Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 546/159)
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Publication number: 20120076732Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.Type: ApplicationFiled: June 23, 2011Publication date: March 29, 2012Inventors: Yan Feng, Ottavio Arancio, Shixian Deng, Donald W. Landry
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Publication number: 20120077981Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.Type: ApplicationFiled: December 6, 2011Publication date: March 29, 2012Applicant: Ardea Biosciences Inc.Inventors: Jean-Luc Girardet, Yung-hyo Koh, Martha de la Rosa, Zhi Hong, Stanley Lang
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Patent number: 8143278Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and/or 11beta-hydroxylase (CYP11B1), and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase and/or CYP11B1. Finally, the present invention also provides a pharmaceutical composition.Type: GrantFiled: December 14, 2007Date of Patent: March 27, 2012Assignee: Novartis AGInventors: Qi-Ying Hu, Gary Michael Ksander
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Publication number: 20120065204Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Publication number: 20120065199Abstract: A compound of formula (I) as well as pharmaceutically acceptable salts thereof and pharmaceutical compositions including a therapeutically effective amount of the compounds. The compound is useful in treatment of cancer, diabetic retinopathy, age-related macular degeneration, inflammation, stroke, ischemic myocardium, atherosclerosis, macular edema and psoriasis.Type: ApplicationFiled: May 20, 2010Publication date: March 15, 2012Applicant: CLANOTECH ABInventors: Johan Malm, Rune Ringom, Patrizia Caldirola, Jacob Westman
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Patent number: 8129533Abstract: The present invention is directed to a lyophilized preparation which contains a synthetic quinolone antibacterial compound and, as a solo additive, a pH-adjusting agent, and which exhibits an excellent reconstituting property. The invention provides a method for producing a lyophilized preparation containing a synthetic quinolone antibacterial compound as an active ingredient, characterized by including, sequentially, cooling an aqueous solution containing a synthetic quinolone antibacterial compound and a pH-adjusting agent to yield a frozen product, elevating the temperature of the frozen product, and re-cooling the resultant to prepare the lyophilized preparation.Type: GrantFiled: September 28, 2006Date of Patent: March 6, 2012Assignee: Dalichi Sankyo Company, LimitedInventor: Norihiro Nishimoto
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Patent number: 8124774Abstract: Disclosed herein is a compound of the formula (I) therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 21, 2008Date of Patent: February 28, 2012Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Todd M. Heidelbaugh, Ken Chow, Smita S. Bhat, Michael E. Garst
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Patent number: 8124623Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; R3 represents H or fluorine; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; R6 represents H, alkoxy or halogen; and n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).Type: GrantFiled: May 8, 2009Date of Patent: February 28, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Hans Locher, Philippe Panchaud, Jean-Luc Specklin
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Patent number: 8119807Abstract: Disclosed herein is a compound of the formula (I): (I). Therapeutic methods, compositions and medicaments related thereto are also disclosed.Type: GrantFiled: January 4, 2008Date of Patent: February 21, 2012Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Phong X. Nguyen, Ken Chow, Michael E. Garst
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Patent number: 8119812Abstract: An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action. The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.Type: GrantFiled: April 19, 2010Date of Patent: February 21, 2012Assignees: SBI Biotech Co., Ltd., Crystalgenomics, Inc.Inventors: Takayuki Irie, Masaaki Sawa, Sayuri Ito, Chika Tanaka, Seong Gu Ro, Choul Hong Park
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Patent number: 8119808Abstract: The invention provides for compounds of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.Type: GrantFiled: January 5, 2011Date of Patent: February 21, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Chongqing Sun, Doree Sitkoff, William R. Ewing, Yanting Huang, Bruce A. Ellsworth, Richard B. Sulsky, Annapurna Pendri, Samuel Gerritz, Natesan Murugesan, Zhengxiang Gu
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Patent number: 8106204Abstract: The invention relates to NHE-3 inhibitor compounds of formula I: In which R1-R11 are more specifically defined herein. These substituted 2-amino-4-phenyl-dihydroquinolines are useful the treatment of various renal and respiratory disorders such as acute or chronic renal failure, for impairments of biliary function and respiratory impairments such as snoring, sleep apneas or stroke. Formulations comprising them and methods for their use are also described herein.Type: GrantFiled: September 17, 2008Date of Patent: January 31, 2012Assignee: Sanofi-AventisInventors: Hans-Jochen Lang, John Weston, Uwe Heinelt
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Patent number: 8101767Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: January 9, 2009Date of Patent: January 24, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida Ruah, Anna Hazlewood, Peter D. J. Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8093379Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: GrantFiled: September 18, 2009Date of Patent: January 10, 2012Assignee: Idenix Pharmaceuticals, Inc.Inventors: Adel Moussa, Benjamin Alexander Mayes, Elodie Rosinovsky, Alistair Stewart
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Patent number: 8093392Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: GrantFiled: February 8, 2011Date of Patent: January 10, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Marie Binch
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Patent number: 8088924Abstract: It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R1 is a group represented by the formula: —Y1—Y2—Y3—Ra wherein Y1 is single bond or the like; Y2 is —C(?O)—NH— or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.Type: GrantFiled: September 2, 2009Date of Patent: January 3, 2012Assignee: Shionogi & Co., Ltd.Inventors: Yukio Tada, Yasuyoshi Iso, Kohji Hanasaki
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Patent number: 8084611Abstract: The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.Type: GrantFiled: March 29, 2007Date of Patent: December 27, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masaki Okamoto, Akira Sakuragi, Yoshikazu Mori, Takeshi Hamada, Hitoshi Kubota, Yoshinori Nakamura, Takanori Higashijima, Norimitsu Hayashi
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Patent number: 8076484Abstract: Modified green tea polyphenols and methods of their use are provided. One aspect provides compounds and compositions containing green tea polyphenols with one on more ester-linked fatty acids.Type: GrantFiled: August 10, 2006Date of Patent: December 13, 2011Assignee: Georgia Health Science University Research Institute, Inc.Inventor: Stephen D. Hsu
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Patent number: 8076358Abstract: The present invention is directed to 6-substituted-thio-2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and/or dementia. The compounds of the present invention are inhibitors of ?-secretase, also known as ?-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.Type: GrantFiled: January 27, 2009Date of Patent: December 13, 2011Assignee: Janssen Pharmaceutica NVInventors: Ellen Baxter, Christopher J. Creighton, Tianbao Lu, Allen B. Reitz, Charles H. Reynolds, Tina Morgan Ross, Ellen Sieber-McMaster
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Patent number: 8071616Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.Type: GrantFiled: January 25, 2010Date of Patent: December 6, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, William J. Scott, Bernd Riedl
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Patent number: 8071621Abstract: Compounds of Formula I wherein R1, A, R2, R3, R4, R5, R8, n, m, q and r are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: GrantFiled: October 9, 2009Date of Patent: December 6, 2011Assignee: AstraZeneca ABInventors: Thomas Simpson, James Kang, Jeffrey Albert, Cristobal Alhambra, Gerard Koether, James Woods, Yan Li
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Patent number: 8071620Abstract: This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C1-7alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the ?-position; and with the proviso that A is not benzimidazol-2-yl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.Type: GrantFiled: December 14, 2009Date of Patent: December 6, 2011Assignee: Topotarget UK LimitedInventors: Paul W. Finn, Ivars Kalvinsh, Einars Loza, Victor Andrianov, Olga Habarova, Daina Lolya, Irina Piskunova
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Patent number: 8071777Abstract: The present invention refers to new compounds derived from artesunate salts with quinolines represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III) depending on the radicals substituted in X (formula II), the relation X to Y (formula III) may vary from 1:1 to 1:7, because the amount of Y depends on the amount of N available in X for the formation of the salt. The radicals R1, R2, R3, R4, R5, e R6 in the general formula (II) are represented by: R1?H, CF3, CH3, OCH3, NH2, halogen; R2?H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3?H, m-OC6H4CF3, NH2; R4?H, CH3, OCH3, NH2, halogen; R5?H, CH3, CF3, NH2, halogen; R6?H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7?(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3(CH2)6, (CH2)8, (CH2)10, (CH2)12; R8?CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3.Type: GrantFiled: April 12, 2005Date of Patent: December 6, 2011Assignee: Fundação Oswaldo Cruz - FIOCRUZInventors: Núbia Boechat, Marcus Vinicius Nora de Souza, Alessandra Leda Valverde, Antoniana Ursine Krettli
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Publication number: 20110286922Abstract: The present invention relates to in vivo imaging and radiotherapeutic methods and agents which target the enzyme aldehyde dehydrogenase (ALDH) and that are suitable for the in vivo imaging of tumours and treatment of cancer.Type: ApplicationFiled: October 20, 2009Publication date: November 24, 2011Inventors: Alan Cuthbertson, Peter Brian Iveson, Rajiv Bhalla, Vijaya Raj Kuniyil Kulangara
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Patent number: 8063200Abstract: A labeled compound is so designed that an aromatic tertiary amine compound is bondable with a biomolecule. One of S1 and S2 contains a group bound with a molecular chain 10 (e.g. an oligonucleotide) capable of binding with a biomolecule or a reactive group covalently binding with a reactive group present in the biomolecule, n is 0 or 1, R3 is a phenyl group or a naphthyl group, Ar1 is a phenylene group or a naphthylene group, and Ar2 is any of a phenylene group, a naphthylene group, an anthrylene group, and a phenanthrene group. The detection of a fluorescence emitted by excitation of the labeled compound bound to a biomolecule ensures the biomolecule being detected at high sensitivity and a high SN ratio.Type: GrantFiled: August 21, 2009Date of Patent: November 22, 2011Assignee: Sony CorporationInventor: Mari Ichimura
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Patent number: 8063222Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.Type: GrantFiled: August 27, 2008Date of Patent: November 22, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Mingshi Dai, Bing Guan, Robert A. Bennett, Douglas F. Burdi, Shomir Ghosh, Gang Li, Charles A. Minor, Tracy J. Jenkins
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Patent number: 8058442Abstract: Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.Type: GrantFiled: November 7, 2003Date of Patent: November 15, 2011Assignees: Technion Research and Development Foundation Ltd., Yeda Research and Development Co., Ltd.Inventors: Moussa Youdim, Matitiyahu Fridkin, Hailin Zheng, Abraham Warshawsky, Rivka Warshawsky, legal representative
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Patent number: 8058441Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is (CO)—O, (SO)2—O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2—NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyType: GrantFiled: June 25, 2002Date of Patent: November 15, 2011Assignee: N.V. OrganonInventors: Nicole Corine Renée Van Straten, Rudolf Gijsbertus Van Someren, Jurgen Schulz
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Publication number: 20110263620Abstract: Quinoline compounds of formula (I): in which A, B, D, E, F, G, R1, R2, R3, X, Y, n, p, and q are defined herein. Also disclosed is a method for treating a viral infection with a compound of formula (I).Type: ApplicationFiled: April 21, 2011Publication date: October 27, 2011Applicant: NATIONAL HEALTH RESEARCH INSTITUTESInventors: Hsing-Pang HSIEH, Tsu-An HSU, Jiann-Yih YEH, Yu-Sheng CHAO
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Publication number: 20110263645Abstract: Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosedType: ApplicationFiled: July 1, 2011Publication date: October 27, 2011Applicant: Neuron Systems, Inc.Inventors: Thomas A. Jordan, John E. Dowling, John Clifford Chabala
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Patent number: 8039486Abstract: This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: GrantFiled: February 8, 2008Date of Patent: October 18, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Kap-Sun Yeung, Michelle E. Farkas, John F. Kadow, Nicholas A. Meanwell, Malcolm Taylor, David Johnston, Thomas Stephen Coulter, J. J. Kim Wright
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Publication number: 20110245375Abstract: The present invention relates to curable compositions comprising a thermolatent amidine base and an organic material which is polymerisable or crosslinkable with a basic or nucleophilic catalyst. In particular, the invention relates to curable coating compositions, especially powder coating compositions, and curable adhesive compositions, as well as to the use a thermo-latent amidine base as a curing catalyst for thermally induced base- catalyzed polymerisation or crosslinking reactions.Type: ApplicationFiled: November 18, 2009Publication date: October 6, 2011Applicant: BASF SEInventors: Peter Nesvadba, Lucienne Bugnon Folger, Ralf Knischka
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Publication number: 20110245353Abstract: The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.Type: ApplicationFiled: March 31, 2011Publication date: October 6, 2011Applicant: SENOMYS, INC.Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy DAVIS, Vincent DARMOHUSODO, Melissa WONG, Victor SELCHAU
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Publication number: 20110218208Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.Type: ApplicationFiled: June 23, 2009Publication date: September 8, 2011Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Publication number: 20110212963Abstract: The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.Type: ApplicationFiled: July 21, 2009Publication date: September 1, 2011Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Jochen Görlitzer, Peter Hamiley, Antoine Ravet
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Patent number: 8003624Abstract: In its many embodiments, the present invention provides a novel class of indolines as inhibitors of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: February 13, 2007Date of Patent: August 23, 2011Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Kevin D. McCormick, Christopher W. Boyce, Younong Yu
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Patent number: 7999108Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: GrantFiled: July 13, 2007Date of Patent: August 16, 2011Assignee: Bayer Schering Pharma AGInventors: Markus Berger, Jan Dahmen, Hartmut Rehwinkel, Stefan Jaroch, Heike Schaecke
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Publication number: 20110195980Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: August 31, 2009Publication date: August 11, 2011Inventors: Matthew Burger, Mika Lindvall
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Patent number: 7994324Abstract: The present invention is concerned with 2-aminoquinoline derivatives, in particular compounds of formula (I) wherein R1 and R2 are as described herein, pharmaceutical compositions containing such compounds, and methods for their manufacture. The compounds of the invention are 5-HT5A receptor antagonists useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.Type: GrantFiled: February 27, 2009Date of Patent: August 9, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 7994194Abstract: This invention relates to novel compounds that are 4-oxoquinoline derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 4-oxoquinoline derivatives that are derivatives of elvitegravir. This invention also provides pyrogen-free compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an HIV integrase inhibitor, such as elvitegravir.Type: GrantFiled: September 12, 2008Date of Patent: August 9, 2011Assignee: Concert Pharmaceuticals, Inc.Inventor: Scott L. Harbeson
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Publication number: 20110190342Abstract: The invention relates to quinoline derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.Type: ApplicationFiled: September 30, 2009Publication date: August 4, 2011Inventors: Markus Henrich, Angela Bauer, Jens Nagel, Meik Sladek, Christopher Graham Raphael Parsons, Wojciech Danysz, Valerjans Kauss, Jevgenijs Rozhkovs, Igos Starchenkovs, Dina Trifanova
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Patent number: 7989628Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein Z, R1, and Ar1 are as defined herein, pharmaceutical compositions containing them, methods for their manufacture. The compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.Type: GrantFiled: February 27, 2009Date of Patent: August 2, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Publication number: 20110178106Abstract: 5-Quinolinone and Imidazopyrimidine compounds are provided that are useful for inhibiting the efflux of any therapeutic agent that is a MRP1 substrate. Also provided is a method for screening to identify additional MRP1 inhibitors.Type: ApplicationFiled: July 10, 2009Publication date: July 21, 2011Applicant: SOUTHERN RESEARCH INSTITUTE OFFICE OF COMMERCIALIZInventors: Joseph A. Maddry, Adam Keeton, Jason Whitt, Gary Piazza
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Publication number: 20110172270Abstract: 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1 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: ApplicationFiled: January 6, 2011Publication date: July 14, 2011Applicant: LABORATORIOS DEL DR. ESTEVE S.AInventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
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Publication number: 20110152301Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.Type: ApplicationFiled: December 22, 2010Publication date: June 23, 2011Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: David Rekosh, Marie-Louise Hammarskjöld
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Patent number: 7964616Abstract: The invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, wherein R1, R2, R3 and n are as defined in the specificationType: GrantFiled: March 21, 2008Date of Patent: June 21, 2011Assignee: AstraZeneca ABInventors: Mark Ebden, Simon David Guile
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Patent number: 7964731Abstract: The invention relates to adenozin A3 receptor ligands labeled with iodine isotops of mass number 125, within those favorably to antagonists and their isomers, to the experimental materials containing them, to a process for the preparation of the compounds of the general formula (I) and their isomers, to the new intermediates of the general formula (II) and to the preparation thereof.Type: GrantFiled: May 14, 2007Date of Patent: June 21, 2011Assignee: Sanofi-AventisInventors: Geza Timari, Kinga Boer, Geza Toth, Csaba Tomboly
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Publication number: 20110144156Abstract: Provided are 2,4-disubstituted quinoline derivatives that are A3 adenosine receptor modulators (A3RM), for use in the treatment of a condition which is treatable by adenosine, an A3 adenosine receptor (A3AR) agonist, or an A3 adenosine receptor antagonist. The 2,4-disubstituted quinoline derivatives can be used in the treatment of a condition treatable by an adenosine or an A3AR agonist, by enhancing activity of a protein (by binding of said 2,4-disubstituted quinoline derivative to the A3AR). Some conditions treatable by the 2,4-disubstituted quinoline derivative when used for enhancing activity include, malignancy, an immuno-compromised affliction, high intraocular pressure, or a condition associated with high intraocular pressure.Type: ApplicationFiled: August 12, 2009Publication date: June 16, 2011Applicants: UNIVERSITEIT LEIDEN, CAN-FITE BIOPHARMA LTD.Inventors: Adriaan P. Ijzerman, Aniko Goblyos, Johannes Brussee
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Patent number: 7960551Abstract: A succinic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof, for use in treating pulmonary disorders.Type: GrantFiled: February 8, 2007Date of Patent: June 14, 2011Assignee: Glaxo Group LimitedInventors: Reshma Chudasama, Andrew Kennedy
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Publication number: 20110136864Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Inventor: Ryan Craig Schoenfeld