Nitrogen Attached Directly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/190)
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Patent number: 8227605Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: GrantFiled: October 29, 2007Date of Patent: July 24, 2012Assignee: Schering CorporationInventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards
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Patent number: 8211412Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a heterocyclic compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein R1, R2, and R2? are each independently C1-3 alkyl; Y is S or O; and p is an integer of 0 to 3, wherein when p is 2 or 3, R1 may be the same or different.Type: GrantFiled: February 7, 2012Date of Patent: July 3, 2012Assignee: Shiseido Company Ltd.Inventors: Naota Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
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Patent number: 8178688Abstract: The present invention relates to novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same. The novel benzamidine derivatives of the present invention are useful for the prevention and treatment of osteoporosis, bone fractures and allergic inflammatory diseases.Type: GrantFiled: August 4, 2005Date of Patent: May 15, 2012Assignee: Dong Wha Pharmaceutical Co., Ltd.Inventors: Jin Soo Lee, Seok Hoon Ahn, Young Goo Jin, Sang Mi Jin, Whui-Jung Park, Sae Kwang Ku, Yun Ha Hwang, Pan Soo Kim, Sun Shin Yi, Jei Man Ryu
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Patent number: 8153560Abstract: Pesticidal mixtures comprising aminothiazoline compounds The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one aminothiazoline compound I of the Formula (I) wherein R1, R2, R3, R4, R5 and R6 are defined in the description; and 2) at least one active compound II selected from a group A comprising acetylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acetylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipidsynthesis and other compounds as defined in the description, in synergistically effective amounts.Type: GrantFiled: February 22, 2008Date of Patent: April 10, 2012Assignee: BASF SEInventors: Jürgen Langewald, Markus Kordes, Deborah L. Culbertson, Douglas D. Anspaugh
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Patent number: 8153792Abstract: The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula (1) which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein.Type: GrantFiled: February 13, 2008Date of Patent: April 10, 2012Assignee: AB ScienceInventors: Alain Moussy, Philippe Reginault, François Bellamy, Anne Lermet
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Patent number: 8153814Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: GrantFiled: January 12, 2010Date of Patent: April 10, 2012Assignees: Pfizer Limited, Icagen, Inc.Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Patent number: 8133911Abstract: The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: GrantFiled: October 17, 2008Date of Patent: March 13, 2012Assignee: Dompe S.p.AInventors: Alessio Moriconi, Andrea Aramini
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Publication number: 20110319616Abstract: An object is to provide a thiazole derivative produced from easily available raw materials by a simplified production process. Provided are a process for producing a novel thiazole derivative represented by the general formula (I), which is characterized by adding a strong base to a thioamide represented by the general formula (II) and reacting the mixture with a thioformamide represented by the general formula (III), and a novel thiazole derivative.Type: ApplicationFiled: March 8, 2010Publication date: December 29, 2011Applicant: GIFU UNIVERSITYInventor: Toshiaki Murai
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Publication number: 20110269748Abstract: This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(?O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(?O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(?O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkylType: ApplicationFiled: February 13, 2008Publication date: November 3, 2011Inventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Christopher James Grantham, Theodorus Dinklo, Anne Simone Josephine Lesage
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Publication number: 20110257193Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: December 23, 2009Publication date: October 20, 2011Applicant: Glenmark Pharmaceuticals, S.A.Inventors: V. S. Prasadarao Lingam, Abraham Thomas, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20110218341Abstract: The use of a compound of formula I wherein X is (i), (ii) or (iii) Y is O, S(O)m, NR3, CR5R6, CR5R6—CR7R8, O—CR7R8, S(O)m—CR7R8, NR3—CR7R8, CR5R6—O, CR5R6—S(O)m, CR5R6—NR3, SO2—NR3, NR3—SO2, NR3—O or O—NR3; m is 0, 1, or 2; the ring (T) is a 5- or 6-membered aromatic or heteroaromatic ring; R1 to R10 are specified organic groups and n and is 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: May 11, 2011Publication date: September 8, 2011Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMITEDInventors: Anthony Cornelius O'Sullivan, Jürgen Harry Schaetzer, Christoph Lüthy, Alison Clare Elliott, Christopher John Mathews
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Patent number: 8013004Abstract: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: December 4, 2009Date of Patent: September 6, 2011Assignee: Bristol-Myers Squibb CompanyInventors: T. G. Murali Dhar, Hai-Yun Xiao, Bingwei Yang
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Patent number: 8003677Abstract: The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.Type: GrantFiled: October 26, 2009Date of Patent: August 23, 2011Assignee: Sanofi-AventisInventors: Gerhard Zoller, Marc Dietrich Voss, Stefanie Keil, Andreas Herling, Hans Matter
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Patent number: 7989394Abstract: The present invention relates to 1-(azolin-2-yl)-amino-2-aryl-1-hetaryl-ethane compounds (I) and 1-(aminothiocarbonylamino)-2-aryl-1-hetaryl-ethane compounds (II) and their salts which are useful for combating animal pest, in particular insects, arachnids and nematodes. Furthermore, the present invention relates to a method for combating animal pests selected from insects, arachnids and nematodes, and to agricultural compositions for combating animal pests. Furthermore, the present invention relates to veterinary compositions for combating animal pests.Type: GrantFiled: June 29, 2007Date of Patent: August 2, 2011Assignee: BASF SEInventors: Markus Kordes, Delphine Breuninger, Ronan Le Vezouet, Christopher Koradin, Livio Tedeschi, Michael Puhl, Deborah L. Culbertson
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Patent number: 7989456Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: May 5, 2010Date of Patent: August 2, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian M. C. Golec
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Publication number: 20110178143Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 14, 2008Publication date: July 21, 2011Applicant: ALLERGAN, INC.Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Dario G. Gomez, Santosh N. Sinha, Smit S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil
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Patent number: 7981437Abstract: The present invention relates to Indanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.Type: GrantFiled: November 15, 2006Date of Patent: July 19, 2011Assignee: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
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Patent number: 7977332Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: December 2, 2004Date of Patent: July 12, 2011Assignee: FMC CorporationInventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
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Patent number: 7977322Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: August 11, 2005Date of Patent: July 12, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida Ruah, Peter Grootenhuis, Mark Miller, Matthew Hamilton
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Patent number: 7973061Abstract: The present invention relates to compounds of the Formula I, wherein L, X, Y, Z, R1, R2, R3 and R4 are defined herein. The invention also provides methods of using the compounds for inhibition of kinases, more specifically ALK kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions; (Formula I).Type: GrantFiled: March 31, 2005Date of Patent: July 5, 2011Assignee: Exelixis, Inc.Inventors: James William Leahy, Gary Lee Lewis, John M. Nuss, Brain Hugh Ridgway, Joan C. Sangalang
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Patent number: 7960310Abstract: The use of a compound of formula (I) wherein X is (i), (ii) or (iii), formula (i), formula (ii), formula (iii) Y is O, S(O)m, NR3, CR5R6, CR5R6—CR7R8, O—CR7R8, S(O)m—CR7R8, NR3—CR7R8, CR5R6—O, CR5R6—S(O)m, CR5R6—NR3, SO2—NR3, NR3—SO2, NR3—O or O—NR3; m is 0, 1, or 2; the ring (T) formula (T) is a 5- or 6-membered aromatic or heteroaromatic ring; R1 to R10 are specified organic groups and n and is 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: GrantFiled: August 2, 2006Date of Patent: June 14, 2011Assignees: Syngenta Participations AG, Syngenta LimitedInventors: Anthony Cornelius O'Sullivan, Jürgen Harry Schaetzer, Christoph Lüthy, Alison Clare Elliott, Christopher John Mathews
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Publication number: 20110123586Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: ApplicationFiled: June 2, 2009Publication date: May 26, 2011Inventors: Bonnie Bassler, Lee Swem
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Publication number: 20110118116Abstract: The present invention relates to azolin-2-ylamino compounds of formula (I), wherein A is a radical of the formulae (A.1) or (A.2), wherein * denotes the binding site and wherein the indices and variables are as defined in the description. The present invention relates as well as to the precursor compounds thereof, which are both useful for combating animal pests selected from insects, arachnids and nematodes. The invention also relates to methods for controlling and/or combating such animal pests by using these compounds, to methods of protecting crops and plant propargation material, and further also to seeds and agricultural and veterinary composition comprising said compounds.Type: ApplicationFiled: July 14, 2009Publication date: May 19, 2011Inventors: Ronan Le Vezouet, Markus Kordes, Ralph Paulini, Deborah L. Culbertson
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Patent number: 7897331Abstract: Thiazolyl tetrazolium salts with increased solubility in aqueous solutions have alkylammonium alkoxy substituents, preferably trimethyl ammonium propoxy groups substituents, on phenyl rings attached to the tetrazolium ring.Type: GrantFiled: June 16, 2010Date of Patent: March 1, 2011Assignee: Bayer HealthCare LLCInventors: James P. Albarella, Steven W. Felman, John J. Landi, Karen L. Marfurt
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Patent number: 7888379Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: May 24, 2006Date of Patent: February 15, 2011Assignee: Merck Serono SAInventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
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Publication number: 20110028523Abstract: Described herein are compounds useful as agonists of alpha 2B/2C receptors. Pharmaceutical compositions including the presently described compounds and methods of treatment of diseases and conditions with the presently described compounds also are disclosed.Type: ApplicationFiled: July 1, 2010Publication date: February 3, 2011Applicant: ALLERGAN, INC.Inventors: Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Wenkui K. Fang, Santosh C. Sinha, Michael E. Garst, Daniel W. Gil
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Patent number: 7879888Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: May 24, 2006Date of Patent: February 1, 2011Assignee: Merck Serono SAInventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
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Patent number: 7875640Abstract: The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, R4, L2 and A are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: GrantFiled: March 19, 2008Date of Patent: January 25, 2011Assignee: Abbott LaboratoriesInventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez-Medrano, Xueqing Wang, Sridhar Peddi, William A. Carroll, Michael J. Dart
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Patent number: 7868030Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in the application and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: May 30, 2007Date of Patent: January 11, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Marcel Gubler, Wolfgang Haap, Paul Hebeisen, Eric A. Kitas, Bernd Kuhn, Rudolf E. Minder, Brigitte Schott, Hans P. Wessel
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Publication number: 20100324096Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a heterocyclic compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein A is C1-6 alkyl, C5-6 cycloalkyl, benzyl, benzylcarbonyl, benzoyl, phenyl, pyridyl or pyrimidyl; Ra is H, C1-6 alkyl, or C2-6 alkenyl; “” represents a single bond or a double bond wherein n=1 or 2; Y is S or O; and R3 and R4 are each independently H, C1-6 alkyl, hydroxy-C1-6 alkyl, C2-7 acyl, phenyl, pyridyl, pyrimidyl, etc.;with the proviso that at least one R3 is a group other than C1-3 alkyl in the case where: the hetero ring containing Y is a thiazoline ring; R4?Ra?H; X1?X2?CH; and either p =0 or R5?C1-6 alkyl.Type: ApplicationFiled: February 6, 2009Publication date: December 23, 2010Applicant: SHISEIDO COMPANY LTD.Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
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Publication number: 20100316584Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a heterocyclic compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein R1, R2, and R2? are each independently C1-3 alkyl; Y is S or O; and p is an integer of 0 to 3, wherein when p is 2 or 3, R1 may be the same or different.Type: ApplicationFiled: February 6, 2009Publication date: December 16, 2010Applicant: SHISEIDO COMPANY LTD.Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
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Patent number: 7846954Abstract: The present invention relates to heterocyclic derivatives useful as inhibitors of 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: July 1, 2009Date of Patent: December 7, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Nicole Zimmermann, Peter D. J. Grootenhuis, Mehdi Michel Djamel Numa, Dean Stamos, Corey Don Anderson, Tara Whitney
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Publication number: 20100280078Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and to their salts which are useful for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a radical of formulae A.1 or A.Type: ApplicationFiled: July 2, 2008Publication date: November 4, 2010Applicant: BASF SEInventors: Markus Kordes, Christopher Koradin, Ronan Le Vezouet, Ernst Baumann, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Cecile Ebuenga
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Patent number: 7807700Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: June 28, 2007Date of Patent: October 5, 2010Assignee: Amgen Inc.Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
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Patent number: 7799814Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: May 24, 2006Date of Patent: September 21, 2010Assignee: Merck Serono S.A.Inventors: Anna Quattropani, Jerome Dorbais, David Covini, Gwenaelle Desforges, Thomas Rueckle
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Patent number: 7795288Abstract: The invention relates to thiazole and pyrazole derivatives of formula (I) wherein Q is S and X is C, or Q is CH and X is N; R1 is unsubstituted or substituted phenyl; and R2 is unsubstituted or substituted aryl or heteroaryl; or a salt of the said compounds, and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour disease, in particular such diseases which respond to an inhibition of the Flt-3 kinase.Type: GrantFiled: November 12, 2004Date of Patent: September 14, 2010Assignee: Novartis AGInventors: Guido Bold, Andreas Floersheimer, Pascal Furet, Vito Guagnano, Keiichi Masuya, Andrea Vaupel, Joseph Schoepfer
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Patent number: 7786153Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.Type: GrantFiled: March 2, 2006Date of Patent: August 31, 2010Assignee: Abbott Laboratories Inc.Inventors: Dale J. Kempf, Charles A. Flentge, John T. Randolph, Peggy Huang, Larry L. Klein
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Patent number: 7777036Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where y, G, K, L, M, W, V, R2, R3, R4a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: September 20, 2005Date of Patent: August 17, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Mehran Seid Bagherzadeh, Serguei Sviridov, Sultan Chowdhury, Shifeng Liu, Vishnumurthy Kodumuru
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Patent number: 7767822Abstract: Thiazolyl tetrazolium salts with increased solubility in aqueous solutions have alkylammonium alkoxy substituents, preferably trimethyl ammonium propoxy groups substituents, on phenyl rings attached to the tetrazolium ring. Thiazolyl tetrazolium salts with increased solubility in aqueous solutions have alkyl ammonium alkoxy substituents, preferably trimethyl ammonium propoxy groups substituents, on phenyl rings attached to the tetrazolium ring, e.g. the compounds of the general formula shown below. Formula (A-)a.Type: GrantFiled: January 13, 2006Date of Patent: August 3, 2010Assignee: Bayer Healthcare LLCInventors: James P. Albarella, Steven W. Felman, John J. Landi, Karen L. Marfurt
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Patent number: 7754745Abstract: Azacyclopentane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.Type: GrantFiled: June 8, 2007Date of Patent: July 13, 2010Assignee: Merck Frosst Canada Ltd.Inventors: Chun Sing Li, Yeeman K. Ramtohul
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Publication number: 20100167925Abstract: The present invention relates to azolin-2-yl-amino compounds of formulae (I. a) and (1.b) and their salts which are useful for combating animal pest, in particular arthropod and nematodes. The present invention also relates to a method for combating such pests and for protecting crops against infestation or infection by such pests. Furthermore, the present invention relates to veterinary compositions for combating animal pests. Formula (I.a), formula (I.b) wherein n is 0 to 4; X is S, O or NR5; A is —C(R6a)(R6b)—, O, NR7, S, S(O) or S(O)2; B is a bond Or CH2; R1 is H, CN, C1-C6-alkyl, C2-C6-alkenyl, C1-C6-alkylcarbonyl, C3-C6-cycloalkyl, phenyl, benzyl, etc.; R2a, R2b are H, CN, C1-C6-alkyl, C2-C6-alkenyl, C1-C6-alkylcarbonyl, (C1-C6-alkyl)-thiocarbonyl, C(O)NRaRb, C(S)NRaRb, (SO2)NRaRb, phenyl, benzyl, 5 or 6 membered heterocyclic ring etc.Type: ApplicationFiled: August 6, 2007Publication date: July 1, 2010Applicant: BASF SEInventors: Christopher Koradin, Markus Kordes, Ronan Le Vezouet, Deborah L. Culbertson, Douglas D. Anspaugh
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Publication number: 20100168190Abstract: The present invention relates to novel heterocyclic compounds, including oxadiazole compounds, pharmaceutical compositions and their use in the inhibition of reverse transcriptase and the treatment of HIV (1 and 2) infections, AIDS and ARC and other viral infections.Type: ApplicationFiled: July 2, 2008Publication date: July 1, 2010Applicant: YALE UNIVERSITYInventor: William L. Jorgensen
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Publication number: 20100166710Abstract: The present invention provides compositions and methods for inducing neuronal cell differentiation.Type: ApplicationFiled: December 1, 2006Publication date: July 1, 2010Applicants: The Scripps Research Institute, The Salk Institute for Biological StudiesInventors: Masaki Warashina, Kyung Hoon Min, Fred Gage, Peter G. Schultz, Sheng Ding, Tomoko Kuwabara
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Patent number: 7741491Abstract: The invention therefore relates to compounds of the formula I in which the variables are as defined in the specification, to pharmaceutical compositions containing them and to their use for therapeutically lowering blood glucose levels.Type: GrantFiled: December 12, 2006Date of Patent: June 22, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefan Petry, Karl-Heinz Baringhaus, Norbert Tennangels, Guenter Mueller, Reinhard Kirsch
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Patent number: 7737151Abstract: The present invention relates to compounds useful as inhibitors of protein kinases of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 17, 2006Date of Patent: June 15, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian M. C. Golec
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Publication number: 20100137385Abstract: Certain substituted amino heterocyclic and heteroaryl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein R, R1, R2, R3, R4, A, B and Q are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: February 2, 2007Publication date: June 3, 2010Applicant: Bayer CropScience AGInventors: John A. Dixon, Benjamin J. Dugan, Zeinab M. Elshenawy, Edward J. Barron, Stephen F. Donovan, Manorama M. Patel, George Theodoridis, Roland Andree, Hans-Georg Schwarz, Eva-Maria Franken, Olga Malsam, Christian Arnold
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Publication number: 20100137315Abstract: The invention relates to compounds, pharmaceutical compositions thereof, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.Type: ApplicationFiled: November 30, 2009Publication date: June 3, 2010Applicant: APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Kevin J. French, Zuping Xia
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Publication number: 20100120874Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: ApplicationFiled: November 4, 2009Publication date: May 13, 2010Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Publication number: 20100076034Abstract: The present invention relates to (R,S) 2-aryl-2-fluoropropanoic acids, their single enantiomers (R) and (S), their derivatives amides and acylsulfonamides and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: December 18, 2007Publication date: March 25, 2010Applicant: DOMPE PHA.R.MA S.P.A.Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta
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Patent number: 7678815Abstract: The present invention is concerned with novel thiazole 4-carboxyamide derivatives of the general formula (I) and with methods for the preparation thereof, which compounds are useful as metabotropic glutamate receptor antagonists: wherein R1 to R4 are as defined in the specification.Type: GrantFiled: January 10, 2006Date of Patent: March 16, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira