Oxadiazoles (including Hydrogenated) Patents (Class 514/364)
-
Publication number: 20130065860Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: September 5, 2012Publication date: March 14, 2013Applicant: ALLERGAN, INC.Inventors: Janet A. Takeuchi, Ling Li, Ken Chow
-
Patent number: 8394840Abstract: The invention provides novel compositions and compounds that inhibit CatSper channel activity, that preferentially inhibits sperm hyperactivity over sperm motility, or both. The compounds of the invention are useful as contraceptive agents that may be adminstered to males, females, or concurrently to both sexual partners. The invention further provides methods of conducting drug discovery business and of conducting a reproductive medicine business. The invention also provides methods of identifying compounds that modulate sperm hypermotility.Type: GrantFiled: June 15, 2006Date of Patent: March 12, 2013Assignee: Hydra Biosciences, Inc.Inventors: Jayhong A. Chong, Magdalene M. Moran
-
Publication number: 20130059883Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 13, 2011Publication date: March 7, 2013Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
-
Patent number: 8389509Abstract: Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, benzyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: GrantFiled: January 22, 2010Date of Patent: March 5, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Alaric J. Dyckman, William J. Pitts, Scott Hunter Watterson
-
Publication number: 20130053416Abstract: 3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 26, 2012Publication date: February 28, 2013Applicant: SANOFIInventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Klaus WIRTH
-
Publication number: 20130053386Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 5, 2010Publication date: February 28, 2013Inventors: William Colby Brown, Richard W. Heidebrecht, Jason Brubaker, Christian Fischer, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
-
Publication number: 20130053380Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 28, 2011Publication date: February 28, 2013Applicant: PHENEX PHARMACEUTICALS AGInventors: Olaf Kinzel, Christoph Steeneck, Gerald Klaymann, Michael Albers, Thomas Hoffman, Claus Kremoser, Sanja Perovic-Ottstadt, Thomas Schlüter
-
Patent number: 8383654Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: November 16, 2009Date of Patent: February 26, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Brian Andrew Stearns, Timothy Parr
-
Patent number: 8383660Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: GrantFiled: January 3, 2007Date of Patent: February 26, 2013Assignee: Pfizer Inc.Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
-
Patent number: 8383622Abstract: 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 Ring A is a group represented by the formula: Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle, R1 is hydrogen or optionally substituted alkyl, R2 is —OR5, —SR5, halogen, halogenated alkyl or the like, R3 is optionally substituted alkyl or the like, R4 is optionally substituted alkyl or the like, R5 is optionally substituted alkyl or the like, R6 is hydrogen or the like, R7 and R8 are each independently hydrogen or the like, R10 and R11 are each independently hydrogen or the like, R12 is optionally substituted alkyl or the like, m and p are each independently integer of 1 to 3.Type: GrantFiled: May 7, 2008Date of Patent: February 26, 2013Assignee: Shionogi & Co., Ltd.Inventors: Koji Masuda, Tomoyuki Ogawa, Takuji Nakatani
-
Publication number: 20130045952Abstract: The present invention relates to ABA agonist compounds which increase plant stress resistance. The invention also relates to methods of using these compounds. The invention further relates to compositions and formulations comprising the ABA agonist compounds, and uses thereof.Type: ApplicationFiled: August 17, 2012Publication date: February 21, 2013Applicant: Van Andel Research InstituteInventors: Yong Xu, Xiaoyin Edward Zhou, Karsten Melcher, Huaqiang Eric Xu
-
Publication number: 20130045964Abstract: Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: Q is, or R1 is phenyl substituted with zero to 3 substituents; and R1, R2, R3, R4, R5, and G are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: April 21, 2011Publication date: February 21, 2013Inventors: Robert J. Cherney, Yanlei Zhang
-
Patent number: 8378118Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.Type: GrantFiled: January 10, 2012Date of Patent: February 19, 2013Assignee: Torrent Pharmaceuticals Ltd.Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
-
Patent number: 8377975Abstract: Novel oxadiazole derivatives of the formula (I), in which R, R?, Y, X1, X2 and X3 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and conditions such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, in general in all types of fibroses, inflammatory processes, tumours and tumour diseases.Type: GrantFiled: July 9, 2009Date of Patent: February 19, 2013Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Markus Klein, Norbert Beier, Florian Lang
-
Patent number: 8377940Abstract: Compounds of Formula (I) wherein R1 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: GrantFiled: June 5, 2008Date of Patent: February 19, 2013Assignee: AstraZeneca ABInventors: Joshua Clayton, Ian Egle, James Empfield, James Folmer, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi
-
Publication number: 20130035360Abstract: Water soluble compounds having a furoxan structure which are capable of inhibiting metabolic pathways involved in the development of the tumours are provided. The use of such compounds as a medicament in the therapy of the tumours and as an adjuvant in the immunotherapy protocols against neoplasms is also described.Type: ApplicationFiled: February 23, 2011Publication date: February 7, 2013Applicant: HUMANITAS MIRASOLE S.p.A.Inventors: Enzo Bronte, Marco Crosetti, Loretta Lazzarato, Roberta Fruttero, Alberto Gasco, Antonella Viola
-
Publication number: 20130030022Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 26, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Boehringer Ingelheim International GmbH
-
Publication number: 20130030000Abstract: The present invention is directed to a composition useful for the treatment of a FAAH mediated disease, disorder or conditions comprising a FAAH inhibitor and a second activation, comprising a selected imidazole or oxazole FAAH inhibitor and a second active agent. The compositions will be useful in the treatment of a wide range of disease, disorder, or conditions including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease. In another aspect the invention discloses herein is directed to compositions useful in the treatment of neuropathic and nociceptive pain, said compositions comprising etoricoxib.Type: ApplicationFiled: January 25, 2011Publication date: January 31, 2013Inventors: Harry R. Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo, Terence G. Hamill, Wenping Li, Darrell Arthur Henze
-
Patent number: 8362047Abstract: The present disclosure relates to novel compounds that can be used as anti-cancer agents in the prostate cancer therapy. In particular, the invention relates N-substituted derivatives of 4-(hetero)aryl-1,2,5-oxadiazol-3-yl amines having the structural Formula (I) and (II), stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or pharmaceutically acceptable salt and/or solvate thereof. Meaning of R1 and R2 in the Formula (I) and (II) are defined in claim 1. The invention also relates to methods for preparing said compounds, and to pharmaceutical compositions comprising said compounds.Type: GrantFiled: June 24, 2010Date of Patent: January 29, 2013Assignee: U.S. Department of EnergyInventors: Andrei A. Gakh, Mikhail Krasavin, Ruben Karapetian, Konstantin A. Rufanov, Igor Konstantinov, Elena Godovykh, Olga Soldatkina, Andrey V. Sosnov
-
Patent number: 8362048Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.Type: GrantFiled: November 15, 2010Date of Patent: January 29, 2013Assignee: Receptos, Inc.Inventors: Esther Martinborough, Marcus F. Boehm, Adam Richard Yeager, Junko Tamiya, Liming Huang, Enugurthi Brahmachary, Manisha Moorjani, Gregg Alan Timony, Jennifer L. Brooks, Robert Peach, Fiona Lorraine Scott, Michael Allen Hanson
-
Publication number: 20130023495Abstract: The present invention relates to the use of a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. The present invention further relates to the use of a pharmaceutical composition comprising a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia.Type: ApplicationFiled: March 29, 2011Publication date: January 24, 2013Applicant: Novartis AGInventors: Charles Meyers, Michael H. Serrano-Wu, Tom Thuren
-
Publication number: 20130023542Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.Type: ApplicationFiled: September 25, 2012Publication date: January 24, 2013Applicant: Aerpio Therapeutics Inc.Inventor: Aerpio Therapeutics Inc.
-
Publication number: 20130023539Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.Type: ApplicationFiled: June 18, 2012Publication date: January 24, 2013Applicant: Euroscreen S.A.Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
-
Patent number: 8357705Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain or other conditions.Type: GrantFiled: March 25, 2009Date of Patent: January 22, 2013Assignee: Gruenenthal GmbHInventors: Saskia Zemolka, Bert Nolte, Klaus Linz, Derek John Saunders, Wolfgang Schröder, Werner Englberger, Fritz Theil, Hans Schick, Jens Kaufmann, Julian Gebauer, Helmut Sonnenschein
-
Patent number: 8357706Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.Type: GrantFiled: November 15, 2010Date of Patent: January 22, 2013Assignee: Receptos, Inc.Inventors: Esther Martinborough, Marcus F. Boehm, Adam Richard Yeager, Junko Tamiya, Liming Huang, Enugurthi Brahmachary, Manisha Moorjani
-
Publication number: 20130018048Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: April 4, 2011Publication date: January 17, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
-
Publication number: 20130018055Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 and n are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: January 17, 2012Publication date: January 17, 2013Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
-
Publication number: 20130017190Abstract: The present invention relates generally to the field of inflammatory diseases of the peripheral nervous system. More particularly, it concerns methods for treating inflammatory diseases of the peripheral nervous system by modulating sphingosine-1-phosphate receptor activity. In one embodiment, the present invention provides a method of treating a subject with chronic inflammatory demyelinating polyneuropathy (CIDP) or other autoimmune neuropathies comprising administering to the subject an effective amount of FTY720.Type: ApplicationFiled: August 6, 2012Publication date: January 17, 2013Inventor: Betty C. Soliven
-
Publication number: 20130018066Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: July 17, 2012Publication date: January 17, 2013Applicant: Schering Corporation & Pharmacopeia Drug Discovery Inc.Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
-
Patent number: 8354436Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: GrantFiled: January 27, 2012Date of Patent: January 15, 2013Assignee: 4SC Discovery GmbHInventors: Johann Leban, Stefan Tasler, Wael Saeb, Carine Chevrier
-
Patent number: 8354403Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: August 17, 2010Date of Patent: January 15, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent J. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
-
Patent number: 8349871Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 21, 2011Date of Patent: January 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
-
Publication number: 20130005771Abstract: The present invention relates to oxadiazole compounds in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable prodrugs and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the oxadiazole compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the treatment of cancer, particularly chronic myeloid leukemia (CML). The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: ApplicationFiled: February 24, 2011Publication date: January 3, 2013Inventors: Meenakshi Sivakumar, Kalpana Sanjay Joshi, Valmik Sopan Aware, Ankush Gangaram Sarde, Sandeep Maruti Bagul, Sonal Mohan Manohar
-
Patent number: 8343970Abstract: 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: GrantFiled: March 10, 2011Date of Patent: January 1, 2013Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
-
Publication number: 20120329649Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
-
Publication number: 20120329838Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.Type: ApplicationFiled: September 6, 2012Publication date: December 27, 2012Applicant: The Scripps Research InstituteInventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
-
Publication number: 20120329781Abstract: The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI) or one or both of a selective serotonin re-uptake inhibitor (SSRI) and a selective noradrenaline re-uptake inhibitor (SNRI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.Type: ApplicationFiled: August 29, 2012Publication date: December 27, 2012Inventors: David James Dooley, Mark John Field, Richard Griffith Williams
-
Publication number: 20120328569Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
-
Publication number: 20120329840Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.Type: ApplicationFiled: September 6, 2012Publication date: December 27, 2012Applicant: The Scripps Research InstituteInventors: Edward Roberts, Hugh Rose, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
-
Publication number: 20120329839Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.Type: ApplicationFiled: September 6, 2012Publication date: December 27, 2012Applicant: The Scripps Research InstituteInventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
-
Publication number: 20120328580Abstract: This invention generally provides compounds, pharmaceutical compositions, and methods for their use, which include methods that result in increased expression in an Atoh1 gene (e.g., Hath1) in a biological cell. More specifically, the invention relates to the treatment of diseases and/or disorders that would benefit from increased Atoh1 expression, e.g., a hearing impairment or imbalance disorder associated with a loss of auditory hair cells, or a disorder associated with abnormal cellular proliferation.Type: ApplicationFiled: April 24, 2012Publication date: December 27, 2012Inventors: Albert Edge, Sang-Jun Jeon, Kathleen Seyb, Marcie Glicksman, Lixin Qiao, Gregory D. Cuny
-
Patent number: 8338418Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: November 17, 2011Date of Patent: December 25, 2012Assignee: Theravance, Inc.Inventors: Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair
-
Patent number: 8338440Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: GrantFiled: April 26, 2012Date of Patent: December 25, 2012Inventors: Mark G. Palermo, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming Wang, Leigh Zawel, Yanlin Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
-
Patent number: 8338614Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: January 13, 2006Date of Patent: December 25, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
-
Publication number: 20120322787Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: Genzyme CorporationInventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
-
Publication number: 20120322827Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, n and L are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 13, 2011Publication date: December 20, 2012Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
-
Patent number: 8334309Abstract: Novel heterocyclic indazole derivatives of the formula (I), in which L, Q, R, X, Y, R3, R4 and R5 have the meanings indicated in Claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: April 18, 2008Date of Patent: December 18, 2012Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Markus Klein, Norbert Beier
-
Publication number: 20120309769Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
-
Publication number: 20120309794Abstract: The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.Type: ApplicationFiled: November 5, 2010Publication date: December 6, 2012Applicant: UNIVERSITÀ DI PISAInventors: Filippo Minutolo, Marco Macchia, Carlotta Granchi, Sarabindu Roy, Gino Giannaccini, Antonio Lucacchini
-
Publication number: 20120309757Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin