Benzene Ring In A Substituent E Patents (Class 564/184)
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Patent number: 7858784Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.Type: GrantFiled: December 12, 2008Date of Patent: December 28, 2010Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
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Publication number: 20100286149Abstract: This invention relates to novel benzamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.Type: ApplicationFiled: November 25, 2008Publication date: November 11, 2010Inventors: Antonio Nardi, Jeppe Kejser Christensen
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Patent number: 7803841Abstract: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.Type: GrantFiled: December 30, 2008Date of Patent: September 28, 2010Assignee: Asterand UK LimitedInventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
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Publication number: 20100216849Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: April 30, 2010Publication date: August 26, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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Publication number: 20100190777Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: PLEXXIKON INC.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Publication number: 20100145060Abstract: Embodiments of the invention provide a method of using Schwartz Reagent, Cp2Zr(H)Cl, without accumulating or isolating it. Methods provide mixtures of Cp2ZrCl2, reductants that selectively reduce Cp2ZrCl2, and substrates. After reaction of Cp2ZrCl2 and the reductant, an intermediate reduction product is formed, apparently Schwartz Reagent. The in situ Schwartz Reagent then selectively reduces certain functional groups on the substrate. Substrates include tertiary amides, tertiary benzamides, aryl O-carbamates, and heteroaryl N-carbamates, which are reduced to aldehydes, benzaldehydes, aromatic alcohols, and heteroaromatics, respectively. Compared to prior methods, reagents are inexpensive and stable, reaction times are short, and reaction temperature in certain cases is conveniently room temperature. It has been estimated that using the in situ method described herein instead of synthesized or commercially obtained Schwartz Reagent provides a 50% reduction in cost.Type: ApplicationFiled: December 3, 2009Publication date: June 10, 2010Inventors: Yigang Zhao, Victor A. Snieckus
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Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Publication number: 20100076078Abstract: Novel compounds of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: September 7, 2007Publication date: March 25, 2010Applicant: SYNGENTA CORP PROTECTION, INC.Inventors: Pierre Jung, Stephen Trah, Christopher Richard Ayles Godfrey, William Lutz, Peter Maienfisch, Werner Zambach
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Publication number: 20100063155Abstract: A compound of general formula (I): Also disclosed is a process for preparing this compound, a fungicidal composition comprising a compound of general formula (I), as well as a method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: February 21, 2008Publication date: March 11, 2010Inventors: Pierre-Yves Coqueron, Marie-Claire Grosjean-Cournoyer, Darren James Mansfield, Benoit Hartmann, Klaus Kunz, Ruediger Fischer, Oliver Gaertzen, Amos Mattes, Oswald Ort
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Publication number: 20100056636Abstract: The present invention relates to substances and compositions having a physiological cooling effect on the skin and the mucosa of the body, especially of the oral cavity, throat and nose. More in particular, the present invention relates to N-substituted-p-menthane-3-carboxamides represented by the following formula (I): and esters thereof. These substances are capable of imparting and/or enhancing a physiological cooling effect in a product in which they are incorporated, much more effectively than the heretofore known N-substituted-p-menthane-3-carboxamides.Type: ApplicationFiled: November 30, 2007Publication date: March 4, 2010Inventors: Stefan Michael Furrer, Sander Tondeur, Chris Winkel, Harry Renes, Adri De klerk
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Publication number: 20100041715Abstract: The invention provides certain well-defined benzamides that are useful as sphingosine-1-phosphate antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: ApplicationFiled: August 12, 2009Publication date: February 18, 2010Applicant: ALLERGAN, INC.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, Ken Chow
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Patent number: 7642378Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) as well as the use of compounds of formula (I) as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: March 27, 2002Date of Patent: January 5, 2010Assignee: Janssen Pharmaceutica NVInventors: Lieven Meerpoel, Marcel Viellevoye
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Publication number: 20090286765Abstract: A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.Type: ApplicationFiled: June 13, 2006Publication date: November 19, 2009Inventors: Wesley Peter Blackaby, Ian Thomas Huscroft, Linda Elizabeth Keown, Richard Thomas Lewis, Piotr Antoni Raubo, Leslie Joseph Street, Christopher George Thomson, Joanne Thomson
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Patent number: 7605164Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: February 14, 2006Date of Patent: October 20, 2009Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
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Patent number: 7601868Abstract: The present invention provides a compound represented by the formula or salts thereof, wherein, Ar1, Ar, R, R1, R2, Ra1, Ra2, Ra3, Ra4 and Y have meanings described in the specification, having a melanin-concentrating hormone antagonistic, action and useful as an agent for the prophylaxis or treatment of obesity and the like.Type: GrantFiled: February 12, 2004Date of Patent: October 13, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Yuji Ishihara, Makoto Kamata, Shiro Takekawa
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Publication number: 20090221820Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.Type: ApplicationFiled: December 12, 2008Publication date: September 3, 2009Applicant: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
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Patent number: 7569723Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against HIV. In particular, the compounds are active against wild type and single or double mutant strains of HIV.Type: GrantFiled: January 15, 2008Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Bruno Simoneau, Jeffrey O'Meara, Christiane Yoakim
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Publication number: 20090149510Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: July 7, 2008Publication date: June 11, 2009Inventor: David G. Hangauer, JR.
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Publication number: 20090112004Abstract: The present invention is directed to a process, having a reduced environmental impact, for preparing phenylamino substituted quaternary salt compounds that are CCR2 antagonists.Type: ApplicationFiled: October 22, 2008Publication date: April 30, 2009Inventors: David C. Palmer, Sergio Casco-Cancian, Tong Xiao, Kirl L. Sorgi, Armin Roessler, Anita Vladislavic, Roger Faessler
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Publication number: 20090105220Abstract: Novel spirobenzoazepine compounds, novel processes for the preparation of nonpeptide substituted spirobenzoazepine derivatives, and novel processes for the preparation of intermediates in the preparation of such derivatives. Novel intermediates in the preparation of nonpeptide substituted spirobenzoazepine derivatives.Type: ApplicationFiled: December 22, 2008Publication date: April 23, 2009Inventors: Xiaohu Deng, Birdella Kenney, Jimmy T. Liang, Neelakandha Mani, Frank J. Villani, Fan Zhang-Plasket, Hua Zhong
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Patent number: 7511043Abstract: The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7?-hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR? and PPAR?.Type: GrantFiled: March 4, 2004Date of Patent: March 31, 2009Assignee: Amgen Inc.Inventors: Jonathan Houze, Sharon McKendry, Joshua Gergely, Yi Xia, Bei Shan, Frank Kayser
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Publication number: 20090062396Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or disorders associated therewith.Type: ApplicationFiled: May 23, 2006Publication date: March 5, 2009Applicant: Novo Nordisk A/SInventors: Preben Houlberg Olesen, Holger Claus Hansen, Lise Brown Christiansen, Anders Klarskov Petersen, Flemming Elmelund Nielsen, Birgit Sehested Hansen
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Publication number: 20090060838Abstract: Substituted n-aryl benzamides, related compounds and their pharmaceutically acceptable salts, their synthesis and labeling, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided. Also provided is the use of the disclosed compounds as imaging agents and methods for in vivo imaging and diagnosis of amyloid and synuclein diseases.Type: ApplicationFiled: August 29, 2008Publication date: March 5, 2009Inventors: Alan Snow, Manfred Weigele, Lesley Larsen, Beth Nguyen, Thomas Lake, Gerardo Castillo
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090030212Abstract: A process for the preparation of a nucleophilic addition product of an aziridine and a nucleophile, the process comprising treating the arizidine with the nucleophile in the presence of a biaryl phosphoric acid catalystType: ApplicationFiled: June 30, 2008Publication date: January 29, 2009Inventors: Jon C. Antilla, Emily B. Rowland, Gerald B. Rowland
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Publication number: 20080255221Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: November 14, 2007Publication date: October 16, 2008Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Hon C. Hui
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Publication number: 20080214654Abstract: The present invention relates to novel substituted benzyloxy-phenylmethylamide derivatives, processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR-1) activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).Type: ApplicationFiled: October 12, 2005Publication date: September 4, 2008Applicant: Bayer HealthCare AGInventors: Thomas Lampe, Cristina Alonso-Alija, Beatrix Stelte-Ludwig, Peter Sandner, Marcus Bauser, Hartmut Beck, Klemens Lustig, Ulrich Rosentreter, Elke Stahl, Hiroko Takagi
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Publication number: 20080085924Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: December 1, 2003Publication date: April 10, 2008Applicant: BAYER CROPSCINCE AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Losel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jorg Nico Greul
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Patent number: 7312236Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, where; X is —C(R4)? or —N?; Ar is phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R1 and R2 are independently hydrogen or C1-C3 alkyl; R3 is hydrogen, fluoro, or methyl; when X is —C(R4)?,R4 is hydrogen, fluoro, or methyl, provided that no more than one of R3and R4 may be other than hydrogen; and R5 is hydrogen, methyl, or ethyl. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting dural protein extravasation, and for the treatment or prevention of migraine in a mammal.Type: GrantFiled: December 6, 2004Date of Patent: December 25, 2007Assignee: Eli Lilly and CompanyInventors: Daniel Timothy Kohlman, Frantz Victor, Yao-Chang Xu, Bai-Ping Ying, Deyi Zhang
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Patent number: 7268252Abstract: Disclosed herein are novel binaphthol derivatives and methods for the optical resolution of amino acids or amino alcohols and for the optical transformation of D, L-forms of amino acids using the same.Type: GrantFiled: January 30, 2006Date of Patent: September 11, 2007Assignee: Green of Life Co., Ltd.Inventors: Kwan Mook Kim, Won Woo Nam, Hyun Jung Park, Jik Chin
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Patent number: 7265246Abstract: The present invention relates to compounds of Formula I: I which are agonists of the M-1 muscarinic receptorType: GrantFiled: June 23, 2004Date of Patent: September 4, 2007Assignee: Eli Lilly and CompanyInventors: Jennifer Rebecca Allen, Stephen Andrew Hitchcock, Bin Liu, William Wilson Turner
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Patent number: 7186862Abstract: The present invention relates to novel microbicidal compositions based on biphenylbenzamide derivatives of the formula (I) in which R1, R2, R3 and m are as defined in the disclosure, to novel biphenylbenzamides, to a plurality of processes for preparing these substances and their use for controlling pests, and to novel intermediates and processes for their preparation.Type: GrantFiled: February 11, 2003Date of Patent: March 6, 2007Assignee: Bayer CropScience AGInventors: Heiko Rieck, Ralf Dunkel, Hans-Ludwig Elbe, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck
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Patent number: 7179946Abstract: The invention relates to copper complexes of phosphorus compounds, to a process for their preparation and to their use in catalytic coupling reactions.Type: GrantFiled: January 6, 2004Date of Patent: February 20, 2007Assignee: Lanxess Deutschland GmbHInventors: Ulrich Scholz, Klaus Kunz, Oliver Gaertzen, Jordi Benet-Buchholz, Joachim Wesener
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Patent number: 7166746Abstract: The invention relates to N-bisaryl- and N-aryl-cycloalkylidenyl-a-hydroxy- and a-alkoxy acetic acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, C1–C12alkyl; C2–C12alkenyl; C2–C12alkynyl; C1–C12haloalkyl; R2 is hydrogen; optionally substituted alkyl; or optionally substituted alkynyl; R3 is optionally substituted aryl or optionally substituted heteroaryl; A is an optionally substituted saturated or unsaturated C3–C8-cycloalkylidene, optionally substituted phenylidene or optionally substituted saturated or unsaturated heterocyclylidene bridge, R4 and R5 are each independently hydrogen or an organic radical, and R6 is hydrogen; tri-C1–C4alkyl-silyl; di-C1–C4alkyl-phenylsilyl; C1–C4alkyl-diphenylsilyl; triphenylsilyl; optionally substituted alkyl; optionally substituted alkenyl or optionally substituted alkynyl.Type: GrantFiled: July 23, 2003Date of Patent: January 23, 2007Assignee: Syngenta Crop Protection, Inc.Inventors: Clemens Lamberth, Martin Zeller, Tibor Goegh
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Patent number: 7041702Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 20, 1998Date of Patent: May 9, 2006Assignee: Scion Pharmaceuticals, Inc.Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
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Patent number: 7030272Abstract: This invention relates to a ?-hydroxyalkylamide having the general Formula I: where R1 is H or a linear or branched C1 to C10 alkyl and R2 is a linear or branched C1 to C5 alkyl.Type: GrantFiled: June 12, 2004Date of Patent: April 18, 2006Inventors: Andreas Kaplan, René Gisler
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Patent number: 6936736Abstract: A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1 is hydogen atom, optionally substituted alkyl, etc.; R2 and R3 are independently optionally substituted alkyl, etc.; R4 and R5 are independently hydrogen atom or optionally substituted alkyl; R6 is hydrogen atom, hydroxy or alkyl; or a pharmaceutically acceptable salt thereof is useful as a medicament for treating retinal degenerative disorders and the like.Type: GrantFiled: March 26, 2002Date of Patent: August 30, 2005Assignee: Sumitomo Manufacturing Company LimitedInventors: Kazuhito Ikeda, Tohru Tatsuno, Hiroki Ogo, Toshio Nishihara, Tatsuya Fujibayashi, Ryu Nagata
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Patent number: 6908923Abstract: Certain substituted benzamide derivatives of Formula I: selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 20, 2002Date of Patent: June 21, 2005Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
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Patent number: 6790965Abstract: Combinatorial libraries are disclosed which are represented by Formula I: (T′—L)q—Ŝ—C(O)—L′—II′ I wherein: Ŝ is a solid support; T′—L— is an identifier residue; and —L′—II′ is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: which interact (i.e., as agonists or antagonists) with &agr; adrenergic receptors, dopamine receptors, &dgr;-opiate receptors, and K+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatement of ocular diseases such as glaucoma.Type: GrantFiled: September 8, 1999Date of Patent: September 14, 2004Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: John J. Baldwin, John C. Reader, Lawrence W. Dillard, Ge Li, Wenguang Zeng
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Patent number: 6777446Abstract: The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7&agr;-hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR&ggr; and PPAR&agr;.Type: GrantFiled: August 31, 2001Date of Patent: August 17, 2004Assignee: Tularik, Inc.Inventors: Jonathan Houze, Sharon McKendry, Joshua P. Gergely, Yi Xia, Bei Shan, Frank Kayser
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Patent number: 6716881Abstract: The present invention provides carbanilides of formula (I), wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with methods of using the compounds to control microorganisms in crops and in the protection of materials. The compounds of the present invention also find use in controlling animal pests.Type: GrantFiled: May 30, 2002Date of Patent: April 6, 2004Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Bernd-Wieland Krüger, Robert Markert, Ralf Tiemann, Dietmar Kuhnt, Stefan Dutzmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Hans-Ulrich Buschhaus
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Patent number: 6699904Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: GrantFiled: February 14, 2002Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Cheryl M. Hayward, David A. Perry
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Patent number: 6696472Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: February 24, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6670400Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.Type: GrantFiled: April 8, 2002Date of Patent: December 30, 2003Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Jacques Pommier, Christiane Martin, Pierre Roubert, Jean Pierre Defaux
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Patent number: 6638980Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: May 24, 2000Date of Patent: October 28, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Ting Su, Bing-Yan Zhu, Kim Kane-Maguire, Robert M. Scarborough, Penglie Zhang
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Patent number: 6548539Abstract: Compounds of the general structure according to Formula (I) wherein R1 is selected from alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, and heterocycloalkyl; R2 is selected from alkyl, alkenyl, alkyny, heteroalkyl, haloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, and heterocycloalkylalkyl; R3 is selected from aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; W is selected from Ch2, O and S; n is 0 to about 3: X is selected from S or O; Y, if present, is selected from a bond, aryl, NH, NR, O or S, where R3 is selected from hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, and heterocycloalkylalkyl; and Z, if present, can represent a bond or is selected from lower alkyl, O or S are disclosed. Also disclosed are uses of such compounds for treating a variety of disease conditions, including cancer.Type: GrantFiled: March 5, 2002Date of Patent: April 15, 2003Assignee: Avalon PharmaceuticalsInventors: Stanislaw Pikul, Daniel R. Soppet, Paul E. Young
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Patent number: 6541473Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: GrantFiled: September 17, 2001Date of Patent: April 1, 2003Assignee: Warner Lambert CompanyInventors: Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, William T. Gattrell, Joanna V. Geden, Peter J. Murray, Martin J. Procter, Robert J. Rowley, Jonathan G. Williams
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Patent number: 6521607Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Subsbitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-phenoxy N-phenyl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: February 18, 2003Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6515027Abstract: This invention relates to substituted benzanilides which are ligands, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzanilides which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.Type: GrantFiled: December 29, 1999Date of Patent: February 4, 2003Assignee: SmithKline Beecham Corp.Inventors: William E Bondinell, James A Chan
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Patent number: 6451823Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: September 17, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel