Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/362.1)
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Patent number: 7872039Abstract: Novel 3-aminoindazoles of the formula (I) are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibrosis and inflammatory processes of any type.Type: GrantFiled: April 4, 2005Date of Patent: January 18, 2011Assignee: Merck Patent GesellschaftInventors: Dieter Dorsch, Lars Thore Burgdorf, Rolf Gericke, Norbert Beier, Werner Mederski, Florian Lang
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Publication number: 20100292207Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 8, 2008Publication date: November 18, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Patent number: 7799930Abstract: Methods of making 1-alkylindazoles are described. The methods involve reacting a 2-alkylaminobenzonitrile with a nitrosating agent followed by reduction-cyclization of the resulting nitrosamine to form a 1-alkyl-3-aminoindazole. The 1-alkyl-3-aminoindazole can be deaminated to form a 1-alkylindazole which ultimately can be used to form desired indazoles which are preferably pharmaceutically active products. The process of the present invention further permits the formation of enantiomerically enriched or pure indazoles such as aminoalkyl indazoles.Type: GrantFiled: February 10, 2009Date of Patent: September 21, 2010Assignee: Alcon, Inc.Inventors: Pete Delgado, Raymond E. Conrow, W. Dennis Dean
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Publication number: 20100216860Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: February 24, 2010Publication date: August 26, 2010Inventors: Simon Teanby Hodgson, Yannick Maurice Lacroix, Pauayiotis Alexandron Procopiou
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Patent number: 7781454Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein V, W, X, Y, Z, R1, R2, R4, R5, R6, ring A, ring B, j and k are defined herein. The compounds of Formula I, and the pharmaceutically acceptable salts and prodrugs thereof, are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: December 6, 2007Date of Patent: August 24, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Neville J. Anthony, Robert Gomez
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Patent number: 7772404Abstract: N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N?-(2-fluoro-5-methylphenyl)urea Crystalline Form 2, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed.Type: GrantFiled: October 15, 2008Date of Patent: August 10, 2010Assignee: Abbott LaboratoriesInventors: Thomas B. Borchardt, Alexander F. Chu-Kung
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Publication number: 20100197665Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).Type: ApplicationFiled: December 14, 2007Publication date: August 5, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Marcella Nesi, Ettore Perrone, Roberto Bossi, Paolo Polucci
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Patent number: 7763624Abstract: The present invention relates to compounds of Formula I or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treatments using the compounds, for example, protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders and methods of preparing medicaments comprising the compounds.Type: GrantFiled: August 18, 2006Date of Patent: July 27, 2010Assignee: Amgen Inc.Inventors: John L. Buchanan, William H. Buckner, Mario G. Cardozo, Erin F. DiMauro, Jiasheng Fu, Xiaolin Hao, Xian Yun Jiao, Frank Kayser, David J. Kopecky, Craig E. Masse, Susan A. Tomlinson, Ryan White, Xiaotian Zhu
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Patent number: 7759344Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as c-Met mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: January 9, 2008Date of Patent: July 20, 2010Assignee: Amgen Inc.Inventors: Shon Booker, Noel D'Angelo, Julie Germain, Jean-Christophe Harmange, Tae-Seong Kim, Michele Potashman
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Publication number: 20100144793Abstract: The present invention relates to compounds of the general formula (I) wherein (formula 2) independently represents a single bond or a double bond, represents a linking group A and A? are each independently a 5- to 7-membered heterocyclic ring, wherein the heterocyclic rings A und A? are optionally substituted by one or more substituents, selected from C1-6 alkyl, C3-6 cycloalkyl, optionally substituted phenyl, optionally substituted heteroaryl, C1-4 alkylene-(optionally substituted phenyl) and C1-4 alkylene-(optionally substituted heteroaryl), or two substituents may be joined to form an optionally substituted, saturated, unsaturated or aromatic 5- to 7-membered ring which is fused with the heterocyclic ring A or A?, and wherein the heterocyclic rings A und A? may contain in addition to the units X, X?, Y and Y? one or more heteroatoms, selected from N, NR, S and Ol wherein R is selected from H and C1-4 alkyl; the units X and X? are each independently a H-bond acceptor; and the units Y and Y? are each indepenType: ApplicationFiled: November 23, 2007Publication date: June 10, 2010Applicant: AC IMMUNE SAInventors: Wolfgang Froestl, Nampally Sreenivasachary, Sophie Lohmann, Maria Pilar Lopez Deber, Andreas Muhs, Maria Pihlgren Bosch
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Publication number: 20100137360Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: October 15, 2009Publication date: June 3, 2010Applicant: ABBOTT LABORATORIESInventors: Arthur R. Gomtsyan, Eric A. Voight, Erol K. Bayburt, Jun Chen, Jerome F. Daanen, Stanley DiDomenico, Michael E. Kort, Philip R. Kym, Heath A. McDonald, Richard J. Perner, Robert G. Schmidt
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Publication number: 20100056573Abstract: 2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.Type: ApplicationFiled: November 19, 2007Publication date: March 4, 2010Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri, Rosella Ombrato, Lorenzo Polenzani
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Publication number: 20090286784Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: July 22, 2009Publication date: November 19, 2009Applicant: ABBOTT LABORATORIESInventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Publication number: 20090253767Abstract: Novel aminoindazolylurea derivatives of the formula I (I), in which R1, R2, R3, R4, R5, X and Y have the meanings indicated in Claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: ApplicationFiled: June 18, 2007Publication date: October 8, 2009Inventors: Markus Klein, Rolf Gericke, Norbert Beier, Florian Lang
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Publication number: 20090197884Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: August 6, 2009Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20090163497Abstract: The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: June 25, 2009Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Publication number: 20090149659Abstract: Methods of making 1-alkylindazoles are described. The methods involve reacting a 2-alkylaminobenzonitrile with a nitrosating agent followed by reduction-cyclization of the resulting nitrosamine to form a 1-alkyl-3-aminoindazole. The 1-alkyl-3-aminoindazole can be deaminated to form a 1-alkylindazole which ultimately can be used to form desired indazoles which are preferably pharmaceutically active products. The process of the present invention further permits the formation of enantiomerically enriched or pure indazoles such as aminoalkyl indazoles.Type: ApplicationFiled: February 10, 2009Publication date: June 11, 2009Applicant: Alcon, Inc.Inventors: Pete Delgado, Raymond E. Conrow, W. Dennis Dean
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Publication number: 20090143376Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: March 3, 2006Publication date: June 4, 2009Applicant: Sitris Pharmaceuticals, Inc.Inventors: Michael Milburn, Jill Milne, Jean Bemis, Joseph J. Nunes, Roger Xie, Karl D. Nomington, Chi B. Vu
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Publication number: 20090124816Abstract: N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N?-(2-fluoro-5-methylphenyl)urea Crystalline Form 2, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed.Type: ApplicationFiled: October 15, 2008Publication date: May 14, 2009Applicant: Abbott LaboratoriesInventor: Thomas B. Borchardt
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Publication number: 20090124815Abstract: N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N?-(2-fluoro-5-methylphenyl)urea Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed.Type: ApplicationFiled: October 15, 2008Publication date: May 14, 2009Applicant: ABBOTT LABORATORIESInventor: Thomas B. Borchardt
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Publication number: 20090118344Abstract: N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N?-(2-fluoro-5-methylphenyl)urea Hydrate Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed.Type: ApplicationFiled: October 15, 2008Publication date: May 7, 2009Applicant: ABBOTT LABORATORIESInventor: Thomas B. Borchardt
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Publication number: 20090105486Abstract: N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N?-(2-fluoro-5-methylphenyl)urea Tolueneate Crystalline Form 1, ways to make it and ways to use it are disclosed.Type: ApplicationFiled: October 15, 2008Publication date: April 23, 2009Applicant: ABBOTT LABORATORIESInventor: Rodger F. Henry
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Publication number: 20090105326Abstract: N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N?-(2-fluoro-5-methylphenyl)urea·¼ Ethanolate Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it is disclosed.Type: ApplicationFiled: October 15, 2008Publication date: April 23, 2009Applicant: ABBOTT LABORATORIESInventor: Rodger F. Henry
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Patent number: 7517901Abstract: Compounds of formula Ia or Ib: wherein X and Y are nitrogen or CRe, and R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the subject compounds and methods of using the compounds for treatment of p38-mediated diseases.Type: GrantFiled: August 23, 2006Date of Patent: April 14, 2009Assignee: Roche Palo Alto LLCInventors: Tobias Gabriel, Michael Soth
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Publication number: 20090054430Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: ApplicationFiled: July 16, 2008Publication date: February 26, 2009Applicant: Abbott LaboratoriesInventors: Yujia Dai, Ji Zhiqin, Michael R. Michaelides
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Publication number: 20090036508Abstract: Compounds of the formula I in which X, Y, R1, R2, R3 and R4 have the meanings indicated in claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: January 10, 2007Publication date: February 5, 2009Inventors: Markus Klein, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang
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Publication number: 20090036449Abstract: Novel squaric acid compounds of the formula (I), in which R, R1, R2, R2?, R2?, R3, B, B? and X have the meanings indicated in Claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be used for the treatment of diseases and complaints such as cancer, diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.Type: ApplicationFiled: March 21, 2006Publication date: February 5, 2009Inventors: Werner Mederski, Rolf Gericke, Markus Klein, Dieter Dorsch, Norbert Beier, Florian Lang
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Publication number: 20080287516Abstract: The present invention relates to phenyl-substituted pyrrolidones and compounds related to phenyl-substituted pyrrolidones. One use of these compounds is for the inhibition of viruses, e.g., HIV. The invention further relates to methods of malting these compounds, methods of identifying the efficacy of these compounds, and methods of using these compounds to inhibit or prevent HIV infection and related disease states such as AIDS.Type: ApplicationFiled: January 30, 2006Publication date: November 20, 2008Applicant: IRM LLCInventors: Baogen Wu, Truc Ngoc Nguyen, David Archer Ellis, Xiaohui He, Beth Marie Anaclerio, Kunyong Yang, Ha-soon Choi, Zhicheng Wang, Thomas H. Marsilje, Yun He
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Patent number: 7449585Abstract: Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).Type: GrantFiled: November 12, 2004Date of Patent: November 11, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Frank Burkamp, Stephen Robert Fletcher
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Publication number: 20080234268Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as c-Met mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 9, 2008Publication date: September 25, 2008Applicant: Amgen Inc.Inventors: Shon Booker, Noel D'Angelo, Julie Germain, Jean-Christophe Harmange, Tae-Seong Kim, Michele Potashman
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Publication number: 20080194557Abstract: This invention relates to methods of treating, managing and preventing pain, inflammation, cancer, and ocular diseases and disorders, and to compounds and pharmaceutical compositions useful in such methods.Type: ApplicationFiled: January 17, 2008Publication date: August 14, 2008Inventors: Joseph Barbosa, Simon D.P. Baugh, Qiang Han, Victoria K. Lombardo, Huy Van Nguyen, Praveen K. Pabba, Kristen M. Terranova
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Patent number: 7390803Abstract: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.Type: GrantFiled: October 24, 2003Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Sander G. Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen D. Goble
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Publication number: 20080119648Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Patent number: 7365211Abstract: This invention relates to a method for modulating ?2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to said heterocyclic compounds and pharmaceutical compositions containing said compounds.Type: GrantFiled: August 11, 2004Date of Patent: April 29, 2008Assignee: Roche Palo Alto LLCInventors: Xao-Fa Lin, David Garrett Loughhead, Sanja Novakovic, Counde O'Yang, Michael Soth, David George Putman
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Patent number: 7321045Abstract: The present invention describes novel compounds of the formula: (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: February 2, 2004Date of Patent: January 22, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
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Publication number: 20070281922Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: May 31, 2007Publication date: December 6, 2007Applicant: WyethInventors: Kevin Liu, Jennifer Rebecca Lo, Albert Jean Robichaud, Hassan Mahmoud Elokdah
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Patent number: 7297709Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: May 10, 2004Date of Patent: November 20, 2007Assignee: Abbott LaboratoriesInventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Patent number: 7214699Abstract: This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein R3 is optionally substituted aryl or heteroaryl, R1 and R2 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.Type: GrantFiled: December 1, 2003Date of Patent: May 8, 2007Assignee: Roche Palo Alto LLCInventors: Richard Leo Cournoyer, David Garrett Loughhead, Counde O'Yang
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Patent number: 7166629Abstract: 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 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, 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: January 23, 2007Assignee: Aventis Pharma S.A.Inventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney
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Patent number: 7138418Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: October 5, 2001Date of Patent: November 21, 2006Assignee: Amgen, Inc.Inventors: John Flygare, Julio C. Medina, Bei Shan, David L. Clark, Terry J. Rosen
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Patent number: 7102001Abstract: The present invention provides a process for preparing compounds of formula (I) or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: GrantFiled: December 9, 2004Date of Patent: September 5, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Shankar Swaminathan, Ashvinikumar V. Gavai, Junying Fan, Bharat P. Patel, Derek J. Norris, Richard Michael Corbett, Bin Zheng
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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
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Patent number: 7015233Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.Type: GrantFiled: June 12, 2003Date of Patent: March 21, 2006Assignee: Abbott LaboratoriesInventors: Arthur Gomtsyan, Erol K. Bayburt, John R. Koenig, Chih-Hung Lee
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Patent number: 7001905Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: GrantFiled: March 12, 2001Date of Patent: February 21, 2006Assignee: Warner-Lambert CompanyInventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
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Patent number: 6933390Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.Type: GrantFiled: July 15, 2004Date of Patent: August 23, 2005Assignee: Warner-Lambert CompanyInventors: Hubert Barth, Klaus Steiner, Simon Schneider, Ulrich Bayer, Manfred Westermayer, Ulrike Wolfsperger, Hans-Jürgen Betche
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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
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Patent number: 6858638Abstract: Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particlar in oncology.Type: GrantFiled: March 11, 2003Date of Patent: February 22, 2005Assignee: Aventis Pharma S.A.Inventors: Dominique Damour, Jean-Christophe Carry, Patrick Nemecek, Corinne Terrier, Frederico Nardi, Bruno Filoche, Marie-Pierre Cherrier, Daniel Bezard
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Patent number: 6855722Abstract: The present invention relates to novel substituted indole compounds that are antagonists of alpha V (?v) integrins, for example ?v?3 and ?v?5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by ?v?3 and ?v?5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.Type: GrantFiled: January 29, 2002Date of Patent: February 15, 2005Assignee: Dimensional Pharmaceuticals, Inc.Inventors: Tianbo Lu, Louis V. LaFrance, Thomas P. Markotan, Juan J. Marugan Sanchez, Victor J. Marder, David C. U'Prichard, Beth M. Anaclerio, Zihong Guo, Wenzi Pan, Kristi A. Leonard, Bruce E. Tomczuk
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Patent number: 6794518Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: December 17, 1999Date of Patent: September 21, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
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Patent number: 6762189Abstract: The present invention relates to novel 5-pyrimidinecarboxamide derivatives and the pharmaceutical compositions containing said derivatives, and more specifically, to 5-pyrimidinecarboxamide derivatives and their pharmacutically able salts, the process for preparing them, and the pharmaceutical compositions containing said compounds as active ingredients. In particular, said 5-pyrimidinecarboxamide derivatives of the present invention, due to their inhibitory activity against the proliferation of human immunodeficiency virus (HIV) as well as hepatitis B virus (HBV), can be used as a therapeutic agent as well as a preventive agent for hepatitis B and acquired immune deficiency syndrome (AIDS).Type: GrantFiled: May 24, 2002Date of Patent: July 13, 2004Assignee: Dong Wha Pharm. Ind. Co., Ltd.Inventors: Sung June Yoon, Sang Wook Lee, Nam Doo Kim, Yong Kyun Park, Geun Hyung Lee, Jong Woo Kim, Sang Jin Park, Hee Jeoung Park, Hwan Bong Jang