Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/322)
  • Patent number: 8481566
    Abstract: Compounds of formula (I) and salts and solvates are provided: wherein R4 is fluoro, R5 is selected from hydrogen, halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6alkoxy, and C1-6alkoxy substituted with one or more fluorine atoms; and R6 is selected from halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6alkoxy and C1-6alkoxy substituted with one or more fluorine atoms, and Q is hydrogen or C1-6alkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
    Type: Grant
    Filed: September 10, 2007
    Date of Patent: July 9, 2013
    Assignee: Glaxo Group Limited
    Inventors: Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Dongchuan Shi, Graham Walker
  • Patent number: 8481585
    Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: July 9, 2013
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
  • Patent number: 8481572
    Abstract: Provided is a pharmaceutical composition including as an active component a compound of formula (I): wherein X and (R1)n are as defined, and a physiological acceptable carrier. Also provided is a method for treating cancer including administering to an individual in need of such treatment an effective amount of the presently described pharmaceutical composition.
    Type: Grant
    Filed: August 10, 2008
    Date of Patent: July 9, 2013
    Assignee: Urifer Ltd.
    Inventors: Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen
  • Publication number: 20130172324
    Abstract: This invention is directed to methods of preventing or treating diseases or conditions associated with excessive cell proliferation, remodeling, inflammation, and vasoconstriction. Particularly, this invention is directed to methods of treating cardiovascular diseases or conditions such as stent restenosis and thrombosis, vascular thrombosis, cerebral vasospasm, atherosclerosis, systemic hypertension, cardiac hypertrophy, and sexual dysfunction. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel Rho kinase inhibitor compound to treat the disease.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: INSPIRE PHARMACEUTICALS, INC.
    Inventor: Inspire Pharmaceuticals, Inc.
  • Publication number: 20130172342
    Abstract: The present invention is directed to methods of treating diseases or conditions mediated by elevated persistent sodium channel, such as ocular disorders, pain, multiple sclerosis, and seizure disorders utilizing a compound of Formula I or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising said compound, wherein variables R, R1, R2, R3, R4, R5, m, and n in Formula I are as defined herein.
    Type: Application
    Filed: December 27, 2012
    Publication date: July 4, 2013
    Applicant: Allergan, Inc.
    Inventor: Allergan, Inc.
  • Publication number: 20130165433
    Abstract: The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection.
    Type: Application
    Filed: September 6, 2011
    Publication date: June 27, 2013
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Zoe Alicia Harrison, Katherine Louise Jones, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Charlotte Jane Mitchell, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christopher Alan Paul Smethurst, Yoshiaki Washio
  • Publication number: 20130165422
    Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 27, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130156731
    Abstract: The present invention relates to novel Fused Tricyclic Compounds, compositions comprising at least one Fused Tricyclic Compound, and methods of using Fused Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 20, 2013
    Inventors: Kevin X. Chen, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Publication number: 20130158047
    Abstract: Provided are heterocyclic compounds, having effects of treating and preventing inflammatory diseases and treating skin wounds, and particularly, exhibiting effects of recovering disrupted skin barriers, mitigating inflammation, and pruritus. Also, a composition containing the compound as an effective component can be used to mitigate various inflammatory diseases and protease activated receptor-2 (PAR-2)-overexpressed diseases, and can be particularly used as a composition having an anti-inflammatory function in inflammatory skin diseases including atopic dermatitis and the like, by inhibiting PAR-2 activity.
    Type: Application
    Filed: August 25, 2011
    Publication date: June 20, 2013
    Applicant: NEOPHARM CO., LTD.
    Inventors: Hyung Sub Gwak, Yong Zu Kim, Uk Il Kim, Byeong Deog Park, Tae Kyo Park, Sung Ho Woo, Joung Yul Yun, Dae Yon Lee, Hyang Sook Lee, Jeong Eun Jeon, Se Kyoo Jeong, Hyung Mook Choi
  • Publication number: 20130158014
    Abstract: This invention is directed to methods of preventing or treating diseases or conditions associated with alterations in cellular integrity including alterations in endothelial permeability, excessive cell proliferation or tissue remodeling. Particularly, this invention is directed to methods of treating diabetic nephropathy, malaria, or cancer. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel rho kinase inhibitor compound to treat the disease.
    Type: Application
    Filed: February 8, 2013
    Publication date: June 20, 2013
    Applicant: Inspire Pharmaceuticals, Inc.
    Inventor: Inspire Pharmaceuticals, Inc.
  • Publication number: 20130158002
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: February 28, 2011
    Publication date: June 20, 2013
    Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
  • Publication number: 20130149311
    Abstract: Methods, uses and kits for increasing the number of hematopoietic stem cells (HSCs) in a biological system, such as for increasing the number of HSCs in the bone marrow and/or blood of a subject, based on the modulation of growth factor independence 1b (Gfi1b), are disclosed.
    Type: Application
    Filed: May 6, 2011
    Publication date: June 13, 2013
    Applicant: INSTITUT DE RECHERCHES CLINIQUES DE MONTREAL
    Inventors: Tarik Moroy, Cyrus Khandanpour, Lothar Vassen, Ehssan Sharif-Askari
  • Publication number: 20130143880
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Application
    Filed: August 5, 2011
    Publication date: June 6, 2013
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Patent number: 8455520
    Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
  • Publication number: 20130137679
    Abstract: The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.
    Type: Application
    Filed: July 1, 2011
    Publication date: May 30, 2013
    Inventors: Jian Jin, Bryan Roth, Stephen Frye
  • Publication number: 20130131059
    Abstract: This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula I to the eyes of the patient in need of.
    Type: Application
    Filed: January 17, 2013
    Publication date: May 23, 2013
    Applicant: INSPIRE PHARMACEUTICALS, INC.
    Inventor: Inspire Pharmaceuticals, Inc.
  • Publication number: 20130131106
    Abstract: This invention relates to synthetic bifunctional compounds comprising a first rho-associated kinase (ROCK) inhibiting compound and a second pharmaceutically active compound with complementary activity; the first and the second compounds are covalently linked by a biologically labile bond. This invention also relates to methods of making such compounds. The invention also relates to methods of using such bifunctional compounds in the prevention or treatment of diseases or conditions that are affected or can be assisted by altering the integrity or rearrangement of the cytoskeleton. Particularly, this invention relates to methods of treating ophthalmic diseases such as disorders in which intraocular pressure is elevated, for example primary open-angle glaucoma, using the bifunctional compounds.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 23, 2013
    Applicant: INSPIRE PHARMACEUTICALS, INC.
    Inventor: INSPIRE PHARMACEUTICALS, INC.
  • Publication number: 20130131034
    Abstract: The instant invention relates to derivatives of formula (I) and their application in therapeutics.
    Type: Application
    Filed: March 1, 2011
    Publication date: May 23, 2013
    Applicant: SANOFI
    Inventors: Markus Follmann, Pascale Goberville, Stéphanie Hachtel, Gerhard Hessler, Heinz-Werner Kleemann, Thomas Maier, Gary MC Cort, Carsten Struebing, Bérangère Thiers, Li-Hsing Wang
  • Patent number: 8445690
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: May 21, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
  • Publication number: 20130123242
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Application
    Filed: October 26, 2012
    Publication date: May 16, 2013
    Applicant: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
  • Publication number: 20130116240
    Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
    Type: Application
    Filed: September 26, 2012
    Publication date: May 9, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventor: Japan Tobacco Inc.
  • Publication number: 20130116284
    Abstract: Provided are bifunctional compounds comprising a poly(ADP-ribose) polymerase (PARP) inhibitor moiety and a reactive oxygen species (ROS) scavenger moiety, more particularly, a lipoic acid or cyclic nitroxide derivative, covalently attached either directly or via a linker, as well as pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful for prevention, treatment, or management of diseases, disorders and conditions associated with elevated PARP activity or expression.
    Type: Application
    Filed: May 9, 2011
    Publication date: May 9, 2013
    Applicant: RADIKAL THERAPEUTICS INC.
    Inventor: Andrew Lurie Salzman
  • Patent number: 8436185
    Abstract: The present invention relates to pharmaceutically acceptable salts of an amide substituted indazole which are inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), previously known as poly(ADP-ribose)synthase and poly(ADP-ribosyl) transferase. The compounds of the present invention are useful as mono-therapies in tumors with specific defects in DNA-repair pathways and as enhancers of certain DNA-damaging agents such as anticancer agents and radiotherapy. Further, the compounds of the present invention are useful for reducing cell necrosis (in stroke and myocardial infarction), down regulating inflammation and tissue injury, treating retroviral infections and protecting against the toxicity of chemotherapy.
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: May 7, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jennifer R. Foley, Robert Darrin Wilson
  • Patent number: 8435970
    Abstract: The invention provides combinations of an ancillary compound and a compound which is a salt of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea selected from the lactate and citrate salts and mixtures thereof. Also provided are crystalline forms of the salts, methods for making the salts and their uses in treating cancers. The invention further provides combinations of an ancillary compound and a compound of the formula (I) as defined in PCT/GB2004/002824 (WO 2005/002552) or a compound of the formula (I?) or a salt, solvate, tautomer or N-oxide thereof, wherein R1, E, A and M are as defined in the claims.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: May 7, 2013
    Assignee: Astex Therapeutics Limited
    Inventors: Jayne Elizabeth Curry, Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson
  • Patent number: 8436002
    Abstract: The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: May 7, 2013
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Timothy Paul Burkholder, Joshua Ryan Clayton, MariJean Eggen, Kenneth James Henry, Jr., Deidre Michelle Johns, Saravanan Parthasarathy, Huaxing Pei, Mark Edward Rempala, Jason Scott Sawyer
  • Publication number: 20130109698
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing retroviral infection in a subject in need thereof, comprising administering to the subject a pharmaceutical composition comprising one or more of the compounds of the invention.
    Type: Application
    Filed: April 25, 2011
    Publication date: May 2, 2013
    Inventor: Simon Cocklin
  • Patent number: 8431597
    Abstract: The present invention relates to a compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3A, R3B, R4, R5, X, m, and n are as defined herein. Such novel benzamidazole derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: April 30, 2013
    Assignee: Pfizer Inc.
    Inventors: Michael J. Munchhof, Lawrence A. Reiter, Susan D. La Greca, Christopher S. Jones, Qifang Li
  • Patent number: 8426604
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: April 23, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
  • Publication number: 20130096084
    Abstract: The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
    Type: Application
    Filed: June 22, 2011
    Publication date: April 18, 2013
    Inventors: Yongqi Deng, Liang Zhu, Gerald W. Shipps, JR., Sie-Mun Lo, Binyuan Sun, Xiaohua Huang, Corey Bienstock, Alan B. Cooper, Xiaolei Gao, Xin Yao, Hugh Y. Zhu, Joseph M. Kelly, Sobhana Babu Boga, Abdul-Basit Alhassan, Jayaram R. Tagat, Umar Faruk Mansoor, Kevin J. Wilson, Brendan M. O'Boyle, Matthew Hersh Daniels, Adam Schell, Phieng Siliphaivanh, Christian Fischer
  • Publication number: 20130090342
    Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.
    Type: Application
    Filed: June 16, 2011
    Publication date: April 11, 2013
    Applicant: NOVARTIS AG
    Inventors: Frederic Berst, Pascal Furet, Andreas Marzinzik
  • Publication number: 20130085150
    Abstract: Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: September 24, 2012
    Publication date: April 4, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Oswy Z. Pereira, John Maxwell, Youssef L. Bennani, Sanjoy Kumar Das, Laval Chan Chun Kong, Jagadeeswar T. Reddy, Simon Giroux, Kevin M. Cottrell, Mark A. Morris
  • Publication number: 20130085161
    Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.
    Type: Application
    Filed: June 16, 2011
    Publication date: April 4, 2013
    Applicant: NOVARTIS AG
    Inventors: Frederic Berst, Pascal Furet, Andreas Marzinzik, Frederic Stauffer
  • Patent number: 8410089
    Abstract: A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, A1: CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: —COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: April 2, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kentaro Rikimaru, Hiroshi Imoto, Masahiro Kamaura
  • Publication number: 20130079339
    Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.
    Type: Application
    Filed: December 22, 2010
    Publication date: March 28, 2013
    Applicant: PHARMESTE S.R.L.
    Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
  • Patent number: 8404682
    Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors.
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: March 26, 2013
    Assignee: Cortex Pharmaceuticals, Inc.
    Inventors: Leslie Street, Rudolf Mueller, Steven Lee
  • Patent number: 8399502
    Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: March 19, 2013
    Assignee: SRI International
    Inventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
  • Publication number: 20130059852
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
    Type: Application
    Filed: April 8, 2011
    Publication date: March 7, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
  • Patent number: 8389511
    Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: March 5, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Hiroyuki Nakahira, Yohei Ikuma, Nobuhisa Fukuda, Kozo Yoshida, Hidenori Kimura, Satoshi Suetsugu, Akira Fusano, Kiyoto Sawamura, Junya Ikeda, Yoshio Nakai
  • Publication number: 20130053382
    Abstract: The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.
    Type: Application
    Filed: April 28, 2011
    Publication date: February 28, 2013
    Inventors: Sunil Paliwal, Matthew Paul Rainka, Ang Li, May Xiaowu Jiang, Hon-chung Tsui, Ronald J. Doll
  • Publication number: 20130045986
    Abstract: The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.
    Type: Application
    Filed: June 8, 2012
    Publication date: February 21, 2013
    Applicant: Rhizen Pharmaceuticals SA
    Inventors: Dhanapalan NAGARATHNAM, Swaroop Kumar V.S. Vakkalanka, Srikant Viswanadha, Gayatri S. Merikapudi
  • Publication number: 20130040932
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: September 24, 2012
    Publication date: February 14, 2013
    Applicants: Neuromed Pharmaceuticals Ltd., Merck Sharp & Dohme Corp.
    Inventors: Merck Sharp & Dohme Corp., Neuromed Pharmaceuticals Ltd.
  • Publication number: 20130035342
    Abstract: The present invention relates to a compound of formula (I): Wherein R1 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; R2 is an alkyl group with 1 to 18 carbon atoms or a substituted or unsubstituted cycloalkyl or aryl group; R3 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; L is a single bond, an alkyl group having 1 to 6 carbon atoms, NHCO, O, S, NHCONH or NHCOO; X, Y and Z are independently 0, N, NH, S or CH; W is a single bond or an alkyl group having from 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of said compound or salt.
    Type: Application
    Filed: December 16, 2010
    Publication date: February 7, 2013
    Applicant: NEUROPORE THERAPIES, INC.
    Inventors: Eliezer Masliah, Edward M. Rockenstein, Wolfgang Wrasidlo, Igor Flint Tsigelny
  • Patent number: 8367704
    Abstract: The present invention relates to a process for preparing 2-methyl-2?-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present invention, pharmaceutically useful 2-methyl-2?-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: February 5, 2013
    Assignee: Yuhan Corporation
    Inventors: Chun-Ho Lee, Ja-Heouk Khoo, Kyoung-Chan Kwon, Hyun Ju
  • Publication number: 20130029995
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Application
    Filed: July 25, 2012
    Publication date: January 31, 2013
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
  • Publication number: 20130029964
    Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.
    Type: Application
    Filed: August 27, 2012
    Publication date: January 31, 2013
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
  • Publication number: 20130024953
    Abstract: The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.
    Type: Application
    Filed: May 3, 2012
    Publication date: January 24, 2013
    Applicant: University of Pittsburgh - of the Commonwealth System of Higher Education
    Inventors: Stephen C. Pak, David Hirsch Perlmutter, Gary A. Silverman
  • Patent number: 8357690
    Abstract: Provided herein are methods of treating a proliferative disease in a subject, comprising administering to the subject a therapeutically effective amount of AC220 and a nucleoside analog, a topoisomerase inhibitor or an anthracycline, or a combination thereof.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: January 22, 2013
    Assignee: Ambit Biosciences Corporation
    Inventors: Robert C. Armstrong, Barbara A. Belli
  • Publication number: 20130018036
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 17, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea LOMBARDI BORGIA, Maria MENICHINCHERI, Paolo ORSINI, Achille PANZERI, Ettore PERRONE, Ermes VANOTTI, Marcella NESI, Chiara MARCHIONNI
  • Publication number: 20130017149
    Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
  • Patent number: 8354399
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: January 15, 2013
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Menichincheri, Jay Aaron Bertrand, Chiara Marchionni, Marcella Nesi, Paolo Orsini, Achille Panzeri