The Five-membered Hetero Ring Has At Least Oxygen And Nitrogen As Ring Hetero Atoms Patents (Class 544/137)
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Publication number: 20120157383Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Applicant: THERAVANCE, INC.Inventors: Roland GENDRON, Melissa FLEURY, Adam D. HUGHES
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Publication number: 20120149706Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Inventors: Jacques DUMAS, Uday KHIRE, Timothy B. Lowinger, Holger PAULSEN, Bernd RIEDL, Willian J. SCOTT, Roger A. SMITH, Jill WOOD, Holia HATOUM-MOKDAD, Wendy LEE, Aniko REDMAN, Jeffrey JOHNSON, Robert SIBLEY
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Publication number: 20120142677Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: December 15, 2009Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khok, Doris Riether, Lifen Wu, Renee M. Zindell
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Patent number: 8188270Abstract: The present invention relates to a novel polymorphic form and the amorphous form of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophene-carboxamide, processes for their preparation, medicaments comprising these forms, and their use in the control of diseases.Type: GrantFiled: September 22, 2006Date of Patent: May 29, 2012Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Alfons Grunenberg, Jana Lenz, Gerhard Arnold Braun, Birgit Keil, Christian R. Thomas
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Patent number: 8173652Abstract: The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: February 12, 2010Date of Patent: May 8, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Maria-Clemencia Hernandez, Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Patent number: 8163747Abstract: The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations.Type: GrantFiled: February 28, 2008Date of Patent: April 24, 2012Assignees: Novartis AG, Vernalis (R&D) Ltd.Inventors: Martin James Drysdale, Brian William Dymock, Christoph Krell, Michael Mutz, Holger Petersen, Weijia Zheng
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Patent number: 8163728Abstract: The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: April 28, 2010Date of Patent: April 24, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120095002Abstract: The present invention relates to isoxazole-5-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-5-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.Type: ApplicationFiled: February 2, 2010Publication date: April 19, 2012Applicant: N.V. OrganonInventors: Paul David Ratcliffe, Ronald Palin
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Publication number: 20120088767Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.Type: ApplicationFiled: October 3, 2011Publication date: April 12, 2012Inventors: Junya Qu, Ralph Rivero, Robert Sanchez, Rosanna Tedesco
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Patent number: 8148372Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: GrantFiled: August 20, 2010Date of Patent: April 3, 2012Assignee: AstraZeneca ABInventors: Joseph Cacciola, James Empfield, James Folmer, Angela M Hunter, Scott Throner
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Publication number: 20120071481Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.Type: ApplicationFiled: February 2, 2010Publication date: March 22, 2012Inventors: Ronald Palin, Paul David Ratcliffe, Steven G. Kultgen, Koc-Kan Ho, Andrew Laird Roughton
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Patent number: 8138184Abstract: An isoxazole derivative is provided. The isoxazole derivative has following formula: wherein R1, R2, R3, R4 and R5, independently, include hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis and cancer including an isoxazole derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.Type: GrantFiled: October 1, 2008Date of Patent: March 20, 2012Assignee: Kaohsiung Medical UniversityInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Gwo-Jaw Wang, Mei-Ling Ho, Je-Ken Chang, Yin-Chih Fu
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Publication number: 20120046266Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: April 16, 2010Publication date: February 23, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
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Publication number: 20120046286Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: April 28, 2010Publication date: February 23, 2012Inventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
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Publication number: 20120035360Abstract: Provided are a method for dual-color imaging of sodium/calcium activities using a two-photon fluorescent probe and a method for preparing the two-photon fluorescent probe. The disclosed two-photon fluorescent probe for detecting calcium ions near the cell membrane reacts with calcium cations to exhibit strong two-photon fluorescence and may be selectively and easily loaded into the cell membrane by forming a complex with a calcium ion. Further, it allows imaging of the distribution of calcium cations in a living cell or tissue since it can selectively detect calcium ions in the living cell or tissue at a depth of 100 to 200 ?m for more than 60 minutes. In addition, by staining the living cell or tissue with two probes of different fluorescent colors, the calcium and sodium activities can be imaged simultaneously at different channels.Type: ApplicationFiled: October 27, 2010Publication date: February 9, 2012Inventor: Hwan Myung Kim
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Patent number: 8110572Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: GrantFiled: July 16, 2008Date of Patent: February 7, 2012Assignee: Abbott LaboratoriesInventors: Yujia Dai, Zhiqin Ji, Michael R. Michaelides
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Patent number: 8106192Abstract: The invention relates to a method for producing 5-chloro-N-({5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide starting from 5-chlorothiophene-2-carbonyl chloride, (2S)-3-amino-propane-1,2-diol and 4-(4-aminophenyl)-3-morpholinone.Type: GrantFiled: September 9, 2009Date of Patent: January 31, 2012Assignee: Bayer Pharma AktiengesellschaftInventor: Christian R. Thomas
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Patent number: 8101609Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:Type: GrantFiled: April 26, 2010Date of Patent: January 24, 2012Assignee: Apotex Pharmachem Inc.Inventors: Prabhudas Bodhuri, Gamini Weeratunga
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Patent number: 8101601Abstract: The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-morpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.Type: GrantFiled: February 6, 2007Date of Patent: January 24, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Hans-Georg Lerchen, Ursula Krenz, Karl-Heinz Schlemmer, Elisabeth Perzborn, Joerg Keldenich
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Publication number: 20120015946Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 18, 2010Publication date: January 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20120010172Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 31, 2009Publication date: January 12, 2012Applicant: McDERMOTT WILL & EMERY LLPInventors: Mette Knak Christensen, Fredrik Bjorkling
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Publication number: 20120010200Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20110312944Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: February 16, 2010Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
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Publication number: 20110301150Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.Type: ApplicationFiled: February 25, 2010Publication date: December 8, 2011Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
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Publication number: 20110294813Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: June 30, 2011Publication date: December 1, 2011Applicants: SHIONOGI & CO., LTD., INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20110288294Abstract: The invention relates to a process for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide (I) from 5-chlorothiophene-2-carboxylic acid and 4-[4-((S)-5-aminomethyl-2-oxooxazolidin-3-yl)phenyl]morpholin-3-one (II) or a salt of this compound with a mineral acid or an organic acid in the presence of propanephosphonic anhydride.Type: ApplicationFiled: May 14, 2011Publication date: November 24, 2011Inventors: Michael Nonnenmacher, Joerg Jung
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Publication number: 20110275805Abstract: A method for preparing the linezolid (compound 1), which comprises the steps of: (1) carrying out the debenzyl reaction of compound 4 in solvent, to obtain the compound 5 or its acetate; (2) carrying out the acetylation reaction in the amino of the compound 5 or its acetate obtained in step (1) in solvent to obtain the compound 1. The intermediates to prepare the compound 1 and the acetate of compound 5. The present preparation method is easy to obtain the chiral materials and the chiral materials are cheap, the process and the post treatment are simple, the intermediate products and the end product are easy to be purified, the total yield is high, their purities are also high, this preparation method is easy to be used in the industry manufacture.Type: ApplicationFiled: January 8, 2010Publication date: November 10, 2011Applicant: LIANHE CHEMICAL TECHNOLOGY CO., LTD.Inventors: Ping Wang, Qiangbiao Pan, Yangzhou Li, Daoliang Zheng
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Publication number: 20110263603Abstract: The present invention relates to imine compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.Type: ApplicationFiled: December 22, 2009Publication date: October 27, 2011Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Matthias Pohlman, Steffen Gross, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Wolfgang Von Deyn, Deborah L. Culberston, Cecille Ebuenga, Douglas D. Anspaugh, Franz-Josef Braun
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Patent number: 8044079Abstract: The invention relates to novel oxindole derivative of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: December 1, 2006Date of Patent: October 25, 2011Assignee: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Publication number: 20110257077Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.Type: ApplicationFiled: April 19, 2011Publication date: October 20, 2011Applicant: IRM LLCInventors: David C. Tully, Amab K. Chatterjee, Agnes Vidal, Hank Michael James Petrassi, Zhiwei Wang, Badry Bursulaya, Glen Spraggon
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Publication number: 20110245221Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 30, 2009Publication date: October 6, 2011Applicant: SIGMA-TAU RESEARCH SWITZERLAND S.A.Inventors: Giuseppe Giannini, Walter Cabri, Daniele Simoni, Riccardo Baruchello, Paolo Carminati, Gabriella Singrossi, Silvia Carminati, Giuseppe Paolo Carminati, Claudio Pisano
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Publication number: 20110245239Abstract: Novel isoxazoline compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for use on non-human animals.Type: ApplicationFiled: December 17, 2009Publication date: October 6, 2011Inventors: Steve Nanchen, Noëlle Gauvry, Thomas Goebel
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Publication number: 20110245243Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.Type: ApplicationFiled: June 16, 2011Publication date: October 6, 2011Inventors: Hong LIU, David C. TULLY, Arnab CHATTERJEE, Phillip B. ALPER, David H. WOODMANSEE, Daniel MUTNICK
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Publication number: 20110224211Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Ron Roberts, Wieslaw Kazmierski, Richard Grimes
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Publication number: 20110224204Abstract: Di-substituted phenyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. The disclosure also relates to methods for treating neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 25, 2009Publication date: September 15, 2011Inventors: Richard Chesworth, Gideon Shapiro, Amy Ripka
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Publication number: 20110195932Abstract: Combinations comprising (or consisting essentially of) one or more compounds of formula (1) with one or more ancillary agents, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations.Type: ApplicationFiled: August 1, 2008Publication date: August 11, 2011Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
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Publication number: 20110190256Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.Type: ApplicationFiled: February 19, 2009Publication date: August 4, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
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Patent number: 7989450Abstract: Isoxazole derivatives, in particular diarylisoxazole derivatives inhibitors of cyclooxygenase (COX), in particular cyclooxygenase-1 (COX-1), their pharmaceutical compositions, the process for their preparation and their use for the chemoprevention and treatment of inflammatory syndromes and in the prevention and treatment of carcinomas, in particular intestinal, ovarian and cutaneous carcinomas, in the treatment of pain syndromes, in particular after surgery, and in the cardiovascular field as antithrombotics/vasoprotectives/cardioprotectives.Type: GrantFiled: January 11, 2008Date of Patent: August 2, 2011Assignees: Universita' Degli Studi Di Bari, Universita' Degli Studi “G.D.'Annunzio”—ChietiInventors: Antonio Scilimati, Paola Vitale, Leonardo Di Nunno, Paola Patrignani, Stefania Tacconelli, Marta Luciana Capone
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Patent number: 7989618Abstract: Linezolid salts, useful as such and as intermediates in a process for the preparation of novel and known crystalline linezolid forms, in particular known as Form III.Type: GrantFiled: September 3, 2008Date of Patent: August 2, 2011Assignee: DiPharma Francis s.r.l.Inventors: Chiara Vladiskovic, Emanuele Attolino, Pietro Allegrini, Gabriele Razzetti
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Patent number: 7985749Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.Type: GrantFiled: April 29, 2005Date of Patent: July 26, 2011Assignee: Novartis AGInventors: Hong Liu, David C. Tully, Arnab Chatterjee, Phillip B. Alper, David H. Woodmansee, Daniel Mutnick
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Patent number: 7985750Abstract: This invention relates to novel compounds that are substituted oxazolidinones derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel oxazolidinones compounds that are derivatives of rivaroxaban. The invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and condition that are beneficially treated by administering a selective inhibitor of factor Xa, such as rivaroxaban.Type: GrantFiled: August 14, 2008Date of Patent: July 26, 2011Assignee: Concert Pharmaceuticals, Inc.Inventor: Craig E. Masse
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Patent number: 7985762Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3—NS4A protease.Type: GrantFiled: August 28, 2006Date of Patent: July 26, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
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Publication number: 20110178042Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.Type: ApplicationFiled: September 1, 2009Publication date: July 21, 2011Applicant: Pfizer Inc.Inventors: Matthew F. Brown, Charles F. Donovan, Edmund L. Eilsworth, Denton W. Hoyer, Timothy A. Johnson, Manjinder S. Lall, Chris Lim-Berakis, Sean T. Murphy, Debra A. Sherry, Clarke B. Taylor, Joseph S. Warmus
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Publication number: 20110177055Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g.Type: ApplicationFiled: March 29, 2011Publication date: July 21, 2011Applicant: IRM LLCInventors: David C. Tully, Arnab K. Chatterjee, Hank Michael James Petrassi, Badry Bursulaya, Glen Spraggon
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Publication number: 20110178083Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: July 9, 2009Publication date: July 21, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110172232Abstract: The present application relates to prodrug derivatives of 5-chloro-N-({(5S)-3-[2-fluoro-4-(3-oxomorpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.Type: ApplicationFiled: June 28, 2008Publication date: July 14, 2011Applicant: Bayers Schering Pharma AktiengesellschaftInventors: Hans-Georg Lerchen, Ursula Krenz, Michael Härter, Mark Jean Gnoth, Georges Von Degenfeld, Elke Dittrich-Wengenroth, Anja Buchmüller, Susanne Röhrig, Swen Allerheiligen, Elisabeth Perzborn, Christoph Gerdes, Karl-Heinz Schlemmer, Metin Akbaba
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Publication number: 20110165188Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Inventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Way Tsun Yue
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Publication number: 20110166130Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: June 12, 2009Publication date: July 7, 2011Applicant: BIONOMICS LIMITEDInventors: Andrew John Harvey, Bernard Luke Flynn, Jorgen Alvar Mould, Dharam Paul, Gurmit Singh Gill, Justin Anthony Ripper, Rachel Christine Cooke, Julia Stephanie Crossman, Jonathan Bayldon Baell, Nathan Wayne Kuchel, Rajinder Singh
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Publication number: 20110165120Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.Type: ApplicationFiled: February 28, 2011Publication date: July 7, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
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Publication number: 20110152255Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J, B, Y, and A are as described in claims 1-13. Methods, compositions, and medicaments related thereto are also disclosed, for treating baldness, glaucoma or inflammatory bowel diseases.Type: ApplicationFiled: April 21, 2009Publication date: June 23, 2011Inventors: Yariv Donde, Jeremiah H. Nguyen