Hetero Ring In The Polycyclo Ring System Patents (Class 514/320)
  • Publication number: 20110165225
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: May 26, 2009
    Publication date: July 7, 2011
    Inventors: Peter Cullis, Marcel Bally
  • Publication number: 20110144159
    Abstract: The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.
    Type: Application
    Filed: April 9, 2009
    Publication date: June 16, 2011
    Inventors: Lorraine Kathleen Fay, Douglas Scott Johnson, Marvin Jay Meyers, Atli Thorarensen, Lijuan Jane Wang
  • Patent number: 7951822
    Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.
    Type: Grant
    Filed: March 30, 2009
    Date of Patent: May 31, 2011
    Assignee: Kowa Company, Ltd.
    Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Koichi Yamazaki, Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
  • Publication number: 20110124674
    Abstract: Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt: wherein Q is CH or N; R1a, R1b, R1c and R1d are independently a C1-6 alkyl, a halo-C1-6 alkyl, etc.; R2 is a hydrogen atom, etc.; R3 is independently a hydrogen atom, a C1-6 alkyl, etc., or two R3's, taken together, form a bridge such as methylene, etc.; R4a and R4b are independently a hydrogen atom, a C1-6 alkyl, etc.; Z is a bicyclic aromatic hetero ring, etc.; Ar is a benzene ring, etc.; m1 and m2 are independently 0, 1 or 2; n is an integer of from 1 to 4. The compound and its salt act as a melanin concentrating hormone receptor antagonist, and are useful as a preventive or remedy for central system disorders, cardiovascular disorders, metabolic disorders, etc.
    Type: Application
    Filed: July 14, 2009
    Publication date: May 26, 2011
    Inventors: Hiroyuki Kishino, Nagaaki Sato, Takao Suzuki
  • Publication number: 20110118312
    Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.
    Type: Application
    Filed: January 20, 2011
    Publication date: May 19, 2011
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
  • Publication number: 20110118262
    Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.
    Type: Application
    Filed: June 24, 2009
    Publication date: May 19, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
  • Publication number: 20110111057
    Abstract: The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.
    Type: Application
    Filed: October 7, 2010
    Publication date: May 12, 2011
    Inventors: John C. Reed, Maurizio Pellecchia
  • Publication number: 20110105463
    Abstract: Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.
    Type: Application
    Filed: June 24, 2009
    Publication date: May 5, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff
  • Publication number: 20110105475
    Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).
    Type: Application
    Filed: March 30, 2009
    Publication date: May 5, 2011
    Applicant: MERXCK PATENT GESELLSCHAFT
    Inventors: Didier Roche, Giséle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
  • Publication number: 20110105506
    Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 28, 2010
    Publication date: May 5, 2011
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Patent number: 7935714
    Abstract: Provided herein is a composition that contains an effective amount of one or more compounds for treating, preventing, or ameliorating a disorder such as insomnia or another sleeping disorder and using the composition.
    Type: Grant
    Filed: May 13, 2005
    Date of Patent: May 3, 2011
    Assignee: Bright Future Pharmaceutical Laboratories
    Inventors: Hsiao Chang Chan, Yu Lin Gou, Dewi Kenneth Rowlands, Yiu Wa Chung
  • Patent number: 7928125
    Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: April 19, 2011
    Assignee: SmithKline Beecham Limited
    Inventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
  • Publication number: 20110082098
    Abstract: Novobiocin analogues are useful in methods of treating, inhibiting, and/or preventing cyst formation in autosomal dominant polycystic kidney disease (ADPKD) in a subject. The disclosure provides methods of treating ADPKD comprising administering a therapeutically effective amount of a coumarin-3-carboxamide novobiocin analogue. Accordingly, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of mTOR pathway phosphoproteins P-mTOR, P-Akt and P-S6K, or combinations thereof. Further, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of Hsp-90 client proteins CFTR, ErbB2, c-Raf and Cdk4, or combinations thereof.
    Type: Application
    Filed: September 30, 2010
    Publication date: April 7, 2011
    Applicant: UNIVERSITY OF KANSAS
    Inventors: James P. Calvet, Brian S.J. Blagg, Shirin V. Sundar, Brenda S. Magenheimer
  • Patent number: 7919509
    Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: April 5, 2011
    Assignee: Kowa Company, Ltd.
    Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Hidefumi Ozawa, Ayako Tosaka, Koichi Yamazaki, Yuki Yamaguchi, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
  • Patent number: 7919508
    Abstract: The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, X and n are defined as defined herein. Additionally, a method for treating dopamine-related neurological disorders selected form the group consisting of neurological, psychological, cardiovascular, cognitive or attention disorders, substance abuse and addictive behavior, or a combination thereof, comprising administering to a patient in need of such treatment a therapeutically effective amount of compounds of formula I.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: April 5, 2011
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Gregory Shutske, Keith J. Harris, Kenneth J. Bordeau, Michael R. Angelastro, Stanly John, Joseph T. Klein, Jinqi Lu, Catherine Bomont
  • Publication number: 20110065743
    Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Application
    Filed: October 25, 2010
    Publication date: March 17, 2011
    Applicant: Research Triangle Institute
    Inventors: Frank Ivy CARROLL, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
  • Publication number: 20110065707
    Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A1, A2, R1, R2, R3, R4, R5 and R6 have the significance given herein.
    Type: Application
    Filed: September 3, 2010
    Publication date: March 17, 2011
    Inventors: Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
  • Publication number: 20110059913
    Abstract: The present invention relates to identification of Oroxylum indicum, Indian medicinal plant as a rich source for flavanoid compounds. Mucoprotective and antigastric ulcer properties in the flavone class of compounds isolated therefrom have been identified along with a flavanoids mixture in substantial yields from hexane and acetone extracts. The hexane extract was fractionated, purified and the compounds identified as Oroxylin A, Chrysin and Baicalein. The acetone extract was purified and the compounds obtained identified as methoxy chrysin, Oroxyloside methyl ester and chrysin-7-O-methyl glycoside.
    Type: Application
    Filed: November 12, 2010
    Publication date: March 10, 2011
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Janaswamy Madusudana RAO, Suresh Babu KATRAGADDA, Hari Babu TATIPAKA, Manjulatha KHANAPUR, Muralidhar Gurachar PUROHIT, Venkata Srinivas PULLELA, Jhillu Singh YADAV
  • Publication number: 20110059945
    Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
    Type: Application
    Filed: November 12, 2010
    Publication date: March 10, 2011
    Applicant: EPIX PHARMACEUTICALS, INC.
    Inventors: Ashis K. Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa Cheruku, Pini Orbach, Anurag Sharadendu, Robert Christian Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker
  • Patent number: 7902253
    Abstract: An isoflavone derivative of tectorigenin compound as shown in formula (II), its preparation method and the antiviral medicine containing it as an effective constituent. The compound structure is shown as follows: Where:: R1 is H, NH2 or SO3M; R2 is OR?; R3 is H or —CH2NR?; where R? is H, —CH2COONa or —CH2CH2NMe2; NR? is or —NMe2; M is H, Na, K or N+H (CH2CH2OH)3.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: March 8, 2011
    Assignees: Chengdu Dikang Pharmaceutical Institute, Sichuan Dikang Sci-Tech Pharmaceutical Co., Ltd.
    Inventors: Xuemin Xu, Chongjun Yuan, Jia Wang, Shangbin Qi, Hai Yin, Yanming Zeng
  • Patent number: 7893090
    Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: February 22, 2011
    Assignee: SmithKline Beecham Limited
    Inventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
  • Patent number: 7888510
    Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: February 15, 2011
    Assignee: Laboratorios del Dr. Esteve S.A.
    Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
  • Publication number: 20110015185
    Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
    Type: Application
    Filed: September 28, 2010
    Publication date: January 20, 2011
    Applicant: BIOVITRUM AB
    Inventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
  • Patent number: 7872002
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: January 18, 2011
    Assignee: Helicon Therapeutics, Inc.
    Inventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
  • Publication number: 20110009396
    Abstract: The present invention provides compounds represented by formula 1: wherein, R1 R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.
    Type: Application
    Filed: July 25, 2008
    Publication date: January 13, 2011
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Rada Dalal, Sapna Parikh, Aditi Amol Tannu
  • Patent number: 7863266
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: January 4, 2011
    Assignee: Helicon Therapeutics, Inc.
    Inventors: Alan P. Kaplan, Varsha Gupta
  • Publication number: 20100331298
    Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
    Type: Application
    Filed: December 10, 2008
    Publication date: December 30, 2010
    Applicant: CytoPathfinder, Inc.
    Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
  • Patent number: 7858614
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: December 28, 2010
    Assignee: Helicon Therapeutics, Inc.
    Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
  • Patent number: 7855193
    Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: December 21, 2010
    Assignee: EPIX Pharmaceuticals, Inc.
    Inventors: Ashis K. Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert Christian Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker
  • Patent number: 7855200
    Abstract: The present invention relates to methods of using Oroxylum indicum as a rich source for flavanoid compounds having mucoprotective and antigastric ulcer properties, and containing Oroxylin A, Chrysin and Baicalein.
    Type: Grant
    Filed: January 9, 2007
    Date of Patent: December 21, 2010
    Assignee: Council of Scientific and Industrial Research
    Inventors: Janaswamy Madusudana Rao, Suresh Babu Katragadda, Hari Babu Tatipaka, Manjulatha Khanapur, Muralidhar Gurachar Purohit, Venkata Srinivas Pullela, Jhillu Singh Yadav
  • Patent number: 7842704
    Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: November 30, 2010
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Sarah Dunham
  • Patent number: 7842716
    Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.
    Type: Grant
    Filed: March 29, 2004
    Date of Patent: November 30, 2010
    Assignee: HeartDrug Research, LLC
    Inventor: Victor L. Serebruany
  • Patent number: 7838535
    Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: November 23, 2010
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Sarah Dunham
  • Publication number: 20100292218
    Abstract: The present invention provides compounds of formulae Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va and the therapeutic use thereof. The present invention also includes methods of treating NF2-deficient or NF1-deficient cells or neurodegenerative diseases with radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va. Furthermore, the present invention is directed to methods of inhibiting the growth of NF2-deficient or NF1-deficient tumors. The methods comprise contacting NF2-deficient or NF1-deficient tumor cells with radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va. The present invention is also directed to the combinational use of radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va with at least one additional active agent, such as one or more HSP90 inhibitors.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 18, 2010
    Inventors: Ruihong CHEN, Allan E. Rubenstein, Jin-Chen Yu, Nicolas Winssinger, Sofia Barluenga
  • Publication number: 20100286124
    Abstract: The present invention relates to new prop-2-yn-1-amine inhibitors of monoamine oxidase type B activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 9, 2010
    Publication date: November 11, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20100286201
    Abstract: New polymorphic forms of (S)-2-((4-benzofuranyl)carbonylamino methyl)-1-((4-(2-methyl-5-(4-fluorophenyl))thiazolyl)carbonyl)piperidine, methods for their preparation and use in medicine.
    Type: Application
    Filed: September 11, 2008
    Publication date: November 11, 2010
    Inventor: Leanda Jane Kindon
  • Patent number: 7816376
    Abstract: The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R1, R3, R4, R8, p, k, E, G, Z and Q are as defined in claim 1, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: October 19, 2010
    Assignee: Merck Patent GmbH
    Inventors: Oliver Schadt, Joachim Leibrock, Helmut Pruecher, Christoph Seyfried
  • Patent number: 7812019
    Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
    Type: Grant
    Filed: November 22, 2005
    Date of Patent: October 12, 2010
    Assignee: Abbott Laboratories
    Inventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
  • Patent number: 7812034
    Abstract: Liposarcomas are treated using HIV protease inhibitors, particularly nelfinavir. The protease inhibitors may be used alone or in combination with traditional cancer treatments, such as chemotherapy, radiotherapy, or surgery.
    Type: Grant
    Filed: November 2, 2004
    Date of Patent: October 12, 2010
    Assignee: City of Hope
    Inventors: Warren Chow, Chu-Chih Shih
  • Publication number: 20100256142
    Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
    Type: Application
    Filed: September 25, 2009
    Publication date: October 7, 2010
    Inventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
  • Publication number: 20100249094
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: March 10, 2010
    Publication date: September 30, 2010
    Inventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
  • Patent number: 7803814
    Abstract: The present invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart disease, hypertension, rheumatoid arthritis or inflammation, comprising administering to a patient in thereof an effective amount of a compound of Formula (I).
    Type: Grant
    Filed: December 8, 2004
    Date of Patent: September 28, 2010
    Assignee: Eli Lilly and Company
    Inventors: Konstantinos Gavardinas, Jonathan Edward Green, Prabhakar Kondaji Jadhav, Donald Paul Matthews
  • Publication number: 20100240679
    Abstract: Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: May 28, 2010
    Publication date: September 23, 2010
    Inventors: Richard Sedrani, Juergen Klaus Maibaum, Werner Breitenstein, Holger Sellner, Claus Ehrhardt, Nils Ostermann
  • Patent number: 7799824
    Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: September 21, 2010
    Assignee: OraPharma, Inc.
    Inventors: Bharat Lagu, Michael Wachter
  • Publication number: 20100233166
    Abstract: Compounds, compositions and methods for the treatment of malignancy are disclosed.
    Type: Application
    Filed: April 13, 2010
    Publication date: September 16, 2010
    Inventors: George C. Prendergast, Alexander J. Muller, James B. Duhadaway, William Malachowski
  • Patent number: 7790750
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(?O)—R9, or -Alk-Y—C(?O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each indepen
    Type: Grant
    Filed: October 20, 2006
    Date of Patent: September 7, 2010
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
  • Patent number: 7790752
    Abstract: This invention relates to indol-3-yl-carbonyl-azaspiro derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the azaspiro-head group A and the residues R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
    Type: Grant
    Filed: September 21, 2006
    Date of Patent: September 7, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Publication number: 20100210657
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
    Type: Application
    Filed: May 4, 2010
    Publication date: August 19, 2010
    Applicant: JANSSEN PHARMACEUTICA N.V.
    Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
  • Patent number: 7776876
    Abstract: Embodiments of this invention provide methods for thereapeutic use of cyclic G-2-Allyl Proline to treat disorders of dopaminergic neurons, including Parkinson's disease. Cyclic G-2Allyl P is neuroprotective and has utility as a therapeutic agent for treatment of diseases and other conditions characterised by degeneration and/or death of dopaminergic neurons and the adverse symptoms of such degeneration and/or death. Such symptoms include loss of cognition and motor function. Compounds are also useful for manufacture of medicaments including tablets, capsules and injectable solutions that are useful for treatment of such conditions.
    Type: Grant
    Filed: April 7, 2006
    Date of Patent: August 17, 2010
    Assignee: Neuren Pharmaceuticals, Ltd.
    Inventors: Margaret Anne Brimble, Jian Guan
  • Publication number: 20100204220
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Application
    Filed: July 14, 2008
    Publication date: August 12, 2010
    Inventors: Mohamed Naquib Attala, Philippe Diaz