The Additional Five-membered Hetero Ring Also Has Chalcogen As A Ring Member Patents (Class 514/254.02)
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Publication number: 20110160211Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).Type: ApplicationFiled: April 27, 2009Publication date: June 30, 2011Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
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Patent number: 7968577Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Publication number: 20110152287Abstract: The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Alfonzo D. Jordan, Renee L. DesJarlais, Dennis J. Hlasta, Michael H. Parker, Carsten Schubert, Kimberly White
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Publication number: 20110150864Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20110152245Abstract: The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Inventors: Katrin Groebke Zbinden, Roger Norcross, Philippe Pflieger
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Patent number: 7964604Abstract: The present disclosure provides novel pharmaceutical dosage forms such as a maintenance treatment dose and methods for making the same, and methods for using said compounds and maintenance treatment doses to treat and prevent diseases and/or disorders.Type: GrantFiled: March 23, 2007Date of Patent: June 21, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Irene Eijgendaal, Gerrit Klein, Maria J. L. Terhorst-Van Amstel, Klaas Zwier, Nico Bruins, Hendrikus T. Rigter, Erik Gout, Caroline Boon, Michiel H. De Vries, Dorte Malling, Anneke Winsemius, Sangeeta Raje, Ellen Bech Christensen, Jeff Paul
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Publication number: 20110144123Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 27, 2010Publication date: June 16, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Mark Thomas Miller, Sara S. Hadida Ruah, Peter Diederik Jan Grootenhuis, Matthew Hamilton
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Patent number: 7960385Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 5, 2008Date of Patent: June 14, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110136735Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 30, 2010Publication date: June 9, 2011Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
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Publication number: 20110136822Abstract: At least one crystalline hydrate of (S)—[N-3-(3?-fluoro-4?-(4?-phenyl piperazinyl))phenyl-2-oxo-5-oxazolidinyl]methyl acetamide, such as those with the following formula: wherein y is a number ranging from 1/12 to 1. Also provided are methods for the preparation of such crystalline hydrates, pharmaceutical compositions comprising such crystalline hydrates, and methods for their uses.Type: ApplicationFiled: November 3, 2010Publication date: June 9, 2011Inventors: Feng Que, Ying Wang
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Publication number: 20110130402Abstract: The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators which increase insulin secretion for the treatment of type II diabetes.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: Novo Nordisk A/SInventors: Lone Jeppesen, Marit Kristiansen
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Publication number: 20110124621Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: October 8, 2008Publication date: May 26, 2011Inventors: Jack McQueen Allen, Roger John Butlin, Clive Green, William Mccoull, Graeme Richard Robb, James Matthew Wood
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Publication number: 20110124624Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: February 3, 2011Publication date: May 26, 2011Inventors: Graham Charles Bloomfield, Ian Bruce, Judy Fox Hayler, Catherine LeBlanc, Darren Mark Le Grand, Clive McCarthy
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Patent number: 7943623Abstract: A pharmaceutical composition according to the present invention comprises: (I) at least one member selected from the group consisting of oxazole compounds, optically active isomers thereof, and salts thereof, the oxazole compounds being represented by general formula (1): wherein R1 represents a hydrogen atom or C1-6 alkyl group; n represents an integer from 0 to 6; and R2 represents, for example, a group of general formula (A) shown below: wherein R3 represents a phenoxy group, optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms, halo-substituted or unsubstituted C1-6 alkyl groups, and halo-substituted or unsubstituted C1-6 alkoxy groups; and (II) at least one cellulose compound selected from the group consisting of hydroxypropyl methylcellulose phthalate and hydroxypropyl methylcellulose acetate succinate. The present pharmaceutical composition has an improved oxazole compound water solubility.Type: GrantFiled: July 19, 2006Date of Patent: May 17, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventor: Junichi Kawasaki
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Publication number: 20110112075Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: August 18, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Markus FOLLMANN, Volkmar WEHNER, Jerome MENEYROL, Jean-Michel ALTENBURGER, Frédéric PETIT, Gilbert LASSALLE, Jean-Pascal HERAULT
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Publication number: 20110111021Abstract: The present invention provides a pharmaceutical preparation including a compartment containing a renin inhibitor as a pharmacologically active ingredient, and a compartment containing an HMG-CoA reductase inhibitor as a pharmacologically active ingredient, wherein one compartment is a prior-release compartment and the other compartment is a delayed-release compartment. The combination preparation of the present invention can deliver a renin inhibitor and an HMG-CoA reductase inhibitor with a time interval at a specific speed, thus reducing undesirable side-effects, improving the drug efficacy and promoting the patient compliance. Further, the pharmaceutical preparation of the present invention has pharmacological, clinical, scientific and economical advantages in the prevention or treatment of metabolic syndromes, cardiovascular diseases, renal diseases and the like, as compared with the complex drug regimens in which medicament ingredients are taken individually or simultaneously.Type: ApplicationFiled: February 23, 2009Publication date: May 12, 2011Applicant: HANALL BIOPHARMA CO., LTD.Inventors: Sung Wuk Kim, Sung Soo Jun, Young Gwan Jo, Ja Seong Koo, Jaw Woon Son, Jin Wook Kim
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Publication number: 20110105469Abstract: Methods and compositions that relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a SULT4A1-1 haplotype are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the haplotype status.Type: ApplicationFiled: November 3, 2010Publication date: May 5, 2011Applicant: Suregene, LLCInventors: Timothy L. Ramsey, Mark D. Brennan
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Publication number: 20110105523Abstract: The present invention relates to bifeprunox derivatives of formula (I) wherein R1 is one substituent chosen from 3-OH, 4-OH, 3-OSO3H and 4-OSO3H; R2 is H; or an N-oxide or a pharmaceutically acceptable salt, or a solvate or hydrate of any of the foregoing. The compounds of the invention may be used in the treatment or alleviation of dopamine D2 receptor mediated diseases or conditions.Type: ApplicationFiled: January 14, 2009Publication date: May 5, 2011Inventors: Herman H. Van Stuivenberg, Gerrit A. Barf
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Publication number: 20110105468Abstract: Methods and compositions relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a SULT4A1-1 haplotype are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the haplotype status.Type: ApplicationFiled: August 18, 2010Publication date: May 5, 2011Inventors: Timothy L. Ramsey, Mark D. Brennan
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Patent number: 7935703Abstract: Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.Type: GrantFiled: January 5, 2007Date of Patent: May 3, 2011Assignee: AstraZeneca ABInventors: Abdelmalik Slassi, Methvin Isaac, Jalaj Arora, Dean Brown
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Publication number: 20110092475Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.Type: ApplicationFiled: October 20, 2010Publication date: April 21, 2011Applicant: H. LUNDBECK A/SInventors: Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Mathivanan Packiarajan, Michel Grenon
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Publication number: 20110092517Abstract: Provided herein are methods for treatment, prevention, or amelioration of one or more symptoms of a disease or condition related to disorders of insulin and/or glucose metabolism, inflammatory conditions, mitochondrial disease, muscle disorders, or pulmonary disorders, involving administering a PPAR? agonist or a pharmaceutical composition comprising a PPAR? agonist. In one embodiment, the disease or condition is selected from myopathy, inflammatory vascular diseases, Parkinson's and Alzheimer's diseases, systemic inflammatory disorders, renal ischemia, inflammatory rheumatic disorders, and inflammatory diseases of the lung. In another embodiment, methods for increasing oxidative muscle fibers, reducing mitochondria disease, decreasing insulin resistance, decreasing plasma glucose, or decreasing weight, involving administering a PPAR? agonist or a pharmaceutical composition comprising a PPAR? agonist, are provided.Type: ApplicationFiled: August 13, 2010Publication date: April 21, 2011Inventors: Ronald Barbaras, Daniela Carmen Oniciu, Jean-Louis H. Dasseux, Robert A. Scott, John R. Wetterau
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Publication number: 20110086833Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.Type: ApplicationFiled: May 27, 2009Publication date: April 14, 2011Inventors: Sergey V. Paushkin, Nikolai Naryshkin, Charles Romfo, Ellen Welch
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Publication number: 20110086843Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: November 23, 2010Publication date: April 14, 2011Applicant: MERCK SERONO SAInventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
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Publication number: 20110086862Abstract: This invention relates to a process for the preparation of 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride, a partial dopamine-D2 receptor agonist and a full serotonin 5-HT1A receptor agonist. 7-(4-methyl-1-piperazinyl)benzoxazol-2(3H)-one hydrochloride The invention also relates to polymorphic forms of said compound, as well as to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, to methods for preparing intermediates useful for their synthesis, and to methods for preparing compositions containing these compounds.Type: ApplicationFiled: October 10, 2010Publication date: April 14, 2011Inventors: Jeroen Van Rheenen, Wilhelmus G.H.M. Muijselaar, Hendrik Teunissen
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Patent number: 7919489Abstract: The invention relates to heterocyclylamide-substituted imidazoles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: August 20, 2007Date of Patent: April 5, 2011Assignee: Aicuris GmbH & Co. KGInventors: Holger Zimmermann, David Brueckner, Kerstin Henninger, Ulrich Rosentreter, Martin Hendrix, Joerg Keldenich, Dieter Lang, Martin Radtke, Daniela Paulsen, Armin Kern
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Patent number: 7915262Abstract: A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.Type: GrantFiled: July 27, 2010Date of Patent: March 29, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Andrew C McCreary, Gustaaf J. M. Van Scharrenburg, Martinus Th. M. Tulp
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Patent number: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20110070319Abstract: The present disclosure is directed to compositions, kits and methods for not only treating schizophrenia, e.g., maintaining, reducing and/or improving at least one symptom of schizophrenia, but also to achieving an absence of or a reduced presence of at least one side effect associated with schizophrenia therapy with a first-generation atypical antipsychotic.Type: ApplicationFiled: November 19, 2010Publication date: March 24, 2011Inventors: Michel BOURIN, Daniel E. Casey, Steven G. Potkin, Mark Rapaport, John Newcomer, Paul P. Yeung, Sangeeta Raje, Jeff Paul, Saeed Ahmed, Luigi M. Barbato, Nathan A. Shapira, Roseline Pardue, Antje A. Winsemius, Michiel H. de Vries, Marc Debelle, Jens Heisterberg, Mette Krog Josiassen, Jette Buch Ostergard, Dorte Malling, Ellen B. Christensen
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Publication number: 20110065691Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.Type: ApplicationFiled: September 22, 2010Publication date: March 17, 2011Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
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Publication number: 20110059970Abstract: The present invention relates to new 4-phenyl-1,3-azole derivatives having the general formula (I) wherein R1, R2, R3, R4, X, A, B, and n are variable, in a racemic form, an enantiomeric form or any combinations thereof. These compounds exhibit affinity for cannabinoid receptors and may therefore be used as drugs to treat or prevent pathological states and diseases in which one or more of these receptors are involved. The invention also relates to pharmaceutical compositions containing said products and to the use thereof to prepare a drug.Type: ApplicationFiled: September 11, 2008Publication date: March 10, 2011Applicant: IPSEN PHARMA S.A.S.Inventor: Jeremiah Harnett
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Publication number: 20110059984Abstract: The present invention relates to compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: November 8, 2010Publication date: March 10, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Dean Wilson, Andreas Termin, Lev T. D. Fanning, Paul Krenitsky, Pramod Joshi
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Publication number: 20110053955Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: February 7, 2008Publication date: March 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
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Publication number: 20110053866Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.Type: ApplicationFiled: August 12, 2010Publication date: March 3, 2011Applicant: Biovail Laboratories International (Barbados) S.R.L.Inventors: Andrew John Duffield, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
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Publication number: 20110046153Abstract: A compound of formal (I) is described: wherein R1 and R2 are as defined in the text and wherein the compounds are intended for use in treating medical conditions characterized by an imbalance in dopamine receptor activity.Type: ApplicationFiled: October 28, 2008Publication date: February 24, 2011Applicant: MOTAC NEUROSCIENCE LIMITEDInventors: Holger Stark, Jukka Matti Leppanen, Britta Caroline Sasse, Oliver Saur, Tim Kottke, Michael Peter Hill
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Patent number: 7893067Abstract: Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq? is H or Rq and Rq? define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.Type: GrantFiled: June 25, 2008Date of Patent: February 22, 2011Assignee: Medivir ABInventors: Magnus Nilsson, Lourdes Oden, Pia Kahnberg, Urszula Grabowska
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Publication number: 20110039862Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoType: ApplicationFiled: September 24, 2009Publication date: February 17, 2011Applicant: MEDIVIR ABInventors: Lourdes Salvadore Odén, Magnus Nilsson, Pia Kahnberg, Bertil Samuelsson, Urszula Grabowska
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Publication number: 20110034460Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.Type: ApplicationFiled: August 4, 2010Publication date: February 10, 2011Applicant: Les Laboratoires ServierInventors: Jean-Claude Ortuno, Alexis Cordi, Jean-Michel Lacoste, Vincent Lacoste, Pauline Lacoste, Imre Fejes, Michael Burbridge, John Hickman, Alain Pierre
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Publication number: 20110034432Abstract: Compounds of Formula (I): wherein: R1 is methoxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described.Type: ApplicationFiled: March 12, 2010Publication date: February 10, 2011Applicant: AstraZeneca ABInventors: Craig JOHNSTONE, Darren MCKERRECHER, Kurt Gordon PIKE
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Patent number: 7880008Abstract: The present invention relates to compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 26, 2006Date of Patent: February 1, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Andreas Termin, Lev T. D. Fanning, Paul Krenitsky, Pramod Joshi
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Patent number: 7880002Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.Type: GrantFiled: December 28, 2005Date of Patent: February 1, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Kenneth G. Carson, Prakash Raman, Francois Soucy, Qing Ye, Shomir Ghosh
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Patent number: 7875606Abstract: The present invention aims at providing an isoxazoline derivative and a pharmaceutically acceptable salt thereof, both having an excellent herbicidal effect and an excellent selectivity between crop and weed. The isoxazoline derivative of the present invention is represented by the following general formula: wherein R1 is a haloalkyl group; R2 is a hydrogen atom, an alkyl group, or the like; R3, R4, R5 and R6 are each a hydrogen atom, or the like; Y is a pyrrolyl group, a pyrazolyl group, an isothiazolyl group, an oxazolyl group, an imidazolyl group, a pyridazinyl group, a pyrimidinyl group, a pyrazinyl group, a triazinyl group, a triazolyl group, an oxadiazolyl group, or the like; and n is an integer of 0 to 2.Type: GrantFiled: June 20, 2002Date of Patent: January 25, 2011Assignees: Ihara Chemical Industry Co., Ltd., Kumiai Chemical Industry Co., Ltd.Inventors: Masao Nakatani, Minoru Ito, Kyoko Kimijima, Masahiro Miyazaki, Makoto Fujinami, Ryohei Ueno, Satoru Takahashi
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Publication number: 20110015156Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.Type: ApplicationFiled: June 24, 2010Publication date: January 20, 2011Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Publication number: 20110003825Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.Type: ApplicationFiled: August 23, 2010Publication date: January 6, 2011Applicant: Schering CorporationInventors: Ying Huang, Guoqing Li, Andrew W. Stamford
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Publication number: 20100331315Abstract: The invention provides compounds that inhibit PIM kinases and/or CK2, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.Type: ApplicationFiled: June 18, 2010Publication date: December 30, 2010Inventors: Mustapha HADDACH, David M. RYCKMAN
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Publication number: 20100330173Abstract: This invention is directed to methods for treating and preventing influenza infection by inhibiting influenza virus HA maturation processes employing compounds of formula I. It is also directed to combinations for treating and preventing influenza infection comprising compounds of formula I and other agents.Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20100331340Abstract: The use of aryl piperazines of formula (I) in manufacturing a medicament for treating acute pain, neuropathic pain or receptive nociceptive pain in mammals including human beings is disclosed.Type: ApplicationFiled: January 15, 2009Publication date: December 30, 2010Inventors: Guisen Zhang, Lin Guo, Xiangping Yang, Xiangqing Xu, Jianqi Li, Guan Wang, Yanqin Ma, Shuming Hu, Shicheng Liu, Shixia Zhou
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Publication number: 20100329978Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: ApplicationFiled: May 21, 2010Publication date: December 30, 2010Applicants: University of Mississippi, I'Universite catholique de LouvainInventors: Christopher R. McCurdy, Christophe Mesangeau, Rae Reiko Matsumoto, Jacques Henri Poupaert, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem
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Publication number: 20100324032Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.Type: ApplicationFiled: August 23, 2010Publication date: December 23, 2010Inventors: Soan Cheng, Daniel D. Comer, Long Mao, Guity P. Balow, David Pleynet
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Publication number: 20100317658Abstract: A subject of the present invention is 4,7-dioxobenzothiazole-2-carboxamide derivatives, which inhibit the cdc25 phosphatases, in particular cdc25-C phosphatase. These compounds can in particular be used in the treatment of cancer.Type: ApplicationFiled: August 3, 2010Publication date: December 16, 2010Applicant: Ipsen Pharma S.A.S.Inventors: Marie-Odile Galcera-Contour, Grégoire Prevost, Alban Sidhu