Three Or More Hetero Atoms In The Tricyclo Ring System Patents (Class 514/293)
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Publication number: 20120301517Abstract: The present invention is drawn to adhesive formulations, methods of drug delivery, and solidified layers for dermal delivery of a drug. The formulation can include a drug, a solvent vehicle, and a solidifying agent. The solvent vehicle can have a volatile solvent system including at least one volatile solvent, and a non-volatile solvent system including at least two non-volatile solvents. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified layer after at least a portion of the volatile solvent system is evaporated.Type: ApplicationFiled: August 3, 2012Publication date: November 29, 2012Inventors: Jie Zhang, Kevin S. Warner, Sanjay Sharma
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Publication number: 20120294930Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.Type: ApplicationFiled: February 23, 2012Publication date: November 22, 2012Applicant: Intellikine LLCInventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
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Publication number: 20120289538Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available for Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.Type: ApplicationFiled: July 26, 2012Publication date: November 15, 2012Applicant: MEDICIS PHARMACEUTICAL CORPORATIONInventors: Michael T. NORDSIEK, Sharon F. LEVY, James H. LEE, James H. KULP, Kodumudi S. BALAJI, Tze-Chiang MENG, Jason J. WU, Valyn S. BAHM, Robert BABILON
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Publication number: 20120289537Abstract: Pharmaceutical formulations and methods for the topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namelyl, viral infections, such as Type I or Type II Herpes simplex infections and genital and perianal warts, actinic deratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis to achieve an antiviral effect, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”).Type: ApplicationFiled: July 18, 2012Publication date: November 15, 2012Applicant: Medicis Pharmaceutical CorporationInventor: Jefferson J. Gregory
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Publication number: 20120289497Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: ApplicationFiled: January 17, 2011Publication date: November 15, 2012Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Publication number: 20120283286Abstract: Pharmaceutical formulations and methods for the topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namely, viral infections, such as Type I or Type II Herpes simplex infections and genital and perianal warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis to achieve an antiviral effect, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”).Type: ApplicationFiled: July 18, 2012Publication date: November 8, 2012Applicant: Medicis Pharmaceutical CorporationInventor: Jefferson J. Gregory
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Publication number: 20120276047Abstract: 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: ApplicationFiled: November 23, 2010Publication date: November 1, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge
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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: 20120276051Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: July 9, 2012Publication date: November 1, 2012Applicant: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
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Patent number: 8299090Abstract: The present invention relates to substituted thiazolyl- and oxazoyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.Type: GrantFiled: June 18, 2009Date of Patent: October 30, 2012Inventors: Roberto Pellicciari, Flavio Moroni, Adam Matthew Gilbert
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Publication number: 20120264778Abstract: Pharmaceutical formulations and methods for the topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namelyl, viral infections, such as Type I or Type II Herpes simplex infections and genital and perianal warts, actinic deratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis to achieve an antiviral effect, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”).Type: ApplicationFiled: June 26, 2012Publication date: October 18, 2012Applicant: MEDICIS PHARMACEUTICAL CORPORATIONInventor: Jefferson J. GREGORY
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Publication number: 20120263759Abstract: A copolymer comprising a block of an elastin pentapeptide and method of making and using the copolymer are provided. The copolymer may be used as a coating on a stent. Methods of using a stent coated with the copolymer are also provided.Type: ApplicationFiled: September 2, 2011Publication date: October 18, 2012Applicant: Abbott Cardiovascular Systems Inc.Inventors: Syed F.A. Hossainy, Yiwen Tang, Lothar W. Kleiner
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Patent number: 8288407Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: March 11, 2011Date of Patent: October 16, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
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Publication number: 20120252799Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: ApplicationFiled: June 11, 2012Publication date: October 4, 2012Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
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Publication number: 20120252740Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.Type: ApplicationFiled: July 2, 2010Publication date: October 4, 2012Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
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Patent number: 8273761Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa to Xe are each a carbon atom or a nitrogen atom, m is 0 to 2, and ring A to ring C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.Type: GrantFiled: December 7, 2007Date of Patent: September 25, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
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Publication number: 20120238562Abstract: The invention relates to the treatment of prostate cancer. In various embodiments, the invention teaches a method of administering one or more compounds that inhibit a molecule that antagonizes the activity of tumor suppressor Mst1 and Mst2 pathway signaling. In certain embodiments, one or more of the compounds include an mTOR and PI3K inhibitor.Type: ApplicationFiled: March 8, 2012Publication date: September 20, 2012Applicant: CEDARS-SINAI MEDICAL CENTERInventors: Bekir Cinar, Filiz Kisaayak Collak
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Publication number: 20120232074Abstract: Novel compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: November 3, 2010Publication date: September 13, 2012Inventors: Anne Marie Jeanne Bouillot, Frederic Donche, Francoise Jeanne Gellibert, Yann Lamotte, Olivier Mirguet
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Patent number: 8263610Abstract: The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 30, 2009Date of Patent: September 11, 2012Assignee: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Chris Brassard, Audra Dalton, Anton Filikov, Jason Hill, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Jianqiang Wang, Neil Westlund
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Patent number: 8263594Abstract: Imidazoquinoline compounds with an aryloxy or arylalkyleneoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: January 18, 2011Date of Patent: September 11, 2012Assignee: 3M Innovative Properties CompanyInventors: Kyle J. Lindstrom, Hugues M. H. Martin, Bryon A. Merrill, Michael J. Rice, Joshua R. Wurst, Chad A. Haraldson, Philip D. Heppner, Shri Niwas, Matthew R. Radmer
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Publication number: 20120225856Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: May 21, 2012Publication date: September 6, 2012Applicant: Corcept Therapeutics, Inc.Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
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Publication number: 20120219641Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: February 14, 2012Publication date: August 30, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20120220565Abstract: The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: August 26, 2011Publication date: August 30, 2012Applicant: Corcept Therapeutics, Inc.Inventors: Robin Clark, Tony Johnson, Hazel Hunt, Ian McDonald
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Publication number: 20120207751Abstract: The invention relates to a combination comprising compounds of formula (I) and one or more other antiproliferative compounds, hormones or radiation, pharmaceutical preparations comprising the combination thereof, and the application thereof in a process for the treatment of tumors.Type: ApplicationFiled: April 23, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
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Publication number: 20120208809Abstract: The invention relates to novel 9H-pyrrolo[2,3-b:5,4-c?]dipyridine azacarbolines of formula (I), where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH alkyl, CONH cycloalkyl; CONH heterocycloalkyl; CON(alkyl)2; CON(alkyl)(heterocycloalkyl); CONHN(alkyl)2; C(O)heterocycloalkyl; Rs is H; Hal, OH; O-alkyl(C1-C10); NH2; N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NHC(O)R3a; N(alkyl(C1-C10)C(O)R3a; NHS(O2)R3a; N(alkyl)(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; Ra and Rs optionally form a cycle; R3a is selected from among Hal, CF3, C1-C10 alkyl; C3-C7 cycloalkyl; C2-C6 alkenyl; C2-C6 alkynyl; OH; O-alkyl(C1-C10); (C3-C7); heterocycloalkyl (C3-C7); NH2; NH-(alkyl(C1-C10) or cycloalkyl(C3-C7)); N(alkyl(C1-C10) or cycloalkyl(C3-C7))2; NH-(alkyl(C1-C10) or heterocycloalkyl(C3-C7)); N(alkyl(C1-C10) or heterocycloalkyl(C3-C7))2, as well as to the isomers anType: ApplicationFiled: November 30, 2009Publication date: August 16, 2012Applicant: SANOFIInventors: Didier Babin, Olivier Bedel, Thierry Gouyon, Serge Mignani, David Papin
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Publication number: 20120208819Abstract: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.Type: ApplicationFiled: October 5, 2010Publication date: August 16, 2012Inventors: Joseph Arndt, Timothy Chan, Kevin Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Daniel Scott, Lihong Sun, Jermaine Thomas, Kurt van Vloten, Deping Wang, Lei Zhang, Daniel Erlanson
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Publication number: 20120208800Abstract: The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions.Type: ApplicationFiled: November 3, 2010Publication date: August 16, 2012Inventors: Chun-Wa Chung, Edwige Nicodeme
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Publication number: 20120202843Abstract: Methods of diagnosing and monitoring cancers and precancerous lesions associated with human papillomavirus (HPV), by detecting abnormal levels of lysine (K)-specific demethylase 6A (KDM6A), KDM6B, or trimethylated Histone H3 Lys27 (H3K27me3).Type: ApplicationFiled: July 14, 2010Publication date: August 9, 2012Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Karl Munger, Christopher Crum, Margaret McLaughlin-Drubin
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Publication number: 20120196856Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 26, 2010Publication date: August 2, 2012Inventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
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Publication number: 20120196880Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: ApplicationFiled: December 19, 2011Publication date: August 2, 2012Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
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Publication number: 20120196854Abstract: A pharmaceutical composition comprising as an active ingredient, an aromatic heterocyclic compound represented by the formula (I): [wherein Q1 represents CR2 (wherein R2 represents a hydrogen atom or the like) or the like; Q2 represents CR3 (wherein R3 represents a hydrogen atom or the like) or the like; Q3 represents a nitrogen atom or the like; R1 represents —C(?O)OR16 (wherein R16 represents a hydrogen atom or the like) or the like; R5 represents a hydrogen atom or the like; R6 represents optionally substituted cycloalkyl or the like; X and Y may be the same or different and each represent CH in which H may be substituted with a substituent or the like; and Z represents a nitrogen atom or the like] or the like is provided.Type: ApplicationFiled: October 6, 2010Publication date: August 2, 2012Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Chie Takada, Koji Saeki, Hirokazu Kawasaki, Miho Tagaya, Masato Komai, Toshihide Ikemura, Shinpei Yamaguchi, Kyoichiro Iida
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Publication number: 20120196845Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
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Publication number: 20120189646Abstract: Disclosed herein are a compound of formula (I) and pharmaceutically acceptable salts thereof, processes for preparing the same, pharmaceutical compositions containing the same, and methods of using the same.Type: ApplicationFiled: December 16, 2011Publication date: July 26, 2012Inventors: Thomas MCINALLY, Austen PIMM
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Publication number: 20120184577Abstract: The present invention provides an imidazo[4,5-c]quinolin-2-one compound, or a pharmaceutically acceptable salt thereof, that inhibits both PI3K and mTOR and, therefore, is useful in the treatment of cancer.Type: ApplicationFiled: January 11, 2012Publication date: July 19, 2012Applicant: ELI LILLY AND COMPANYInventors: David Anthony Barda, Mary Margaret Mader
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Publication number: 20120178760Abstract: The present invention is directed to heterocyclic fused pyrazole[4,3-c]pyridine-3-one compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: September 20, 2010Publication date: July 12, 2012Inventors: Douglas C. Beshore, Scott D. Kuduk
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Publication number: 20120178748Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: January 10, 2012Publication date: July 12, 2012Applicant: Sunovion Pharmaceuticals Inc.Inventors: John Emmerson CAMPBELL, Philip JONES, Michael Charles HEWITT
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Publication number: 20120157460Abstract: The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.Type: ApplicationFiled: December 20, 2011Publication date: June 21, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Matthew D. SURMAN, Peter R. GUZZO, Emily FREEMAN, Alan J. HENDERSON
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Publication number: 20120149665Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.Type: ApplicationFiled: August 25, 2010Publication date: June 14, 2012Applicant: Bionomics LimitedInventors: Gabriel Kremmidiotis, David Bibby, Annabell Leske
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Patent number: 8193356Abstract: The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.Type: GrantFiled: September 15, 2006Date of Patent: June 5, 2012Assignee: Aska Pharmaceutical Co., Ltd.Inventors: Hashime Kanazawa, Tomoji Aotsuka, Kentarou Kumazawa, Kouki Ishitani, Takashi Nose
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Publication number: 20120135998Abstract: The present invention relates to compounds of formula (I), racemates, isomers and/or salts thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds.Type: ApplicationFiled: November 22, 2011Publication date: May 31, 2012Inventors: Penelope Anne Mayes, Jeffrey Peter Mitchell, Alistair George Draffan, Gary Robert William Pitt, Kelly Helen Anderson, Chin Yu Lim
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Publication number: 20120129811Abstract: This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Aihua WANG, Yan Zhang, Kristi Anne Leonard, Michael Hawkins, Brett Andrew Tounge, Umar S.M. Maharoof, Joseph Kent Barbay
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Publication number: 20120128665Abstract: The present invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of hypoxia in cancerous cells in the subject. In one embodiment, the invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of lactate dehydrogenase (LDH) in a cell, e.g., a cancerous cell. The invention also provides methods for treating cancer in a subject by administering an effective amount of an agent to the subject, wherein the subject has been selected based on a modulated level of hypoxia. The invention further provides kits to practice the methods of the invention.Type: ApplicationFiled: November 18, 2011Publication date: May 24, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Ronald K. Blackman, Vojo Vukovic
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Publication number: 20120115898Abstract: The invention relates to a compound of formula (I), where: R1 is a phenyl group optionally substituted by one or more halogen atoms; R2 is: a hydrogen atom or a halogen atom or a cyano group; a —C(?O)Y group where Y is a hydrogen atom, or a —NH2 or —OR3 group; a —C(?S)NH2 group; a —C(?NH)NH—OH group; a —CH2OH or —CH2F group; a —CH?N—OH group; a —CH?CH2 or —C?C—R3 group; a H or H R1 group being a hydrogen or (C1-C4)alkyl group; R3 is a hydrogen atom or (C1-C4)alkyl group; and R4 is a —NH2, (C1-C4)alkyl, (C1-C4)fluoroalkyl or (C3-C7)cycloalkyl group.Type: ApplicationFiled: April 22, 2010Publication date: May 10, 2012Applicant: SANOFIInventors: Georges Delettre, Stéphanie Deprets, Frank Halley, Laurent Schio, Fabienne Thompson
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Publication number: 20120114601Abstract: The invention provides certain compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: ApplicationFiled: January 12, 2012Publication date: May 10, 2012Applicant: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Godwin Pais, Quiping Wang, Milind Deshpande, Michael Pucci, Yongsheng Song, Edlaine Lucien, Jason Allan Wiles, Akihiro Hashimoto
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Publication number: 20120114637Abstract: Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are ophthalmic formulations that deliver a variety of therapeutic agents, including but not limited to rapamycin (sirolimus), analogs thereof (rapalogs) or other mTOR inhibitors, to a subject for an extended period of time. The ophthalmic formulations may be placed in an aqueous medium of a subject, including but not limited to intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer a therapeutic agent to treat or prevent age-related macular degeneration, macular edema, diabetic retinopathy, uveitis, dry eye, or a hyperpermeability disease in a subject.Type: ApplicationFiled: May 4, 2010Publication date: May 10, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Thierry Nivaggioli, David A. Weber, Philippe JM Dor, Philip Reilly
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Publication number: 20120115820Abstract: The present invention relates to a use of a compound having an acid pump antagonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for prevention or treatment of diseases in which abnormal gastrointestinal motility is involved. In addition, the present invention relates to the method of prevention or treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agent. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound having an acid pump antagonistic activity or a pharmaceutically acceptable salt thereof for the prevention or treatment of said diseases.Type: ApplicationFiled: July 9, 2010Publication date: May 10, 2012Inventors: Nobuyuki Takahashi, Shinichi Koizumi
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Publication number: 20120115821Abstract: Compositions and methods for treatment of conditions affecting skin and/or mucosal surfaces of a subject that make use of an imidazoquinoline compound and a retinoid agent are described.Type: ApplicationFiled: November 3, 2011Publication date: May 10, 2012Applicant: 442 VENTURES, LLCInventor: J. Mark Jackson
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Patent number: 8173120Abstract: The present invention relates to a method for substantially preventing a reduction in feed intake in an animal which occurs when said animal is administered an antibiotic, the method comprising administering to an animal in need of prevention of a reduction in feed intake, increasing doses of a composition comprising one or more antibiotics. The present invention also relates to a method for treating laminitis and fermentative acidosis in an animal in need of said treatment, the method comprising administering increasing doses of a composition comprising one or more antibiotics. The present invention further relates to a method for treating equine grass sickness and pulpy kidney in an animal in need of said treatment, the method comprising administering increasing doses of a composition comprising one or more antibiotics.Type: GrantFiled: December 15, 2006Date of Patent: May 8, 2012Assignee: Precision Nutrition Pty LtdInventors: James Baber Rowe, Christopher William Rowe
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Publication number: 20120108581Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.Type: ApplicationFiled: March 25, 2010Publication date: May 3, 2012Applicant: Kowa Company, LtdInventors: Masanori Ashikawa, Toshiharu Morimoto, Hajime Yamada, Shunji Takemura, Tatsuaki Nishiyama, Takeshi Doi, Hiroyuki Ishiwata