Additional Hetero Ring Attached Directly Or Indirectly To The Quinazoline Ring System By Nonionic Bonding Patents (Class 514/266.2)
-
Patent number: 7081460Abstract: The invention is directed to novel quinazoline and quinazoline-like derivatives of Formula (I): useful as integrin antagonists and methods for the treatment of integrin-mediated disorders.Type: GrantFiled: April 5, 2002Date of Patent: July 25, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: William J. Hoekstra, Edward C. Lawson, Michael J. Costanzo
-
Patent number: 7074800Abstract: The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1–3 heteroatoms selected independently from O, N and S; Z is —O—, —NH—, —S—, —CH2— or a direct bond; n is 0–5; m is 0–3; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein X1 and R5 are as defined herein; R1 represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N—C1-4alkylcarbamoyl, N,N-di(C1-4alkylcarbamoyl, aminosulphonyl, N—C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N—(C1-4alkylsulphonyl)amino, N—(C1-4alkylsulphType: GrantFiled: February 8, 2000Date of Patent: July 11, 2006Assignee: AstraZeneca ABInventors: Elaine S E Stokes, Darren Mckerrecher, Laurent F A Hennequin, Patrick Ple
-
Patent number: 7060705Abstract: The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: November 1, 2002Date of Patent: June 13, 2006Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, William F. Hoffman
-
Patent number: 7053215Abstract: Compounds are provided that have the formula: where X, A4, Ra, R1, R2, R3, R4, R14, L and Q are as described herein. These compounds are useful, for example, as modulators of a chemokine receptor and for treatment of inflammatory and immunoregulatory disorders and diseases. Pharmaceutical compositions and methods of using these compounds for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes, are also provided.Type: GrantFiled: August 29, 2002Date of Patent: May 30, 2006Assignee: Amgen SF, LLCInventors: Julio C. Medina, Michael G. Johnson, An-Rong Li, Jiwen Liu, Alan Xi Huang, Liusheng Zhu, Andrew P. Marcus
-
Patent number: 7045526Abstract: The present invention relates to compounds of formula I: wherein R1, R2, and R3 have the meanings indicated in the specification, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases such as cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses, or atherosclerosis. Compounds of formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for the preparation of compounds of formula I, methods of therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, and pharmaceutical compositions which comprise at least one compound of formula I.Type: GrantFiled: October 1, 2003Date of Patent: May 16, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel
-
Patent number: 7034033Abstract: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.Type: GrantFiled: May 23, 2003Date of Patent: April 25, 2006Assignee: Chiron CorporationInventors: Rustum S. Boyce, Natalia Aurrecoechea, Daniel Chu, Aaron Smith, Bryan Chang
-
Patent number: 7022678Abstract: In accordance with the present invention, there is provided pregabalin lactose conjugate compounds. Also provided as part of the present invention is a novel method of central nervous system disorders or diseases including seizure disorders, pain, depression, anxiety, sleep disorders, consumptive disorders, psychosis, tardive dyskinesia, Huntington's disease, or Parkinson's disease in a subject by administering to the subject a pharmaceutically effective amount of a pregabalin lactose conjugate.Type: GrantFiled: January 28, 2002Date of Patent: April 4, 2006Assignee: Warner-Lambert CompanyInventors: Timothy Robert Hurley, Michael James Lovdahl, Brian Tobias
-
Patent number: 7022849Abstract: Quinazoline and pyrido[2,3-d]pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, L, Y1, Y2, Y3 and Z are as described herein, are provided which are useful in treating T-cell mediated diseases.Type: GrantFiled: June 17, 2002Date of Patent: April 4, 2006Assignee: Bristol-Myers Squibb Co.Inventors: William J. Pitts, Joseph Barbosa
-
Patent number: 7019011Abstract: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.Type: GrantFiled: September 4, 2003Date of Patent: March 28, 2006Assignee: Aventis Pharma S.A.Inventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney, Gilles Tiraboschi
-
Patent number: 7001910Abstract: The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.Type: GrantFiled: November 15, 2000Date of Patent: February 21, 2006Assignee: Vita-Invest S.A.Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Elisabet De Ramon Amat
-
Patent number: 7001904Abstract: The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2, R3 and R5 is hydrogen or (1-6C)alkyl, provides that one of the parts of groups R2 and R4 together, R3 and R4 together and R5 and R4 together forms a bond; R6 is an optionally substituted group selected from (2-6C) alkenyl, (2-6C) alkynyl, (3-7C)cycloalkyl and (3-7C) cycloalkenyl, or R6 is a substituted (1-6C) alkyl group; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-bloodedType: GrantFiled: June 19, 2001Date of Patent: February 21, 2006Assignee: AstraZeneca ABInventor: Jeffrey Philip Poyser
-
Patent number: 6962922Abstract: A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N?X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.Type: GrantFiled: October 11, 2002Date of Patent: November 8, 2005Assignee: Warner-Lambert Company LLCInventors: Bernard Gaudilliere, Henri Jacobelli, Joseph Armand Picard, Michael William Wilson
-
Patent number: 6949535Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: GrantFiled: October 30, 2003Date of Patent: September 27, 2005Assignee: ICOS CorporationInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
-
Patent number: 6936619Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, wherein R1 represents C1-4 alkyl; R2 represents halo, C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyloxy, —SO2(C1-4 alkyl), optionally substituted C1-4 alkyloxy, Het or —OHet; R3 represents a bicyclic group of the formula ?wherein X and Y are selected from C and N, provided that at least one is C; Ring A together with X and Y represents a 5- or 6-membered aromatic ring containing 0, 1, 2 or 3 nitrogen atoms in the ring; n is), 1 or 2 L represents a direct link, C1-4 alkylene or C1-4 alkoxyalkylene; R4 represents H, —NR5R6, C3-6 cycloalkyl, —OR7, Het1 or Het4; R5 and R6 are independently selected from H, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-4 alkylene, —SO2(C1-4 alkyl) and optionally substituted C1-4 alkyl R7 is selected from H, C1-4 alkyl, C1-4 alkoxyalkyl, C3-6cycloalkyl, Het2 and C1-4alkyl-Het3; R8 is H or C1-4 alkyl; Het, Het1, Het2 and Het3 independently represent an optionally substituted 4 to 7 membered saturatType: GrantFiled: March 12, 2003Date of Patent: August 30, 2005Assignee: Pfizer, Inc.Inventors: Julian Blagg, Michael Jonathan Fray, Mark Llewellyn Lewis, John Paul Mathias, Mark Henryk Stefaniak, Alan Stobie
-
Patent number: 6921766Abstract: There is provided a preventive or therapeutic agent for diseases accompanied by abnormal vascular function in which lipid deposition in the blood vessel is involved, said agent comprising a chymase inhibitor as an active ingredient. As the chymase inhibitor, a quinazoline derivative represented by the following formula is used. In the above formula, the ring A represents an aromatic ring.Type: GrantFiled: November 1, 2000Date of Patent: July 26, 2005Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Harukazu Fukami, Hidenori Urata
-
Patent number: 6919338Abstract: The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6alkyl; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2, R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed.Type: GrantFiled: June 21, 2001Date of Patent: July 19, 2005Assignee: AstraZeneca ABInventors: Andrew Mortlock, Frederic Jung
-
Patent number: 6911446Abstract: The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the invention describes methods of preventing and treating serine/threonine protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to quinazoline compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: January 26, 2001Date of Patent: June 28, 2005Assignee: Sugen, Inc.Inventors: Peng C. Tang, Gerald McMahon, Heinz Weinberger, Bernhard Kutscher, Harald App
-
Patent number: 6906070Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: August 8, 2001Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
-
Patent number: 6903096Abstract: The invention is directed to methods to inhibit TGF-? and/or p38-? kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar? is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.Type: GrantFiled: October 5, 2001Date of Patent: June 7, 2005Assignee: Scios, Inc.Inventors: Sarvajit Chakravarty, Sundeep Dugar, John J. Perumattam, George F. Schreiner, David Y. Liu, John A. Lewicki
-
Patent number: 6900226Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.Type: GrantFiled: August 27, 2001Date of Patent: May 31, 2005Assignee: Hoffman-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Philippe Guerry, Matthias Heinrich Nettekoven, Philippe Pflieger
-
Patent number: 6900219Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.Type: GrantFiled: April 4, 2003Date of Patent: May 31, 2005Assignee: CV Therapeutics, Inc.Inventors: Prabha Ibrahim, Michael Campbell, Robert Jiang, Christopher Morrison, Kevin Shenk, William Shirley, Jeff Zablocki, Dmitry Koltun, Reina Natero
-
Patent number: 6900220Abstract: This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X—Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: January 2, 2002Date of Patent: May 31, 2005Assignee: Syntex (U.S.A.) LLCInventors: Cyrus Kephra Becker, Joan Marie Caroon, Chris Richard Melville, Fernando Padilla, Jürg Roland Pfister, Xiaoming Zhang
-
Patent number: 6897214Abstract: The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.Type: GrantFiled: May 2, 2002Date of Patent: May 24, 2005Assignee: Zeneca LimitedInventors: Andrew John Barker, Craig Johnstone
-
Patent number: 6890930Abstract: Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, Z, and m have the meaning indicated in patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists.Type: GrantFiled: September 13, 2000Date of Patent: May 10, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Werner Mederski, Maria Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, Guido Melzer, Bertram Cezane, Dalijit Dhanoa, Bao-Ping Zhoa, James Rinker, Mark Player, Richard Soll, Ralf Devant
-
Patent number: 6890924Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.Type: GrantFiled: June 18, 2001Date of Patent: May 10, 2005Assignee: Pfizer IncInventors: John Charles Kath, Joel Morris, Samit Kumar Bhattacharya
-
Patent number: 6867201Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3 and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.Type: GrantFiled: August 22, 2002Date of Patent: March 15, 2005Assignee: Pfizer IncInventors: John Charles Kath, Norma Jacqueline Tom, Eric David Cox, Samit Kumar Bhattacharya
-
Patent number: 6852720Abstract: A compound selected from those of formula (I): wherein: R1, R2, R3 are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as inhibitors of phosphosdiesterase-7.Type: GrantFiled: March 27, 2003Date of Patent: February 8, 2005Assignee: Pfizer Inc.Inventors: Fabrice Vergne, Patrick Bernardelli, Edwige Lorthiois, Pierre Ducrot
-
Publication number: 20040259886Abstract: This invention relates to methods, pharmaceutical compositions and kits useful in promoting bone formation and/or preventing bone loss and lowering blood cholesterol. The compositions are comprised of an estrogen agonist/antagonist as a first active component and a statin as a second active component and a pharmaceutically acceptable vehicle, carrier or diluent. The compositions and methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with estrogen administration.Type: ApplicationFiled: May 6, 2004Publication date: December 23, 2004Applicant: Pfizer IncInventors: Wesley W. Day, Andrew G. Lee, David D. Thompson
-
Publication number: 20040254203Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: ApplicationFiled: July 20, 2004Publication date: December 16, 2004Applicant: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, Gustave Bergnes, Whitney W. Smith, John C. Chabala, Bainian Feng
-
Patent number: 6831085Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.Type: GrantFiled: November 28, 2000Date of Patent: December 14, 2004Assignee: Cytokinetics, Inc.Inventors: Gustave Bergnes, Whitney W. Smith, John C. Chabala
-
Publication number: 20040248890Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: March 3, 2004Publication date: December 9, 2004Inventors: Jesus E. Gonzalez, Dean Mitchell Wilson, Andreas Peter Termin, Peter Diederik Jan Grootenhuis, Yulian Zhang, Benjamin John Petzoldt, Lev Tyler Dewey Fanning, Timothy Donald Neubert, Roger Tung, Esther Martinborough, Nicole Zimmermann
-
Publication number: 20040242574Abstract: The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl), R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro, X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or hetrocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may containType: ApplicationFiled: November 3, 2003Publication date: December 2, 2004Applicants: ZENECA LIMITED, ZENECA PHARMA S.A.Inventors: Andrew Peter Thomas, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
-
Publication number: 20040242602Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I 1Type: ApplicationFiled: February 10, 2004Publication date: December 2, 2004Inventors: Timur Gungor, John K. Dickson
-
Publication number: 20040229860Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I 1Type: ApplicationFiled: January 27, 2004Publication date: November 18, 2004Inventors: Ashvinikumar V. Gavai, Roy J. Vaz, John K. Dickson, Jacques Y. Roberge, Wu Yang, Timur Gungor, James R. Corte, David P. Rotella, Yufeng Wang
-
Publication number: 20040224946Abstract: The invention relates to 4-substituted quinoline compounds of general formula: 1Type: ApplicationFiled: March 26, 2004Publication date: November 11, 2004Applicant: Aventis Pharma S.A.Inventors: Antony Bigot, Youssef El-Ahmad, Jean-Luc Malleron, Jean-Paul Martin, Serge Mignani, Guy Pantel, Baptiste Ronan, Michel Tabart, Michel Cheve, Fabrice Viviani
-
Publication number: 20040220188Abstract: The present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) for the treatment and/or prevention of diabetes type I and/or II, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity and polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel alkylidene pyrazolidinedione derivatives. (I) R1 and R2 represent independently from each other an unsubstituted or substituted aryl or heteroaryl.Type: ApplicationFiled: May 21, 2004Publication date: November 4, 2004Inventors: Agnes Bombrun, Thomas Rueckle, Dominique Swinnen, Jerome Gonzalez, Dennis Church
-
Publication number: 20040220174Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I:Type: ApplicationFiled: May 20, 2004Publication date: November 4, 2004Inventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
-
Publication number: 20040214808Abstract: The present application describes linear chain substituted monocyclic and bicyclic compounds and derivatives thereof of Formula I:Type: ApplicationFiled: March 16, 2004Publication date: October 28, 2004Inventor: Donald J. Pinto
-
Publication number: 20040214820Abstract: The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation.Type: ApplicationFiled: December 31, 2003Publication date: October 28, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GmbHInventors: Heinz-Werner Kleemann, Jean-Christophe Carry, Pascal Desmazeau, Serge Mignani, Jean Bouoquerel, Arielle Genevois-Borella, Baptiste Ronan
-
Publication number: 20040214828Abstract: This invention pertains to methods for controlling invertebrate pests comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula (I) wherein B is O, S or NR1; J is a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5; and R1, R2, R4, R5 and n are as defined in the disclosure. This invention also pertains to certain compounds of Formula (I) and compositions for controlling invertebrate pests comprising a biologically effective amount of a compound of Formula (I) and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents and optionally further comprising an effective amount of at least one additional biologically active compound or agent.Type: ApplicationFiled: February 26, 2004Publication date: October 28, 2004Inventor: Thomas Paul Selby
-
Publication number: 20040214841Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.Type: ApplicationFiled: November 5, 2002Publication date: October 28, 2004Inventors: Laurent Francois Andre Hennequin, Patrick Ple
-
Publication number: 20040209904Abstract: Compounds having the formula (I), 1Type: ApplicationFiled: April 15, 2004Publication date: October 21, 2004Inventors: James Patrick Dunn, David Michael Goldstein, Christoph Martin Stahl, Teresa Alejandra Trejo-Martin
-
Publication number: 20040209863Abstract: The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula I:Type: ApplicationFiled: March 16, 2004Publication date: October 21, 2004Inventors: Donald J. Pinto, Jennifer X. Qiao, Timur Gungor, Patrick Y.S. Lam, Yun-Long Li
-
Patent number: 6806274Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.Type: GrantFiled: January 7, 2002Date of Patent: October 19, 2004Assignee: AstraZeneca UK LimitedInventors: Graham C Crawley, Laurent F A Hennequin, Darren McKerrecher, Patrick Ple, Jeffrey Philip Poyser, Christine M P Lambert
-
Publication number: 20040204431Abstract: This invention provides compounds that are useful for treating patients having a TGF-&bgr;-mediated disease, particularly an ALK5-mediated disease.Type: ApplicationFiled: March 8, 2004Publication date: October 14, 2004Applicant: Millennium Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Anjali Pandey, Meenakshi S. Venkatraman
-
Publication number: 20040204417Abstract: The invention concerns compounds of general formula (1), wherein, in particular; W represents H, SO2R5. CO(CH2)nR5, (CH2)nR6, CS(CH2)nR5; X represents S or NH; Y represents (CH2)p, CO, (CH2)pCO, CH═CH—CO; Z represents a hetcrocycle, imidazole, benzimidazole, isoxazole, tetrazole, oxadiazole, thiadazole, pyridine, quinazoline, quinoxaline, quinoline, thiophene; R1 represents COOR6, CONR6R7, CO—NH—CH(R6)—COOR7, CH2NR6R7, CH2OR6, (CH2)pR6, CH═CHR6; R2 represents in particular hydrogen, C1-C10 alkyl, a substituted or unsubstituted phenyl; R5 and R6 represents hydrogen, C1—C6 alkyl; R5 represents a substituted or unsubstituted phenyl or naphthyl; R6 and R7, identical or different, represent hydrogen, C1—C15 alkyl, a hetcrocycle. an aryl; n represents 0 to 10; p represents 1 to 6.Type: ApplicationFiled: May 20, 2004Publication date: October 14, 2004Inventors: Michel Perez, Marie Lamothe, Bridget Hill, Chantal Etievant
-
Patent number: 6800620Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K&dgr;) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K&dgr; plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K&dgr;, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K&dgr; activity, including compounds that selectively inhibit PI3K&dgr; activity. Methods of using PI3K&dgr; inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K&dgr; inhibitory compounds to inhibit PI3K&dgr;-mediated processes in vitro and in vivo.Type: GrantFiled: January 6, 2003Date of Patent: October 5, 2004Assignee: ICOSInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
-
Publication number: 20040192704Abstract: This invention relates to novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I.Type: ApplicationFiled: March 23, 2004Publication date: September 30, 2004Applicant: Roche Palo Alto LLCInventors: James Patrick Dunn, Steven Swallow, Zachary Kevin Sweeney
-
Patent number: 6797710Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.Type: GrantFiled: June 20, 2002Date of Patent: September 28, 2004Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
-
Patent number: RE39096Abstract: An effective treatment for skin disorders characterized by abnormal skin cell behavior, including a pharmaceutically effective amount of Halofuginone. Skin disorders which can be treated include keloids, hypertrophic scars, psoriasis, acne, seborrhea and alopecia. Halofuginone can reduce or eliminate clinical symptoms of these disorders, as well as substantially prevent the formation of keloids and hypertrophic scars.Type: GrantFiled: April 3, 2003Date of Patent: May 16, 2006Assignee: Hadasit Medical Research Services and Development Company LTDInventors: Mark Pines, Arnon Nagler