SO2R7, NR6CONR7R8, CH2NR6COR7, CH2NR6CO2R7, CH2NR6SO2R7, CR6═NOR7 where R6, R7 and R8 are independently hydrogen or C1-6alkyl, a is 1, 1, 2, or 3; or Ra is a group of formula (ii) where P2 is phenyl, naphthyl, heteroaryl or a 5 to 7 membered heterocyclic ring; P3 is phenyl, naphthyl or heteroaryl; R2 is a defined above for R1 in formula (I) or R2 is heteroaryl optionally substituted By C1alkyl, halogen or COC1-6alkyl or is a 5-7 membered heterocyclic ring optionally substituted by oxo; R3 is halogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyl, COC1-6alkyl, hydroxy, intro, haloC1-6alkyl, cyano, CO2R6, CONR6R7, NR6R7 where R6 and R7 are as dType: ApplicationFiled: March 9, 2004Publication date: July 8, 2004Inventors: Howard Marshall, Mervyn Thompson, Paul Adrian Wyman
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Publication number: 20040132718Abstract: The present application describes monocyclic or bicyclic carbocycles and heterocycles and derivatives thereof of Formula I: 1Type: ApplicationFiled: December 8, 2003Publication date: July 8, 2004Inventors: Irina C. Jacobson, Ruth R. Wexler, Suanne Nakajima, Mimi L. Quan, Shuaige Wang, Joanne M. Smallheer, Jennifer X. Qiao
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Publication number: 20040106600Abstract: Disclosed herein are compounds of Formula I, 1Type: ApplicationFiled: June 20, 2003Publication date: June 3, 2004Inventors: Carl-Magnus Andersson, Nathalie Schlienger, Alma Fejzic, Eva Louise Hansen, Jan Pawlas
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Publication number: 20040106599Abstract: 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.Type: ApplicationFiled: September 12, 2002Publication date: June 3, 2004Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
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Patent number: 6743788Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: May 17, 2002Date of Patent: June 1, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
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Publication number: 20040102436Abstract: The present invention provides a compound which is useful as a PGI2 receptor agonist, and a pharmaceutical composition.Type: ApplicationFiled: October 23, 2003Publication date: May 27, 2004Inventors: Tetsuo Asaki, Taisuke Hamamoto, Keiichi Kuwano
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Publication number: 20040097486Abstract: Compositions and methods for treating VKC, GPC, AKC and allergic conjunctivitis with H1 antagonists and ocularly safe steroids are disclosed.Type: ApplicationFiled: November 7, 2003Publication date: May 20, 2004Inventor: John M. Yanni
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Publication number: 20040082566Abstract: The present invention relates to pyrrolidine sulfonamides, pharmaceutical compositions containing them and their use as urotensin II antagonists.Type: ApplicationFiled: September 26, 2003Publication date: April 29, 2004Inventors: Dashyant Dhanak, Steven D Knight, Jian Jin, Ralph A Rivera, Anthony Sapienza
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Publication number: 20040077658Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: (I) wherein: R1 is H or C1-6 alkyl; R2 is aryl or C3-7 cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is R8R9; R8 is a single bond, C1-6 alkyl, or aryl; R9 is H, COO R10, or N R11R12; R10 is H or C1-6 alkyl; R11 and R12 are independently selected from H and C1-6 alkyl; R5 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R6 represents H or up to three substituents independently selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- or di-C1-6 alkylamino; R7 is H or halo; a is 1-6; and any of R2, R5, R8, R10, R11, and R12 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy or oxo; aType: ApplicationFiled: October 23, 2003Publication date: April 22, 2004Inventors: Carlo Farina, Giuseppe Giardina, Mario Grugni, Guy Marguerite Marie Gerard
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Publication number: 20040076587Abstract: The invention relates to pharmaceutical compositions for nasal application, comprising selected CGRP antagonists which are described in WO 98/11128, as well as a process for the preparation thereof.Type: ApplicationFiled: June 17, 2003Publication date: April 22, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Bernd Kruss, Ulrich Busch, Klaus Jost, Marc Anton Gaiser
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Publication number: 20040072840Abstract: The invention relates to the compounds of formula: 1Type: ApplicationFiled: September 16, 2003Publication date: April 15, 2004Inventors: Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
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Publication number: 20040063679Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: September 27, 2002Publication date: April 1, 2004Applicant: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R.R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel