At 4- Or 6-position Patents (Class 544/326)
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Publication number: 20130030171Abstract: The invention relates to heteroaryl aryl ureas of the formula IA, wherein the radicals and symbols have the meanings as defined herein, the use of such compounds in the treatment of protein kinase dependent diseases; to pharmaceutical preparations comprising said heteroaryl aryl ureas, to processes for the manufacture of such novel compounds and to methods of treatment comprising the use of such heteroaryl aryl ureas.Type: ApplicationFiled: September 21, 2012Publication date: January 31, 2013Applicant: Novartis AGInventor: Novartis AG
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Patent number: 8343990Abstract: Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: GrantFiled: March 26, 2009Date of Patent: January 1, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Harold B. Wood, Jason W. Szewczyk, Yong Huang, Alan D. Adams
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Patent number: 8334382Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: February 15, 2010Date of Patent: December 18, 2012Assignee: Neurogen CorporationInventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
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Patent number: 8329901Abstract: The present invention provides 4,6-disubstituted pyrimidine compound useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: February 1, 2011Date of Patent: December 11, 2012Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Patent number: 8324220Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: September 8, 2010Date of Patent: December 4, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Mitchell Wilson, Esther Ann Martinborough, Timothy Donald Neubert, Andreas P. Termin, Jesus E. Gonzalez, III, Nicole Hilgraf
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Patent number: 8318752Abstract: The invention concerns quinazoline derivatives of Formula (I): wherein each of R1, X1, R2, R3, R5, n and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors which are sensitive to inhibition of EGF and erbB receptor tyrosine kinases.Type: GrantFiled: September 15, 2004Date of Patent: November 27, 2012Assignee: Astrazeneca ABInventor: Bernard Barlaam
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Publication number: 20120294835Abstract: Provided is a compound of formula (I), and/or salt thereof, wherein the radicals have various meanings, a process for producing cardiomyocyte-like cells from mammalian cells by culturing mammalian cells in the presence of the compound of formula (I), the pharmaceutical use of compounds of formula (I) for producing cardiomyocyte-like cells from omnipotent, pluripotent, or lineage committed mammalian cells, and the use of thus produced cardiomyocyte-like cells for treating disorders associated with impaired function of the heart.Type: ApplicationFiled: December 28, 2010Publication date: November 22, 2012Applicants: MEDIZINISCHE UNIVERSITAET WIEN, TECHNISCHE UNIVERSITAET WIENInventors: Marko Mihovilovic, Michael Schnuerch, Moumita Koley, Karlheinz Hilber, Xaver Koenig
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Patent number: 8288318Abstract: 6-Amino-5-halo-4-pyrimidinecarboxylic acids having poly-substituted aryl substituents in the 2-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: January 4, 2011Date of Patent: October 16, 2012Assignee: Dow AgroSciences, LLC.Inventors: Jeffrey B. Epp, Paul R. Schmitzer, James M. Ruiz, Terry W. Balko, Thomas L. Siddall, Carla N. Yerkes
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Patent number: 8278446Abstract: The present invention is directed to a process for chemoselective substitution on a halopyrimidine carboxaldehyde having multiple reactive sites and subsequent stereoselective oxime formation.Type: GrantFiled: June 21, 2007Date of Patent: October 2, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Hongfeng Chen, Peter J. Connolly, Kirk L. Sorgi, Anusuya Choudhury, Christopher N. Nilsen
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Publication number: 20120238575Abstract: The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.Type: ApplicationFiled: May 31, 2012Publication date: September 20, 2012Applicant: MERCK SERONO SAInventors: BRIAN HEALEY, Zhong Zhao, Amanda Sutton, Matthias Schwarz
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Patent number: 8252798Abstract: A compound of the formula: and pharmaceutical compositions for the treatment of pain.Type: GrantFiled: December 9, 2009Date of Patent: August 28, 2012Assignee: Eli Lilly and CompanyInventors: Peter Charles Astles, Rossella Guidetti, Sean Patrick Hollinshead, Michael Wade Tidwell
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Patent number: 8252927Abstract: The present invention is directed to a process for the manufacture of compounds of formula IV wherein R1 is an amino protecting group, and R2 is hydrogen or C1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M+ is a cation, preferably selected from the group consisting of Li+, Na+, K+, ½ Mg2+ and ½ Zn2+, (formula 1a) with an ammonium salt NH4+X?, wherein X? is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R2—CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B1.Type: GrantFiled: July 22, 2009Date of Patent: August 28, 2012Assignee: DSM IP Assets B.V.Inventors: Reinhard Karge, Ulla Letinois, Gerhard Shiefer
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Publication number: 20120208820Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: January 31, 2012Publication date: August 16, 2012Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20120157412Abstract: The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.Type: ApplicationFiled: February 28, 2012Publication date: June 21, 2012Inventors: Kathleen A. Battista, Gilles C. Bignan, Guozhang Xu, Lily Lee, Terry V. Hughes, Steven K. Wetter, Peter J. Connolly, Marta C. Abad, Stuart L. Emanuel, Prabha S. Karnachi, Steven A. Middleton
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Patent number: 8202877Abstract: The present application relates to novel aminopyrimidinamides, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: GrantFiled: February 17, 2010Date of Patent: June 19, 2012Assignee: Bayer CropScience AGInventors: Simon Maechling, Arnd Voerste, Eva-Maria Franken, Angela Becker, Ulrich Görgens, Mazen Es-Sayed, Markus Heil, Graham Holmwood, Johannes-Rudolf Jansen, Otto Schallner, Ulrich Ebbinghaus-Kintscher, Peter Lümmen, Silvia Cerezo-Galvez, Sachio Kudo, Takashi Hashihayata, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Publication number: 20120149687Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: October 31, 2011Publication date: June 14, 2012Applicant: AVILA THERAPEUTICS, INC.Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
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Publication number: 20120149696Abstract: Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.Type: ApplicationFiled: August 17, 2010Publication date: June 14, 2012Inventors: Natalie A. Hawryluk, J. Guy Breitenbucher, William M. Jones, Alison L. Chambers, John M. Keith, Mark Selerstad
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Patent number: 8198443Abstract: Process for the manufacture of a compound of the structure (I) with R1=hydrogen, alkyl (C1-C10, linear, cyclic or branched, aliphatic or aromatic), NR?R? (wherein R? and R? are independently selected from H, alkyl [C1-C10, linear, cyclic or branched, aliphatic or aromatic] and R2=CH2R3 wherein R3 is selected from NHR1?? (with R??=C(O)H, C(O)CH3, C(O)alkyl, CH2C6H2(OMe)3 or other saponifiable residues), alkyl (C1-C10, linear, cyclic or branched) aromatic residues, heteroaryl residues, substituted aryl residues, e.g. 3,4,5-trimethoxy-phenyl) wherein 1 equivalent of an ?-formyl-propionitrile salt is reacted with 0.75 to 2 equivalents of an acetamidine salt in the presence of a Lewis acid.Type: GrantFiled: January 7, 2008Date of Patent: June 12, 2012Assignee: DSM IP Assets B.V.Inventors: Werner Bonrath, Ralph Haerter, Reinhard Karge, Ulla Letinois
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Patent number: 8198442Abstract: A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid compound of Formula 1 is disclosed wherein R1 is H or an optionally substituted carbon moiety.Type: GrantFiled: April 28, 2006Date of Patent: June 12, 2012Assignee: E.I. du Pont de Nemours and CompanyInventor: Rafael Shapiro
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Publication number: 20120136150Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.Type: ApplicationFiled: July 15, 2010Publication date: May 31, 2012Applicant: SDS BIOTECH K.K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
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Publication number: 20120095230Abstract: A process for the preparation of 5-substituted 4-amino-2-methylpyrimidines of the formula (I) wherein R is CONH2 or CN, and of acid addition salts thereof, characterized in that a compound of formula H2N CH?C(R) CN (II) is reacted with acetimidic acid methyl ester or an acid addition salt thereof and that, if desired, a compound of formula (I) is transferred into an acid addition salt, and the transformation of a compound of formula (II) wherein R is CONH2 into a compound of formula (II) wherein R is CN by treatment with POCI3.Type: ApplicationFiled: April 8, 2010Publication date: April 19, 2012Inventors: Reinhard Karge, Jan Schutz
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Patent number: 8153791Abstract: The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.Type: GrantFiled: December 12, 2006Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Guozhang Xu, Lily Lee, Terry V. Hughes, Steven K. Wetter, Peter J. Connolly, Marta C. Abad, Stuart L. Emanuel, Prabha S. Karnachi, Steven A. Middleton, Kathleen A. Battista, Gilles C. Bignan
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Publication number: 20120077812Abstract: The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: November 30, 2011Publication date: March 29, 2012Inventors: JING FANG, Jun Tang, Andrew J. Carpenter, Gregory Peckham, Christopher R. Conlee, Kien S. Du, Subba Reddy Katamreddy
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Publication number: 20120071496Abstract: The present application relates to novel aminopyrimidinamides, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: ApplicationFiled: February 5, 2010Publication date: March 22, 2012Applicant: Bayer CropScience AGInventors: Simon Maechling, Arnd Voerste, Eva-Maria Franken, Angela Becker, Ulrich Görgens, Mazen Es-Sayed, Markus Heil, Graham Holmwood, Johannes-Rudolf Jansen, Otto Schallner, Ulrich Ebbinghaus-Kintscher, Peter Lümmen, Silvia Cerezo-Galvez, Sachio Kudo, Takashi Hashihayata, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Patent number: 8129526Abstract: The present invention relates to a pyrimidine compound of the formula (II?): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X3 represents C5 polymethylene, in which a single CH2—CH2 may be replaced with a single CH?CH, substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls.Type: GrantFiled: October 15, 2009Date of Patent: March 6, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Hajime Mizuno, Akio Manabe
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Publication number: 20120040955Abstract: The invention relates to compounds of formula (I) wherein AA, R2 to R7 and X1 to X3 have the meaning as cited in the description and the claims. Said compounds are useful as selective inhibitors of JAK3 over JAK2 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: April 9, 2010Publication date: February 16, 2012Inventors: Richard John Harrison, Andrew Hobson, Nigel Ramsden
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Patent number: 8101621Abstract: The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1?, (ii) either one of Ra2 and Ra2?, (iii) either one of Rb1 and Rb1?, and (iv) either one of Rb2 and Rb2?, are combined to form —(CH2)n— where n is 1, 2 or 3; and among Ra1, Ra1?, Ra2, Ra2?, Rb1, Rb1?, Rb2 and Rb2?, the groups which do not form —(CH2)n— are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: April 25, 2007Date of Patent: January 24, 2012Assignee: MSD K.K.Inventors: Tetsuya Kato, Nobuhiko Kawanishi, Takashi Mita, Keita Nagai, Katsumasa Nonoshita, Mitsuru Ohkubo
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Patent number: 8088769Abstract: The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.Type: GrantFiled: December 31, 2004Date of Patent: January 3, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Martin Hendrix, Lars Bärfacker, Heike Heckroth, Dagmar Karthaus, Adrian Tersteegen
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Publication number: 20110319615Abstract: Pyrimidinyl aryl hydrazones are effective at controlling insects.Type: ApplicationFiled: September 8, 2011Publication date: December 29, 2011Applicant: DOW AGROSCIENCES LLCInventors: Katherine A. Guenthenspberger, Timothy C. Johnson, Noormohamed M. Niyaz, Ricky Hunter, Annette V. Brown, Tony K. Trullinger
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Patent number: 8071763Abstract: A method for the treatment of nocturia which consists of administering to a mammal in need of such treatment a therapeutically effective amount of a nonsteroidal anti-inflammatory drug consisting of loxoprofen or a pharmacologically acceptable salt thereof, wherein the mammal is a human who has a neurogenic bladder.Type: GrantFiled: May 4, 2009Date of Patent: December 6, 2011Assignee: Daiichi Sankyo Company, LimitedInventor: Tohru Araki
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Patent number: 8044040Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: July 16, 2007Date of Patent: October 25, 2011Assignees: Bristol-Myers Squibb Company, Pharmacopeia, Inc.Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
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Publication number: 20110245242Abstract: Heterocyclically substituted anilinopyrimidines of the formula (I) in which R1 to R10 and L1, L2, E1, E2, E3, Y and Z have the meanings given in the description, and agrochemically active salts thereof, their use and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing heterocyclically substituted anilinopyrimidinenes of the formula (I).Type: ApplicationFiled: August 21, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Jörg Nico Greul, Oliver Gaertzen, Hendrik Helmke, Stefan Hille, Kerstin Ilgö, Amos Mattes, Pierre Wasnaire, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Arnd Voerste, Peter Dahmen, Rurth Meissner, Christoph Andreas Braun, Martin Kaubmann, Hiroyuki Hadano
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Publication number: 20110245284Abstract: Alkoxy- and alkylthio-substituted anilinopyrimidines of the formula (I) in which R1 to R14 and E1, E2, E3, X and Y have the meanings given in the description, and agrochemically active salts thereof, their use, and methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seeds of plants, processes for preparing such compositions and treated seeds and also their use for controlling phytopathogenic hal inful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for the preparation of alkoxy- and alkylthio-substituted anilinopyrimidines of the formula (I).Type: ApplicationFiled: August 21, 2009Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Jörg Nico Greul, Hendrik Helmke, Stefan Hillebrand, Amos Mattes, Pierre Wasnaire, Carl Friedrich Nising, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Ruth Meissner, Chirstoph Andreas Braun, Martin Kaubmann, Hiroyuki Hadano, Ulrich Heinemann
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Publication number: 20110230485Abstract: This invention relates to novel 6-phenyl-phymidin-4-yl-(phenylannine or phenoxy) derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 9, 2009Publication date: September 22, 2011Applicant: NEUROSEARCH A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters
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Patent number: 8013155Abstract: Disclosed a method for preparing a compound of Formula 1, wherein R1 is cyclopropyl, 4-chlorophenyl or 4-bromophenyl; and R2 is C1-C14 alkyl; comprising contacting a compound of Formula 2 with a persulfate oxidant in the presence of a strong sulfur- or phosphorus-containing mineral acid and an oxidation resistant solvent. Also disclosed are methods for preparing the compound of Formula 2 from a compound of Formula 5 as well as compounds of Formula 6 and salts thereof, wherein R is NH2, Cl or OH; X is H or Cl; R1 is cyclopropyl, 4-chlorophenyl or 4-bromophenyl; and R2 is C1-C14 alkyl; provided that when R is NH2 or Cl, then X is Cl; which are useful a process intermediates.Type: GrantFiled: May 12, 2006Date of Patent: September 6, 2011Assignee: E. I. du Pont de Nemours and CompanyInventor: Gary David Annis
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Publication number: 20110201592Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: October 23, 2008Publication date: August 18, 2011Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Jamieson Caldwell, Antony William Oliver, Tony Michael Raynham, Emma Jane Welsh, Cornelius Albertus Johannes Matijssen
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Patent number: 7994167Abstract: The present invention relates to pentafluorosulphanyl-substituted compounds, methods for their production, medicaments containing such compounds and the use of such compounds for producing medicaments.Type: GrantFiled: May 17, 2006Date of Patent: August 9, 2011Assignee: Gruenenthal GmbHInventors: Robert Frank, Bernd Sundermann, Hans Schick
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Patent number: 7989458Abstract: Compounds of formula (I) in free or salt or solvate form, where T1, T2, Ra and Rb have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: July 12, 2007Date of Patent: August 2, 2011Assignee: Novartis AGInventors: Catherine Leblanc, Maude Nadine Pierrette Pipet, Robin Alec Fairhurst, Claire Adcock, Robert Alexander Pulz, Duncan Shaw, Nikolaus Johannes Stiefl
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Patent number: 7989459Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC?. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I: wherein R1 is chosen from nitrogen-attached heterocyclyl, nitrogen-attached substituted heterocyclyl wherein the point of attachment is a nitrogen heteroatom, and R2 is chosen from aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, hetroarylalkyl, and substituted heteroarylalkyl.Type: GrantFiled: February 2, 2007Date of Patent: August 2, 2011Assignee: Pharmacopeia, LLCInventors: Andrew Roughton, Yajing Rong, Koc Kan Ho, Michael Ohlmeyer, David Diller
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Patent number: 7989465Abstract: The present invention provides 4,6-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable salts and compositions thereof, and methods of using the same. The present invention also provides probe compounds, such as compounds of formula V: wherein each of Ring A, Ring B, R1?, T, Rt, m, Rx, Ry, and W is described herein.Type: GrantFiled: April 20, 2009Date of Patent: August 2, 2011Assignee: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Publication number: 20110178300Abstract: The present invention is directed to a process for the manufacture of compounds of formula IV wherein R1 is an amino protecting group, and R2 is hydrogen or C1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M+ is a cation, preferably selected from the group consisting of Li+, Na+, K+, ms, ½ Mg2+ and ½ Zn2+, (formula 1a) with an ammonium salt NH4X?, wherein X? is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R2—CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B1.Type: ApplicationFiled: July 22, 2009Publication date: July 21, 2011Inventors: Reinhard Karge, Ulla Letinois, Gerhard Shiefer
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Patent number: 7982036Abstract: The present invention provides compounds of formula I wherein Ring A, Ring B, m, Rx, Ry, W and R1 are as defined herein, pharmaceutically acceptable salts and compositions thereof, and methods of using the same.Type: GrantFiled: October 17, 2008Date of Patent: July 19, 2011Assignee: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Patent number: 7981900Abstract: Compounds of general formula (I), (II) (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).Type: GrantFiled: December 3, 2004Date of Patent: July 19, 2011Assignee: YM Biosciences Australia Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
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Publication number: 20110166116Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: ApplicationFiled: June 23, 2010Publication date: July 7, 2011Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.Inventors: Brian DYCK, Joe A. TRAN, Junko TAMIYA, Florence JOVIC, Troy VICKERS, Chen CHEN, Nicole HARRIOTT, Timothy COON, Neil J. ASHWEEK
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Publication number: 20110160206Abstract: The present invention provides a tri-substituted pyrimidine compound having an excellent PDE10 inhibitory activity. The present invention relates to a tri-substituted pyrimidine compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compound for PDE10 inhibitor, and a pharmaceutical composition comprising said compounds as an active ingredient: wherein: either one of X1 and X2 is N, and the other of X1 and X2 is CH; A is *-CH?CH—, *-C(Alk)=CH—, *-CH2—CH2— or *-O—CH2— (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted quinoxalinyl or an optionally substituted quinolyl; Y0 is mono- or di-substituted amino group, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 3, 2009Publication date: June 30, 2011Inventors: Eiji Kawanishi, Takehiko Matsumura
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Patent number: 7951803Abstract: Compounds of the formula wherein R1 represents optionally substituted C1-C10 alkyl, aryl or heteroaryl, and R3 represents alkoxy-substituted aryl or optionally substituted heteroaryl, are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.Type: GrantFiled: March 9, 2007Date of Patent: May 31, 2011Assignee: Pharmacopeia, LLCInventors: Andrew G. Cole, Marc-Raleigh Brescia, Joan J. Zhang, Zahid Hussain, David J. Diller, Axel Metzger, Gulzar Ahmed, Ian Henderson
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Patent number: 7928110Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C4 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.Type: GrantFiled: April 17, 2009Date of Patent: April 19, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Hajime Mizuno, Akio Manabe
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Patent number: 7919490Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: RE42462Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: October 7, 1995Date of Patent: June 14, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: RE42477Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: March 27, 1997Date of Patent: June 21, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack