Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/214.02)
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Publication number: 20120329781Abstract: The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI) or one or both of a selective serotonin re-uptake inhibitor (SSRI) and a selective noradrenaline re-uptake inhibitor (SNRI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.Type: ApplicationFiled: August 29, 2012Publication date: December 27, 2012Inventors: David James Dooley, Mark John Field, Richard Griffith Williams
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Publication number: 20120316148Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.Type: ApplicationFiled: June 7, 2012Publication date: December 13, 2012Applicant: Dynamix Pharmaceuticals LTD.Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
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Publication number: 20120316138Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing obesity or diabetes, optionally in combination with a second treatment therapy such a diet restriction or an increase in duration or exertion in physical activity.Type: ApplicationFiled: December 15, 2010Publication date: December 13, 2012Applicant: METABOLIC SOLUTIONS DEVELOPMENT COMPANY, LLCInventors: Gerard R. Colca, Rolf F. Kletzien, Steven P. Tanis, Scott D. Larsen
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Publication number: 20120309745Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: December 7, 2011Publication date: December 6, 2012Inventors: Kevin Peese, B. Narasimhulu Naidu, Manoj Patel, Chen Li, Michael A. Walker
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Publication number: 20120309698Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: December 6, 2011Publication date: December 6, 2012Inventors: Yasutsugu Ueda, Timothy P. Connolly, Barry L. Johnson, Chen Li, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Margaret E. Sorenson, Michael A. Walker, Michael S. Bowsher, Rongti Li
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Publication number: 20120302524Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).Type: ApplicationFiled: December 28, 2010Publication date: November 29, 2012Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTUREInventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
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Publication number: 20120301458Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereofType: ApplicationFiled: July 27, 2010Publication date: November 29, 2012Applicant: Auspex Pharmaceuticals, Inc.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20120302552Abstract: The invention provides a method of treatment of hot flush with S-mirtazapine and the use of S-mirtazapine for the manufacture of a medicament for the treatment of hot flush.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Applicant: N. V. OrganonInventors: Bernardus Wijnand Mathys Marie Peeters, Anton Egbert Peter Adang
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Patent number: 8318720Abstract: In part, the present invention is directed to antibacterial compounds.Type: GrantFiled: July 19, 2007Date of Patent: November 27, 2012Assignee: Affinium Pharmaceuticals, Inc.Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
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Publication number: 20120295888Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: January 13, 2011Publication date: November 22, 2012Inventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
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Publication number: 20120277214Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: November 24, 2010Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Publication number: 20120277215Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.Type: ApplicationFiled: July 2, 2012Publication date: November 1, 2012Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
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Patent number: 8299061Abstract: This invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof; as well as a method for treating obesity, a method for treating diabetes, and a pharmaceutical composition.Type: GrantFiled: December 7, 2010Date of Patent: October 30, 2012Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Thomas James Beauchamp, Emily Jane Canada, Erik James Hembre, Jianliang Lu, John Robert Rizzo, John Mehnert Schaus, Qing Shi
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Patent number: 8293276Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic)acid-poly(ethylene)glycol.Type: GrantFiled: May 17, 2011Date of Patent: October 23, 2012Assignee: Bind Biosciences, Inc.Inventors: Greg Troiano, Michael Figa, Abhimanyu Sabnis
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Publication number: 20120252748Abstract: The present invention relates to methods for predicting the responsiveness of a patient to a breast cancer treatment regimen by assaying a biological sample to determine the level of expression of the long-chain fatty acyl-CoA synthetase 4 (ACSL4) in the biological sample. The present invention also provides ACSL4 inhibitors and uses of ACSL4 inhibitors as adjuvant therapies in breast cancer treatment regimens.Type: ApplicationFiled: March 28, 2012Publication date: October 4, 2012Inventor: Marie Monaco
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Publication number: 20120245146Abstract: The invention provides a method to effectively wean a woman from hormone therapy for treatment of vasomotor symptoms by reducing the dosage of the hormonal agent to zero, while a non-hormonal drug in an amount, which is therapeutically effective for treating vasomotor symptoms, is administered or initiated and continued for a limited period of a duration between 3 and 8 months.Type: ApplicationFiled: May 15, 2012Publication date: September 27, 2012Inventor: Edward Baker
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Publication number: 20120245126Abstract: Nitromethylene analogues of imidacloprid and divalent and oxabridged heterocyclic neonicotinoid compounds constructed by dialdehydes, preparation methods and uses thereof are disclosed. Compounds represented by formula (A) or (B), their optical isomers or agrochemically acceptable salts are provided. Agrochemical compositions comprising the said compounds, their optical isomers or agrochemically acceptable salts, the uses of the said agrochemical compositions and the preparation methods of the said compounds, their optical isomers or agrochemically acceptable salts are also disclosed. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm and armyworm.Type: ApplicationFiled: December 9, 2010Publication date: September 27, 2012Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Xuhong Qian, Zhong Li, Xusheng Shao, Xiaoyong Xu, Zhiping Xu, Gonghua Song
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Patent number: 8268813Abstract: This invention is directed generally to zilpaterol enantiomer compositions, and, in particular, to compositions comprising the 6R,7R zilpaterol enantiomer. This invention is also directed to processes for making such compositions; methods for using such compositions to, for example, increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and/or fish; and uses of such compositions to make medicaments. This invention is further directed to methods for determining the absolute configurations of zilpaterol enantiomers.Type: GrantFiled: July 10, 2007Date of Patent: September 18, 2012Assignee: Intervet International B.V.Inventors: Christian Miculka, Thorsten Meyer, Christopher Kern, Serge Francois Droux
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Publication number: 20120220571Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein X is O or N(R3); and R1, R2, R3 and Y are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: August 16, 2010Publication date: August 30, 2012Inventors: John S. Wai, Dai-shi Su, Catherine M. Wiscount
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Patent number: 8252784Abstract: Base-polymerizable or base-crosslinkable compositions comprising select bicyclic amines with benzylic substitution undergo photochemically induced, base-catalysed reactions upon photochemical conversion of the benzylically substituted amine to an amidine derivative.Type: GrantFiled: November 12, 2008Date of Patent: August 28, 2012Assignee: BASF SEInventors: Gisèle Baudin, Kurt Dietliker, Tunja Jung
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Publication number: 20120208795Abstract: The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamopituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.Type: ApplicationFiled: January 13, 2012Publication date: August 16, 2012Applicant: Board of Supervisors of Louisiana State University & Agricultural & Mechanical CollegeInventor: Nicholas E. Goeders
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Publication number: 20120207766Abstract: The present invention is directed to the identification of novel mechanisms involved in the initiation and spreading of axonal degeneration. In particular, the instant invention relates to the identification of a relationship between Toll-Like Receptors (TLRs) and axonal degeneration and the use of TLR inhibitors as antagonists of axonal degeneration.Type: ApplicationFiled: January 30, 2012Publication date: August 16, 2012Inventors: Athena Soulika, David Pleasure
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Publication number: 20120196824Abstract: The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.Type: ApplicationFiled: October 8, 2010Publication date: August 2, 2012Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Tomofumi Setsuta, Maki Seki, Hiroshi Iwasaki, Minoru Tanaka
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Publication number: 20120157445Abstract: Provided herein are methods, drug formulations, and dosing regimens for improving cognitive function in a normal or cognitively impaired subject. For instance, methods provided herein comprise administering a GABAA receptor antagonist so that peak concentration of the GABAA receptor antagonist occurs when the subject is asleep.Type: ApplicationFiled: December 15, 2011Publication date: June 21, 2012Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Craig C. Garner, H. Craig Heller, Damien Colas, Daniel Z. Wetmore
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Publication number: 20120149689Abstract: The invention provides a method to effectively wean a woman from hormonal therapy for treatment of vasomotor symptoms by reducing the dosage of the hormonal agent to zero, while a non-hormonal drug in an amount, which is therapeutically effective for treating vasomotor symptoms, is administered or initiated and continued for one or more periods of durations determined by assessment of the effect of a treatment free period, which follows each period of continuous non-hormonal drug treatment.Type: ApplicationFiled: February 23, 2012Publication date: June 14, 2012Inventors: Edward Baker, Simon Johannes van den Berg
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Publication number: 20120142672Abstract: The present invention provides a heterocycle derivative having a superior amyloid ? production inhibitory activity and use thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: July 12, 2010Publication date: June 7, 2012Inventors: Tatsuki Koike, Yasutaka Hoashi, Yoshihide Tomata
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Publication number: 20120135980Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: December 18, 2009Publication date: May 31, 2012Inventors: Theodros Asberom, Zhaoning Zhu, John W. Clader, Zhong-Yue Sun, Mihirbaran Mandal, Gioconda Gallo, Xiaoxiang Liu
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Publication number: 20120135981Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: July 13, 2010Publication date: May 31, 2012Inventors: Tongfei Wu, Henricus Jacobus Maria Gijsen, Frederik Jan Rita Rombouts, François Paul Bischoff, Didier Jean-Claude Berthelot, Daniel Oehlrich, Michel Anna Jozef De Cleyn, Serge Maria Aloysius Pieters, Garrett Berlond Minne, Adriana Ingrid Velter', Sven Franciscus Anna Van Brandt, Michel Surkyn
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Publication number: 20120115848Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, U1, U2, U3, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: October 6, 2011Publication date: May 10, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Robert A. Galemmo, JR., Dean Richard Artis, I, Xiaocong Michael Ye, Danielle L. Aubele, Anh P. Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20120115849Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.Type: ApplicationFiled: November 7, 2011Publication date: May 10, 2012Inventors: Gregory A. Demopulos, George A. Gaitanaris
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Publication number: 20120108570Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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Publication number: 20120094978Abstract: Compositions, kits and methods for the treatment or prevention of ocular allergies and inflammation and the symptoms thereof comprising alcaftadine or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 4, 2011Publication date: April 19, 2012Inventors: Jagdish Parasrampuria, Avner Ingerman, Frans Janssens, Anton Megens
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Publication number: 20120083485Abstract: The present invention is directed to methods of treating patients for pain by administering noribogaine. Noribogaine may also be used to treat patients for the symptoms associated with withdrawal from drug dependency. In the latter case, the noribogaine treatment should be supplemented with the administration of an opioid antagonist such as naloxone.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Inventor: Deborah C. Mash
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Patent number: 8148364Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: GrantFiled: May 16, 2008Date of Patent: April 3, 2012Assignees: Sanofi-Aventis, Mitsubishi Tanabe Pharma CorporationInventors: Nathalie Chereze, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Publication number: 20120065187Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Applicants: ALCON RESEARCH, LTD, KALYPSYS, INC.Inventors: Allen J. Borchardt, Clay Beauregard, Travis Cook, Robert L. Davis, Daniel A. Gamache, John M. Yanni
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Publication number: 20120058940Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: March 8, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG
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Publication number: 20120058189Abstract: This invention generally relates to processes for making a crystalline zilpaterol salt, particularly zilpaterol hydrochloride. This invention also relates to methods of treatment using a crystalline zilpaterol salt prepared in accordance with this invention to increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and fish.Type: ApplicationFiled: March 3, 2011Publication date: March 8, 2012Inventors: Oliver Krebs, Philipp Kuenti, Christoph Michlig, Karl Reuter
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Publication number: 20120058989Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, D, E, G, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: April 7, 2011Publication date: March 8, 2012Applicant: Achaogen, Inc.Inventors: Allan S. Wagman, Heinz E. Moser, Glenn A. McEnroe, James B. Aggen, Martin S. Linsell, Adam A. Goldblum, John H. Griffin, Lloyd J. Simons, Thomas R. Belliotti, Christina R. Harris, Toni-Jo Poel, Michael J. Melnick, Ricky D. Gaston
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Patent number: 8119628Abstract: 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 are useful in treating those infected with HCV.Type: GrantFiled: March 25, 2009Date of Patent: February 21, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Zhong Yang, John A. Bender, John F. Kadow
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Publication number: 20120022045Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, ?3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: January 25, 2010Publication date: January 26, 2012Inventors: Shankar Venkatraman, John S. Wai, Wayne Thompson, Boyoung Kim, Richard C.A. Isaacs, H. Marie Loughran, Dai-Shi Su, John Lim, Mark W. Embrey, Peter D. Williams
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Patent number: 8101595Abstract: Compounds of the formula (I) wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.Type: GrantFiled: December 19, 2007Date of Patent: January 24, 2012Assignee: Istituto di Ricerche di Biologia Molecolare P. Angletti SpAInventors: Ian Stansfield, Uwe Koch, Joerg Habermann, Frank Narjes
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Publication number: 20120015930Abstract: The present invention provides substituted imidazoheterocycles having the general structure of formula I: wherein Y is chosen from —O—, —OCRgRh—, —CRgRhO—, —CRgRh—, —(CRgRh)2—, —NRi—, —CRgRhNRi— and —NRiCRgRh—. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: December 1, 2009Publication date: January 19, 2012Applicant: CARA THERAPEUTICS, INC.Inventors: Stephen J. O'Connor, Jason S. Newcom, Janet L. Ralbovsky, Gary R. Gustafson, R. Paul Beckett, Robert Zhiyong Luo
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Publication number: 20110312940Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: October 15, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars Van Der Veen, Darryl McConnell, Tobias Wunberg
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Publication number: 20110305636Abstract: Briefly described, embodiments of this disclosure include compounds as described herein, labeled compounds as described herein, pharmaceutical composition including compounds described herein, methods of imaging, method of forming a compound as described herein, and the like. In particular, embodiments of the disclosure include a series of triamino-pyridine derivatives and labeled triamino-pyridine derivatives, methods of synthesizing these compounds, intermediate compounds, methods of treatment using these compounds, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a condition (e.g., corticotropin releasing factor type-1 (CRF1)) and/or related biological events, using triamino-pyridine derivatives, and the like. In addition, the present disclosure includes compositions (e.g., labeled triamino-pyridine derivatives that are ligands for the CRF1 receptor) used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging or SPECT imaging).Type: ApplicationFiled: March 12, 2010Publication date: December 15, 2011Applicant: EMORY UNIVERSITYInventors: Jeff Stehouwer, Mark Goodman, Clint Kilts, Charles Nemeroff
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Publication number: 20110306552Abstract: The present invention relates to new pyrimidinone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereofType: ApplicationFiled: July 21, 2010Publication date: December 15, 2011Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
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Patent number: 8076324Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: December 3, 2009Date of Patent: December 13, 2011Assignee: Sanofi-AventisInventors: Thomas Bohme, Uwe Gerlach, Dirk Gretzke, Heinz-Werner Kleemann, Stefania Pfeiffer-Marek, Henning Vollert, Jean-Michel Altenburger, Sergio Mallart
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Publication number: 20110294786Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: ApplicationFiled: August 3, 2011Publication date: December 1, 2011Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTISInventors: Nathalie CHEREZE, Alistair LOCHEAD, Mourad SAADY, Franck SLOWINSKI, Philippe YAICHE
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Patent number: 8063040Abstract: Novel triazabenzo[e]azulene derivatives of the formula, (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of TGF-beta receptor kinase and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: September 29, 2007Date of Patent: November 22, 2011Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Guenter Hoelzemann, Hartmut Greiner, Christiane Amendt
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BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20110281846Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20110275558Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.Type: ApplicationFiled: May 4, 2011Publication date: November 10, 2011Applicant: Virginia Tech Intellectual Properties, Inc.Inventors: Josep BASSAGANYA-RIERA, Pinyi LU, Raquel HONTECILLAS