Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/322)
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Publication number: 20110046132Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: April 28, 2009Publication date: February 24, 2011Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, JR., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Publication number: 20110039891Abstract: A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: wherein the ring X is a benzene ring or a pyridine ring; R1 and R2 are hydrogen or alkyl or together form a cycloalkene ring; R3 is hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; R4 is hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and R5 is a halogen atom or a hydrogen atom.Type: ApplicationFiled: October 20, 2010Publication date: February 17, 2011Applicants: UBE INDUSTRIES, LTD., SANTEN PHARMACEUTICAL CO., LTD.Inventors: Masahiko Hagihara, Ken-ichi Komori, Hidetoshi Sunamoto, Hiroshi Nishida, Takeshi Matsugi, Tadashi Nakajima, Masakazu Hatano, Kazutaka Kido, Hideaki Hara
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Publication number: 20110039857Abstract: The invention relates to piperidine and pyrrolidine compounds of formula (I) wherein A, B, n and X are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: April 29, 2009Publication date: February 17, 2011Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20110034512Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: April 23, 2009Publication date: February 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darren Disalvo, Daniel Kuzmich, Can Mao, Hossein Razavi, Christopher Sarko, Alan David Swinamer, David Smith Thomson, Qiang Zhang
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Publication number: 20110034441Abstract: Described herein are methods of treating a disorder or disease in which aberrant Wnt signaling is implicated, with a variety of compounds, including Wnt inhibitor compounds. More particularly, it concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components.Type: ApplicationFiled: August 9, 2010Publication date: February 10, 2011Applicant: EPITHERIX, LLCInventors: John Hood, Sunil Kumar KC
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Patent number: 7884102Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: April 28, 2008Date of Patent: February 8, 2011Assignee: Adolor CorporationInventors: Roland Ellwood Dolle, Bertrand Le Bourdonnec
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Publication number: 20110028447Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.Type: ApplicationFiled: February 26, 2009Publication date: February 3, 2011Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
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Patent number: 7879850Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: GrantFiled: September 26, 2008Date of Patent: February 1, 2011Assignee: Novartis AGInventors: Young-Shin Kwak, Gary Mark Coppola
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Publication number: 20110014127Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.Type: ApplicationFiled: January 5, 2009Publication date: January 20, 2011Inventor: Bernard P. Schachtel
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Publication number: 20110015183Abstract: The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to pyrazole derivatives of formula I and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.Type: ApplicationFiled: September 29, 2010Publication date: January 20, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jordi CORBERA ARJONA, Maria Rosa CUBERES-ALTISENT, Joerg HOLENZ, Daniel MARTÍNEZ-OLMO, David VAÑO-DOMENECH
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Publication number: 20110009389Abstract: There is provided an imidazole derivative useful as a thrombosis treating agent, which is represented by the formula (I): wherein R represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent linear hydrocarbon group, X represents an optionally substituted divalent hydrocarbon group, Y represents —CO—, —S(O)—, —S(O)2— or a bond, ring A represents an optionally substituted pyrrolidine ring, an optionally substituted piperidine ring or an optionally substituted perhydroazepine ring, Z1 and Z3 independently represent a bond or an optionally substituted divalent linear hydrocarbon group, Z2 represents —N(R1)—, —O—, —S(O)—, —S(O)2—, —CO—, —CH(R1)— or a bond, ring B represents an optionally substituted imidazole ring, wherein a substituent which the optionally substituted imidazole ring represented by ring B may have may be taken together with R1 to form an optionally substituted ring, and a represents 0Type: ApplicationFiled: September 10, 2010Publication date: January 13, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Keiji KUBO, Takanobu KUROITA, Yasuhiro IMAEDA, Masaki KAWAMURA
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Publication number: 20110003797Abstract: The present invention is directed to hexahydrocyclopentyl[f]imidazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 16, 2009Publication date: January 6, 2011Inventors: William P. Dankulich, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Patent number: 7863310Abstract: The present invention provides kinase inhibitors of Formula I:Type: GrantFiled: January 21, 2005Date of Patent: January 4, 2011Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Robert Dean Dally, Alfonso de Dios, Mirian Filadelfa del Prado Catalina, Carmen Dominguez-Fernandez, Carlos Jaramillo Aguado, Beatriz Lopez de Uralde-Garmendia, Timothy Alan Shepherd
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Publication number: 20100324020Abstract: The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R1-R5 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Stanton F. McHardy, John A. Lowe, III
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Publication number: 20100317618Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1.Type: ApplicationFiled: March 6, 2009Publication date: December 16, 2010Applicant: AZIENDE CHIM. RIUN. ANGEL. FRA. A.C.R.A.F. S.p.A.Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
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Patent number: 7851630Abstract: The invention relates to a group of hydronopol substituted benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel benzimidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.Type: GrantFiled: September 29, 2004Date of Patent: December 14, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Jacobus A. J. Den Hartog, Samuel David, Daniel Jasserand, Gustaaf J. M. Van Scharrenburg, Herman H. Van Stuivenberg, Tinka Tuinstra
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Publication number: 20100311709Abstract: The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 23, 2007Publication date: December 9, 2010Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
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Publication number: 20100305140Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein X, A, R1, R2, R3 and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: June 11, 2007Publication date: December 2, 2010Applicant: AstraZeneca ABInventors: William Brown, Daniel Page, Sanjay Srivastava, Christopher Walpole, Zhong-Yong Wei, Hua Yang
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Publication number: 20100305120Abstract: Compounds of formula (I): wherein X, L1, R1, L2, R2, R3, and R4 are as defined herein, are useful in the treatment or prophylaxis of Duchenne muscular dystrophy, Becker muscular dystrophy, or cachexia.Type: ApplicationFiled: April 3, 2009Publication date: December 2, 2010Inventors: Graham Michael Wynne, Stephen Paul Wren, Renate Maria Van Well, Daniel Robert Chancellor, Frank Schroer, Francis Xavier Wilson
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Publication number: 20100298313Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: ApplicationFiled: August 4, 2010Publication date: November 25, 2010Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Publication number: 20100298305Abstract: Disclosed herein are methods of treating a psychiatric disorder, such as a sleep disorder, an anxiety disorder, a mood disorder or a perceptual disturbance. In one example, a method of treating a sleep disorder or anxiety disorder includes selecting a subject with a sleep disturbance or anxiety disorder in the absence of an underlying physical disorder and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the sleep disorder or anxiety disorder. In another example, a method of treating a mood disorder or a perceptual disturbance is disclosed. This method includes selecting a subject with a mood disorder or perceptual disturbance and administering a therapeutically effective amount of tizanidine, thereby reducing or inhibiting a symptom of the mood disorder or perceptual disturbance.Type: ApplicationFiled: November 25, 2009Publication date: November 25, 2010Inventor: Bruce Capehart
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Publication number: 20100298380Abstract: This invention relates to novel N-aryl-N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: July 31, 2008Publication date: November 25, 2010Applicant: NeuroSearch A/SInventors: Dan Peters, John Paul Redrobe, Gordon Munro, Elsebet Østergaard Nielsen
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Publication number: 20100298378Abstract: The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description, as well as to pharmaceutical compositions containing them and to methods of treatment using them.Type: ApplicationFiled: July 29, 2010Publication date: November 25, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Petra LENNIG
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Publication number: 20100298377Abstract: This disclosure relates to compounds of formula (I): wherein R1, R2, R3, R4, E, and n1 are as defined in the disclosure, to compositions containing them, to processes for preparing them, and the use thereof.Type: ApplicationFiled: December 11, 2009Publication date: November 25, 2010Applicant: SANOFI-AVENTISInventors: Michel ALETRU, Dominique DAMOUR, Patrick MOUGENOT, Frederico NARDI, Patrick NEMECEK, Christophe PHILIPPO, Catherine MONSEAU, Claudie NAMANE
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Publication number: 20100292214Abstract: The Invention relates to compounds having an antiparasitic activity, and to their use as a drug, in particular as a drug for the prevention and/or treatment of parasitic diseases caused by apicomplexans. The invention also relates to pharmaceutical compositions containing those compounds.Type: ApplicationFiled: June 2, 2008Publication date: November 18, 2010Applicants: commissariat a l'Energie Atomique, Centre National De La Recherche ScientifiqueInventors: Michael Deligny, Nadia Saidani, Anne-Laure Bonneau, Cyrille Botte, Helene Hardre, Bernard Rousseau, Henri Vial, Corinne Mercier, Roman Lopez, Eric Marechal
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Publication number: 20100292266Abstract: Certain oxazolyl piperidine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: May 25, 2007Publication date: November 18, 2010Inventors: Richard Apodaca, James Guy Breitenbucher, Alison L. Chambers, Mark Seierstad, Wei Xiao
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Publication number: 20100292207Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 8, 2008Publication date: November 18, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20100292234Abstract: The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R1 and R5 are defined herein. The invention further provides pharmaceutical compositions including one or more compounds of Formula I, use of such compounds and compositions for treatment of p38 MAP kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: September 19, 2008Publication date: November 18, 2010Applicant: Amgen Inc.Inventors: Liping H. Pettus, Kelvin K.C. Sham, Andrew Tasker, Shimin Xu
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Publication number: 20100286202Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: October 14, 2009Publication date: November 11, 2010Applicant: AstraZeneca ABInventors: Yevgeni Besidski, Martin Nylöf, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
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Publication number: 20100286191Abstract: The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.Type: ApplicationFiled: December 8, 2006Publication date: November 11, 2010Inventors: Rachel G. Samuel, Conrad Santini
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Publication number: 20100286114Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: ApplicationFiled: December 10, 2008Publication date: November 11, 2010Applicant: SIENA BIOTECH S.P.A.Inventors: Russell John Thomas, Gal.la Pericot Mohr, Giacomo Minetto, Annette Cornelia Bakker, Pietro Ferruzzi
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Publication number: 20100286203Abstract: The present invention relates to pharmaceutically acceptable salts of an amide substituted indazole which are inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), previously known as poly(ADP-ribose)synthase and poly(ADP-ribosyl) transferase. The compounds of the present invention are useful as mono-therapies in tumors with specific defects in DNA-repair pathways and as enhancers of certain DNA-damaging agents such as anticancer agents and radiotherapy. Further, the compounds of the present invention are useful for reducing cell necrosis (in stroke and myocardial infarction), down regulating inflammation and tissue injury, treating retroviral infections and protecting against the toxicity of chemotherapy.Type: ApplicationFiled: January 8, 2009Publication date: November 11, 2010Inventors: Jennifer R. Foley, Robert Darrin Wilson
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Publication number: 20100286088Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.Type: ApplicationFiled: December 16, 2008Publication date: November 11, 2010Applicant: PHARMINOX LIMITEDInventors: Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
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Patent number: 7829559Abstract: The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to pyrazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.Type: GrantFiled: August 29, 2005Date of Patent: November 9, 2010Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent, Joerg Holenz, Daniel Martínez-Olmo, David Vaño-Domenech
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Publication number: 20100279991Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: ApplicationFiled: July 15, 2010Publication date: November 4, 2010Inventors: Fina Liotta, Mingde Xia, Michael P. Wachter, Scott A. Beers
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Publication number: 20100280016Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Marvin J. Meyers, Graciela B. Arhancet, XiangYang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
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Publication number: 20100280071Abstract: Compounds of formula (I), salts and solvates are provided: Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.Type: ApplicationFiled: March 20, 2007Publication date: November 4, 2010Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Publication number: 20100273794Abstract: This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.Type: ApplicationFiled: July 7, 2010Publication date: October 28, 2010Applicant: Pfizer Inc.Inventors: Yasuhiro Katsu, Satoru Iguchi, Hiroki Sone, Chikara Uchida, Takashi Kojima
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Publication number: 20100273791Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.Type: ApplicationFiled: April 29, 2010Publication date: October 28, 2010Inventors: Braj Bhushan LOHRAY, Vidya Bhushan Lohray, Brijesh Srivastava
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Publication number: 20100273778Abstract: This invention discloses a method of treatment of osteoarthritis pain by administration of a histamine H3 receptor antagonist, described herein, a salt thereof, or a composition comprising such compound or salt.Type: ApplicationFiled: April 26, 2010Publication date: October 28, 2010Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Gin C. Hsieh, Jorge D. Brioni, James P. Sullivan
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Patent number: 7820657Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: March 16, 2007Date of Patent: October 26, 2010Assignee: Ambit Biosciences CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Patent number: 7820659Abstract: The present invention discloses novel compounds of Formula I: (I) having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: GrantFiled: April 19, 2007Date of Patent: October 26, 2010Assignee: Eli Lilly and CompanyInventors: Ashraf Saeed, Owen Brendan Wallace, Yanping Xu, Thomas Edward Mabry, Rebecca Lynn Rezac Guenther, Nancy June Snyder
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Publication number: 20100267704Abstract: This invention pertains to a class of autophagy inducing compounds that treat diseases caused by misfolded protein aggregates and a screening method for identifying these compounds.Type: ApplicationFiled: October 10, 2008Publication date: October 21, 2010Applicants: President an Fellows of Harvard Colege, Shangha Institute of Organic Chemistry Chineesse Academy of SciencesInventors: Junying Yuan, Dawei Ma, Lihong Zhang
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Publication number: 20100266699Abstract: A pharmaceutical suspension having a therapeutically effective amount of phenylephrine and a therapeutically effective amount of a first active agent consisting essentially of a first substantially water insoluble active agent having an average particle size of between about 10 and about 100 microns, an effective amount of non-reducing sweetener; an effective amount of water; and an effective amount of a suspending system; wherein the pharmaceutical suspension has a pH of from about 4 to about 6 and is substantially free of a reducing sugar and related methods.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Inventors: Gail K. Buehler, Edward A. Koch, Dana J. Rechen
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Publication number: 20100267710Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 21, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20100261717Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 14, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20100256138Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).Type: ApplicationFiled: June 14, 2010Publication date: October 7, 2010Applicant: S*BIO Pte Ltd.Inventors: Dizhong Chen, Hong Y. Song, Eric T. Sun, Niefang Yu, Yong Zou
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Publication number: 20100255096Abstract: Compositions of domperidone formulated for transmucosal delivery are provided. Also provided are methods for the treatment of nausea, vomiting, and gastrointestinal motility disorders, and methods for the enhancement of breast milk production. The methods utilize domperidone compositions formulated for transmucosal administration, administered to patients in an amount effective to treat nausea, vomiting, or gastrointestinal motility disorders, or to enhance breast milk production.Type: ApplicationFiled: April 25, 2008Publication date: October 7, 2010Inventor: Craig A. Aronchick
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Publication number: 20100256188Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.Type: ApplicationFiled: March 4, 2010Publication date: October 7, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
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Publication number: 20100256140Abstract: The present invention relates to Indol-3-yl-carbonyl-piperidin-benzoimidazol derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R7 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephritic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.Type: ApplicationFiled: June 21, 2010Publication date: October 7, 2010Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider