Hetero Ring Is Five-membered Patents (Class 514/91)
  • Patent number: 10869856
    Abstract: Substituted phenylpyrrolecarboxamide compounds such as those represented by Formula A can be used in the treatment of HIV infection and related conditions.
    Type: Grant
    Filed: January 30, 2020
    Date of Patent: December 22, 2020
    Assignees: New York Blood Center, Inc., The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 10576059
    Abstract: Substituted phenylpyrrolecarboxamide compounds such as those represented by Formula A can be used in the treatment of HIV infection and related conditions.
    Type: Grant
    Filed: July 24, 2019
    Date of Patent: March 3, 2020
    Assignees: New York Blood Center, Inc., The United States of America, as Represented by the Secretary, Department of Human Services
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 10413527
    Abstract: Substituted phenylpyrrolecarboxamide compounds such as those represented by Formula A can be used in the treatment of HIV infection and related conditions.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: September 17, 2019
    Assignees: New York Blood Center, Inc., The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 10137107
    Abstract: Substituted phenylpyrrolecarboxamide compounds such as those represented by Formula A can be used in the treatment of HIV infection and related conditions.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: November 27, 2018
    Assignees: New York Blood Center, Inc., National Institutes of Health
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 10065133
    Abstract: The present invention provides phosphoryl choline derivatives of general formula (I), which are suitable to be immobilized on a solid support to provide a separation material of general formula (II), which bind with both high affinity and high specificity to a protein, more specifically to C-reactive protein and anti-phosphoryl choline antibodies. Said separation materials are particularly useful in the extracorporeal removal of C-reactive protein and anti-phosphoryl choline antibodies from a biological fluid of a patient for prophylaxis and/or treatment of immune dysfunctions and cardiovascular diseases. Also provided is a column that comprises the separation material of general formula (II), as well as a device containing the column. Formula (I), wherein variable X is selected from: —SH, —NHR3, —C?CH, —CH?CH2, —N3 and —CHO; the other variables are as defined in the claims: Formula (II), wherein variable “A” represents a solid support. “A” as well as the other variables are defined in detail in the claims.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: September 4, 2018
    Assignee: Pentracor GmbH
    Inventors: Victor Prisyazhnoy, Stephan Mattecka, Ahmed Sheriff, Roderich Süssmuth
  • Patent number: 10010532
    Abstract: The present technology provides compositions and methods for treating chronic kidney disease, end-stage renal disease, or diabetic nephropathy. The compositions comprise a nitrated lipid and an inhibitor of the renin-angiotensin-aldosterone system. The methods comprise administering a nitrated lipid in combination with an inhibitor of the renin-angiotensin-aldosterone system to a subject in need thereof, in an amount effective to treat diabetic nephropathy, chronic kidney disease, and/or end-stage renal disease. The use of a nitrated lipid with an inhibitor of the renin-angiotensin-aldosterone system exhibits a synergistic effect in treating chronic kidney disease and diabetic nephropathy.
    Type: Grant
    Filed: October 23, 2015
    Date of Patent: July 3, 2018
    Assignee: The University of Utah Research Foundation
    Inventor: Tianxin Yang
  • Patent number: 9926317
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: July 9, 2015
    Date of Patent: March 27, 2018
    Assignee: Merck Sharp Dohme Corp.
    Inventors: Alexander Pasternak, Ian Davies, Fa-Xiang Ding, Jinglong Jiang, Shuzhi Dong, Xin Gu
  • Patent number: 9730949
    Abstract: The present invention relates to an ophthalmic composition comprising at least one angiotensin converting enzyme (ACE) inhibitor and a pharmaceutically acceptable vehicle for use as an ophthalmic neuroprotector in treating an optic neuropathy or congenital optic atrophy.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: August 15, 2017
    Inventor: Raouf Rekik
  • Patent number: 9573961
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: February 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Reynalda Keh DeJesus, Jessica L. Frie, Barbara Pio, Haifeng Tang, Shawn P. Walsh
  • Patent number: 9493412
    Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: November 15, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends
  • Patent number: 9278922
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Grant
    Filed: April 14, 2010
    Date of Patent: March 8, 2016
    Assignee: ABBVIE INC.
    Inventors: Pamela L. Donner, Lissa T. Nelson, Tammie K. Jinkerson, Ryan G. Keddy, Christopher E. Motter, Mark A. Matulenko, Allan C. Krueger, David A. DeGoey, Sachin V. Patel, John T. Randolph, Warren M. Kati, Charles W. Hutchins, Todd N. Soltwedel
  • Publication number: 20150141251
    Abstract: The present disclosure relates to a pesticidal formulation including i) at least one pesticide, typically an organophosphate compound in an amount between 5.0% w/w and 40.0% w/w, preferably between 15.0% w/w and 30.0% w/w, ii) Solvent system comprising at least one glycol ether and at least one lactone in an amount between 10.0% to 80.0% w/w, preferably between 30.0% w/w and 55% w/w, with ratio of the glycol ether and the lactone is the in the range of 1:9 and 9:1, preferably in the range of 2:8 and 4:6, iii) Surfactant system containing at least two nonionic surfactants where the primary surfactant has an HLB range of 10 to 20 and the co-surfactant has a HLB range 1 to 5, in an amount ranging between 0.1% w/w to 60.0% w/w preferably in the range of 20.0% w/w to 40.0% w/w, and iv) at least one excipient in the range of 0.1% w/w to 10% w/w and preferably 0.5% w/w to 5.0% w/w.
    Type: Application
    Filed: October 15, 2013
    Publication date: May 21, 2015
    Applicant: GOWAN COMERCIO INTERNACIONAL E SERVICOS LIMIADA
    Inventors: Howard Bernard DAWSON, Rachel BRANAGHAN, Eric James MCEWEN, Sandra ALCARAZ, Tak Wai CHEUNG
  • Publication number: 20150005260
    Abstract: The present invention relates to methods and kits for detecting diastolic dysfunction in subjects without clinical signs of heart failure.
    Type: Application
    Filed: January 2, 2013
    Publication date: January 1, 2015
    Inventors: Faiez Zannad, Patrick Rossignol
  • Publication number: 20140309193
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 16, 2014
    Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang
  • Publication number: 20140274962
    Abstract: Described herein are methods of inhibiting or reversing the progression of presbyopia in an eye by administering a ?L-crystallin electrostatic interaction inhibitor. Presbyopia is caused by aggregation of the soluble crystalline lens proteins called the crystallins, particularly ?L-crystallin. It has been found that the aggregation of ?L-crystallin is an electrostatic phenomenon and that electrostatic interaction inhibitors can be employed to prevent the formation of ?L-crystallin aggregates as well as to deaggregate already formed aggregates.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 18, 2014
    Applicant: UNIVERSITY OF MASSACHUSETTS
    Inventors: Murugappan Muthukumar, Zhaoyang Ou, Deniz Civay
  • Patent number: 8835394
    Abstract: The present invention provides a method of treating basal cell carcinoma in a subject. Generally, the method includes administering to the subject an amount of IRM compound effective for treating basal cell carcinoma in a treatment cycle that includes at least two consecutive days in which the IRM compound is administered and at least one day in which the IRM compound is not administered.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: September 16, 2014
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Mary L. Owens, Terrance L. Fox, Angela M. Ginkel
  • Publication number: 20140255517
    Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.
    Type: Application
    Filed: March 5, 2014
    Publication date: September 11, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Kerry J. Ressler, Paul J. Marvar
  • Patent number: 8828974
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: September 9, 2014
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz
  • Publication number: 20140228323
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Scott Louis COHEN, Dean Franklin Rigel
  • Publication number: 20140206618
    Abstract: The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 24, 2014
    Inventors: Alexander Pasternak, Timothy Blizzard, Harry Chobanian, Reynalda de Jesus, Fa-Xiang Ding, Shuzhi Dong, Candido Gude, Dooseop Kim, Haifeng Tang, Shawn Walsh, Barbara Pio, Jinlong Jiang
  • Publication number: 20140206632
    Abstract: A method for determining the risk, severity or progression of cardiovascular disease, such as cardiac heart failure. A method for determining the likelihood of admission to the hospital for cardiac heart failure. The methods include determining the concentration of ET-1 and the concentration of one or more of biomarkers selected from the group consisting of cardiac troponin (e.g., cTnI, cTnT), VEGF, BNP, NT-proBNP, and IL-6 in a blood, serum or plasma sample from the patient.
    Type: Application
    Filed: January 22, 2014
    Publication date: July 24, 2014
    Applicant: Singulex, Inc.
    Inventors: John Todd, Joel Estis, Victoria Torres
  • Publication number: 20140093513
    Abstract: The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
    Type: Application
    Filed: May 24, 2013
    Publication date: April 3, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Chi B. Vu
  • Publication number: 20140057873
    Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.
    Type: Application
    Filed: November 1, 2013
    Publication date: February 27, 2014
    Inventor: Michael Farber
  • Publication number: 20130338110
    Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.
    Type: Application
    Filed: May 20, 2013
    Publication date: December 19, 2013
    Inventors: David A. ZARLING, Hirak S. BASU, Balaraman KALYANARAMAN, Joy JOSEPH
  • Publication number: 20130324531
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2 and R3 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: May 29, 2013
    Publication date: December 5, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, George Kenneth Ehrlich, Jin-Jun Liu, Hanspeter Michel, Binh Thanh Vu, Chunlin Zhao
  • Patent number: 8592399
    Abstract: The invention relates to novel compounds that have S1P receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as autoimmune response.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: November 26, 2013
    Assignee: Akaal Pharma Pty Ltd.
    Inventors: Gurmit S. Gill, Damian W. Grobelny
  • Publication number: 20130287688
    Abstract: Methods and compositions for improving the delivery and/or efficacy of a therapy (e.g., a cancer therapy) are disclosed. In one embodiment, methods and compositions for treating or preventing a cancer (e.g., a solid tumor such as a desmoplastic tumor) by administering to a subject an anti-hypertensive agent, as a single agent or in combination with a microenvironment modulator and/or a therapy, e.g., a cancer therapy (for example, a therapeutic agent or therapy, including immunotherapy (e.g., antibodies, vaccine, cell-based), nanotherapeutics, radiation therapy, photodynamic therapy, low molecular weight chemotherapeutics, molecularly targeted therapeutics and/or oxygen radical) are disclosed.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 31, 2013
    Applicants: XTUIT PHARMACEUTICALS, INC., THE GENERAL HOSPITAL CORPORATION
    Inventors: The General Hospital Corporation, Xtuit Pharmaceuticals, Inc.
  • Patent number: 8569267
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain with binding affinities towards dopamine receptors, in particular dopamine D2 receptors, towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: June 16, 2006
    Date of Patent: October 29, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez
  • Publication number: 20130244958
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: March 5, 2013
    Publication date: September 19, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Binh Thanh Vu, Chunlin Zhao, Daniel Fishlock
  • Publication number: 20130225530
    Abstract: The present invention relates to a pharmaceutical composition for use as a medicament for the treatment or prophylaxis of cardiac hypertrophy, comprising at least one compound of formula (I), wherein: R1 is e.g. hydrogen, —CH3, R2 is e.g. hydrogen, —CH3, R4 is hydrogen, —OH, —NH2; R5 is hydrogen, —OH; R6 is hydrogen, —OH; R3 is e.g. —OCH3 or a pharmaceutically acceptable salt, and at least one pharmaceutical excipient.
    Type: Application
    Filed: July 6, 2011
    Publication date: August 29, 2013
    Applicant: DKFZ DEUTSCHES KREBSFORSCHUNGSZENTRUM
    Inventors: Min Li-Weber, H. Peter Krammer, Gernot Polier
  • Publication number: 20130225529
    Abstract: Phospho-ester compounds and pharmaceutical compositions thereof administered by the respiratory and other routes for the prevention and/or treatment of lung and brain cancer and precancerous conditions thereof, for the treatment of pain, for the treatment of skin disorders, for treating and/or preventing inflammation-related diseases, and for the treatment and prevention of cancer.
    Type: Application
    Filed: February 27, 2013
    Publication date: August 29, 2013
    Inventor: Basil RIGAS
  • Patent number: 8513220
    Abstract: Novel aromatic compounds which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: August 8, 2012
    Date of Patent: August 20, 2013
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Xiaoxia Liu
  • Publication number: 20130178445
    Abstract: Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP-1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.
    Type: Application
    Filed: December 17, 2012
    Publication date: July 11, 2013
    Applicant: OLEMA PHARMACEUTICALS, INC.
    Inventor: OLEMA PHARMACEUTICALS, INC.
  • Publication number: 20130178424
    Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
    Type: Application
    Filed: February 13, 2013
    Publication date: July 11, 2013
    Applicant: AbbVie Deutschland GmbH & Co. KG
    Inventor: AbbVie Deutschland GmbH & Co. KG
  • Publication number: 20130157982
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 11, 2013
    Publication date: June 20, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130157984
    Abstract: The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds.
    Type: Application
    Filed: November 28, 2012
    Publication date: June 20, 2013
    Inventor: Simon Fraser University
  • Publication number: 20130101514
    Abstract: Activated fatty acids, pharmaceutical composition compositions including activated fatty acids, methods for using activated fatty acids to treat nephropathy, and methods for preparing activated fatty acids are provided herein.
    Type: Application
    Filed: October 10, 2012
    Publication date: April 25, 2013
    Applicant: Complexa, Inc.
    Inventor: Complexa, Inc.
  • Patent number: 8394785
    Abstract: The present invention relates to a method for the treatment and/or amelioration of urticaria, the method comprising the administration of a pharmaceutically active dose of a compound of formula I to a subject in need of such a treatment and/or amelioration.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: March 12, 2013
    Assignee: Jado Technologies GmbH
    Inventors: Tobias Braxmeier, Tim Friedrichson, Gary Jennings
  • Publication number: 20130018019
    Abstract: Novel aromatic compounds which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 8, 2012
    Publication date: January 17, 2013
    Applicant: ALLERGAN, INC.
    Inventors: Janet A. Takeuchi, Ling Li, Xiaoxia Liu
  • Publication number: 20130012479
    Abstract: The present invention relates to new crystalline polymorphs of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and their use, in particular for the preparation of medicaments.
    Type: Application
    Filed: June 27, 2012
    Publication date: January 10, 2013
    Applicant: SANOFI
    Inventors: Norbert NAGEL, Bruno BAUMGARTNER, Harald BERCHTOLD, Oliver PLETTENBURG, Dieter KADEREIT, Mandy MOHNICKE, Simon GESSLER, Joachim TILLNER
  • Publication number: 20130012444
    Abstract: The present invention relates to crystalline solvates of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and the use thereof.
    Type: Application
    Filed: June 27, 2012
    Publication date: January 10, 2013
    Applicant: SANOFI
    Inventors: Norbert NAGEL, Bruno BAUMGARTNER, Harald BERCHTOLD, Oliver PLETTENBURG, Dieter KADEREIT, Mandy MOHNICKE, Simon GESSLER, Joachim TILLNER
  • Publication number: 20130004518
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Publication number: 20120301458
    Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof
    Type: Application
    Filed: July 27, 2010
    Publication date: November 29, 2012
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 8309536
    Abstract: A bone implant comprises an active agent on at least a portion thereof. The active agent is locally deliverable to bone proximate the implant in at least a two-phased release scheme. A first phase rapidly releases a first quantity of the active agent, and at least a second phase gradually releases a second quantity of the active agent, whereby bone formation stimulated by the active agent is modulated. In one embodiment, a porous implant comprises a porous portion coated with a calcium phosphate compound and which is contacted with a bisphosphonate compound to form a bisphosphonate layer chemically bound to the calcium phosphate at the surface of the porous portion and to form bisphosphonate molecules being non-chemically attached inside the pores of the porous portion. The non-chemically attached bisphosphonate molecules are released in the subject at a rate greater than that of the chemically bound bisphosphonate layer.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: November 13, 2012
    Inventors: John Dennis Bobyn, Michael Tanzer
  • Publication number: 20120225846
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Publication number: 20120208784
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Application
    Filed: April 24, 2012
    Publication date: August 16, 2012
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: Yong Mi CHOI-SLEDESKI, Julian LEVELL, Gregory Bernard POLI, Mark CZEKAJ, Alan John COLLIS, Roy VAZ
  • Publication number: 20120178681
    Abstract: Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 12, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: HAROLD B. WOOD, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang
  • Publication number: 20120142638
    Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising a therapeutic agent acting on the renin-angiotensin system (RAS) or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention of, delay of progression of, treatment of diseases and disorders that may be modulated by action on the renin-angiotensin system (RAS), appetency disorders or substance abuse disorders.
    Type: Application
    Filed: February 13, 2012
    Publication date: June 7, 2012
    Inventor: Randy Lee Webb
  • Patent number: 8183231
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: May 22, 2012
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz