1,4-oxazines Patents (Class 544/98)
  • Patent number: 9834526
    Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: December 5, 2017
    Assignees: MERCK SHARP & DOHME CORP., MERCK CANADA INC.
    Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Satyanarayana Tummanapalli, Vouy Linh Truong, Peter D. Williams
  • Publication number: 20150018338
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: July 7, 2014
    Publication date: January 15, 2015
    Applicant: NOVARTIS AG
    Inventors: Sangamesh BADIGER, Murali CHEBROLU, Mathias FREDERIKSEN, Philipp HOLZER, Konstanze HURTH, Rainer Martin LEUOEND, Rainer MACHAUER, Henrik MOEBITZ, Ulf NEUMANN, Rita RAMOS, Henrich RUEEGER, Michael SCHAEFER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
  • Publication number: 20140364428
    Abstract: The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Application
    Filed: December 4, 2012
    Publication date: December 11, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Henricus Jacobus Maria Gijsen, Sven Franciscus Anna Van Brandt
  • Publication number: 20140343048
    Abstract: The invention relates to novel 6-difluoromethyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, cerebral amyloid angiopathy, multi-infarct dementia, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Application
    Filed: December 4, 2012
    Publication date: November 20, 2014
    Inventors: Andrés Avelino Trabanco-Suárez, Henricus Jacobus Maria Gijsen, Michel Surkyn, Hana Prokopcová
  • Patent number: 8865052
    Abstract: The TPU of this invention contains unsaturation in its polymeric backbone. The unsaturation can be present in the soft segment or in the hard segment or in both the soft and hard segments of the TPU. The TPU can be molded like a thermoplastic, and can be subsequently crosslinked by exposure to electron beam irradiation into thermoset articles having excellent chemical resistance, dimensional stability, set properties, heat resistance, oxidative resistance, and creep resistance. In one embodiment, the TPUs of this invention are the reaction product (1) a hydroxyl terminated intermediate, (2) a polyisocyanate, (3) a saturated glycol chain extender, and (4) a glycol chain extender containing carbon-carbon double bonds, such as the allyl moieties present in trimethylolpropane monoallyl ether.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: October 21, 2014
    Assignee: Lubrizol Advanced Materials, Inc.
    Inventors: Umit G. Makal, Louis J. Brandewiede, George H. Loeber
  • Publication number: 20140303127
    Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
    Type: Application
    Filed: November 9, 2012
    Publication date: October 9, 2014
    Inventors: Jose Aiguade Bosch, Silvia Gual Roig, Maria Prat Quinones, Carlos Puig Duran
  • Publication number: 20140256715
    Abstract: The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
    Type: Application
    Filed: October 11, 2012
    Publication date: September 11, 2014
    Applicant: NOVARTIS AG
    Inventors: Konstanze Hurth, Sebastien Jacquier, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
  • Publication number: 20140113894
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Philipp Holzer, Rainer Machauer, Marina Tintelnot-Blomley
  • Publication number: 20140088084
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: July 12, 2013
    Publication date: March 27, 2014
    Inventors: Philipp Holzer, Rainer Machauer, Marina Tintelnot-Blomley
  • Patent number: 8524897
    Abstract: The invention relates to 5-cyano-3-methyl-pyridine-2-carboxylic acid [3-((3R,6R)-5-amino-3,6-dimethyl-6-trifluoromethyl-3,6-dihydro-2H-[1,4]oxazin-3-yl)-4-fluoro-phenyl]-amide in crystalline form, to its preparation, its medical use and to medicaments comprising said compound in crystalline form.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: September 3, 2013
    Assignee: Novartis AG
    Inventor: Rita Ramos
  • Publication number: 20130109656
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
    Type: Application
    Filed: August 15, 2012
    Publication date: May 2, 2013
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robinson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtli
  • Publication number: 20130109683
    Abstract: The present invention relates to novel 5,6-dihydro-2H-[1,4]oxazin-3-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease and dementia associated with beta-amyloid.
    Type: Application
    Filed: June 8, 2011
    Publication date: May 2, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Andrés Avelino Trabanco-Suárez, Frederik Jan Rita Rombouts, Gary John Tresadern, Michiel Luc Maria Van Gool, Gregor James MacDonald, Carolina Martinez Lamenca, Henricus Jacobus Maria Gijsen
  • Publication number: 20130089624
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein. Additionally, the present invention also relates to novel processes for the production of various morpoholine based intermediates.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 11, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Stephen Clinton Young, Christopher John Davis, John Studley
  • Patent number: 8399459
    Abstract: The present invention provides 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: March 19, 2013
    Assignees: Hoffmann-La Roche Inc., Siena Biotech SpA
    Inventors: Matteo Andreini, Emanuele Gabellieri, Robert Narquizian, Massimiliano Travagli, Wolfgang Wostl
  • Patent number: 8372833
    Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: its pharmaceutically acceptable salt or solvate thereof, wherein X is hydrogen or the like, Y is a group of the formula: Z is —NR7— or the like, R1 is hydrogen or the like, R2 and R3 are each independently hydrogen or the like, n is 0 or 1, p is 0 to 6.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: February 12, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventor: Toshisada Yano
  • Publication number: 20120302558
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
    Type: Application
    Filed: July 13, 2011
    Publication date: November 29, 2012
    Inventors: Sangamesh Badiger, Murali Chebrolu, Mathias Frederiksen, Philipp Holzer, Konstanze Hurth, Rainer Martin Lueoend, Rainer Machauer, Henrik Moebitz, Ulf Neumann, Rita Ramos, Heinrich Rueeger, Michael Schaefer, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle, Lei Li, Hui Liu, Xin Xiong
  • Publication number: 20120214806
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: May 1, 2012
    Publication date: August 23, 2012
    Inventors: Matteo Andreini, David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Massimiliano Travagli, Michela Valacchi, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20120196863
    Abstract: The present invention provides 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: January 25, 2012
    Publication date: August 2, 2012
    Inventors: Matteo Andreini, Emanuele Gabellieri, Robert Narquizian, Massimiliano Travagli, Wolfgang Wostl
  • Publication number: 20120184540
    Abstract: The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: January 12, 2012
    Publication date: July 19, 2012
    Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl, Harald Mauser
  • Publication number: 20120184539
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
    Type: Application
    Filed: January 11, 2012
    Publication date: July 19, 2012
    Inventors: Sangamesh BADIGER, Murali CHEBROLU, Konstanze HURTH, Sébastien JACQUIER, Rainer Martin LUEOEND, Rainer MACHAUER, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
  • Publication number: 20120178745
    Abstract: The invention relates to 5-cyano-3-methyl-pyridine-2-carboxylic acid [3-((3R,6R)-5-amino-3,6-dimethyl-6-trifluoromethyl-3,6-dihydro-2H-[1,4]oxazin-3-yl)-4-fluoro-phenyl]-amide in crystalline form, to its preparation, its medical use and to medicaments comprising said compound in crystalline form.
    Type: Application
    Filed: January 10, 2012
    Publication date: July 12, 2012
    Inventor: Rita RAMOS
  • Patent number: 7947675
    Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • Patent number: 7939537
    Abstract: Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: September 26, 2006
    Date of Patent: May 10, 2011
    Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Vincenzo Summa, Olaf Kinzel, Monica Donghi
  • Publication number: 20110046122
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: August 9, 2010
    Publication date: February 24, 2011
    Inventors: Matteo Andreini, David Banner, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Roger-Evans, Massimiliano Travagli, Michela Valacchi, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20110015392
    Abstract: A route for preparing a compound of formula (I) where X, R1, R2, R7, R8 and R9 are as defined in the specification, is described. Process steps used in the route and novel intermediates prepared during the route are also described and claimed. Compounds of formula (I) are used in the preparation of pharmaceutical compounds, in particular inhibitors of MEK, useful in the treatment of hyperproliferative disease such as cancer and inflammatory conditions.
    Type: Application
    Filed: August 11, 2010
    Publication date: January 20, 2011
    Inventors: Mark Richard Fielding, John Leonard
  • Publication number: 20100331283
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
    Type: Application
    Filed: June 23, 2010
    Publication date: December 30, 2010
    Applicant: Array BioPharma Inc.
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
  • Patent number: 7807669
    Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: October 5, 2010
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
  • Patent number: 7772225
    Abstract: The present invention relates to novel N-sulfamoyl-piperidineamides of Formula I and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment of obesity and its concomitant and/or secondary diseases and related or other conditions.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: August 10, 2010
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Jochen Antel, Michael Firnges, Uwe Schoen, Harald Waldeck, Michael Wurl, Dania Reiche, Peter-Colin Gregory
  • Patent number: 7763602
    Abstract: Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
    Type: Grant
    Filed: June 11, 2008
    Date of Patent: July 27, 2010
    Assignee: Lupin Limited
    Inventors: Sudershan Kumar Arora, Neelima Sinha, Sanjay Jain, Ram Shankar Upadhayaya, Gourhari Jana, Shankar Ajay, Rakesh Kumar Sinha
  • Patent number: 7659280
    Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: February 9, 2010
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jeffrey Wayne Clough, Somasekhar Bhamidipati, Rajinder Singh, Esteban Masuda, Haoran Zhao
  • Publication number: 20090291945
    Abstract: To provide a compound having an excellent cysteine protease inhibitory effect, and to provide a drug for treatment or prevention of the disease selected from the group consisting of osteoporosis, osteoarthritis, chronic rheumatoid arthritis, Paget's disease of bone, hypercalcemia, bone metastasis of cancer, and ostealgia. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a drug or pharmaceutical composition containing the same as an effective component.
    Type: Application
    Filed: April 7, 2009
    Publication date: November 26, 2009
    Applicant: Teijin Pharma Limited
    Inventors: Gen Unoki, Takashi Hayamizu, Hiroshi Eguchi, Yumiko Muroga, Toshiyuki Kaneko, Naoki Yajima
  • Patent number: 7605261
    Abstract: The invention relates to new products of formula (I): in which: Y represents oxygen or sulphur, Z represents C?CH2, CH—CH3 or CH2, R1 represents hydrogen, morpholinyl or the radical. In which the two nitrogen atoms are linear or form a cyclic radical, X represents carbonyl, alkylene or alkenylene, linear or branched, containing at most 6 carbon atoms optionally interrupted by oxygen or sulphur, R4, R5 and R6 represent hydrogen, a protective group of the nitrogen, alkyl, cycloalkyl, aryl and arylalkyl optionally substituted, R2 represents alkyl optionally substituted by aryl, heteroaryl or —NR4R5, R3 represents alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl optionally substituted, these products being in all isomer forms and the salts, as medicaments.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: October 20, 2009
    Assignee: Amgen Inc.
    Inventors: Pierre Deprez, Marcel Patek
  • Patent number: 7572793
    Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
    Type: Grant
    Filed: September 20, 2002
    Date of Patent: August 11, 2009
    Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-Aventis
    Inventors: Fumiaki Uehara, Keiichi Aritomo, Aya Shoda, Shinsuke Hiki, Masahiro Okuyama, Yoshihiro Usui, Mitsuru Ooizumi, Kazutoshi Watanabe
  • Patent number: 7569687
    Abstract: The invention encompasses processes for synthesizing 1-[17?-acetyloxy-3?-hydroxy-2?-(4-morpholinyl)-5?-androstan-16?-yl]-1-(2-propenyl)pyrrolidinium bromide (rocuronium bromide) and intermediates thereof.
    Type: Grant
    Filed: September 13, 2006
    Date of Patent: August 4, 2009
    Assignee: Sicor, Inc.
    Inventors: Juana Araceli Mendez, Marco A. De La Mora, Angel A. Rodriguez, Efrain Barragán, Hugo Herrera, Alejandro Guillen
  • Patent number: 7550461
    Abstract: Disclosed are amide compounds of formula (I): wherein Ar1, Q, Y and R3-R6 of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 10, 2003
    Date of Patent: June 23, 2009
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
  • Patent number: 7531651
    Abstract: Compounds of formula (I): wherein A? represents the benzenesulphonate (besylate) anion;. R represents H or C1-6 alkyl; and n is a number from 0.8 to 2.2 are CCR3 antagonists and are therefore indicated to be useful in therapy are described.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: May 12, 2009
    Assignee: Glaxo Group Limited
    Inventors: John Spencer Cook, Robert Philip Landon, Andrew John Walker, Mark Wilkinson
  • Patent number: 7511034
    Abstract: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Grant
    Filed: January 11, 2006
    Date of Patent: March 31, 2009
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
  • Patent number: 7507817
    Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.
    Type: Grant
    Filed: November 13, 2007
    Date of Patent: March 24, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo, Wha-Bin Im
  • Publication number: 20090062285
    Abstract: The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds.
    Type: Application
    Filed: July 14, 2008
    Publication date: March 5, 2009
    Applicant: National Sun Yat-Sen University
    Inventors: Jyh-Horng Sheu, Chih-Hua Chao, Zhi-Hong Wen
  • Patent number: 7452878
    Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
    Type: Grant
    Filed: May 18, 2005
    Date of Patent: November 18, 2008
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
  • Patent number: 7446210
    Abstract: The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.
    Type: Grant
    Filed: October 24, 2005
    Date of Patent: November 4, 2008
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Tianbao Lu, Tho V. Thieu, Yu-Kai Lee, Daniel J. Parks, Thomas P. Markotan, Wenxi Pan, Karen L. Milkiewicz, Mark R. Player
  • Patent number: 7371746
    Abstract: The present invention relates to a 1,2,4-thiadiazole compound of the formula (I) represented by the formula (1): wherein R1? represents C3-C7 alkynyl and X represents C4-C7 straight alkylene optionally substituted with one to four of R2?, C4-C7 straight alkenylene optionally substituted with one to four of R2?, ethylene-oxy-ethylene optionally substituted with one to four of R4?, or ethylene-thio-ethylene optionally substituted with one to four of R4?, R2? represents a halogen atom, trifluoromethyl or C1-C4 alkyl, and R4 represents a fluorine atom or C1-C3 alkyl.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: May 13, 2008
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Hideki Ihara, Daisuke Takaoka, Hajime Mizuno
  • Publication number: 20080081907
    Abstract: The present invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein X, Y, Ar1, and Ar2 are as defined in the specification.
    Type: Application
    Filed: September 21, 2007
    Publication date: April 3, 2008
    Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Patent number: 7285568
    Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
    Type: Grant
    Filed: May 24, 2005
    Date of Patent: October 23, 2007
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
  • Patent number: 7256191
    Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.
    Type: Grant
    Filed: August 31, 2004
    Date of Patent: August 14, 2007
    Assignee: Aryx Therapeutics
    Inventor: Pascal Druzgala
  • Patent number: 7229988
    Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: June 12, 2007
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
  • Patent number: 7166609
    Abstract: Pyrimidine-4,6-dicarboxylic acid diamides of the formula I are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for treating degenerative joint diseases.
    Type: Grant
    Filed: November 3, 2003
    Date of Patent: January 23, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Otmar Klingler, Reinhard Kirsch, Joerg Habermann, Klaus-Ulrich Weithmann, Christian Engel, Bernard Pirard
  • Patent number: 7112684
    Abstract: Dye reagents useful in labeling biological materials are provided along with methods for their use.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: September 26, 2006
    Assignee: Epoch Biosciences, Inc.
    Inventors: Eugeny A. Lukhtanov, Alexei V. Vorobiev, Michael W. Reed, Nicolaas M. J. Vermeulen
  • Patent number: 7041668
    Abstract: The present invention discloses and claims benzimidazole compounds of formula (I): in which A is aryl or heteroaryl; R1 is selected from optionally substituted alkyl, alkoxy, aryl or heteroaryl, NH-lower alkyl or NH-cycloalkyl, or halogen, NH2; 1-imidazolyl or SO2Me; R2 is selected from optionally substituted —CO-alkyl, —CO-cycloalkyl, —CO-aralkyl, —CO-aryl, —CO-alkoxy, aryl or aralkyl, or —CO-amino, CO—NHR3 or CO—R3R4 wherein R3 and R4 are selecteded independently from hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, fluoroalkyl, alkynyl, heteroalkyl, alkylheteroalkyl, aryl, aralkyl or together form an alkylene chain optionally containing one to 4 heteroatoms; a pharmaceutically acceptable salt or a prodrug thereof; the use of compounds of formula (I) for the treatment of cancer, and pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents.
    Type: Grant
    Filed: March 25, 2004
    Date of Patent: May 9, 2006
    Assignee: Aventis Pharma S.A.
    Inventors: Francois Clerc, Francois Hamy, Isabelle Depaty, Odile Angouillant-Boniface, Stéphanie Deprets, Chantal Carrez, Manfred Roesner
  • Patent number: 6777403
    Abstract: Therefore, it is critical that the roles these enzymes play in biological processes outside of extracellular matrix degradation or remodeling be understood in order to assess their potential as targets for therapeutic intervention, and to design safe, conveniently produced, orally active inhibitors. Elastase inhibitors can differ with respect to their ability to inhibit different elastases. As a result, the spectrum of elastases inhibited by a specific drug candidate as well as the spectrum of activities these enzymes have with respect to proteins other than elastin are properties to consider in evaluating the drug candidates.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: August 17, 2004
    Assignee: Cortech, Inc.
    Inventor: John C. Cheronis