Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/354)
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Publication number: 20090197888Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis c virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis c virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: December 4, 2008Publication date: August 6, 2009Inventors: YONGHUA GAI, Yat Sun Or, Zhe Wang
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Patent number: 7538109Abstract: The invention relates to quinoxalinone derivatives of general Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.Type: GrantFiled: April 26, 2004Date of Patent: May 26, 2009Assignee: Actelion Pharmaceuticals LtdInventors: Hamed Aissaoui, Martine Clozel, Thomas Weller, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20090123423Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: May 14, 2009Inventors: Yonghua Gai, Yat Sun Or, Zhe Wang
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Publication number: 20090111807Abstract: An object of the present invention is to synthesize a novel 1,2,3,4-tetrahydroquinoxaline derivative represented by formula (1) and to find a pharmacological action of the derivative. In the formula, the R1 represents a halogen, an alkyl, cycloalkyl, aryl or heterocyclic group, or the like; p represents 0 to 5; R2 represents a halogen, an alkyl, hydroxyl or alkoxy group, or the like; q represents 0 to 2; R3 represents hydrogen, an alkyl, alkenyl, alkylcarbonyl or arylcarbonyl group, or the like; R4 and R5 independently represent hydrogen, a halogen, an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, or the like; R6 represents hydrogen, an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, or the like; A represents an alkylene; R7 represents OR8, NR8R9, SR8, S(O)R8, S(O)2R8; and X represents O or S.Type: ApplicationFiled: March 14, 2007Publication date: April 30, 2009Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Mamoru Matsuda, Toshiyuki Mori, Kenji Kawashima, Minoru Yamamoto, Masatomo Kato, Miwa Takai, Masato Nagatsuka, Sachiko Kobayashi
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Publication number: 20090062280Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: ApplicationFiled: March 9, 2007Publication date: March 5, 2009Inventors: James B. Doherty, Min Shu, Dong-Ming Shen, Fengqi Zhang
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Publication number: 20090054417Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activation of steroid hormone nuclear receptors.Type: ApplicationFiled: July 28, 2005Publication date: February 26, 2009Applicant: IRM LLCInventors: Pierre-Yves Michellys, H. Michael Petrassi, Wendy Richmond, Wei Pei
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Publication number: 20090048445Abstract: There is disclosed a method of synthesizing a quinoxaline derivative in which toxicity, corrosiveness and permeation are low and which is excellent in safety and which attains a reduced reaction time, a greatly improved yield and excellent economical efficiency. The object is achieved by a method of synthesizing a quinoxaline derivative which comprises adsorbing a benzofuroxan derivative and a ?-diketone derivative on a solid support, and then heating the derivatives in a solid state by microwave irradiation to dehydrocyclize them.Type: ApplicationFiled: October 16, 2006Publication date: February 19, 2009Inventors: Toru Takabatake, Hiroaki Saito, Yusuke Sumiyoshi
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Publication number: 20090042881Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, s, R1, R2, R3, Q, X and Y have defined meanings.Type: ApplicationFiled: November 18, 2004Publication date: February 12, 2009Inventors: Dominique Jean-Pierre Mabire, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20080318963Abstract: The present invention relates to novel quinoxaline-piperazine compounds, 1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives and their pharmaceutically acceptable salts, a process for their preparation thereof, and compositions containing such compounds. Therapeutic methods for the treatment of hyperproliferative disorders, including cancers, by administering quinoxalin-piperazine compounds are also included.Type: ApplicationFiled: October 18, 2005Publication date: December 25, 2008Applicants: REXAHN PHARMACEUTICALS, INC., KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Young-Dae Gong, Moon-Kook Jeon, Dong-Su Kim, Jae Yang Kong, Gun-Do Kim, Chang-Ho Ahn, Young Bok Lee
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Publication number: 20080287449Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: November 20, 2008Inventors: Deqiang Niu, Yat Sun Or, Zhe Wang
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Publication number: 20080267918Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: October 30, 2008Inventors: Yonghua Gai, Yat Sun Or, Zhe Wang
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Publication number: 20080269228Abstract: The present invention relates to novel hydrazide-containing compounds of Formula I or Formula II, including pharmaceutically acceptable salts, esters, or prodrugs thereof which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 26, 2007Publication date: October 30, 2008Inventors: JOEL D. MOORE, ERIC L. ELLIOTT, YAT SUN OR, ZHE WANG
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Publication number: 20080255109Abstract: Compounds according to general formula 1, wherein A1-A3 are selected from A5 and A6 where A5 is either ?CR13— or ?N— and A6 is —NR14—, —O— or —S—; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1-A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1-A3 must be A5; R1 is selected from H, NHY? and COY2, in which case R2 is H, or R1 and R2 may both be methyl or together represent ?O; R3, R4 and R5 are each independently selected from H and lower alkyl groups; R6, R7, R8, R9, R10, R11 and R12 are each independently selected from H, lower alkyl groups, NH2, halogens (F, Cl and Br) O-alkyl, CH2NM2 and CF3; R13 is selected from H, F, Cl, Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF3; R14 is selected from H, methyl and ethyl; W is selected from ?CH— and ?N—; X is selected from CH2, O, S, SO2, NH and N-lower alkyl; Y1 is selected from CO-lower alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH2)bNHCOY3, where b is 1-3; Y2 is selected from OR15, NR16R17 and NH(CH2)cCOY3,Type: ApplicationFiled: April 28, 2008Publication date: October 16, 2008Inventors: Michael Bryan Roe, Andrzej Roman Batt, David Michael Evans, Gary Robert William Pitt, David Philip Rooker
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Publication number: 20080255130Abstract: The present invention discloses bicyclic nitrogen-containing heterocyclic compounds for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.Type: ApplicationFiled: April 9, 2008Publication date: October 16, 2008Inventors: Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrei Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov, Jeffrey Chisholm
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Publication number: 20080249099Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4, R5, R6 and X have defined meanings.Type: ApplicationFiled: November 18, 2004Publication date: October 9, 2008Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Dominique Jean-Pierre Mabire, Jerome Emile Georges Guillemont, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20080249101Abstract: This invention relates to compounds of the formula wherein A, R1 to R3 are as defined in the specification and G is benzoimidazole, quinoxaline, benzotriazole, dihydro-imidazo[4,5-c]pyridine and dihydro-isoindolone group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: March 24, 2008Publication date: October 9, 2008Inventors: Konrad Bleicher, Andreas D. Christ, Rainer E. Martin, Peter Mohr
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Patent number: 7432270Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3; m represents 1, 2, or 3; p represents ) or 1; X is NR, wherein R is H or (C1-4)alkyl; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; any of which may be optionally substituted; A2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R1 represents hydrogen, optionally substituted (C1-4)alkoxy, halo, cyano, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclyl group containing up to 4 hetType: GrantFiled: May 2, 2002Date of Patent: October 7, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Patent number: 7432264Abstract: Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain.Type: GrantFiled: August 9, 2004Date of Patent: October 7, 2008Assignee: Isis Pharmaceuticals, Inc.Inventors: Elizabeth Anne Jefferson, Eric E. Swayze, Punit P. Seth, Dale E. Robinson, Jr.
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Publication number: 20080234250Abstract: The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.Type: ApplicationFiled: August 18, 2005Publication date: September 25, 2008Inventor: Gary Robert William Pitt
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Publication number: 20080161292Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: December 27, 2007Publication date: July 3, 2008Applicant: Abbott LaboratoriesInventors: Vincent L. Giranda, Julie M. Miyashiro, Thomas D. Penning, Keith W. Woods
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Patent number: 7368445Abstract: The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds.Type: GrantFiled: February 16, 2005Date of Patent: May 6, 2008Assignee: Eli Lilly and CompanyInventors: Hong-Yu Li, William Thomas McMillen, Yan Wang
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Publication number: 20080039470Abstract: The present invention discloses compounds of formulae I and II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: August 11, 2006Publication date: February 14, 2008Inventors: Deqiang Niu, Joel D. Moore, Dong Liu, Yonghua Gai, Zhigang Chen, Yat Sun Or, Zhe Wang
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Patent number: 7294716Abstract: Synthetic methods for preparing isomerically pure N-arylsulfonyl derivatives of proton pump inhibitors which include a substituted benzimidazole nucleus are shown by the synthetic schemes and experimental description.Type: GrantFiled: July 13, 2004Date of Patent: November 13, 2007Assignee: Allergan, Inc.Inventors: Michael E. Garst, Lloyd Jay Dolby, Shervin Esfandiari, Vivian Rose MacKenzie, Alfred Arthur Avey, Jr., David Charles Muchmore, Geoffrey Kenneth Cooper, Thomas C. Malone
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Patent number: 7259161Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: November 4, 2003Date of Patent: August 21, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Randy S. Bethiel, Mark Ledeboer
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Patent number: 7244722Abstract: Compounds of the general formula (I): wherein m, n, R1, R2, R3 and R4 are as described in the specification. Further included are pharmaceutical compositions comprising the compounds, processes for their preparation, as well as the use of the compounds for the preparation of a medicament for the treatment of 5-HT2A receptor-related disorders or medical conditions.Type: GrantFiled: July 17, 2003Date of Patent: July 17, 2007Assignee: Biovitrum ABInventors: Magnus Cernerud, Helena Lundström, Björn M Nilsson, Markus Thor
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Patent number: 7205408Abstract: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.Type: GrantFiled: January 22, 2002Date of Patent: April 17, 2007Assignee: SmithKline Beecham, p.l.c.Inventors: David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, William Miller, Neil David Pearson
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Patent number: 7183281Abstract: Disclosed are sulfonylquinoxalone derivatives of the general formula: These compounds are useful as bradykinin antagonists.Type: GrantFiled: May 2, 2003Date of Patent: February 27, 2007Assignee: Elan Pharmaceuticals, Inc.Inventors: Francine S. Grant, Sarah Bartulis, Louis Brogley, Michael S. Dappen, Ramesh Kasar, Mohammed A. Khan, Martin Neitzel, Michael A. Pleiss, Eugene D. Thorsett, John Tucker, Michael Ye, Jon E. Hawkinson
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Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Patent number: 7148224Abstract: The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wn is —(CH2)n— (n is zero to four), R1, is H or optionally substituted lower alkyl, etc., R2 is H, etc., R3 and R4 are the same or different and are each H, etc., R5 and R6 are the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.Type: GrantFiled: April 14, 2005Date of Patent: December 12, 2006Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Hayama, Nobuhiko Kawanishi, Tooru Takaki
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7094784Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in theType: GrantFiled: January 21, 2004Date of Patent: August 22, 2006Assignee: Schering CorporationInventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Patent number: 7071180Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are asType: GrantFiled: June 22, 2004Date of Patent: July 4, 2006Assignee: Biovitrum ABInventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
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Patent number: 7030125Abstract: Novel isothiazole and isoxazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.Type: GrantFiled: September 17, 2003Date of Patent: April 18, 2006Assignee: Pfizer, Inc.Inventors: Michael J. Munchhof, Laura C. Blumberg
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Patent number: 6995154Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: October 21, 2003Date of Patent: February 7, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
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Patent number: 6989384Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.Type: GrantFiled: July 23, 2003Date of Patent: January 24, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Ye Hua, Hiep The Luu, Fora P. Chan, Theodore O. Johnson, Jr., Siegfried Heinz Reich, Donald James Skalitzky, Yi Yang, Thomas F. Hendrickson, Shao Song Chu, Brian Walter Eastman
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Patent number: 6943170Abstract: This invention relates generally to N-cycloalkylglycines of the Formula (I): or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits including the same, methods for using the same for treating viral infection or an assay standards or reagents, and intermediates and processes for making the same.Type: GrantFiled: October 30, 2003Date of Patent: September 13, 2005Assignee: Bristol-Myers Squibb CompanyInventor: David J. Carini
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Patent number: 6927214Abstract: Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.Type: GrantFiled: January 14, 2000Date of Patent: August 9, 2005Assignee: Novo Nordisk A/SInventors: Min Teng, Larry Kenneth Truesdale, Dilip Bhumralkar, Dan Kiel, Michael D. Johnson, Christine Thomas, Anker Steen Jorgensen, Peter Madsen, Preben Houlberg Olesen, Liselotte Bjerre Knudsen, Ingrid Vivika Petterson, Johannes Cornelis de Jong, Carsten Behrens, Janos Tibor Kodra, Jesper Lau
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Patent number: 6914062Abstract: The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wn is —(CH2)n— (n is zero to four), R1 is H or optionally substituted lower alkyl, etc., R2 is H, etc., R3 and R4 are the same or different and are each H, etc., R5 and R6 are the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.Type: GrantFiled: June 28, 2001Date of Patent: July 5, 2005Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Hayama, Nobuhiko Kawanishi, Tooru Takaki
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Patent number: 6908921Abstract: 2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: July 7, 2003Date of Patent: June 21, 2005Assignee: Merck & Co., Inc.Inventors: Dai-Shi Su, Mark G. Bock
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Patent number: 6897312Abstract: A method for producing ? crystals of ethyl (R)-2-[4-(6-chloro-2-quinoxalin-2-yloxy)phenoxy]propionate, which is characterized by heating ? crystals, or ? crystals and ? crystals, within a range of from 50° C. to lower than the melting point of the ? crystals.Type: GrantFiled: December 4, 2001Date of Patent: May 24, 2005Assignee: Nissan Chemical Industries, Ltd.Inventors: Masami Yasukawa, Shinji Kuwahara
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Patent number: 6890926Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: July 20, 2001Date of Patent: May 10, 2005Assignee: Zentaris AGInventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Patent number: 6852712Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.Type: GrantFiled: February 4, 2003Date of Patent: February 8, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
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Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze
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Patent number: 6846815Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.Type: GrantFiled: February 3, 2003Date of Patent: January 25, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael R. Myers, Alfred P. Spada, Paul E. Persons, Martin P. Maguire
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Publication number: 20040224954Abstract: The invention relates to substituted (1H)quinoxalin-2-one compounds, methods for production thereof, medicaments containing said compounds and the use of said compounds for the production of medicaments. The invention further relates to substituted 4-aryl- and 4-heteroarylcyclohexane compounds and methods for production thereof.Type: ApplicationFiled: April 26, 2004Publication date: November 11, 2004Inventors: Michael Sattlegger, Helmut Buschmann, Michael Przewosny, Werner Englberger, Babette-Yvonne Koegel, Hans Schick
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Patent number: 6815442Abstract: The present invention provides 1H-quinoxalinones, of the formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, and n are as defined herein. Also disclosed are pharmaceutical compositions comprising such compounds, and methods for using the compounds to increase the therapeutic efficacy of drugs.Type: GrantFiled: March 25, 2003Date of Patent: November 9, 2004Assignee: The Penn State Research FoundationInventors: Charles D. Smith, David S. Lawrence
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Patent number: 6777413Abstract: Novel compounds of general formula I: including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivative having activity against mammalian factor Xa is described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.Type: GrantFiled: February 1, 2001Date of Patent: August 17, 2004Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20040152707Abstract: Novel compounds of the formula 1Type: ApplicationFiled: January 21, 2004Publication date: August 5, 2004Inventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Publication number: 20040147520Abstract: Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists.Type: ApplicationFiled: May 2, 2003Publication date: July 29, 2004Inventors: Francine S. Grant, Sarah Bartulis, Louis Brogley, Michael S. Dappen, Ramesh Kasar, Mohammed A. Khan, Martin Neitzel, Michael A. Pleiss, Eugene D. Thorsett, John Tucker, Michael Ye, Jon E. Hawkinson
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Publication number: 20040147519Abstract: Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists.Type: ApplicationFiled: May 2, 2003Publication date: July 29, 2004Inventors: Francine S. Grant, Sarah Bartulis, Louis Brogley, Michael S. Dappen, Ramesh Kasar, Ryan Holcomb, Michael A. Pleiss, Eugene D. Thorsett, Michael Ye, Jon E. Hawkinson