Additional Hetero Ring Attached Directly Or Indirectly By Nonionic Bonding To The Seven-membered Hetero Ring Patents (Class 514/212.08)
-
Patent number: 7265114Abstract: 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: November 22, 2005Date of Patent: September 4, 2007Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Yeleswarapu Koteswar Rao, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy
-
Patent number: 7253159Abstract: The invention relates to novel CD1a-presented antigens. These antigens can be used as antigens, adjuvants or as immunomodulatory agents in a variety of diagnostic, therapeutic and prophylactic applications.Type: GrantFiled: April 19, 2004Date of Patent: August 7, 2007Assignees: The Brigham and Women's Hospital, Inc., Trustees of Boston UniversityInventors: D. Branch Moody, David C. Young, Catherine E. Costello
-
Patent number: 7253158Abstract: The invention relates to compounds of the general formula in which R1, R2, R3, R4, R2?, R3?, R4?, R5, and X is —CHR— are as defined in the specification. The invention also provides pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates and diastereomeric mixtures of such compounds. The invention further provides methods for the treatment of Alzheimer's disease or common cancers.Type: GrantFiled: July 12, 2005Date of Patent: August 7, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Eric Argirios Kitas, Roland Jakob-Roetne
-
Patent number: 7235545Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: June 14, 2005Date of Patent: June 26, 2007Assignee: Merck & Co., Inc.Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
-
Patent number: 7208487Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: December 12, 2003Date of Patent: April 24, 2007Assignee: Cytokinetics, IncorporatedInventors: Gustave Bergnes, Dashyant Dhanak, Steven David Knight, Pu Ping Lu, David J. Morgans, Jr., Kenneth Allen Newlander
-
Patent number: 7208488Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).Type: GrantFiled: October 29, 2004Date of Patent: April 24, 2007Assignee: Elan Pharmaceuticals, Inc.Inventors: Martin Neitzel, Michael S. Dappen, Jennifer Marugg
-
Patent number: 7205292Abstract: The present invention is directed to compounds of Formula I and Formula II: (where variables R1, R2, R3, R4, R6, A, B, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: April 9, 2004Date of Patent: April 17, 2007Assignee: Merck & Co., Inc.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
-
Patent number: 7144880Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.Type: GrantFiled: May 1, 2003Date of Patent: December 5, 2006Assignee: Regents of the University of MichiganInventor: Gary D. Glick
-
Patent number: 7125865Abstract: The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.Type: GrantFiled: July 21, 2003Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: A. Brian Jones, Alan D. Adams, Ahren I. Green, Shaei Y. Huang, Bruno Tse, Clare E. Gutteridge, Yuan Cheng
-
Patent number: 7112587Abstract: 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 26, 2003Date of Patent: September 26, 2006Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Bhatlapenumarthy Sesha Sridevi, Potlapally Rajendar Kumar, Gaddam Om Reddy
-
Patent number: 7091203Abstract: The invention relates to imidazo[1,3,5]triazinones, a method for their production and methods of use, in particular as inhibitors of cyclic GMP metabolizing phosphodiesterases.Type: GrantFiled: July 15, 2004Date of Patent: August 15, 2006Assignee: Bayer Healthcare AGInventors: Ulrich Niewöhner, Helmut Haning, Thomas Lampe, Mazen Es-Sayed, Gunter Schmidt, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Karl-Heinz Schlemmer
-
Patent number: 7091198Abstract: The present invention relates to novel 2,5-disubstituted pyrimidine derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of central nervous system diseases.Type: GrantFiled: July 7, 2003Date of Patent: August 15, 2006Assignee: Bayer HealthCare AGInventors: Achim Feurer, Joachim Luithle, Stephan-Nicholas Wirtz, Gerhard König, Johannes-Peter Stasch, Elke Stahl, Rudy Schreiber, Frank Wunder
-
Patent number: 7087597Abstract: Compounds of the formula wherein R1, R2, R3, R4, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis, and the like; allergic diseases such as asthma, or disorders of male or female genital function and the like.Type: GrantFiled: October 11, 2000Date of Patent: August 8, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Tetsuo Miwa, Mitsuo Yamamoto, Takayuki Doi, Naoki Tarui
-
Patent number: 7081456Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: GrantFiled: November 21, 2003Date of Patent: July 25, 2006Assignee: Active Biotech ABInventors: Ian Richard Matthews, Thomas Stephen Coulter, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Göran Pettersson, Dorthe da Graca Thrige, Philip Huxley
-
Patent number: 7064136Abstract: A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: December 20, 2001Date of Patent: June 20, 2006Assignee: AstraZeneca ABInventor: Ashokkumar Bhikkappa Shenvi
-
Patent number: 7060705Abstract: The present invention relates to quinazolinone 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: November 1, 2002Date of Patent: June 13, 2006Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, William F. Hoffman
-
Patent number: 7030110Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: October 4, 2002Date of Patent: April 18, 2006Assignee: Ortho-McNeil Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
-
Patent number: 7026310Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: April 14, 2005Date of Patent: April 11, 2006Assignee: Zentaris GmbHInventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
-
Patent number: 7001899Abstract: The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: wherein each X is independently selected from: i) —C(W)2—; ii) —C(O)—; iii) —NR2—; iv) —S—; v) —S(O)—; vi) —S(O)2—; vii) two units, one from each adjacent X unit, can be taken together to form a substituted or unsubstituted double bond having the formula —CW?CW—; wherein each W is hydrogen of a unit having the formula —(L2)j—R2, the index j is 0 or 1; R is a carbocyclic or heterocyclic aryl ring; R1 is a cysteine trap; each R2 is independently a suitable substituent; and L, L1, and L2 are linking units.Type: GrantFiled: June 9, 2003Date of Patent: February 21, 2006Assignee: The Procter & Gamble CompanyInventors: John August Wos, Yili Wang, Kofi Abeka Oppong, Steven Victor O'Neil, Michael Christopher Laufersweiler, David Lindsey Soper, Biswanath De, Thomas Prosser Demuth, Jr.
-
Patent number: 6992077Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.Type: GrantFiled: July 13, 2004Date of Patent: January 31, 2006Assignee: Sepracor Inc.Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
-
Patent number: 6958330Abstract: Disclosed are polycyclic ?-amino-?-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of ?-amyloid peptide release and/or its synthesis.Type: GrantFiled: June 14, 2001Date of Patent: October 25, 2005Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: James E. Audia, Thomas E. Mabry, Jeffrey A. Nissen, Stacey L. McDaniel, Warren J. Porter
-
Patent number: 6958329Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: November 4, 2002Date of Patent: October 25, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard E. Olson
-
Patent number: 6953788Abstract: The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.Type: GrantFiled: December 19, 1997Date of Patent: October 11, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Joseph T. Tsay, Michael J. Janusz, Jian Shen, Gary A. Flynn, Ramalinga M. Dharanipragada, Joseph P. Burkhart, Douglas W. Beight, Meena V. Patel
-
Patent number: 6953790Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: May 4, 2004Date of Patent: October 11, 2005Assignee: Merck & Co., Inc.Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
-
Patent number: 6953789Abstract: The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc.Type: GrantFiled: January 13, 2004Date of Patent: October 11, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
-
Patent number: 6903089Abstract: The invention relates to novel pyrazolopyridine derivatives of formula (I) wherein R1 represents NH2 or NHCO-C1-6-alkyl, and R2 represents a radical of formula R3NCOR4 which is bonded to the remainder of the molecule by means of the nitrogen atom, R3 and R4 forming, together with the amide group to which they are bonded, a five to seven-membered heterocycle which may be saturated or partially unsaturated, may optionally contain a further heteroatom selected from the group N, O, and S and may comprise between one and five other substituents chosen from oxo, C1-6alkyl, hydroxyl, hydroxy-C1-6-alkyl, halogen, or may be fused to a C6-10 ARYL ring or a C3-8 cycloalkyl ring in which optionally two carbon atoms are bonded to each other by means of an oxygen atom.Type: GrantFiled: November 9, 2001Date of Patent: June 7, 2005Assignee: Bayer AktiengesellschaftInventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
-
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
-
Patent number: 6852713Abstract: Lactam derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.Type: GrantFiled: April 16, 2003Date of Patent: February 8, 2005Assignee: Adolor CorporationInventors: Roland E. Dolle, Paul Anson Tuthill
-
Publication number: 20040229861Abstract: The present invention is directed to compounds of Formula I: 1Type: ApplicationFiled: May 4, 2004Publication date: November 18, 2004Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
-
Patent number: 6803365Abstract: The invention relates to imidazo[1.3.5]triazinones, a method for their production and methods of use, in particular as inhibitors of cyclic GMP metabolizing phosphodiesterases.Type: GrantFiled: November 4, 2002Date of Patent: October 12, 2004Assignee: Bayer AktlengesellschaftInventors: Ulrich Niewöhner, Helmut Haning, Thomas Lampe, Mazen Es-Sayed, Gunter Schmidt, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Karl-Heinz Schlemmer
-
Patent number: 6794381Abstract: This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: February 17, 2000Date of Patent: September 21, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
-
Publication number: 20040157825Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.Type: ApplicationFiled: February 2, 2004Publication date: August 12, 2004Inventors: Samir Roy, Santosh Kumar Chandrasekaran, Katsumi Imamori, Takemitsu Asaoka, Akihiro Shibata, Masami Takahashi, Lyle M. Bowman
-
Publication number: 20040157804Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.Type: ApplicationFiled: October 15, 2003Publication date: August 12, 2004Applicant: GILEAD SCIENCES, INC.Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
-
Patent number: 6770640Abstract: The present invention relates to certain novel 1-carboxymethyl-2-oxo-azepan derivatives of the formula useful as inhibitors of matrix metalloproteinases (MMPs). The compounds of formula (1) are especially useful as selective inhibitors of MMP-12. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.Type: GrantFiled: December 17, 1999Date of Patent: August 3, 2004Assignee: Aventis Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Michael J. Janusz
-
Patent number: 6767907Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cykcloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7 membered ring; R8 is hydrogen or alkyl; have effects at cType: GrantFiled: April 14, 2000Date of Patent: July 27, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
-
Patent number: 6762177Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.Type: GrantFiled: November 5, 2002Date of Patent: July 13, 2004Assignee: Sepracor, Inc.Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
-
Publication number: 20040132710Abstract: Compounds of the formula (I): 1Type: ApplicationFiled: December 17, 2002Publication date: July 8, 2004Applicant: Pfizer Inc.Inventors: Donald Stuart Middleton, Alan Stobie
-
Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
-
Patent number: 6683081Abstract: The invention relates to novel triazolotriazinones of the general formula (I), to a method for their production and to the pharmaceutical use thereof.Type: GrantFiled: October 21, 2002Date of Patent: January 27, 2004Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewöhner, Helmut Haning, Thomas Lampe, Mazen Es-Sayed, Gunter Schmidt, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Karl-Heinz Schlemmer
-
Publication number: 20040006062Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: 1Type: ApplicationFiled: May 5, 2003Publication date: January 8, 2004Inventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
-
Patent number: 6656932Abstract: Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.Type: GrantFiled: February 13, 2002Date of Patent: December 2, 2003Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Michael William Wilson
-
Patent number: 6635632Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: December 22, 1997Date of Patent: October 21, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
-
Patent number: 6627626Abstract: The present invention relates to 5-heterocyclo-pyrazoles of the formula I: wherein ring W, m, n, and R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.Type: GrantFiled: November 1, 2002Date of Patent: September 30, 2003Assignee: Pfizer Inc.Inventors: Martha L. Minich, Subas M. Sakya
-
Publication number: 20030166636Abstract: This invention relates to novel lactams having the formula (I): 1Type: ApplicationFiled: November 4, 2002Publication date: September 4, 2003Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
-
Patent number: 6602864Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: June 3, 1998Date of Patent: August 5, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
-
Patent number: 6599898Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: GrantFiled: May 17, 2002Date of Patent: July 29, 2003Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Richard William Versace, Kenneth Walter Bair
-
Publication number: 20030134841Abstract: This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: ApplicationFiled: November 1, 2002Publication date: July 17, 2003Inventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
-
Publication number: 20030130251Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: November 4, 2002Publication date: July 10, 2003Inventors: Lorin A. Thompson, Amy Qi Han
-
Publication number: 20030119815Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: November 4, 2002Publication date: June 26, 2003Inventor: Richard E. Olson
-
Publication number: 20030114437Abstract: The present invention provides methods which use 4-amino-azepan-3-one protease inhibitors of cathepsin S in the treatment of diseases in which cathepsin S is implicated, especially treatment or prevention of autoimmune disease; treatment or prevention of a disease state caused by the formation of atherosclerotic lesions and complications arising therefrom; and diseases requiring inhibition, for therapy, of a class II MHC-restricted immune response, inhibition of an asthmatic response, inhibition of an allergic response, inhibition of immune response against a transplanted organ or tissue, or inhibition of elastase activity in atheroma, and novel compounds for use therewith.Type: ApplicationFiled: October 17, 2002Publication date: June 19, 2003Inventors: Maxwell D. Cummings, Robert W. Marquis Jr, Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita