Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/225)
  • Patent number: 9434694
    Abstract: The invention discloses a method for the preparation of medetomidine starting from 1-bromo 2,3-dimethylbenzene and chloroacetone.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: September 6, 2016
    Assignee: Lonza Ltd.
    Inventors: Florencio Zaragoza Doerwald, Anna Kulesza, Stephan Elzner, Robert Bujok, Zbigniew Wrobel, Krzysztof Wojciechowski
  • Publication number: 20150099889
    Abstract: The invention discloses a method for the preparation of medetomidine starting from 1-bromo 2,3-dimethylbenzene and chloroacetone.
    Type: Application
    Filed: November 15, 2012
    Publication date: April 9, 2015
    Inventors: Florencio Zaragoza Doerwald, Anna Kulesza, Stephen Elzner, Robert Bujok, Zbigniew Wrobel, Krzysztof Wojciechowski
  • Patent number: 8829002
    Abstract: 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: Grant
    Filed: December 13, 2011
    Date of Patent: September 9, 2014
    Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
  • Patent number: 8822516
    Abstract: 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: Grant
    Filed: June 9, 2011
    Date of Patent: September 2, 2014
    Assignee: Technion Research & Development Foundation Limited
    Inventors: Gennady Nisnevich, Mark Gandelman, Kseniya Kulbitski
  • Patent number: 8759383
    Abstract: 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: Grant
    Filed: March 14, 2008
    Date of Patent: June 24, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger Tung
  • Patent number: 8673941
    Abstract: 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: Grant
    Filed: July 30, 2009
    Date of Patent: March 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
  • Publication number: 20130281366
    Abstract: 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: Application
    Filed: December 26, 2011
    Publication date: October 24, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
  • Publication number: 20130267536
    Abstract: 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: Application
    Filed: December 13, 2011
    Publication date: October 10, 2013
    Applicant: ALLA CHEM, LLC
    Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
  • Patent number: 8420680
    Abstract: 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: Grant
    Filed: June 30, 2008
    Date of Patent: April 16, 2013
    Assignees: 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
  • Patent number: 8329706
    Abstract: 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: Grant
    Filed: May 11, 2010
    Date of Patent: December 11, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, Romain Siegrist, Thierry Sifferlen, Jodi T Williams
  • Publication number: 20120302607
    Abstract: 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: Application
    Filed: August 2, 2012
    Publication date: November 29, 2012
    Applicant: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Patent number: 8222425
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: July 17, 2012
    Assignee: Novartis AG
    Inventors: 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
  • Publication number: 20120129830
    Abstract: 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: Application
    Filed: May 11, 2010
    Publication date: May 24, 2012
    Applicant: SANOFI
    Inventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
  • Publication number: 20120101111
    Abstract: 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: Application
    Filed: May 11, 2010
    Publication date: April 26, 2012
    Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, Romain Siegrist, Thierry Sifferlen, Jodi T. Williams
  • Patent number: 8158186
    Abstract: 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: Grant
    Filed: December 19, 2008
    Date of Patent: April 17, 2012
    Assignee: Evonik Degussa GmbH
    Inventors: Christoph Kobler, Philipp Roth, Christoph Weckbecker, Klaus Huthmacher
  • Patent number: 8124633
    Abstract: 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: Grant
    Filed: April 7, 2008
    Date of Patent: February 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao
  • Patent number: 8119813
    Abstract: 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: Grant
    Filed: November 12, 2009
    Date of Patent: February 21, 2012
    Assignee: sanofi-aventis
    Inventors: Antony Bigot, Maxime Lampilas
  • Publication number: 20110275802
    Abstract: 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: Application
    Filed: November 26, 2009
    Publication date: November 10, 2011
    Applicant: BAYER MATERIALSCIENCE AG
    Inventors: Frank Richter, Reinhard Halpaap
  • Patent number: 8048901
    Abstract: 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: Grant
    Filed: July 10, 2007
    Date of Patent: November 1, 2011
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Jochen Goerlitzer, Heiner Glombik, Eugen Falk, Dirk Gretzke, Stefanie Keil, Hans-Ludwig Schaefer, Christian Stapper, Wolfgang Wendler
  • Patent number: 8003803
    Abstract: 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: Grant
    Filed: April 11, 2007
    Date of Patent: August 23, 2011
    Assignee: Schering Corporation
    Inventors: Yan Xia, Samuel Chackalamannil
  • Patent number: 8003678
    Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: August 23, 2011
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Patent number: 7939678
    Abstract: 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: Grant
    Filed: December 14, 2007
    Date of Patent: May 10, 2011
    Assignee: Xerox Corporation
    Inventors: Jeffrey H Banning, Clifford R King, Donald R Titterington, Michael B Meinhardt
  • Patent number: 7807841
    Abstract: 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: Grant
    Filed: February 16, 2006
    Date of Patent: October 5, 2010
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Chi Ching Mak, Wei Pei
  • Patent number: 7781465
    Abstract: Disclosed herein is a compound represented by a formula Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: August 24, 2010
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Publication number: 20100105747
    Abstract: 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: Application
    Filed: April 7, 2008
    Publication date: April 29, 2010
    Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao
  • Patent number: 7659300
    Abstract: 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: Grant
    Filed: September 6, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump
  • Publication number: 20090286988
    Abstract: 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: Application
    Filed: July 27, 2009
    Publication date: November 19, 2009
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Wolfgang HOLLA, Rolf-Ludwig HOERLEIN, Berndt KULITZSCHER, Wolfgang LAUX, Thomas STUEDEMANN, Christoph TAPPERTZHOFEN, Robert J. H. SCHEFFER
  • Patent number: 7612210
    Abstract: 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: Grant
    Filed: December 4, 2006
    Date of Patent: November 3, 2009
    Assignee: Wyeth
    Inventors: Paige Erin Mahaney, Madelene Miyoko Antane, Jerry Shunneng Sun
  • Patent number: 7563904
    Abstract: 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 provi
    Type: Grant
    Filed: November 15, 2007
    Date of Patent: July 21, 2009
    Assignee: Inke, S.A.
    Inventors: Pere Dalmases Barjoan, Montserrat Armengol Asparo
  • Patent number: 7556797
    Abstract: 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: Grant
    Filed: September 2, 2003
    Date of Patent: July 7, 2009
    Assignee: Mallinckrodt Inc.
    Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
  • Patent number: 7541474
    Abstract: 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: Grant
    Filed: November 1, 2006
    Date of Patent: June 2, 2009
    Assignee: Amgen Inc.
    Inventors: Emilio Bunel, Anil Guram, Qingyian Liu
  • Publication number: 20090137817
    Abstract: 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: Application
    Filed: August 25, 2008
    Publication date: May 28, 2009
    Inventors: 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
  • Patent number: 7511149
    Abstract: 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: Grant
    Filed: February 9, 2007
    Date of Patent: March 31, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
  • Publication number: 20090054505
    Abstract: Disclosed herein is a compound represented by a formula Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: August 15, 2008
    Publication date: February 26, 2009
    Applicant: ALLERGAN, INC.
    Inventor: David W. Old
  • Patent number: 7435751
    Abstract: 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: Grant
    Filed: March 30, 2006
    Date of Patent: October 14, 2008
    Inventors: Vara Prasad Venkata Nagendra Josyula, Mikhail Gordeev, Gary Luehr
  • Patent number: 7432290
    Abstract: 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: Grant
    Filed: November 24, 2004
    Date of Patent: October 7, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Stamos, Martin Trudeau, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Jeffrey O. Saunders
  • Patent number: 7420061
    Abstract: Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.
    Type: Grant
    Filed: September 13, 2004
    Date of Patent: September 2, 2008
    Assignee: Pharmacia Corporation
    Inventors: 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
  • Patent number: 7396847
    Abstract: 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: Grant
    Filed: September 9, 2002
    Date of Patent: July 8, 2008
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Neil James Hales, Michael Lingard Swain, Sheila Irene Hauck, Stuart Dennett Mills
  • Patent number: 7378530
    Abstract: 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: Grant
    Filed: February 21, 2006
    Date of Patent: May 27, 2008
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Venkata Rami Reddy Macherla, Benjamin Nicholson, Kin Sing Lam
  • Patent number: 7368578
    Abstract: 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 acti
    Type: Grant
    Filed: September 9, 2003
    Date of Patent: May 6, 2008
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yu Momose, Nobuyuki Takakura, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
  • Patent number: 7342035
    Abstract: 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: Grant
    Filed: August 5, 2003
    Date of Patent: March 11, 2008
    Assignee: Inke, S.A.
    Inventors: Montserrat Armengol Asparo, Pere Dalmases Barjoan
  • Patent number: 7273885
    Abstract: 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: Grant
    Filed: April 11, 2003
    Date of Patent: September 25, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Janos Pitlik, Kevin M. Cottrell, Luc J. Farmer, Robert B. Perni, Lawrence F. Courtney, John H. van Drie, Mark A. Murcko
  • Patent number: 7265140
    Abstract: 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: Grant
    Filed: September 9, 2004
    Date of Patent: September 4, 2007
    Assignee: Pfizer Inc
    Inventors: Vara Prasad Venkata Nagendra Josyula, Robert C. Gadwood, Lisa Marie Thomasco, Ji-Young Kim, Allison Laura Choy, Frederick Earl Boyer
  • Patent number: 7160912
    Abstract: 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: Grant
    Filed: July 3, 2003
    Date of Patent: January 9, 2007
    Assignees: 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
  • Patent number: 7129259
    Abstract: 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: Grant
    Filed: December 1, 2004
    Date of Patent: October 31, 2006
    Assignee: Rib-X Pharmaceuticals, Inc.
    Inventors: Shili Chen, Jiacheng Zhou, Yusheng Wu, Deping Wang, Joseph M. Salvino, Adegboyega K. Oyelere, Rongliang Lou
  • Patent number: 7105556
    Abstract: 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: Grant
    Filed: May 22, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Yoon Jeon, Wei Wang
  • Patent number: 6962936
    Abstract: 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: Grant
    Filed: April 26, 2002
    Date of Patent: November 8, 2005
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Francois Maltais
  • Publication number: 20040267015
    Abstract: PDF inhibitors and novel methods for their use are provided.
    Type: Application
    Filed: September 29, 2003
    Publication date: December 30, 2004
    Inventors: Ajita Bhat, Siegfried B. Christensen, James S. Frazee, Martha S. Head, Jack D. Leber, Mei Li
  • Patent number: 6821994
    Abstract: 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: Grant
    Filed: May 2, 2003
    Date of Patent: November 23, 2004
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
  • Patent number: 6821991
    Abstract: 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: Grant
    Filed: May 19, 2003
    Date of Patent: November 23, 2004
    Assignee: Wyeth
    Inventor: Baihua Hu