Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/153)
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Publication number: 20120208989Abstract: Fluorinated aromatic materials, their synthesis and their use in optoelectronics. In some cases, the fluorinated aromatic materials are perfluoroalkylated aromatic materials that may include perfluoropolyether substituents.Type: ApplicationFiled: August 20, 2010Publication date: August 16, 2012Applicant: THE UNIVERSITY OF SOUTH DAKOTAInventor: Haoran Sun
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Patent number: 8242102Abstract: The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R is a moiety of the formula wherein A, R1 to R4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; Ra, Rb are independently selected from the group consisting of halogen, CN, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C(O)Raa, C(O)NRccRbb and NRccRbb; X is CH2, C(O), S, S(O) or S(O)2; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar1, Ar2—Ar3 or Ar2—O—Ar3, wherein Ar1, Ar2 and Ar3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents Rx, wherein and physiologically tolerated acid addition salts and the N-oxides thereof.Type: GrantFiled: March 23, 2008Date of Patent: August 14, 2012Assignee: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Andreas Haupt, Wilfried Braje, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Wolfgang Wernet, Alfred Hahn, legal representative, Matthias Mayrer
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Publication number: 20120202848Abstract: This invention is in the fields of immunology and autoimmunity. More particularly it concerns methods of treating patients with compounds which are useful agents for inhibiting the functions of TIP60 in the treatment of an individual suffering, for example, from ulcerative colitis and other irritable bowel diseases.Type: ApplicationFiled: December 2, 2011Publication date: August 9, 2012Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: MARK I. GREENE, WAYNE W. HANCOCK, MAKOTO KATSUMATO, YAN XIAO
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Patent number: 8236947Abstract: Disclosed are quinoline compounds having affinity for the 5-HT6 receptor and having the formula: where R1, R2, R3, R4, R5, n, m, p and A are defined herein, and salts thereof, compositions containing these compounds and salts and processes for making and using the same.Type: GrantFiled: June 3, 2011Date of Patent: August 7, 2012Assignee: Glaxo Group LimitedInventors: Mahmood Ahmed, Christopher Norbert Johnson, Martin C Jones, Gregor James MacDonald, Stephen Frederick Moss, Mervyn Thompson, Charles Edward Wade, David R Witty
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Patent number: 8232402Abstract: Novel quinolinone farnesyl transferase inhibitors are provided. These new compounds are useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, multiple system atrophy, and disorders of brain iron concentration including pantothenate kinase-associated neurodegeneration (e.g., PANK1), or other neurodegenerative/neurological diseases. Provided compounds are also useful in the treatment of proliferative diseases such as cancer, and in the treatment of neurological diseases, such as cognitive impairment, depression, and anxiety. The treatment including administering to a subject a therapeutically effective amount of an inventive farnesyl transferase inhibitor compound.Type: GrantFiled: March 12, 2009Date of Patent: July 31, 2012Assignee: Link Medicine CorporationInventors: Peter T. Lansbury, Jr., Craig J. Justman, Ross A. Fredenburg, Robin Kate Meray, Mark E. Duggan, Peter Lin
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Patent number: 8232293Abstract: This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:Type: GrantFiled: September 15, 2009Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Thilo Berkenbusch, Carl Alan Busacca, Burkhard Jaeger, Richard J. Varsolona
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Patent number: 8232294Abstract: The present invention provides amino ester compounds, salts, and pharmaceutical formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: GrantFiled: March 19, 2010Date of Patent: July 31, 2012Assignees: Sunshine Lake Pharma Co., Ltd.Inventor: Ning Xi
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Patent number: 8227612Abstract: The present invention discloses a quinoline compound represented by the formula A or pharmaceutically acceptable solvate, optical isomer or polymorph thereof, wherein X is S or O; M is H, Na+, NH4+ or Ca2+; each of R1, R2 and R3 is independently H, halogen, the group represented by formula D or formula E; R is H, halogen, C1˜C4 alkyl or C1˜C4 alkoxy. The present invention also discloses its pharmaceutical composition and the preparation method thereof and application in manufacturing a medicament for inhibiting HMG-CoA reductase or for the treatment and prophylaxis of the diseases which can be treated effectively by inhibiting HMG-CoA reductase. The quinloline compound and pharmaceutical composition thereof of the present invention have an excellent lipid reduction effect in vivo and can be applied for treatment of a hyperlipidemia-related disease.Type: GrantFiled: April 29, 2009Date of Patent: July 24, 2012Assignee: Shanghai Institute of Pharmaceutical IndustryInventors: Zhengyan Cai, Weicheng Zhou, Qun Hao, Zhenhua Shi, Yuchen Sheng, Mingyu Shi, Qingning Liang
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Publication number: 20120184523Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: March 22, 2012Publication date: July 19, 2012Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takbuchi, Yong Wang, Wei Xu
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Publication number: 20120184579Abstract: Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1C6alkyl or C3-C6cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(?O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.Type: ApplicationFiled: March 30, 2012Publication date: July 19, 2012Inventors: John Gary Montana, Harry Finch, George Hynd, Michael Colin Cramp, Rosa Arienzo, Neville McLean
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Publication number: 20120177749Abstract: A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.Type: ApplicationFiled: November 30, 2011Publication date: July 12, 2012Applicants: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC., ADVANCED CANCER THERAPEUTICS, LLCInventors: Gilles Tapolsky, Pooran Chand, John O. Trent, Sucheta Telang, Brian F. Clem, Jason A. Chesney
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Patent number: 8211897Abstract: The present invention is directed to a method of using compounds of Formula (I) to inhibit Cathepsin B. Specifically the compounds of the present invention are useful as therapeutic agents for the treatment of tumor invasion, metastasis, Alzheimer's Disease, arthritis, inflammatory diseases such as chronic and acute pancreatitis, inflammatory airway disease, and bone and joint disorders, including osteoporosis, osteoarthritis, rheumatoid arthritis, psoriasis, and other autoimmune disorders, liver fibrosis, including liver fibrosis associated with HCV, all types of steatosis (including non-alcoholic steatohepatitis) and alcohol-associated steatohepatitis, non-alcoholic fatty liver disease, forms of pulmonary fibrosis including idiopathic pulmonary fibrosis, pathological diagnosis of interstitial pneumonia following lung biopsy, renal fibrosis, cardiac fibrosis, retinal angiogenesis and fibrosis/gliosis in the eye, schleroderma, and systemic sclerosis.Type: GrantFiled: February 5, 2009Date of Patent: July 3, 2012Assignee: ViroBay, Inc.Inventor: Leslie Holsinger
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Patent number: 8211910Abstract: A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided.Type: GrantFiled: April 13, 2009Date of Patent: July 3, 2012Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hisashi Takahashi, Hiroaki Inagaki, Satoshi Komoriya, Makoto Takemura, Rie Miyauchi
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Naphthamide derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors
Patent number: 8211901Abstract: Isolated compounds of formula I: and stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts thereof are described, as well as processes for production, and methods of use of these compounds and compositions thereof for the treatment of diseases associated with abnormal protein kinase activities and/or abnormal histone deacetylase activities including, for example, inflammatory diseases, autoimmune diseases, cancer, neurological and neurodegenerative diseases, cardiovascular diseases, metabolic disease, allergies and asthma and/or hormone-related diseases.Type: GrantFiled: May 21, 2010Date of Patent: July 3, 2012Assignee: Shenzhen Chipscreen Biosciences Ltd.Inventors: Xian-Ping Lu, Zhibin Li, Song Shan, Jindi Yu, Zhiqiang Ning -
Patent number: 8211911Abstract: The present invention relates to compounds of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.Type: GrantFiled: August 12, 2009Date of Patent: July 3, 2012Inventor: Guoqing Paul Chen
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Publication number: 20120165369Abstract: The present invention relates to quinolinium antiinfective agents in which the qunolinium nucleus is fused to an indole ring or the qunolinium nucleus is linked to a cyclic structure through an opened indole or a benzothiophene or benzofuran ring. The compound is further substituted with various substituent groups. The compounds are represented by formula (I), (II) and (III): Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: July 8, 2008Publication date: June 28, 2012Inventor: Seth Y. Ablordeppey
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Publication number: 20120142727Abstract: [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided. [Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.Type: ApplicationFiled: August 5, 2010Publication date: June 7, 2012Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Takuya Washio, Wataru Hamaguchi
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Publication number: 20120142929Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are useful as intermediates in the preparation of potent active agents for the treatment of hepatitis C virus (HCV) infection.Type: ApplicationFiled: March 18, 2010Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Nitinchandra D. Patel, Chris H. Senanayake, Xudong Wei, Nathan K. Yee
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Publication number: 20120123126Abstract: The present invention relates to compounds, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with the inhibition of the protein tyrosine kinase activity of growth factor receptors such as c-Met, thereby making them useful as anticancer agents, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.Type: ApplicationFiled: September 8, 2011Publication date: May 17, 2012Inventor: Guoqing Paul Chen
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Publication number: 20120122853Abstract: Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: May 22, 2009Publication date: May 17, 2012Applicant: SANOFI-AVENTISInventors: Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Maike Glien, Hans Matter, Eugen Falk, Ulrike Wendler
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Publication number: 20120116072Abstract: Benzenesulfonamide compounds having a structure of the following general formula (I) are described. Also described, are methods for synthesizing the compounds, and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: June 28, 2010Publication date: May 10, 2012Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlene Schuppli
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Publication number: 20120115904Abstract: Compounds of formula I: or formula II: or a pharmaceutically acceptable salt of formula I or formula II, wherein: R1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R2 is methyl or haloalkyl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R3 is aliphatic, aryl, aralkyl, or alkylaryl; and R5, R6, R7 and R8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO2R10, wherein R10 is H, alkyl, amino or haloalkyl; provided that in formula I, R5 and R are not both H or R6 is not H or methoxy; and in formula II that if R4 is carbonyldioxy then R7 is not methoxy.Type: ApplicationFiled: June 3, 2011Publication date: May 10, 2012Inventors: Michael K. Riscoe, Jane X. Kelly, Rolf W. Winter, David J. Hinrichs, Martin J. Smilkstein, Aaron Nilsen, Jeremy Burrows, Dennis Kyle, Roman Manetsch, Richard M. Cross, Andrii Monastyrskyi, David L. Flanigan
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Patent number: 8173812Abstract: Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R1 is halogen or cyano; R2 is hydrogen or methyl; R3 and R4 are independently —OR6, C1-C6alkyl or C3-C6cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R5 is hydrogen or halogen; R6 is C1-C6 alkyl or C3-C6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is —CH2—, —S—, or —O—; one of Y and Y1 is hydrogen and the other is OR6, —C(?O)R7, NR8SO2R6 or a heterocyclic group selected from those referred to in the specification; and R6, R7 and R8 are as defined in the specification.Type: GrantFiled: April 3, 2008Date of Patent: May 8, 2012Assignee: Pulmagen Therapeutics (Asthma) LimitedInventors: John Gary Montana, Harry Finch, George Hynd, Michael Colin Cramp, Rosa Arienzo, Neville McLean
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Publication number: 20120108631Abstract: The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.Type: ApplicationFiled: October 26, 2011Publication date: May 3, 2012Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Tzofit Kehat, Sima Mirilashvili, Alex Aizikovich, Daniel Sherman, Vered Behar, Osnat Kashtan
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Patent number: 8163753Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: GrantFiled: October 29, 2004Date of Patent: April 24, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Yoshikazu Haraguchi, Shin Miyamura, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Kinue Ohguro, Takumi Sumida, Takeshi Hasegawa, Kazuho Tanaka, Isao Takemura
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Patent number: 8163756Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions, hyperproliferative diseases, cancer, and diseases characterized by hyper-vascularization are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein, abl kinase protein, ber-abl kinase protein, braf kinase protein, VEGFR kinase protein, or PDGFR kinase protein comprises the step of contacting said kinase protein with the novel compounds.Type: GrantFiled: December 21, 2007Date of Patent: April 24, 2012Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: 8148531Abstract: Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, —CH2—, —O—, —S—, —S(?O)2—, or —NR5— where R5 is hydrogen or C1-C4 alkyl; Q is ?N—, ?CH— or ?C(X1)— wherein X1 is cyano, cyclopropyl or halo; linker radicals L2 are as defined in the claims; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and DType: GrantFiled: May 4, 2006Date of Patent: April 3, 2012Assignee: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Stephen John Davies, David Festus Charles Moffat
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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: 8143402Abstract: Provided are crystalline forms of the compound of formula (I), which is a macrocyclic inhibitor of HCV, processes for the preparation thereof, and pharmaceutical compositions comprising these crystalline forms.Type: GrantFiled: February 1, 2008Date of Patent: March 27, 2012Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Sigrid Carl Maria Stokbroekx, Carina Leys, Kelly Ann Swinney, Stijn Wuyts, Andras Horvath
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Publication number: 20120071506Abstract: The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification, and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms.Type: ApplicationFiled: November 23, 2011Publication date: March 22, 2012Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20120071466Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type I (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: ApplicationFiled: June 4, 2010Publication date: March 22, 2012Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleomas
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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: 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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Publication number: 20120046250Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: March 2, 2010Publication date: February 23, 2012Applicant: STEMSYNERGY THERAPEUTICS, INCInventor: Darren Orton
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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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Publication number: 20120040957Abstract: Compounds of formula (I) wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; R1 and R2, independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, carboxy, amino, C1-C6alkylamino, di(C1-C6alkyl)amino, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylamino-carbonyloxy, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkylcarbonyloxy, C1-C6alkyl-sulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclyl-carbonyloxy, C1-C6heteroalkyl, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted by halogeno, cyano, hydroxy, C1-C4alkoxy, C1-C4alkylcarboType: ApplicationFiled: January 21, 2010Publication date: February 16, 2012Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
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Publication number: 20120035212Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-ffluorophenyl)cyclopropane-1,1-dicarboxamide.Type: ApplicationFiled: January 15, 2010Publication date: February 9, 2012Applicant: Exelixis, Inc.Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
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Patent number: 8106055Abstract: Substituted amide compounds corresponding to formula I: processes for preparing them, pharmaceutical compositions containing these compounds, and the use of substituted amide derivatives for the preparation of medicaments for the treatment of pain and various other conditions.Type: GrantFiled: April 30, 2008Date of Patent: January 31, 2012Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Melanie Reich, Bernd Sundermann, Utz-Peter Jagusch, Beatrix Merla, Stefan Schunk, Werner Englberger, Timo Struenker, Hagen-Heinrich Hennies, Edward Bijsterveld, Fritz Theil, Heinz Graubaum
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Publication number: 20120022065Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: September 30, 2011Publication date: January 26, 2012Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
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Publication number: 20120021909Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: January 25, 2010Publication date: January 26, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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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: 8101765Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.Type: GrantFiled: January 16, 2009Date of Patent: January 24, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Carl Alan Busacca, Rogelio Perez Frutos, Nizar Haddad, Suresh R. Kapadia, Jon Charles Lorenz, Anjan Saha, Chris Hugh Senanayake, Xudong Wei
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Publication number: 20120015908Abstract: A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(?O)(OH)2, P(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(?O)(OH)(OM), P(?O)(OM)2, P?O(O2M), S(?O)(OH)2, S(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(?O)(OH)(OM), S(?O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 iType: ApplicationFiled: July 13, 2011Publication date: January 19, 2012Applicant: Efficient Pharma Management CorporateInventors: Sheng-Chu Kuo, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Tian-Shung Wu, Tzong-Der Way, Jing-Gung Chung, Jai-Sing Yang, Chi-Hung Huang, Meng-Tung Tsai
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Patent number: 8097627Abstract: The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents.Type: GrantFiled: December 18, 2009Date of Patent: January 17, 2012Assignee: Bayer Pharma AGInventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
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Publication number: 20120010183Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 11, 2011Publication date: January 12, 2012Applicant: PFIZER LIMITEDInventors: Andrew Simon Bell, Alan Daniel Brown, Marcel John De Groot, Russell Andrew Lewthwaite, Ian Roger Marsh, David Simon Millan, Manuel Perez Pacheco, David James Rawson, Nunzio Sciammetta, Robert Ian Storer, Nigel Alan Swain, Steven Matthieu Gaulier
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Publication number: 20120010415Abstract: A process for the preparation in high yields and purity of the compound 6-(7-4(1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.Type: ApplicationFiled: March 11, 2010Publication date: January 12, 2012Inventors: Silvano Spinelli, Valeria Livi
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Publication number: 20120004197Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: ApplicationFiled: March 31, 2010Publication date: January 5, 2012Applicant: KOWA COMPANY, LTD.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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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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Publication number: 20110318691Abstract: An embodiment of the composition contains any of compounds of general formula (I) below:Type: ApplicationFiled: June 28, 2011Publication date: December 29, 2011Applicant: FUJIFILM CORPORATIONInventors: Tomotaka TSUCHIMURA, Hideaki TSUBAKI, Takeshi KAWABATA
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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