One Of The Cyclos Is Five-membered Patents (Class 546/84)
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Publication number: 20090149491Abstract: The present invention discloses compounds of formula I, II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. More specifically, the invention relates to oxime compounds containing a carbocyclic P2 unit. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: November 13, 2008Publication date: June 11, 2009Inventors: Dong Liu, Yat Sun Or, Zhe Wang
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Publication number: 20090099226Abstract: The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.Type: ApplicationFiled: May 15, 2006Publication date: April 16, 2009Inventors: Michel Belley, Jason Burch, John Colucci, Julie Farand, Mario Girard, Yongxin Han
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Publication number: 20090093454Abstract: The present invention provides compounds of Formula (I) comprising: including salts, solvates, and physiologically functional derivatives thereof, pharmaceutical formulations containing them, processes for their preparation, and methods of treatment using them.Type: ApplicationFiled: March 1, 2006Publication date: April 9, 2009Inventors: Kristjan Gudmundsson, John G. Catalano, Angilique Svolto
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Publication number: 20090062327Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: April 10, 2006Publication date: March 5, 2009Inventors: Chixu Chen, Brian W. Eastman, Essa H. Hu
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Patent number: 7495111Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.Type: GrantFiled: June 15, 2006Date of Patent: February 24, 2009Assignee: WyethInventors: P. Sivaramakrishnan Ramamoorthy, Zhongqi Shen, Boyd L. Harrison
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Publication number: 20090042876Abstract: The present invention relates to inhibitors of protein kinases of formula I: which can be used in the treatment of various diseases, notably cancer, inflammation or disorders of the central nervous system. It also relates to pharmaceutical compositions containing the compounds according to the invention and their use in therapy.Type: ApplicationFiled: June 30, 2006Publication date: February 12, 2009Applicant: Pierre Fabre MedicamentInventors: Hugues Bienayme, Antoine Dumoulin, Serge Grisoni, Bachir Kaloun El, Stephane Poigny, Remi Rabot, Rachid Rahali, Eric Tam, Pascaline Klein, Karim Bedjeguelal, Houcine Rahali
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Publication number: 20090030027Abstract: Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors, and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: ApplicationFiled: June 12, 2006Publication date: January 29, 2009Applicant: LIGAND PHARMACEUTICALS INCORPORATEDInventors: Bijan Pedram, Cornelis Arjan Van Oeveren, Lin Zhi, Shuo Zhao, Yixing Shen
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Publication number: 20090029939Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl, Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.Type: ApplicationFiled: May 25, 2007Publication date: January 29, 2009Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
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Publication number: 20080318943Abstract: This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. These novel compounds provide a treatment or prophylaxis of anxiety disorders, schizophrenia, cognitive disorders, and/or mood disorders.Type: ApplicationFiled: June 18, 2008Publication date: December 25, 2008Applicant: ASTRAZENECA ABInventors: Hui-Fang Chang, Marc Chapdelaine, Bruce Thomas Dembofsky, Keith John Herzog, Carey Horchler, Richard Jon Schmiesing
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Publication number: 20080293694Abstract: The present invention relates to novel compounds of formula (I): wherein R1, R2, R3, R4, and R5 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: ApplicationFiled: March 13, 2008Publication date: November 27, 2008Applicant: Biovitrum AB (publ.)Inventors: Johan Angbrant, Peter Brandt, Rune Ringom, Bengt Lindqvist
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Publication number: 20080269230Abstract: This invention relates to the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH.Type: ApplicationFiled: September 18, 2007Publication date: October 30, 2008Applicant: PainCeptor Pharma CorporationInventors: Thomas Varming, Frank Watjen
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Patent number: 7439253Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and ?-lactamase inhibitors.Type: GrantFiled: December 4, 2003Date of Patent: October 21, 2008Assignee: NovexelInventors: Maxime Lampilas, Branislav Musicki, Michel Klich, David Alan Rowlands
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Publication number: 20080214597Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents C or N; Y represents C or N; L represents a methyl or a direct bond; Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH? (a) or —CH? (b); Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH? (a) or —CH? (b); R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR3R4 or C1-4alkyl optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8; R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-; R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R7 and R8 each inType: ApplicationFiled: August 26, 2005Publication date: September 4, 2008Applicant: JANSSEN PHARMACEUTICAL N.V.Inventors: Libuse Jaraskova, Joannes Theodorus Maria Linders, Louis Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Willemsens
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Patent number: 7407963Abstract: A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing the compound, their use, and processes for preparing them.Type: GrantFiled: June 27, 2005Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
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Patent number: 7390819Abstract: The compounds of formula I in which R1, R2, R3 and A have the meanings as given in the description are novel effective INOS inhibitors.Type: GrantFiled: February 24, 2004Date of Patent: June 24, 2008Assignee: Altana Pharma AGInventors: Thomas Martin, Wolf-Ruediger Ulrich
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Patent number: 7390818Abstract: The present invention relates to pyridoindolone derivatives substituted in the 3-position by a phenyl of general formula (I): to processes for preparing the same and to their use in therapeutics.Type: GrantFiled: April 19, 2005Date of Patent: June 24, 2008Assignee: Sanofi-AventisInventors: Bernard Bourrie, Pierre Casellas, Paola Ciapetti, Jean-Marie Derocq, Samir Jegham, Yvette Muneaux, Camille-Georges Wermuth
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Publication number: 20080146546Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.Type: ApplicationFiled: February 4, 2008Publication date: June 19, 2008Inventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
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Publication number: 20080132486Abstract: One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.Type: ApplicationFiled: June 9, 2004Publication date: June 5, 2008Applicant: Georgetown UniversityInventors: Alan P. Kozikowski, John L. Musachio, Kenneth J. Kellar, Yingxian Xiao, Zhi-Liang Wei
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Publication number: 20080125455Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system, cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apneaType: ApplicationFiled: November 21, 2007Publication date: May 29, 2008Inventors: Jonathan Richard Anthony Roffey, James Edward Paul Davidson, Howard Langham Mansell, Richard John Hamlyn, David Reginald Adams
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Publication number: 20080119507Abstract: This invention relates to isoindole derivates of Formula I to pharmaceutical compositions comprising such derivatives, and to methods of treatment comprising administering of such derivatives.Type: ApplicationFiled: September 28, 2007Publication date: May 22, 2008Applicant: Aventis Pharma S.A.Inventors: Patrick MAILLIET, Luc BERTIN, Didier BENARD, Chantal CARREZ, Francois VALLEE, Eric BACQUE
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Publication number: 20080113962Abstract: The invention relates to condensed tricyclic benzimidazoles of formula (I) in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.Type: ApplicationFiled: September 30, 2005Publication date: May 15, 2008Applicant: Aitana Pharma AGInventors: Peter Jan Zimmermann, Wilm Buhr, Christof Brehm, Andreas Palmer, M. Vittoria Chiesa, Wolfgang-Alexander Simon, Stefan Postius, Wolfgang Kromer
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Patent number: 7323473Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apneaType: GrantFiled: December 12, 2006Date of Patent: January 29, 2008Assignee: Vernalis Research LimitedInventors: Jonathan Richard Anthony Roffey, James Edward Paul Davidson, Howard Langham Mansell, Richard John Hamlyn, David Reginald Adams
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Patent number: 7323567Abstract: Compounds or enantiomers of formula (I) or a salt thereof: wherein R1, R2, R3, R4 and R5 are as defined herein, are useful for the manufacture of a medicament for the treatment or prevention of respiratory syncytial virus infection in a mammal.Type: GrantFiled: October 28, 2004Date of Patent: January 29, 2008Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Bruno Simoneau, Josee Bordeleau, Gulrez Fazal, Serge Landry, Steve Mason, Jean Rancourt
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Patent number: 7317020Abstract: Cribrostatin 6, a dark blue cancer cell growth inhibiting constituent of the Republic of Maldives marine sponge Cribrochalina sp. has been isolated, and its structure (shown below) elucidated, based on a combination of RMS, high field (500 MHz, HMBC, and GOESY experiments) 15N, 1H- and 13C NMR, and X-ray crystal structure analyses. Cribrostatin 6 also was found to inhibit the growth of a number of pathogenic bacteria and fungi.Type: GrantFiled: February 19, 2004Date of Patent: January 8, 2008Assignee: Arizona Board of Regents, a body corporate of the State of ArizonaInventors: George R. Pettit, John C. Knight
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Patent number: 7309789Abstract: Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.Type: GrantFiled: May 22, 2006Date of Patent: December 18, 2007Assignee: AMR Technology, Inc.Inventors: James P. Beck, Anthony D. Pechulis, Arthur E. Harms
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Patent number: 7288653Abstract: This invention relates to the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH.Type: GrantFiled: September 30, 2005Date of Patent: October 30, 2007Assignee: PainCeptor Pharma CorporationInventors: Thomas Varming, Frank Wätjen
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Patent number: 7288549Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds, as well as their use as medicaments, in particular as anti-bacterial agents.Type: GrantFiled: June 4, 2002Date of Patent: October 30, 2007Assignee: Aventis Pharma S.A.Inventors: Joseph Aszodi, Maxime Lampilas, Branislav Musicki, David Alan Rowlands, Pascal Colette
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Patent number: 7253180Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.Type: GrantFiled: October 16, 2003Date of Patent: August 7, 2007Assignee: Gilead Sciences, Inc.Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
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Patent number: 7238699Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: February 4, 2004Date of Patent: July 3, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Bireshwar Dasgupta, Gene M. Dubowchik, John E. Macor
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Patent number: 7211669Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: January 29, 2004Date of Patent: May 1, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta
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Patent number: 7176213Abstract: The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and (III) and to the preparation thereof.Type: GrantFiled: December 17, 2002Date of Patent: February 13, 2007Assignee: Sanofi-AventisInventors: Péter Arányi, László Balázs, Mária Balogh, Sándor Bátori, Kinga Boér, Katalin Gerber, Zoltán Kapui, Endre Mikus, Geza Tímári, T. Nagy Lajos, Katalin Urbán-Szabó, Judit Vargáné Szeredi
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Patent number: 7166613Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apneaType: GrantFiled: April 29, 2005Date of Patent: January 23, 2007Assignee: Vernalis Research LimitedInventors: Jonathan Richard Anthony Roffey, James Edward Paul Davidson, Howard Langham Mansell, Richard John Hamlyn, David Reginald Adams
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Patent number: 7153967Abstract: The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.Type: GrantFiled: December 23, 2004Date of Patent: December 26, 2006Assignee: TEVA Gyógyszergyár Zártkörüen Müködö RészvénytársaságInventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi
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Patent number: 7115621Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disordersType: GrantFiled: April 2, 2002Date of Patent: October 3, 2006Assignee: Lilly Icos LLCInventors: Jason S. Sawyer, Mark W. Orme, James D. Copp
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Patent number: 7105663Abstract: Compounds of general formula (I) wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6)alkylamino or C2-7 acylamino group, each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkythio, C1-6 alkoxy or C3-6 cycloalkyl group; X represents OCH2 or a group CR3R4, wherein each of R3 and R4 independently represents a hydrogen atom or a C1-3 alkyl group; each of R10 and R11 independently represents a hydrogen atom, a C1-3 alkyl, C3-6 cycloalkyl or phenyl group; y represents an oxygen atom or a group CHNO2, NCN, NH or NNO2, n is aType: GrantFiled: February 24, 2004Date of Patent: September 12, 2006Assignee: Rhinopharma LimitedInventors: Alexander William Oxford, David Jack
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Patent number: 7091214Abstract: Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.Type: GrantFiled: December 18, 2003Date of Patent: August 15, 2006Assignee: 3M Innovative Properties Co.Inventors: David S. Hays, Shri Niwas, Tushar Kshirsagar, Philip D. Heppner, Bryon A. Merrill, Michael E. Danielson, John F. Gerster, Chad A. Haraldson, Maureen A. Kavanagh, Michael J. Rice, Sarah A. Strong, Joshua R. Wurst
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Patent number: 7087607Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.Type: GrantFiled: October 18, 2002Date of Patent: August 8, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Sundermann
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Patent number: 7074927Abstract: Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 and R2 are independently hydrogen, C1-6 alkyl or R1 and R2 are joined to form pyrrolidine, piperidine, morpholine or imidazole. X is OCH3, SO2R3, SO2CF3 or CN where R3 is C1-6 alkyl or an Aryl; and Y is hydrogen, Cl, Br, F, CN, CONR1R2, CF3, OCH3, SO2NR1R2. These new compounds are suitable for treating anxiolytic disorder, schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure or treating migraine headaches in patients in need of such treatment.Type: GrantFiled: December 23, 2004Date of Patent: July 11, 2006Assignee: Pharmacia & Upjohn CompanyInventor: Arthur G. Romero
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Patent number: 7071180Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are asType: GrantFiled: June 22, 2004Date of Patent: July 4, 2006Assignee: Biovitrum ABInventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
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Patent number: 7037919Abstract: Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical compositions containing the derivatives or the salts.Type: GrantFiled: October 6, 2000Date of Patent: May 2, 2006Assignee: Kaken Pharmaceutical Co. Ltd.Inventors: Keigo Hanada, Kazuyuki Furuya, Kiyoshi Inoguchi, Motonori Miyakawa, Naoya Nagata
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Patent number: 7026484Abstract: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.Type: GrantFiled: February 22, 2002Date of Patent: April 11, 2006Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Robert I. Higuchi
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Patent number: 6992192Abstract: Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: May 2, 2002Date of Patent: January 31, 2006Assignee: Lilly Icos LLC.Inventors: Jason S. Sawyer, Mark W. Orme
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Patent number: 6989389Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and aryl or alkenyl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.Type: GrantFiled: October 29, 2003Date of Patent: January 24, 2006Assignee: 3M Innovative Properties Co.Inventors: Philip D. Heppner, Leslie J. Charles, Joseph F. Dellaria, Bryon A. Merrill, John W. Mickelson
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Patent number: 6989388Abstract: The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula: wherein the constituent variables are as defined herein. The invention further provides methods for the use of the compounds disclosed herein.Type: GrantFiled: October 30, 2001Date of Patent: January 24, 2006Inventors: Roberto Pellicciari, Flavio Moroni
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Patent number: 6984646Abstract: The invention relates to imidazopyridinones of the formula wherein the groups R1, R2, R3, and R4 are as defined in claim 1, to the process for their preparation, to pharmaceutical compositions containing them, and to a method of using them for treatment of chronic inflammatory processes in humans or animals.Type: GrantFiled: July 15, 2002Date of Patent: January 10, 2006Assignee: Bayer Healhcare AGInventors: Cristina Alonso-Alija, Martin Michels, Hartmut Schirok, Karl-Heinz Schlemmer, Sara Dodd, Mary Fitzgerald, John Bell, Andrew Gill
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Patent number: 6977298Abstract: Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.Type: GrantFiled: December 3, 2004Date of Patent: December 20, 2005Assignees: Agouron Pharmacetucals, Inc., Cancer Research Campaign Technology LimitedInventors: Stephen Evan Webber, Stacie S. Canan-Koch, Jayashree Tikhe, Lars Henrik Thoresen
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Patent number: 6974824Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors relative to nor-BNI, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: GrantFiled: January 8, 2001Date of Patent: December 13, 2005Assignee: Research Triangle InstituteInventors: F. Ivy Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 6953791Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: February 21, 2003Date of Patent: October 11, 2005Assignee: Pfizer, Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Patent number: 6953804Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and aryl or alkenyl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.Type: GrantFiled: October 29, 2003Date of Patent: October 11, 2005Assignee: 3M Innovative Properties Co.Inventors: Joseph F. Dellaria, John W. Mickelson
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Patent number: 6949649Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.Type: GrantFiled: October 29, 2003Date of Patent: September 27, 2005Assignee: 3M Innovative Properties Co.Inventors: Jason D. Bonk, Joseph F. Dellaria, Bryon A. Merrill, Matthew R. Radmer