The Additional Hetero Ring And The Bicyclo Ring System Are Attached Directly To The Same Acyclic Carbon Or Acyclic Carbon Chain Patents (Class 548/468)
-
Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
-
Patent number: 7399868Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: GrantFiled: September 20, 2005Date of Patent: July 15, 2008Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
-
Patent number: 7361682Abstract: The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: June 20, 2005Date of Patent: April 22, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Silvia Gatti McArthur, Cornelia Hertel, Matthias Heinrich Nettekoven, Susanne Raab, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Franz Schuler, Jean-Marc Plancher
-
Publication number: 20080051327Abstract: The present invention relates to crystals of phosphorylated Aurora-A kinase fragment alone and in complex with a ligand, amino acid residues 1-43 of human TPX2. This invention also relates to methods for designing and selecting ligands, in particular allosteric inhibitors of Aurora-A, that bind to the Aurora-A kinase and their use. Further, the present invention relates to certain indene and indole derivatives. The present invention relates to crystals of phosphorylated Aurora-A kinase alone and in complex with a ligand, amino acid residues 1-43 of human TPX2. This invention also relates to methods for designing and selecting ligands that bind to the Aurora-A kinase and their use. Further, the present invention relates to certain indene and indole derivative.Type: ApplicationFiled: October 11, 2004Publication date: February 28, 2008Applicant: EMBLInventors: Elena Conti, Richard Bayliss, Carsten Schultz, Isabelle Vernos, Teresa Sardon
-
Publication number: 20080044881Abstract: Hydroxy carboxy pyrrolyl-indolinone derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: November 26, 2004Publication date: February 21, 2008Inventor: Congxin Liang
-
Patent number: 7238723Abstract: The present invention provides eletriptan hydrobromide monohydrate of the formula (I): together with processes for preparing, uses of, and compositions containing, said monohydrate.Type: GrantFiled: February 27, 2003Date of Patent: July 3, 2007Assignee: Pfizer Inc.Inventors: Christopher Ian Dallman, Ronald James Ogilvie
-
Patent number: 7202265Abstract: The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1? position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety.Type: GrantFiled: February 24, 2004Date of Patent: April 10, 2007Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Connie Li Sun, Gerald McMahon, Klaus Peter Hirth, Laura Kay Shawver
-
Patent number: 7186709Abstract: The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.Type: GrantFiled: August 27, 2003Date of Patent: March 6, 2007Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Robert A. Stavenger, Timothy J. Mitchison, Zoltan Maliga
-
Patent number: 7179910Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: September 8, 2003Date of Patent: February 20, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu (Alan) Jin, Paul M. Herrinton, Michael A. Mauragis
-
Patent number: 7173048Abstract: The invention relates to compounds of formula (I): and pharmaceutically acceptable salts and pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5, R6, A, m, n and p are defined as in claim 1. These compounds can be used as pharmaceutical compositions for the treatment of, for example, diabetes.Type: GrantFiled: April 27, 2005Date of Patent: February 6, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Narendra Panday, Hasane Ratni, Tanja Schulz-Gasch, Matthew Blake Wright
-
Patent number: 7164030Abstract: The present invention provides an improved process for the preparation of ?-polymorphic eletriptan hydrobromide.Type: GrantFiled: June 30, 2005Date of Patent: January 16, 2007Assignee: Pfizer Inc.Inventors: Patrick Joseph Furlong, Cornelius Joseph Kelly, Ronald James Ogilvie, Vincent Ryan
-
Patent number: 7157577Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: March 8, 2004Date of Patent: January 2, 2007Assignee: Sugen Inc.Inventors: Peng Cho Tang, Congxin Liang, Todd Miller, Kenneth E. Lipson
-
Patent number: 7148249Abstract: The present invention relates to heterocyclically substituted indolinones of general formula wherein R1 to R5 and X are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: September 5, 2003Date of Patent: December 12, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Joerg Kley, Frank Hilberg, Armin Heckel, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Ulrike Tontsch-Grunt, Jacobus C. A. Van Meel
-
Patent number: 7125905Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: January 4, 2005Date of Patent: October 24, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
-
Patent number: 7119090Abstract: The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 25, 2002Date of Patent: October 10, 2006Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
-
Patent number: 7119209Abstract: The present invention refers to a process for preparing indolinone derivatives of the general formula (VI) as defined in the specification and intermediates of that process.Type: GrantFiled: February 14, 2003Date of Patent: October 10, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Qingwu Jin, Michael A. Mauragis, Paul D. May
-
Patent number: 7112603Abstract: The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: February 10, 2004Date of Patent: September 26, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Marcel Koenig
-
Patent number: 7105563Abstract: Indolinone derivatives, such as compounds of the formula (I): wherein A, m, n, R1, R2, R3, R5 and R6 are described herein, are disclosed herein as being useful in treating mammal having disease-states alleviated by the inhibition of PDK-1 activity.Type: GrantFiled: October 22, 2004Date of Patent: September 12, 2006Assignee: Schering AktiengesellschaftInventors: Damian Arnaiz, Judi Bryant, Yuo-Ling Chou, Richard Feldman, Paul Hrvatin, Imadul Islam, Monica Kochanny, Wheeseong Lee, Mark Polokoff, Hongyi Yu, Shendong Yuan
-
Patent number: 7091220Abstract: The present invention relates to substituted indole Mannich bases, processes of preparing substituted indole Mannich base, a medicament containing the same, and a pharmaceutical composition containing the same.Type: GrantFiled: December 20, 2000Date of Patent: August 15, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
-
Patent number: 7053113Abstract: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: December 24, 2003Date of Patent: May 30, 2006Assignees: Sugen, Inc., Pharmacia & Upjohn Company LLCInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Peng Cho Tang
-
Patent number: 7030214Abstract: Ureins are obtained by reaction, in basic medium, between an N?-(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.Type: GrantFiled: September 4, 2001Date of Patent: April 18, 2006Assignee: Solvay (Societe Anonyme)Inventors: Roland Callens, Georges Blondeel, Marc Anteunis, Frank Becu
-
Patent number: 7008943Abstract: The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: May 5, 2003Date of Patent: March 7, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao
-
Patent number: 6939565Abstract: The present invention is directed toward a composition comprising a compound isolated from Dysidea species sponges that is capable of inhibiting serine proteases of the coagulation cascade. In particular, this composition inhibits the TF/VIIa complex of the coagulation cascade. The invention is also directed toward methods employing this composition as a part of anticoagulant therapy.Type: GrantFiled: January 16, 2004Date of Patent: September 6, 2005Assignee: Pharmacia CorporationInventors: Gilles H. Goetz, George G. Harrigan, John J. Likos, Thomas P. Kasten
-
Patent number: 6930124Abstract: The invention relates to compounds of formula (I) in which R5 is chosen from the group consisting of: in which R2 is a C1-C3 alkyl group in which X may be Cl, Br, or F in which n is between 1 and 3, in the E or Z form, or a mixture of the two isomeric forms, possessing antimitotic, antiproliferative and antivascular properties through inhibition of the polymerization of tubulin into microtubulesType: GrantFiled: September 10, 2003Date of Patent: August 16, 2005Assignee: Aventis Pharma S. A.Inventors: Cécile Combeau, Patrick Mailliet, Marielle Chiron
-
Patent number: 6914145Abstract: The present invention is concerned with the acylation of indoles, specifically the preparation of 3-acylated indoles which may be further treated to provide indoles having an alternative substituent at the 3-position.Type: GrantFiled: July 17, 2002Date of Patent: July 5, 2005Assignee: Pfizer, Inc.Inventor: Jolyon Francis Perkins
-
Patent number: 6906093Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 3, 2001Date of Patent: June 14, 2005Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon, Klaus Peter Hirth, Laura Kay Shawver
-
Patent number: 6852751Abstract: Compounds according to the following Formula (I): are effective in treating conditions characterized by excess metalloprotease activity.Type: GrantFiled: September 18, 2002Date of Patent: February 8, 2005Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Katherine King Mieling, Kelly Michelle Solinsky, Biswanath De, Neil Gregory Almstead, Michael George Natchus, Glen Edward Mieling
-
Patent number: 6846818Abstract: The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the invention are particularly useful in the treatment or alleviation of inflammation and inflammation associated disorders, such as, for example, rheumatoid arthritis and osteoarthritis, and in the relief of pain, such as, for example, pain associated with surgery or trauma, in mammals, preferably felines and canines.Type: GrantFiled: April 16, 2003Date of Patent: January 25, 2005Assignee: Pfizer Inc.Inventors: Kristin Lundy DeMello, Brian S. Bronk, Rhonda Marie Crosson
-
Patent number: 6797725Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: April 9, 2002Date of Patent: September 28, 2004Assignee: Sugen, Inc.Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
-
Patent number: 6784167Abstract: 17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula wherein the phenyl group labeled A and the group —C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents —H or optionally substituted —(C1-C4)alkyl; n represents 0 or an integer of 1-3; and R2 represents any of a variety of substituents on ring A. R4 generally represents —H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, —OR5, or —SR5, and R5 represents —H, optionally substituted —(C1-C4)alkyl, optionally substituted -phenyl, optionally substituted —(C1-C4)alkyl-phenyl, or optionally substituted —(C1-C4)acyl. R6 represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl.Type: GrantFiled: September 28, 2001Date of Patent: August 31, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Jill E. Wood, Jeremy L. Baryza, Catherine R. Brennan, Soongyu Choi, James H. Cook, Brian R. Dixon, Paul P. Ehrlich, David E. Gunn, Ian McAlexander, Peiying Liu, Derek B. Lowe, Anikó M. Redman, William J. Scott, Yamin Wang
-
Patent number: 6750240Abstract: The present invention relates to novel synthetic methods for the preparation of indolylquinones. The methods of the present invention are directed to synthetic reactions involving indoles and halo-quinones in solvent and in the presence of a metal carbonate. The invention also relates to bis- and mono-indolylquinones of high purity and pharmaceutical compositions containing the same.Type: GrantFiled: May 3, 2000Date of Patent: June 15, 2004Assignee: Sugen, Inc.Inventors: Peng C. Tang, G. Davis Harris
-
Patent number: 6716837Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c aType: GrantFiled: November 13, 2000Date of Patent: April 6, 2004Assignee: NPS Allelix Biopharmaceuticals, Inc.Inventors: Louise Edwards, Methvin Isaac, Shawn Maddaford, Abdelmalik Slassi, Tao Xin
-
Patent number: 6716870Abstract: The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: September 16, 2002Date of Patent: April 6, 2004Assignees: Sugen, Inc., Pharmacia & Upjohn CompanyInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Marcel Koenig
-
Patent number: 6716869Abstract: The present invention is directed toward a composition comprising a compound isolated from Dysidea species sponges that is capable of inhibiting serine proteases of the coagulation cascade. In particular, this composition inhibits the TF/VIIa complex of the coagulation cascade. The invention is also directed toward methods employing this composition as a part of anticoagulant therapy.Type: GrantFiled: December 2, 2002Date of Patent: April 6, 2004Assignee: Pharmacia CorporationInventors: Gilles H. Goetz, George G. Harrigan, John J. Likos, Thomas P. Kasten
-
Patent number: 6710067Abstract: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: May 24, 2001Date of Patent: March 23, 2004Assignees: Sugen Incorporated, Pharmacia & UpJohn CompanyInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Peng Cho Tang
-
Patent number: 6699863Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: November 27, 2002Date of Patent: March 2, 2004Assignee: Allergan, Inc.Inventors: Steven W. Andrews, Jonathan J. Hebert
-
Patent number: 6693201Abstract: Photochromic chemicals consisting essentially of colored fluorescent heterocyclic fulgides are particularly suitable for optical memories. The preferred heterocyclic photochromic fulgides consist essentially of colored 2-indolyfulgides capable of excitation by ultraviolet light to fluoresce. These heterocyclic photochromic fulgides are preferably synthesized by process of (1) condensation of 1,3-dimethyl-(5-substituted)indole-2-carboxaldehyde with diethyl IV iospropylidenesuccinate as a key intermediate; followed by (2) hydrolysis; and (3) intramolecular acid anhydride formation.Type: GrantFiled: September 7, 1999Date of Patent: February 17, 2004Assignee: The Regents Of the University of CaliforniaInventors: Peter M. Rentzepis, Alexander Dvornikov
-
Patent number: 6689806Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds of the invention. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds of the invention and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.Type: GrantFiled: March 22, 2000Date of Patent: February 10, 2004Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon, Todd Anthony Miller, Shahrzad Shirazian, Chung Chen Wei, G. Davis Harris, Jr., Xiaoyuan Li, Congxin Liang
-
Patent number: 6686362Abstract: Compounds of formula (I) in which R1, R2, R3 and R4 have the meanings given in the specification, are receptor tyrosine kinase inhibitors useful in the treatment of proliferative disorders, such as cancer.Type: GrantFiled: December 20, 2002Date of Patent: February 3, 2004Assignee: Theravance, Inc.Inventors: John H. Griffin, Roger Briesewitz, Jonathan W. Wray
-
Patent number: 6677367Abstract: A compound selected from the group consisting of a compound of formula I a compound of formula II and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R1, R2, Cx, n, R3, R4, R5, Y are as defined in the specification.Type: GrantFiled: October 24, 2002Date of Patent: January 13, 2004Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Gilles Sauvé, Abderrahim Bouzide, Alexandre Coté, Gervais Bérubé, Patrick Soucy, Yongsen Zhao, Jocelyn Yelle
-
Patent number: 6653308Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 15, 2002Date of Patent: November 25, 2003Assignees: Sugen, Inc., Pharmacia & Upjohn CompanyInventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu Jin, Paul M. Herrinton, Michael A. Mauragis
-
Patent number: 6642232Abstract: The present invention relates to certain 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives that inhibit kinases, in particular VEGFR and/or PDGFR kinases. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.Type: GrantFiled: October 10, 2002Date of Patent: November 4, 2003Assignee: Sugen, Inc.Inventors: Matthew Mattson, Tomas Vojkovsky, Congxin Liang, Peng Cho Tang, Huiping Guan
-
Patent number: 6608079Abstract: The present invention relates to a compound of formula (I), or a pharmaceutical acid addition salt thereof, which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal.Type: GrantFiled: June 5, 2001Date of Patent: August 19, 2003Assignee: Eli Lilly and CompanyInventors: John Mehnert Schaus, Yao-Chang Xu
-
Patent number: 6599902Abstract: The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.Type: GrantFiled: May 30, 2002Date of Patent: July 29, 2003Assignee: Sugen, Inc.Inventors: Jingrong Cui, John Ramphal, Congxin Liang, Connie Li Sun, Chung Chen Wei, Peng Cho Tang
-
Patent number: 6573293Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 15, 2001Date of Patent: June 3, 2003Assignees: Sugen, Inc., Pharmacia & Upjohn Co.Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
-
Publication number: 20030092917Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: ApplicationFiled: February 15, 2002Publication date: May 15, 2003Applicant: SUGEN, INC.Inventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu Jin, Paul M. Herrinton, Michael A. Mauragis
-
Patent number: 6531502Abstract: The present invention relates to novel 3-methylidenyl-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 5, 2001Date of Patent: March 11, 2003Assignee: Sugen, Inc.Inventors: Pen Cho Tang, Li Sun, Todd Anthony Miller, Congxin Liang, Ngoc My Tran, Anh Thi Nguyen, Asaad Nematalla
-
Patent number: 6531612Abstract: Compounds of the formula: wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.Type: GrantFiled: December 21, 2000Date of Patent: March 11, 2003Assignee: Hoffman-La Roche Inc.Inventors: Tobias Gabriel, Michael Pech, Sabine Wallbaum
-
Patent number: 6482848Abstract: The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: May 24, 2001Date of Patent: November 19, 2002Assignee: Sugen IncorporatedInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Marcel Koenig
-
Patent number: 6451838Abstract: The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: May 24, 2001Date of Patent: September 17, 2002Assignee: Pharmacia & Upjohn companyInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao