The Additional Hetero Ring Is Five-membered Patents (Class 544/152)
  • Patent number: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • Publication number: 20150025069
    Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Inventors: Timothy Scott Daynard, Geoffrey C. Winters, David W.C. Hunt
  • Publication number: 20140343049
    Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 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 (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: August 10, 2012
    Publication date: November 20, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Julie Clementine Toueg, Tomas Smejkal, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere, Nicolas Poirier
  • 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: 20140309208
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated pathologies.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Publication number: 20140200197
    Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset 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: Application
    Filed: September 9, 2013
    Publication date: July 17, 2014
    Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
  • Publication number: 20140148448
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: January 30, 2014
    Publication date: May 29, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Renee Louise DESJARLAIS, Sanath K. MEEGALLA, Mark WALL, Kenneth WILSON
  • Publication number: 20140128385
    Abstract: The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased ? cell mass and/or function.
    Type: Application
    Filed: January 13, 2012
    Publication date: May 8, 2014
    Inventor: Heinrich Ruegger
  • Patent number: 8685975
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 1, 2014
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20140088077
    Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.
    Type: Application
    Filed: December 3, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
  • Patent number: 8669260
    Abstract: The application discloses ketoconazole derivatives that are antagonists of the human pregnane X receptor (PXR), methods of preparing the derivatives, uses of the derivatives with drug therapy, and methods of inhibiting tumor cell proliferation and multidrug resistance using inhibitors of PXR.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: March 11, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Sridhar Mani, Bhaskar C. Das
  • Publication number: 20140058021
    Abstract: A composition, which comprises a) an organic material susceptible to oxidative, thermal or light-induced degradation; and b) a compound of formula I (Formula I) (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently from each other H, C1-C8-alkyl, C4-C8-cycloalkyl, phenyl, C1-C4-alkoxy or halogen; n is 1, 2, 3, or 4; and when n is 1 A is —C(=0)-OR?1, —C(=0)-N(R?2)(R?3), —CN, phenyl, which is unsubstituted or substituted by one or more C1-C8-alkyl, C4-C8-alkoxy, C5-C7-cycloalkyl or halogen, —H or —S02-phenyl; when n is 2 A is —C(=0)-O—Z1—O—C(=0)-, —C(=0)-N(R?1)—Z2—N(R?2)—C(=0)- or piperazine-N,N?-biscarbonyl.
    Type: Application
    Filed: April 25, 2012
    Publication date: February 27, 2014
    Applicant: BASF SE
    Inventors: Walter Fischer, Abdel-Ilah Basbas, Kai-Uwe Schoning, Cinzia Tartarini, Werner Holzl, Bruno Rotzinger
  • Patent number: 8614211
    Abstract: Chemical entities that are arctigenin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 24, 2013
    Assignee: NeuPharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Patent number: 8606529
    Abstract: The application relates to methods and systems for analysis of dissociation behavior of nucleic acids and identification of nucleic acids. In one aspect, methods and systems are disclosed for identifying a nucleic acid in a sample including an unknown nucleic acid and for detecting a single nucleotide polymorphism in a nucleic acid in a sample. Methods and systems are also disclosed for identification of a nucleic acid in a biological sample including at least one unknown nucleic acid by fitting denaturation data including measurements of a quantifiable physical change of the sample at a plurality of independent sample property points to a function to determine an intrinsic physical value and to obtain an estimated physical change function, and identifying the nucleic acid in the biological sample by comparing the intrinsic physical value for at least one unknown nucleic acid to an intrinsic physical value for a known nucleic acid.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: December 10, 2013
    Assignee: Canon U.S. Life Sciences, Inc.
    Inventors: Deborah Boles, Kenton C. Hasson, Sami Kanderian
  • Publication number: 20130281452
    Abstract: Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Inventors: Gregor BAHRENBERG, Sven KUEHNERT, Simon LUCAS, Wolfgang SCHROEDER
  • Publication number: 20130196984
    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: March 13, 2013
    Publication date: August 1, 2013
    Applicants: Siena Biotech S.p.A., Hoffmann-La Roche Inc.
    Inventors: Hoffmann-La Roche Inc., Siena Biotech S.p.A.
  • Publication number: 20130123253
    Abstract: Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents.
    Type: Application
    Filed: May 1, 2012
    Publication date: May 16, 2013
    Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTE
    Inventor: John CASHMAN
  • Publication number: 20130040945
    Abstract: Chemical entities that are arctigenin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Patent number: 8343970
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: January 1, 2013
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20120270877
    Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
    Type: Application
    Filed: November 1, 2010
    Publication date: October 25, 2012
    Applicant: MannKind Corporation
    Inventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
  • Publication number: 20120252801
    Abstract: The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.
    Type: Application
    Filed: December 15, 2010
    Publication date: October 4, 2012
    Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Dorothée Bardiot, Bruno Cammue, Patrick Chaltin, Arnaud Marchand, Karin Thevissen
  • Publication number: 20120208807
    Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.
    Type: Application
    Filed: July 1, 2010
    Publication date: August 16, 2012
    Applicant: VALOCOR THERAPEUTICS, INC.
    Inventors: Timothy Scott Daynard, Geoffrey C. Winters, David W.C. Hunt
  • Patent number: 8180572
    Abstract: The present invention relates to methods and systems for the analysis of the dissociation behavior of nucleic acids and the identification of nucleic acids. In one aspect, methods and systems are disclosed for resolving a denaturation curve of a sample containing a first and second nucleic acid into a resolved denaturation curve for the first nucleic acid and a resolved denuration curve for the second nucleic acid.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: May 15, 2012
    Assignee: Canon U.S. Life Sciences, Inc.
    Inventor: Weidong Cao
  • Patent number: 8145433
    Abstract: The present invention relates to methods and systems for the analysis of the dissociation behavior of nucleic acids and the identification of nucleic acids. In one aspect, methods and systems are disclosed for identifying a nucleic acid in a sample including an unknown nucleic acid and for detecting a single nucleotide polymorphism in a nucleic acid in a sample. In another aspect, methods and systems are disclosed for identification of a nucleic acid in a biological sample including at least one unknown nucleic acid by fitting denaturation data including measurements of a quantifiable physical change of the sample at a plurality of independent sample property points to a function to determine an intrinsic physical value and to obtain an estimated physical change function, and identifying the nucleic acid in the biological sample by comparing the intrinsic physical value for at least one unknown nucleic acid to an intrinsic physical value for a known nucleic acid.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: March 27, 2012
    Assignee: Canon U.S. Life Sciences, Inc.
    Inventors: Deborah Boles, Kenton C. Hasson, Sami Kanderian
  • Publication number: 20120035175
    Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 9, 2012
    Applicant: 4SC AG
    Inventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
  • Publication number: 20120022059
    Abstract: The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.
    Type: Application
    Filed: June 16, 2011
    Publication date: January 26, 2012
    Applicant: AiCuris GmbH & Co. KG
    Inventors: Kai THEDE, Susanne Greschat, Steffen Wildum, Daniela Paulsen
  • Publication number: 20120004225
    Abstract: The present invention provides bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma, Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.
    Type: Application
    Filed: January 22, 2010
    Publication date: January 5, 2012
    Applicant: NeuroTherapeutics Pharma, Inc.
    Inventors: Stephen Wanaski, John J. Partridge, Stephen D. Collins
  • Patent number: 8076330
    Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: December 13, 2011
    Assignee: Amgen Inc.
    Inventors: Heiko Kroth, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochgürtel, Fritz-Frieder Frickel, Arthur G. Taveras, Christoph Steeneck
  • Publication number: 20110275625
    Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).
    Type: Application
    Filed: November 5, 2009
    Publication date: November 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Shuang Liang, Sabine Schlyer, Lana Louise Smith Keenan, Steven John Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Zhaoming Xiong, Qiang Zhang
  • Publication number: 20110275797
    Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Publication number: 20110256175
    Abstract: The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
    Type: Application
    Filed: October 9, 2009
    Publication date: October 20, 2011
    Applicants: THE UNIVERSITY OF BRITISH COLUMBIA, TEKMIRA PHARMACEUTICALS CORPORATION
    Inventors: Michael J. Hope, Sean C. Semple, Jianxin Chen, Thomas D. Madden, Pieter R. Cullis, Marco A. Ciufolini, Barbara Low Shoud Mui
  • Publication number: 20110245243
    Abstract: 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: Application
    Filed: June 16, 2011
    Publication date: October 6, 2011
    Inventors: Hong LIU, David C. TULLY, Arnab CHATTERJEE, Phillip B. ALPER, David H. WOODMANSEE, Daniel MUTNICK
  • Publication number: 20110224202
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Application
    Filed: March 10, 2011
    Publication date: September 15, 2011
    Applicant: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20110152255
    Abstract: 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: Application
    Filed: April 21, 2009
    Publication date: June 23, 2011
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20110059967
    Abstract: Compounds comprising Formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-16. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.
    Type: Application
    Filed: May 4, 2009
    Publication date: March 10, 2011
    Applicant: Allergan Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20110046129
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
    Type: Application
    Filed: September 9, 2010
    Publication date: February 24, 2011
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
  • Patent number: 7893282
    Abstract: 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: February 22, 2011
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Laura Honeyman
  • Publication number: 20100311727
    Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.
    Type: Application
    Filed: June 8, 2010
    Publication date: December 9, 2010
    Applicant: ALGEBRA, INC.
    Inventors: Philip F. MORGAN, James L. KELLEY
  • Publication number: 20100249097
    Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.
    Type: Application
    Filed: February 12, 2010
    Publication date: September 30, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Torsten HAACK, Petra LENNIG
  • Patent number: 7763612
    Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: July 27, 2010
    Assignee: Algebra, Inc.
    Inventors: Philip F. Morgan, James L. Kelley
  • Publication number: 20100168422
    Abstract: Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.
    Type: Application
    Filed: December 30, 2008
    Publication date: July 1, 2010
    Inventor: Weiping Chen
  • Publication number: 20100125071
    Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.
    Type: Application
    Filed: June 4, 2008
    Publication date: May 20, 2010
    Inventors: Neil John Press, Simon James Watson
  • Patent number: 7666863
    Abstract: The present invention relates to benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: February 23, 2010
    Assignees: ViroPharma Incorporated, WYETH
    Inventors: Ashis K. Saha, Christopher J Burns, Alfred M. Del Vecchio, Thomas R. Bailey, Jason A. Reinhardt, Bheemashankar A. Kulkarni, Thomas H. Faitg, Hao Feng, Susan R. Rippin, Charles W. Blackledge, David J. Rys, Thomas A. Lessen, John Swestock, Yijun Deng, Theodore J. Nitz
  • Publication number: 20090306022
    Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: June 9, 2009
    Publication date: December 10, 2009
    Applicants: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Beena Bhatia, David Messersmith, Laura McIntyre, Darrell Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul Verma, Tadeusz Warchol, Upul Bandarage
  • Publication number: 20090285849
    Abstract: Novel immune potentiators, novel vaccine adjuvants, novel compounds and pharmaceutical compositions, as well as novel methods for treating viral infections, including HCV, by administering the compounds and compositions, and novel methods for modulating the immune response by administering the compounds and/or compositions.
    Type: Application
    Filed: February 26, 2009
    Publication date: November 19, 2009
    Inventors: Paul A. Barsanti, Nathan Brammeier, Anthony Diebes, Liana Marie Lagniton, Simon NG, Zhi Jie Ni, Keith B. Pfister, Casey Philbin, Nicholas Valiante, Allan S. Wagman, Weibo Wang, Amy J. Weiner
  • Patent number: 7615549
    Abstract: The present invention relates to new substituted pyrrolidinones of general formula wherein A, X, B and R1 to R9 are as defined above, or a tautomer or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: November 10, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Henning Priepke, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar, Peter Kuehn, Georg Dahmann
  • Publication number: 20090275575
    Abstract: Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells.
    Type: Application
    Filed: September 21, 2007
    Publication date: November 5, 2009
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Nam-Song Choi, Young-Mi Kim, Young-Hoon Kim, Jae-Kwang Lee, In-Taek Lim, Ho-Jin Choi, Hyun-Mo Yang, Seung-Kee Moon, Soo-Jin Kim, Hyun-Jung Yu, Jae-Su Shin, Young-Min Kwon, Sung-Sook Lee, Soon-Kil Ahn
  • Publication number: 20090253656
    Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.
    Type: Application
    Filed: March 29, 2006
    Publication date: October 8, 2009
    Applicant: Kabushiki Kaisha Yakult Honsha
    Inventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
  • Publication number: 20090036439
    Abstract: The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.
    Type: Application
    Filed: September 19, 2008
    Publication date: February 5, 2009
    Applicant: Wyeth
    Inventors: Craig Eugene Caufield, Schuyler Adam Antane, Koi Michele Morris, Shaughnessy McGrath Naughton, Dominick Anthony Quagliato, Patrick Michael Andrae, Annmarie Enos, John F. Chiarello
  • Publication number: 20080287430
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof wherein X, Z, R1, R2a, R2b, R3, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Application
    Filed: April 24, 2006
    Publication date: November 20, 2008
    Inventors: Rino Antonio Bit, Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Tiziana Scoccitti