Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 546/146)
-
Patent number: 7125871Abstract: Compounds of the formula (I) in which R1, R2 and X1 have the meanings given in the specification, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous systemType: GrantFiled: May 24, 2001Date of Patent: October 24, 2006Assignee: Eli Lilly and CompanyInventors: Ivan Collado Cano, Jesus Ezquerra-Carrera, Alicia Marcos Liorente, Luisa Maria Martin-Cabrejas, James Allen Monn
-
Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
-
Patent number: 7126001Abstract: The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.Type: GrantFiled: October 25, 2002Date of Patent: October 24, 2006Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
-
Patent number: 7122559Abstract: Compounds having the formula (I), or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is —NR6S(O)pR16; W is hydrogen or —(CR7R8)q—W1; W1 is hydrogen or a bond with R6; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R1, R2, R3, R6, R7, and R16 are as defined in the specification.Type: GrantFiled: February 10, 2004Date of Patent: October 17, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter W. Glunz, Gregory S. Bisacchi, George C. Morton, Alexandra A. Holubec, E. Scott Priestley, Xiaojun Zhang, Uwe D. Treuner
-
Patent number: 7122547Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.Type: GrantFiled: November 9, 1999Date of Patent: October 17, 2006Assignees: Schering AG, Novartis AGInventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch, Guido Bold, Paul William Manley, Pascal Furet, Jeanette Marjorie Wood, Jürgen Mestan, Jose Brüggen, Stefano Ferrari, Martin Krüger, Eckhard Ottow, Andreas Menrad, Michael Schirner
-
Patent number: 7122673Abstract: A method for the preparation of a compound of general Formula: or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof comprising cyclizing an azomethine ylide of general Formula: wherein, A is a cyclic or non-cyclic group; Z is a carbon or a heteroatom; n is selected from 0, 1, 2 or 3; W, X and Y may be the same or different and each are selected from hydrogen; optionally substituted alkyl, alkenyl, alkynyl, amino, alkoxy, alkenoxy, alkynoxy, aryl, alkylthio, heterocyclyl; carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto, halogen, nitro, sulfate, phosphate, cyano and optionally protected hydroxy; or W and X, together with the nitrogen and carbon atoms to which they are attached, form a saturated or unsaturated nitrogen containing heterocyclic group which may be optionally substituted or optionally fused to a saturated or unsaturated carbocyclic group, aryl group or heterocyclic group is provided.Type: GrantFiled: December 4, 2002Date of Patent: October 17, 2006Assignee: The Australian National UniversityInventors: Martin Gerhardt Banwell, Bernard Luke Flynn
-
Patent number: 7105507Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: May 16, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
-
Patent number: 7094262Abstract: A dye composition for dyeing human keratin fibres, such as hair, comprising at least one dissymmetrical polycationic direct dye of formula (I) below: Col1-Z-Col2??(I) wherein: Col1 and Col2, which differ in structure, are chosen from tazo dyes, methine dyes, azomethine dyes, phenothiazine dyes, triarylmethane dyes, xanthene dyes, phenanthridine dyes and phthalocyanin dyes and Z is chosen from linear and branched, saturated, unsaturated and cyclic C1–C20 hydrocarbon-based groups comprising at least one nitrogen atom and bearing at least one cationic charge; and also to processes for dyeing human keratin fibres using the composition, to the use of the at least one dissymmetrical polycationic direct dye of formula (I) as direct dyes, and to multi-compartment devices.Type: GrantFiled: December 23, 2003Date of Patent: August 22, 2006Assignee: L'Oreal S.A.Inventor: Alain Lagrange
-
Patent number: 7078565Abstract: Disclosed are phenyl-alkylene benzamides useful as orexin antagonistsType: GrantFiled: October 30, 2002Date of Patent: July 18, 2006Assignee: SmithKline Beecham plcInventors: Wai Ngor Chan, Amanda Johns, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Mythily Vimal
-
Patent number: 7074796Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6Type: GrantFiled: June 27, 2002Date of Patent: July 11, 2006Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
-
Patent number: 7067533Abstract: The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q?, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C?O, NHC(?), and C(?O)NH, and Q? is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.Type: GrantFiled: April 13, 2001Date of Patent: June 27, 2006Assignee: Daiichi Asubio Pharma Co., Ltd.Inventors: Naohiro Takemoto, Hirokazu Annoura, Norihito Murayama
-
Patent number: 7067529Abstract: Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents are as disclosed in the specification. The compounds have utility for the treatment of type 2 diabetes mellitus.Type: GrantFiled: April 19, 2004Date of Patent: June 27, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David Robert Bolin, Shoaqing Chen, Steven Gregory Mischke, Yimin Qian
-
Patent number: 7053057Abstract: This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2, R, or —CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3 is hydrogen, an optionally substituted C1-6 alkyl, F2, CN, aryl or R3 is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0–2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.Type: GrantFiled: May 23, 2001Date of Patent: May 30, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, David Bebbington, Guy Brenchley, Ronald Knegtel, Michael Mortimore
-
Patent number: 7041681Abstract: This invention is directed towards novel compounds as opioid receptor modulators, antagonists, and agonists useful for the treatment of opioid modulated disorders such as pain and gastrointestinal disorders.Type: GrantFiled: March 26, 2003Date of Patent: May 9, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Henry J. Breslin, Wei He, Robert W. Kavash
-
Patent number: 7041667Abstract: Compounds of Formula 1 [Region ?]—[Region ?]—[Region ?]—[Region ?]??(1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: December 1, 1999Date of Patent: May 9, 2006Assignee: Pfizer, Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
-
Patent number: 7041829Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: GrantFiled: December 21, 2004Date of Patent: May 9, 2006Assignee: Magnesium Diagnostics, Inc.Inventor: Ibert Clifton Wells
-
Patent number: 7037924Abstract: Compounds of formula (I) are provided, wherein R1 and R2 are as designated in the specification. The compounds have utility for the treatment of type 2 diabetes mellitus.Type: GrantFiled: October 8, 2004Date of Patent: May 2, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David Robert Bolin, Shaoqing Chen, Steven Gregory Mischke, Yimin Qian
-
Patent number: 7030239Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: May 18, 2004Date of Patent: April 18, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
-
Patent number: 7026485Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 5, 2004Date of Patent: April 11, 2006Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
-
Patent number: 7026333Abstract: HIV protease inhibitors are disclosed which are characterized as having both hydroxyethylamine and N-heterocyclic moieties.Type: GrantFiled: July 26, 2000Date of Patent: April 11, 2006Assignee: G. D. Searle & Co.Inventors: Richard A Mueller, Daniel P. Getman
-
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
-
Patent number: 6992092Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2, Ra, Rb, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.Type: GrantFiled: April 15, 2004Date of Patent: January 31, 2006Assignee: Pfizer Inc.Inventors: Donald L. Bussolotti, Ronald B. Gammill
-
Patent number: 6987118Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: GrantFiled: May 5, 2004Date of Patent: January 17, 2006Assignee: Pfizer Inc.Inventor: George Chang
-
Patent number: 6984735Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.Type: GrantFiled: November 26, 2003Date of Patent: January 10, 2006Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark, Wei Li
-
Patent number: 6956033Abstract: A 3,4-dihydroisoquinoline derivative compound of formula (I) or a non-toxic salt thereof and a pharmaceutical agent comprising it as active ingredient (wherein all symbols have the same meaning as described in the specification). The compound of formula (I) has agonizing activity on CB2 receptor and therefore it is useful for the prophilaxis and/or treatment of various diseases such as asthma, nasal allergy, atopic dermatitis, autoimmune diseases, rheumatoid arthritis, immune dysfunction, postoperative pain, carcinomatous pain, etc.Type: GrantFiled: July 30, 2001Date of Patent: October 18, 2005Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mikio Ogawa, Yoshikazu Takaoka, Akira Ohhata
-
Patent number: 6949565Abstract: Novel isoquinoline derivatives which are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes are disclosed. Preferred compounds which are specific inhibitors of protein kinase B are also disclosed. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune diseases, are also disclosed.Type: GrantFiled: May 30, 2001Date of Patent: September 27, 2005Assignees: Develogen Israel Ltd., Yissum Research Development Co. of the Hebrew University of JerusalemInventors: Nurit Livnah, Alexander Levitzki, Hadas Reuveni
-
Patent number: 6943183Abstract: The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis.Type: GrantFiled: April 16, 2001Date of Patent: September 13, 2005Assignee: Pfizer IncInventors: William Alexander Denny, Richard H. Hutchings, Douglas S. Johnson, James Stanley Kaltenbronn, Ho Huat Lee, Daniele Marie Leonard, Jared Bruce John Milbank, Joseph Thomas Repine, Gordon William Rewcastle, Andrew David White
-
Patent number: 6939986Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.Type: GrantFiled: February 22, 2002Date of Patent: September 6, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Martin Karpf, René Trussardi
-
Patent number: 6936602Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.Type: GrantFiled: June 15, 2000Date of Patent: August 30, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
-
Patent number: 6930208Abstract: What is described are derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides. In this formula (I), R1a, R1b, R1c, R2, R3, R4 and R5 denote various radicals, X1 is a bridging atom, X2 is a carbon chain and X3 is a chalcogen atom or an oximino radical.Type: GrantFiled: April 8, 2003Date of Patent: August 16, 2005Assignee: Bayer CropScience GmbHInventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Monika H. Schmitt, Thomas Auler, Hermann Bieringer, Hubert Menne
-
Patent number: 6924294Abstract: The present invention provides novel compounds of Formula (I), or the pharmaceutically acceptable salts or prodrugs thereof, and methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine.Type: GrantFiled: December 19, 2001Date of Patent: August 2, 2005Assignee: Eli Lilly and CompanyInventors: Thomas John Bleisch, Ana Maria Castano Mansanet, Esteban Dominguez-Manzanares, Ana Maria Escribano
-
Patent number: 6916905Abstract: A compound of formula: wherein X is a spacer comprising one or more amino acid residues and Y comprises an aromatic group and related compositions and methods of use.Type: GrantFiled: December 21, 2001Date of Patent: July 12, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Lawrence H. Lazarus, Severo Salvadori
-
Patent number: 6908931Abstract: The invention encompasses a series of tetrahydroisoquinolines of formula I which are antagonists of the human melatonin MT2 receptor and are useful as chronobiotic and sleep agents.Type: GrantFiled: March 29, 2004Date of Patent: June 21, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Gene M. Dubowchik, Jonathan L. Ditta, Stephen R. Bertenshaw
-
Patent number: 6903103Abstract: Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): wherein: X represents carbonyl, sulphonyl or sulphoxide, G1, G2 and G3 are as defined in the description, T represents a fused phenyl group or a fused pyridyl group, R1 represents hydrogen, linear or branched (C1-C6)alkyl, aryl or aryl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, R2a and R2b, which are the same or different, are as defined in the description, R3 represents aryl or heteroaryl-A as defined in the description, each of which groups may optionally be substituted, Y represents aryloxy, heteroaryloxy or heteroaryl-B as defined in the description, each of which groups may optionally be substituted, its isomers, its hydrates, its solvates and addition salts thereof with a pharmaceutically aType: GrantFiled: February 20, 2003Date of Patent: June 7, 2005Assignee: Les Laboratories ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
-
Patent number: 6900319Abstract: The invention relates to a compound of the formula I: or a salt thereof with a physiologically tolerated acid, or stereoisomers thereof, wherein R1, R2, A, B, C and D have the meanings described in the specification.Type: GrantFiled: March 19, 2002Date of Patent: May 31, 2005Assignee: Abbott GmbH & Co. KGInventors: Hans-Joachim Boehm, Hans Wolfgang Höffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
-
Patent number: 6897319Abstract: This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.Type: GrantFiled: December 10, 2002Date of Patent: May 24, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John R. Carson, Ellen E. Codd, Philip M. Pitis
-
Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
-
Patent number: 6878706Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.Type: GrantFiled: March 27, 2003Date of Patent: April 12, 2005Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
-
Patent number: 6855717Abstract: Compounds of formula (I): wherein: R2 represents a hydrogen atom or a C1-4alkyl group; q is 1 or 2; A represents a group of formula (a) or (b) wherein T, U, V and Y independently represent CH or a nitrogen atom; R5 is a group selected from: a hydrogen or halogen atom, cyano, C1-4 alkyl or C1-4 alkoxy group s is 1 or 2; Ar2 represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; and salts thereof. The compounds are useful for the treatment of conditions which require modulaton of a dopamine receptor such as schizophrenia.Type: GrantFiled: February 14, 2003Date of Patent: February 15, 2005Assignee: SmithKline Beecham, plcInventors: Clive Leslie Branch, Christopher Norbert Johnson, Geoffrey Stemp
-
Patent number: 6849644Abstract: The invention relates to novel tetrahydroquinoline compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of various CNS disorders.Type: GrantFiled: November 16, 2001Date of Patent: February 1, 2005Assignee: SmithKline Beecham p.l.c.Inventors: Steven Mark Bromidge, Stephen Frederick Moss
-
Patent number: 6849622Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: October 5, 2001Date of Patent: February 1, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
-
Patent number: 6838465Abstract: This invention relates to novel compounds represented by the general formula [I]: (wherein, R1 and R4 are the same or different, and represent hydrogen atoms, lower alkyl groups or the like; R2 and R3 are the same or different, and represent lower alkoxy groups or lower alkyl groups; R5 represents a lower alkyl group or aralkyl group optionally having substituent(s); R6 represents a hydrogen atom or a lower alkyl group; X represents O, S or NH; m represents an integer of 0 to 3; n represents an integer of 0 or 1; and Ar represents a phenyl group or heteroaryl group optionally having substituent(s)). The compounds of the invention have an antagonistic action on orexin receptors, and are useful for treatment of appetite abnormality, obesity, sleeping disorder or the like.Type: GrantFiled: April 27, 2001Date of Patent: January 4, 2005Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Koji Yamada, Masaaki Hirose, Hisashi Iwaasa
-
Patent number: 6838479Abstract: Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.Type: GrantFiled: September 5, 2001Date of Patent: January 4, 2005Assignee: Genentech, Inc.Inventors: Richard M Pastor, Dean R. Artis, Alan G. Olivero
-
Publication number: 20040267010Abstract: Compounds possessing 5HT7 activity of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: 1Type: ApplicationFiled: July 27, 2004Publication date: December 30, 2004Inventors: Ian Thomson Forbes, Andrew Derrik Gribble
-
Publication number: 20040266817Abstract: The invention relates to novel tetrahydroisoquinoline derivatives of general formula I and theirs use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and their use as anti-infectives, wherein R1, R2 and R3 are as defined in claim 1.Type: ApplicationFiled: August 18, 2004Publication date: December 30, 2004Inventors: Kaspar Burri, Laurent Schmitt, Khalid Islam
-
Publication number: 20040266775Abstract: The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-pyrrole derivatives of formula (I) 1Type: ApplicationFiled: December 23, 2003Publication date: December 30, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Heinz-Werner Kleemann, Pascal Desmazeau, Jean-Christophe Carry, Baptiste Ronan, Serge Mignani, Jean Bououerel, Arielle Genevois-Borella
-
Publication number: 20040259843Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: ApplicationFiled: February 27, 2004Publication date: December 23, 2004Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
-
Publication number: 20040259910Abstract: Compounds of formula I are provided 1Type: ApplicationFiled: April 19, 2004Publication date: December 23, 2004Inventors: David Robert Bolin, Shoqing Chen, Steven Gregory Mischke, Yimin Qian
-
Publication number: 20040254215Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.Type: ApplicationFiled: June 4, 2004Publication date: December 16, 2004Applicant: FibroGen, Inc.Inventors: Michael P. Arend, Lee A. Flippin, Volkmar Guenzler-Pukall, Wen-Bin Ho, Eric D. Turtle, Xiaohui Du
-
Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley