Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperazine Ring Patents (Class 514/255.01)
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Publication number: 20080119486Abstract: The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as 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: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Inventors: Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
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Publication number: 20080119471Abstract: Use of a compound of the following formula (Ia): for the production of a medicament for the treatment of endometriosis in human wherein the treatment comprises administering to a human female in need of such treatment a therapeutically effective amount of said compound.Type: ApplicationFiled: February 23, 2005Publication date: May 22, 2008Inventors: Ulrike Kaufmann, Richard Horuk
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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: 7351703Abstract: The present invention relates to compounds of the formula I in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention relates to the use of compounds of the formula I for the therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, novel compounds of the formula I, pharmaceutical preparations comprising them and processes for their preparation.Type: GrantFiled: October 5, 2004Date of Patent: April 1, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
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Patent number: 7342018Abstract: The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases.Type: GrantFiled: October 24, 2003Date of Patent: March 11, 2008Assignee: Wilex AGInventors: Olaf Wilhelm, Viktor Magdolen, Jörg Stürzebecker, John Foekens, Verena Lutz
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Publication number: 20080058336Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: ApplicationFiled: October 10, 2006Publication date: March 6, 2008Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Publication number: 20080045509Abstract: Certain substituted benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: ApplicationFiled: June 21, 2007Publication date: February 21, 2008Inventors: Brett Allison, Michael P. Curtis, Cheryl A. Grice, John M. Keith, Michael A. Letavic, Jennifer M. B. Miller, Emily M. Stocking
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Publication number: 20080045507Abstract: Certain substituted benzamide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: June 21, 2007Publication date: February 21, 2008Inventors: Brett D. Allison, Nicholas I. Carruthers, Michael A. Letavic, Alejandro Santillan, Chandravadan R. Shah
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Patent number: 7332495Abstract: Arylalkyl ketone piperazine derivatives of the formula: and pharmaceutical compositions comprising the same. Also disclosed are methods for using the compounds as analgesic and sedative agents. The compounds of the present invention have good analgesic and sedative activities but few side effects.Type: GrantFiled: April 16, 2003Date of Patent: February 19, 2008Assignees: Nhwa Pharma. Corporation, Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Liying Huang, Chunnian Zhang, Xican Tang, Guoyuan Hu
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Patent number: 7326710Abstract: Aralkyl formyl alkyl piperazine derivatives Pharmaceutical compositions comprising the same, and methods of using them as a neuroprotective agent. Pharmaceutical results indicate that these compounds have excellent neuroprotective activities and fewer side effects.Type: GrantFiled: April 16, 2003Date of Patent: February 5, 2008Assignee: Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Liying Huang, Yang Min, Zhijie Weng, Chunnian Zhang
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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: 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
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Publication number: 20070238710Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: April 11, 2007Publication date: October 11, 2007Applicant: ARDEA BIOSCIENCESInventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong
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Patent number: 7273946Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.Type: GrantFiled: January 5, 2005Date of Patent: September 25, 2007Assignee: Nicox S.A.Inventors: Eninnio Ongini, Valerio Chiroli, Francesca Benedini, Piero Del Soldato
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Patent number: 7271168Abstract: The invention provides compounds of formula (1) wherein X, R1 and R2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and bipolar disorders.Type: GrantFiled: November 8, 2002Date of Patent: September 18, 2007Assignee: Novartis AGInventors: Thomas J. Troxler, Daniel Hoyer
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Patent number: 7268140Abstract: This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.Type: GrantFiled: October 13, 2005Date of Patent: September 11, 2007Assignee: Schering AGInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
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Patent number: 7256194Abstract: The present invention relates to compounds of the Formula or a pharmaceutically acceptable salt, solvate, hydrate or formulation thereof. These compounds can be used for the inhibition of Factor Xa and for the treatment and/or prevention of diseases that are mediated by Factor Xa activity.Type: GrantFiled: February 22, 2002Date of Patent: August 14, 2007Assignee: MorphochemInventors: Sven Nerdinger, Thilo Fuchs, Katrin Illgen, Robert Eckl
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Publication number: 20070179148Abstract: The present application describes modulators of MIP-1? of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, T, W, R1, R4, R5, R5a and R5b are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.Type: ApplicationFiled: January 23, 2007Publication date: August 2, 2007Inventors: Percy H. Carter, Cullen L. Cavallaro, George V. De Lucca
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Publication number: 20070173511Abstract: The present invention relates to compounds of formula I wherein R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 16, 2007Publication date: July 26, 2007Inventors: Matthias Nettekoven, Olivier Roche
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Publication number: 20070167436Abstract: The present invention relates to compounds of formula I wherein s, R1a and R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 4, 2007Publication date: July 19, 2007Inventors: Matthias Nettekoven, Jean-Marc Plancher, Olivier Roche, Tadakatsu Takahashi, Sven Taylor
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Patent number: 7220749Abstract: The invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent. The invention also provides novel compositions comprising at least one COX-2 selective inhibitor, that is optionally sitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: GrantFiled: June 10, 2003Date of Patent: May 22, 2007Assignee: NitroMed, Inc.Inventors: L. Gordon Letts, David S. Garvey
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Patent number: 7214681Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: GrantFiled: February 10, 2004Date of Patent: May 8, 2007Assignee: Prosidion LimitedInventors: Matthew Colin Thor Fyfe, Lisa Sarah Gardner, Maseo Nawano, Martin James Procter, Chrystelle Marie Rasamison, Karen Lesley Schofield, Vilasben Kanji Shah, Kosuke Yasuda
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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: 7214680Abstract: The present invention relates to piperazine of formula (I) wherein R represents halogen, C1-4 alkyl, trifluoromethoxy or trifluoromethyl; R1 is trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, halogen or trifluoromethoxy; R2 is hydrogen, C1-4 alkyl or C2-6 alkenyl; R3 represents hydrogen or C1-4 alkyl; n and m are independently 0 or an integer from 1 to 3; and pharmaceutically acceptable salts and solvates thereof, process for their preparation and their use in the treatment of condition mediated by tachykinins and/or by selective inhibition of the serotonin reuptake transporter protein.Type: GrantFiled: August 13, 2002Date of Patent: May 8, 2007Assignee: Glaxo Group LimitedInventors: Giuseppe Alvaro, Torquil I. M. Jack, Maria Elvira Tranquillini
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Patent number: 7208600Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: GrantFiled: October 12, 2004Date of Patent: April 24, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, Robert B. Perni, Janos Pitlik
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Patent number: 7208497Abstract: 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: GrantFiled: June 27, 2002Date of Patent: April 24, 2007Assignee: Novo Nordisk A/SInventors: Florencio Zaragoza Dorwald, Knud Erik Andersen, Jan Lindy Sørensen
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Patent number: 7186726Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.Type: GrantFiled: September 3, 2003Date of Patent: March 6, 2007Assignee: Neuromed Pharmaceuticals Ltd.Inventors: Terrance P. Snutch, Gerald W. Zamponi, Hassan Pajouhesh, Hossein Pajouhesh, Francesco Belardetti
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Patent number: 7176207Abstract: Compounds of the following formula (I): where A, a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: February 2, 2006Date of Patent: February 13, 2007Assignee: Schering AktiengesellschaftInventors: Judi A Bryant, Brad O Buckman, Imadul Islam, Raju Mohan, Michael M Morrissey, Robert Guo-Ping Wei, Wei Xu, Shendong Yuan
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Patent number: 7166600Abstract: The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1–R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.Type: GrantFiled: January 11, 2006Date of Patent: January 23, 2007Assignee: Genentech, Inc.Inventor: David Y. Jackson
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Patent number: 7160874Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: November 15, 2004Date of Patent: January 9, 2007Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
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Patent number: 7132539Abstract: The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R1 alkyl units selected from the group consisting of C1–C12 linear or branched alkyl, C3–C8 cyclic alkyl, C2–C12 linear or branched alkenyl, or haloalkyl, for example, the 2-keto-3-alkylpiperazines having the formula: wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, and 4-chlorophenyl; R1 is selected from the group consisting of methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, sec-butyl, tert-butyl, cyclopropyl, cyclopropylmethyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cyclohexylmethyl, benzyl, allyl, 1-methylallyl, 2-methylallyl, but-2-enyl, and propargyll; R7a is selected from the group consisting of hydrogen, —CO2H, —CONH2, —CONHCH3, and —CON(CH3)2; R8 is benzyl, substituted benzyl, or naphthalen-2-ylmethyl.Type: GrantFiled: October 20, 2003Date of Patent: November 7, 2006Assignee: The Procter & Gamble CompanyInventors: Frank Hallock Ebetino, Xinrong Tian, Wieslaw Adam Mazur, Anny-Odile Colson
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7098212Abstract: The present invention relates to compounds of the formula I and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R1, R2, R3, R4 and R5 are as defined herein. Moreover, the present invention is also directed at pharmaceutical compositions comprising a compound of the formula I and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed at methods of using the herein described compounds and compositions for treating or preventing a disorder or condition that can be treated or prevented by antagonizing the CCR1 receptor in a mammal.Type: GrantFiled: October 18, 2002Date of Patent: August 29, 2006Inventors: Laura C. Blumberg, Matthew F. Brown, Matthew M. Hayward, Gregory D. Lundquist, Christopher S. Poss, Andrei Shavnya
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Patent number: 7094779Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity.Type: GrantFiled: July 3, 2002Date of Patent: August 22, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Wouter I. Iwema Bakker, Jan H. van Maarseveen, Hein K. A. C. Coolen, Martinus Th. M. Tulp, Arnoldus H. J. Herremans, Andrew C. Mccreary, Gustaaf J. M. van Scharrenburg, Adrianus van den Hoogenband
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Patent number: 7078407Abstract: The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives showing superior antioxidant activity compared to the known antioxidant compounds, their pharmaceutically acceptable salt, and pharmaceutical compositions containing them. It can be usefully used in treating neurodegerative diseases such as aging, cancer, diabetes, ischemic stroke, Parkin's disease, dementia and Huntinton's disease.Type: GrantFiled: November 22, 2002Date of Patent: July 18, 2006Assignee: Korea Research Institute of Chemical TechnologyInventors: No-Sang Park, Young-Sik Jung, Churl-Min Seong, Hee-Jong Lim, Joong-Ho Yoon, Jae-Yang Kong, Woo-Kyu Park
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Patent number: 7064128Abstract: Compounds of the formula and their salts, wherein Cy represents cyclohexyl; Y is CH?CH?, CH?2, ? or Cy, X is trivalent straight-chain alkylene (3–10C) or trivalent straight-chain 1-alkenylene (3–10C) optionally substituted by oxo at the C adjacent N when n is 0 and Y is ?2CH; and is otherwise trivalent straight-chain alkylene (5–10C) or trivalent straight-chain 1-alkenylene (5–10C) optionally substituted by oxo at the C adjacent N; Z is N, NCO, CHNCOR1 or CHNR1, wherein R1 is alkyl (1–6C); and n is 0–5; wherein each ? and Cy independently may optionally be substituted by alkyl (1–6C) or by halo, CF3, OCF3, NO2, NR2, OR, SR, COR, COOR, CONR2, NROCR or OOCR where R is H or alkyl (1–4C), or two substituents may form a 5–7 membered ring with the proviso that the compounds of formula (1) contain at least one aromatic moiety, are useful as calcium channel blockers.Type: GrantFiled: December 23, 2003Date of Patent: June 20, 2006Assignee: NeuroMed Technologies, Inc.Inventors: Terrance P. Snutch, Gerald W. Zamponi
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Patent number: 7056524Abstract: A method of hydrating nasal airway surfaces in a subject in need of such treatment comprises topically applying a sodium channel blocker to a nasal airway surface of the subject in an amount effective to inhibit the reabsorption of water by the surface. The channel blocker may be a pyrazinoylguanidine sodium channel blocker, such as benzamil, phenamil, amiloride, or a pharmaceutically acceptable salts thereof. The method may further comprise the step of topically applying a P2Y2 receptor agonist to a nasal airway surface of the subject in an amount effective to stimulate chloride secretion by the nasal airway surface. In a preferred embodiment, the sodium channel blocker is a covalent conjugate of a pyrazinoylguanidine sodium channel blocker and a non-absorbable carrier moiety (e.g., albumin, polyethylene glycol). Such compounds may also be administered to other mucosal surfaces where it is desired to inhibit the reabsorption of water.Type: GrantFiled: February 20, 2001Date of Patent: June 6, 2006Assignee: The University of North Carolina at Chapel HillInventor: Richard C. Boucher, Jr.
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Patent number: 7048924Abstract: Methods for promoting immunologic control of human immunodeficiency virus (HIV) in an HIV-infected subject are provided. The methods comprise administering to the subject highly active antiretroviral therapy (HAART) for at least one cycle of an intermittent dosing regimen in combination with administration of a pharmaceutical composition comprising a therapeutically effective amount of interleukin-2 (IL-2) or variant thereof. The combination of daily or intermittent administration of IL-2 (or variant thereof) and intermittent HAART promotes immunologic control of viral replication in the absence of HAART, thereby prolonging the length of time a patient may discontinue HAART before viral rebound necessitates further administration of HAART. Administration of IL-2 therapy in combination with an intermittent HAART dosing regimen provides an effective method for treating a subject infected with HIV.Type: GrantFiled: May 14, 2003Date of Patent: May 23, 2006Assignee: Chiron CorporationInventor: David Sahner
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Patent number: 7045524Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.Type: GrantFiled: November 12, 2001Date of Patent: May 16, 2006Assignee: SmithKline Beecham p.l.c.Inventors: David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle
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Patent number: 7030115Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: March 21, 2003Date of Patent: April 18, 2006Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Patent number: 7030242Abstract: This invention relates to a method of treatment for osteoarthritis involving inhibitors of aggrecanase that demonstrate IC50s of less than 20 nM and demonstrate differential potency against matrix metalloproteinases (MMPs) and a disintegrin and metalloproteinases (ADAMs or reprolysins).Type: GrantFiled: May 3, 2005Date of Patent: April 18, 2006Assignees: Pfizer Inc, Pfizer Products Inc.Inventors: Mark C. Noe, Michael A. Letavic, Louis S. Chupak, Kim F. McClure
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Patent number: 7022707Abstract: The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R4, A1, A2 m and n are as described in the specification.Type: GrantFiled: June 23, 2004Date of Patent: April 4, 2006Assignees: Hoffman-La Roche Inc., Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, James Edward Paul Davidson, Claire Elizabeth Dawson, Ashley Roger George, Howard Langham Mansell, Patrizio Mattei, Jacques Mizrahi, Matthias Heinrich Nettekoven, Robert Mark Pratt, Stephan Roever, Jonathan Richard Anthony Roffey, Jean-Luc Specklin, Henri Stalder, Kerry Wilkinson
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Patent number: 7019003Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: March 1, 2002Date of Patent: March 28, 2006Assignee: Smithkline Beecham CorporationInventors: Jia-Ning Xiang, Siegfried B. Christensen, IV, Jinhwa Lee, Daniel J. Mercer
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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
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Patent number: 6992081Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: September 21, 2001Date of Patent: January 31, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
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Patent number: 6989383Abstract: The present invention relates to methods of treating cancer using a combination of a compound which is an antineoplastic agent and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at lest two therapeutic agents selected from a group consisting of a compound which is an antineoplastic agent and a compound which is an inhibitor or prenyl-protein transferase. The invention also relates to methods of preparing such compositions.Type: GrantFiled: June 4, 1998Date of Patent: January 24, 2006Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Neal Rosen, Laura Sepp-Lorenzino, Mark M. Moasser, Allen I. Oliff, Jackson B. Gibbs, Nancy Kohl, Samuel L. Graham, George C. Prendergast
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Patent number: 6984652Abstract: Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each independently optionally substituted, are useful for the treatment or prophylaxis of bacterial infections in mammals. The compounds are believed to function by inhibiting gyrase B.Type: GrantFiled: May 17, 2004Date of Patent: January 10, 2006Assignee: Warner-Lambert Company LLCInventors: Kraig Yager, Shaosong Chu, Krzysztof Appelt, Xiaoming Li
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Patent number: 6982256Abstract: The invention relates to new formulations for improving the local tolerance of intravenously administered 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of the pharmacologically acceptable acid addition salts thereof.Type: GrantFiled: September 9, 2002Date of Patent: January 3, 2006Assignee: Boehringer Ingelheim Pharma KGInventors: Christine Votteler, Bernd Kruss
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Patent number: 6977258Abstract: This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R1a, R2, R3, R4, R5 and R6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.Type: GrantFiled: January 17, 2003Date of Patent: December 20, 2005Assignee: Schering AktiengesellschaftInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
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Patent number: RE39921Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.Type: GrantFiled: October 5, 2004Date of Patent: November 13, 2007Assignee: SmithKline Beecham CorporationInventors: Giuseppe Alvaro, Romano DiFabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini