Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/225)
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Patent number: 9434694Abstract: The invention discloses a method for the preparation of medetomidine starting from 1-bromo 2,3-dimethylbenzene and chloroacetone.Type: GrantFiled: July 30, 2015Date of Patent: September 6, 2016Assignee: Lonza Ltd.Inventors: Florencio Zaragoza Doerwald, Anna Kulesza, Stephan Elzner, Robert Bujok, Zbigniew Wrobel, Krzysztof Wojciechowski
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Publication number: 20150099889Abstract: The invention discloses a method for the preparation of medetomidine starting from 1-bromo 2,3-dimethylbenzene and chloroacetone.Type: ApplicationFiled: November 15, 2012Publication date: April 9, 2015Inventors: Florencio Zaragoza Doerwald, Anna Kulesza, Stephen Elzner, Robert Bujok, Zbigniew Wrobel, Krzysztof Wojciechowski
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Patent number: 8829002Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.Type: GrantFiled: December 13, 2011Date of Patent: September 9, 2014Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Patent number: 8822516Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.Type: GrantFiled: June 9, 2011Date of Patent: September 2, 2014Assignee: Technion Research & Development Foundation LimitedInventors: Gennady Nisnevich, Mark Gandelman, Kseniya Kulbitski
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Patent number: 8759383Abstract: The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors.Type: GrantFiled: March 14, 2008Date of Patent: June 24, 2014Assignee: Concert Pharmaceuticals, Inc.Inventor: Roger Tung
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Patent number: 8673941Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: GrantFiled: July 30, 2009Date of Patent: March 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
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Publication number: 20130281366Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.Type: ApplicationFiled: December 26, 2011Publication date: October 24, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
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Publication number: 20130267536Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.Type: ApplicationFiled: December 13, 2011Publication date: October 10, 2013Applicant: ALLA CHEM, LLCInventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Patent number: 8420680Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3?R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.Type: GrantFiled: June 30, 2008Date of Patent: April 16, 2013Assignees: Emory University, NeurOp, Inc.Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Yesim Altas Tahirovic, Scott J. Myers
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Patent number: 8329706Abstract: The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.Type: GrantFiled: May 11, 2010Date of Patent: December 11, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, Romain Siegrist, Thierry Sifferlen, Jodi T Williams
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Publication number: 20120302607Abstract: The invention provides a series of C4-substituted oxazole compounds having an alpha keto side chain at the 2 position, for example, compounds of formula I. The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula I, useful intermediates in the preparation of compounds of formula I, and methods of using compounds of formula 1 and compositions thereof.Type: ApplicationFiled: August 2, 2012Publication date: November 29, 2012Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 8222425Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: July 19, 2011Date of Patent: July 17, 2012Assignee: Novartis AGInventors: Shawn D. Britt, Lech Andrzej Ciszewski, Jiping Fu, Subramanian Karur, Yugang Liu, Peichao Lu, David Thomas Parker, Mahavir Prashad, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng
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Publication number: 20120129830Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3, provided that m+n?7 and that o+p?7; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compounds; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: May 24, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Publication number: 20120101111Abstract: The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.Type: ApplicationFiled: May 11, 2010Publication date: April 26, 2012Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, Romain Siegrist, Thierry Sifferlen, Jodi T. Williams
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Patent number: 8158186Abstract: A chemical compound of the general formula I or II is useful as feed additive: wherein X=O or NR, and R=H, C1-C6-alkyl (optionally branched), C3-C6-cycloalkyl, aryl, or aralkyl, and wherein R1, R2, are identical or different and in each case H, C1-C6-alkyl (optionally branched), C3-C6-cycloalkyl, allyl, aryl, or aralkyl; or R1 and R2 together are an C2- to C6-alkylene group (optionally C1-C6-alkyl substituted).Type: GrantFiled: December 19, 2008Date of Patent: April 17, 2012Assignee: Evonik Degussa GmbHInventors: Christoph Kobler, Philipp Roth, Christoph Weckbecker, Klaus Huthmacher
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Patent number: 8124633Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.Type: GrantFiled: April 7, 2008Date of Patent: February 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao
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Patent number: 8119813Abstract: This disclosure relates to methods for preparing an enantiomerically enriched N-carboxyanhydride of an amino alpha acid of the formula (IIIa) or (IIIb): from a compound of the formula (IIa) or (IIb), respectively: wherein R1, R2, and R3 are as defined in the disclosure.Type: GrantFiled: November 12, 2009Date of Patent: February 21, 2012Assignee: sanofi-aventisInventors: Antony Bigot, Maxime Lampilas
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Publication number: 20110275802Abstract: The present invention relates to a process for modifying diisocyanates for preparing polyisocyanates, where the diisocyanate is reacted using a catalyst, wherein the diisocyanate used is obtained by quenching a gaseous reaction mixture in the phosgenation of diamines in the gas phase, wherein the gaseous reaction mixture comprises at least a diisocyanate, phosgene and hydrogen chloride, wherein a quenching liquid is sprayed into the gas mixture which flows continuously from a reaction zone into a downstream quenching zone, and wherein the quenching liquid is sprayed in by at least two spray nozzles which are arranged at the inlet of the quenching zone at equal intervals along the circumference of the quenching zone.Type: ApplicationFiled: November 26, 2009Publication date: November 10, 2011Applicant: BAYER MATERIALSCIENCE AGInventors: Frank Richter, Reinhard Halpaap
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Patent number: 8048901Abstract: The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved.Type: GrantFiled: July 10, 2007Date of Patent: November 1, 2011Assignee: Aventis Pharma Deutschland GmbHInventors: Jochen Goerlitzer, Heiner Glombik, Eugen Falk, Dirk Gretzke, Stefanie Keil, Hans-Ludwig Schaefer, Christian Stapper, Wolfgang Wendler
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Patent number: 8003678Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: December 15, 2009Date of Patent: August 23, 2011Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 8003803Abstract: Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein ? represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: GrantFiled: April 11, 2007Date of Patent: August 23, 2011Assignee: Schering CorporationInventors: Yan Xia, Samuel Chackalamannil
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Patent number: 7939678Abstract: A compound having the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, wherein R1 comprises a chromophore that absorbs light from the visible wavelength range, and wherein n is an integer of at least 12. A solid phase change ink composition is also disclosed containing a colorant comprising a chromophore that absorbs light from the visible wavelength range and has the formula wherein R1, Z, and the carbonyl can be comprised by a common ring, and wherein n is an integer of at least 12. Also disclosed is a method of forming a colorant wherein a first compound having the formula is reacted with a second compound having the formula Z(CH2)nCH3 wherein n is an integer of at least 12 to form a third compound having the formula wherein the third compound comprises a chromophore that absorbs light from the visible wavelength range.Type: GrantFiled: December 14, 2007Date of Patent: May 10, 2011Assignee: Xerox CorporationInventors: Jeffrey H Banning, Clifford R King, Donald R Titterington, Michael B Meinhardt
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Patent number: 7807841Abstract: Described herein are compounds that have a spiro structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of steroid hormone nuclear receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent diseases or conditions associated with the activity of steroid hormone nuclear receptors.Type: GrantFiled: February 16, 2006Date of Patent: October 5, 2010Assignee: IRM LLCInventors: Pierre-Yves Michellys, Chi Ching Mak, Wei Pei
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Patent number: 7781465Abstract: Disclosed herein is a compound represented by a formula Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: August 15, 2008Date of Patent: August 24, 2010Assignee: Allergan, Inc.Inventor: David W. Old
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Publication number: 20100105747Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.Type: ApplicationFiled: April 7, 2008Publication date: April 29, 2010Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao
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Patent number: 7659300Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: September 6, 2005Date of Patent: February 9, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump
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Publication number: 20090286988Abstract: The invention is related to a process for preparing compounds of the formula IV by means of conversion of aromatic aldehydes of the formula I using ?-ketoximes of the formula II via N-oxides of the formula III to halomethyloxazoles of the formula IV, wherein R1, R2, R3, R4, R5, R6, R7, R8, X1, X2, X3, o, n1 and n2 are as defined herein.Type: ApplicationFiled: July 27, 2009Publication date: November 19, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Wolfgang HOLLA, Rolf-Ludwig HOERLEIN, Berndt KULITZSCHER, Wolfgang LAUX, Thomas STUEDEMANN, Christoph TAPPERTZHOFEN, Robert J. H. SCHEFFER
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Patent number: 7612210Abstract: A process for the enantioselective synthesis of an (S)- or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described.Type: GrantFiled: December 4, 2006Date of Patent: November 3, 2009Assignee: WyethInventors: Paige Erin Mahaney, Madelene Miyoko Antane, Jerry Shunneng Sun
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Patent number: 7563904Abstract: In particular, this invention relates to the synthesis intermediates (IV), (V), (VI) and (VIII) useful for preparing zolmitriptanzohnitriptan or a pharmaceutically acceptable salt thereof, which includes a) Ppreparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Ttransesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Ssaponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Ddecarboxylation of the indolecarboxylic acid (VIII), to proviType: GrantFiled: November 15, 2007Date of Patent: July 21, 2009Assignee: Inke, S.A.Inventors: Pere Dalmases Barjoan, Montserrat Armengol Asparo
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Patent number: 7556797Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: GrantFiled: September 2, 2003Date of Patent: July 7, 2009Assignee: Mallinckrodt Inc.Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
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Patent number: 7541474Abstract: The invention provides a process for preparing 11 ?-hydroxy steroid dehydrogenase type 1 inhibitors of formula 2 via a catalyzed reaction between a compound of formula 1 and a compound of formula R2LG in the presence of base: where R1, R2, X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.Type: GrantFiled: November 1, 2006Date of Patent: June 2, 2009Assignee: Amgen Inc.Inventors: Emilio Bunel, Anil Guram, Qingyian Liu
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Publication number: 20090137817Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.Type: ApplicationFiled: August 25, 2008Publication date: May 28, 2009Inventors: Pierre Deslongchamps, Yves Dory, Kamel Benakli, Eric Marsault, Luc Ouellet, Mahesh Ramaseshan, Martin Vezina, Daniel Fortin, Ruoxi Lan, Shigui Li, Gerald Villeneuve, Hamid R. Hoveyda, Sylvie Beaubien, Mark L. Peterson
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20090054505Abstract: Disclosed herein is a compound represented by a formula Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 15, 2008Publication date: February 26, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
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Patent number: 7435751Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein R1 is C1-4alkyl, optionally substituted with a fluoro atom, or R1 is a cyclopropyl or cyclopropylmethyl; and R2 is methyl or ethyl. These compounds are useful as antibacterial agents.Type: GrantFiled: March 30, 2006Date of Patent: October 14, 2008Inventors: Vara Prasad Venkata Nagendra Josyula, Mikhail Gordeev, Gary Luehr
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Patent number: 7432290Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: November 24, 2004Date of Patent: October 7, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Stamos, Martin Trudeau, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Jeffrey O. Saunders
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Patent number: 7420061Abstract: Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.Type: GrantFiled: September 13, 2004Date of Patent: September 2, 2008Assignee: Pharmacia CorporationInventors: John J. Talley, James W. Malecha, Stephen Bertenshaw, Matthew J. Graneto, Jeffery S. Carter, Jinglin Li, Srinivasan R. Nagarajan, David L. Brown, Donald J. Rogier, Jr., Thomas D. Penning, Ish K. Khanna, Xiangdong Xu, Richard M. Weier
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Patent number: 7396847Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in (I) wherein C is for example wherein A and B are independently selected from R2a to R3b are independently selected from hydrogen and fluorine; R1a and R1b are independently selected from, for example, hydroxy, —NHC(?W)R4, wherein W is O or S; R4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: September 9, 2002Date of Patent: July 8, 2008Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hales, Michael Lingard Swain, Sheila Irene Hauck, Stuart Dennett Mills
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Patent number: 7378530Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.Type: GrantFiled: February 21, 2006Date of Patent: May 27, 2008Assignee: Nereus Pharmaceuticals, Inc.Inventors: Venkata Rami Reddy Macherla, Benjamin Nicholson, Kin Sing Lam
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Patent number: 7368578Abstract: The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1- or -Z1-(CH2)n— (n is an integer of 0 to 8, Z1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R2 is a hydrogen atom, a cyano group, —PO(OR9)(OR10) (R9 and R10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R9 and R10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic actiType: GrantFiled: September 9, 2003Date of Patent: May 6, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Nobuyuki Takakura, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
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Patent number: 7342035Abstract: In particular, zolmitriptan or a pharmaceutically acceptable salt thereof, which includes a) Preparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Transesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Saponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Decarboxylation of the indolecarboxylic acid (VIII), to provide zolmitriptan and, eventually, to provide a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 5, 2003Date of Patent: March 11, 2008Assignee: Inke, S.A.Inventors: Montserrat Armengol Asparo, Pere Dalmases Barjoan
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Patent number: 7273885Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: GrantFiled: April 11, 2003Date of Patent: September 25, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Janos Pitlik, Kevin M. Cottrell, Luc J. Farmer, Robert B. Perni, Lawrence F. Courtney, John H. van Drie, Mark A. Murcko
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Patent number: 7265140Abstract: The present invention relates to acyloxymethylcarbamate oxazolidinones. The compounds of the present invention have potent activity with excellent oral bioavailability against Gram-positive and Gram-negative bacteria.Type: GrantFiled: September 9, 2004Date of Patent: September 4, 2007Assignee: Pfizer IncInventors: Vara Prasad Venkata Nagendra Josyula, Robert C. Gadwood, Lisa Marie Thomasco, Ji-Young Kim, Allison Laura Choy, Frederick Earl Boyer
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Patent number: 7160912Abstract: The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their stereoisomers, their salts and pharmaceutical compositions.Type: GrantFiled: July 3, 2003Date of Patent: January 9, 2007Assignees: Dr.Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.Inventors: Natesan Selvakumar, Jagattaran Das, Sanjay Trehan, Javed Iqbal, Magadi Sitaram Kumar, Ramanujam Rajagopalan, Mamidi Naga Venkata Srinivasa Rao
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Patent number: 7129259Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having at least one halogenated hydrocarbon moiety, a biaryl moiety, and at least one heterocyclic moiety, that are useful as such agents.Type: GrantFiled: December 1, 2004Date of Patent: October 31, 2006Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Shili Chen, Jiacheng Zhou, Yusheng Wu, Deping Wang, Joseph M. Salvino, Adegboyega K. Oyelere, Rongliang Lou
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 6962936Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where Ht, R2, T, and m are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: April 26, 2002Date of Patent: November 8, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Francois Maltais
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Publication number: 20040267015Abstract: PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: September 29, 2003Publication date: December 30, 2004Inventors: Ajita Bhat, Siegfried B. Christensen, James S. Frazee, Martha S. Head, Jack D. Leber, Mei Li
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Patent number: 6821991Abstract: This invention provides compounds of Formula I having the structure wherein: A, X, Y, Z, R1, R2, R3, R4, R5, and R6 are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: May 19, 2003Date of Patent: November 23, 2004Assignee: WyethInventor: Baihua Hu
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Patent number: 6821994Abstract: A peroxisome proliferator activated receptor regulator containing a compound of formula (I) (wherein all symbols are as defined in the specification), or a salt thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.Type: GrantFiled: May 2, 2003Date of Patent: November 23, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima