Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/362.1)
  • Patent number: 9914707
    Abstract: The present invention relates to a naphthylamide compound of the structure as represented by formula (I), medicinal salts, prodrugs and hydrates or solvates thereof, and also relates to a method of preparing the compounds, pharmaceutical compositions comprising the compounds and the uses thereof as protein tyrosine kinase inhibitors, particularly as VEGFR-2 inhibitors, in preparing drugs for preventing and treating diseases related to abnormal angiogenesis.
    Type: Grant
    Filed: February 15, 2015
    Date of Patent: March 13, 2018
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Wenhu Duan, Jian Ding, Yongcong Lv, Hua Xie
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Patent number: 9029356
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; 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: Grant
    Filed: March 14, 2014
    Date of Patent: May 12, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20150119439
    Abstract: The invention provides saturated acyl guanidine compounds that inhibit F1F0-ATPase, and methods of using saturated acyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: April 30, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Patent number: 8987275
    Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: March 24, 2015
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael Gray, Wenjun Zhou, Xianming Deng
  • Publication number: 20150072986
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Application
    Filed: June 11, 2014
    Publication date: March 12, 2015
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
  • Patent number: 8815871
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 26, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Publication number: 20140228351
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; 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: Application
    Filed: March 14, 2014
    Publication date: August 14, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20140228378
    Abstract: The invention provides novel substituted cyclopropane carboxamide compounds according to Formula (I), their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Application
    Filed: July 7, 2012
    Publication date: August 14, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Patent number: 8802711
    Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, wherein X1, X2, X3, X4, J, K, L, X5, X6, Rb, G2, 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: Grant
    Filed: March 22, 2012
    Date of Patent: August 12, 2014
    Assignee: AbbVie Inc.
    Inventors: Arthur Gomtsyan, Jerome F. Daanen, Gregory A. Gfesser, Michael E. Kort, Chih-Hung Lee, Heath A. McDonald, Pamela S. Puttfarcken, Eric A. Voight, Philip R. Kym
  • Patent number: 8765748
    Abstract: The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: July 1, 2014
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • Patent number: 8759538
    Abstract: 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: Grant
    Filed: June 13, 2013
    Date of Patent: June 24, 2014
    Assignee: AbbVie Inc.
    Inventor: Thomas B. Borchardt
  • Patent number: 8686021
    Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.
    Type: Grant
    Filed: May 3, 2006
    Date of Patent: April 1, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
  • Publication number: 20140080807
    Abstract: The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 20, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
  • Publication number: 20140031341
    Abstract: An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.
    Type: Application
    Filed: December 19, 2011
    Publication date: January 30, 2014
    Applicants: UNIVERSITAT MUNSTER, GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Jerome Aubert, Martin Steinhoff
  • Publication number: 20130245015
    Abstract: 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: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Inventors: YUJIA DAI, STEVEN K. DAVIDSEN, ANNA M. ERICSSON, KRESNA HARTANDI, ZHIQIN JI, MICHAEL R. MICHAELIDES
  • Publication number: 20130184287
    Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
    Type: Application
    Filed: February 18, 2011
    Publication date: July 18, 2013
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael Gray, Wenjun Zhou, Xianming Deng
  • Patent number: 8486988
    Abstract: 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: Grant
    Filed: April 18, 2011
    Date of Patent: July 16, 2013
    Assignee: AbbVie Inc.
    Inventor: Thomas B. Borchardt
  • Patent number: 8461194
    Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: June 11, 2013
    Assignee: Aziende Chimiche Riunite Angelini Francesco A. C. R. A. F. S. p. A.
    Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
  • Patent number: 8436023
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: May 7, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
  • Patent number: 8394843
    Abstract: Compounds are provided which have the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture which contain such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to activate glucokinase.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: March 12, 2013
    Assignee: Takeda California, Inc.
    Inventors: Jun Feng, Stephen L. Gwaltney, Robert J. Skene, Mingnam Tang, Sheldon X. Cao, David J. Hossfield, Jeffrey A. Stafford
  • Patent number: 8357716
    Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: January 22, 2013
    Assignee: Glaxo Group Limited
    Inventors: Heather Hobbs, Simon Teanby Hodgson, Yannick Maurice LaCroix, Deborah Needham, Nigel James Parr, Panayiotis Alexandrou Procopiou, Timothy John Ritchie, Michael David Woodrow
  • Publication number: 20130018038
    Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: March 23, 2011
    Publication date: January 17, 2013
    Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
  • Patent number: 8354399
    Abstract: 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: Grant
    Filed: December 15, 2009
    Date of Patent: January 15, 2013
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Menichincheri, Jay Aaron Bertrand, Chiara Marchionni, Marcella Nesi, Paolo Orsini, Achille Panzeri
  • Patent number: 8349885
    Abstract: The present invention relates to a composition for preserving cells, tissues and organs, comprising as an active ingredient indole and indazole compounds of formula (1), or a pharmaceutically acceptable salt or isomer thereof, which are effective for preventing injury of organs, isolated cell systems or tissues caused by cold storage, transplant operation or post-transplantation reperfusion; a preservation method; and a preparation method of the composition.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: January 8, 2013
    Assignee: LG Life Sciences Ltd.
    Inventors: Soon Ha Kim, Hyoung Jin Kim, Chul Woong Chung, Heui Sul Park, Hyo Shin Kwak, Sung Ho Kim, Jin Gu Park
  • Patent number: 8304446
    Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: November 6, 2012
    Assignee: Glaxo Group Limited
    Inventors: Simon Teanby Hodgson, Yannick Maurice Lacroix, Pauayiotis Alexandron Procopiou
  • Patent number: 8299243
    Abstract: 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: Grant
    Filed: September 29, 2011
    Date of Patent: October 30, 2012
    Assignee: AbbVie Inc.
    Inventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
  • Patent number: 8299057
    Abstract: 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: Grant
    Filed: July 8, 2008
    Date of Patent: October 30, 2012
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Patent number: 8299096
    Abstract: This invention is directed to methods of preventing or treating diseases or conditions of the lungs associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.
    Type: Grant
    Filed: June 26, 2009
    Date of Patent: October 30, 2012
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: Tomas Navratil, Ward M. Peterson, John W. Lampe, Emilee H. Fulcher, Scott D. Sorensen
  • Publication number: 20120208818
    Abstract: 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: Application
    Filed: October 10, 2011
    Publication date: August 16, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
  • Patent number: 8211928
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: July 3, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rico Lavoie, Clint A. James, Edward H. Ruediger
  • Patent number: 8207210
    Abstract: 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: Grant
    Filed: June 18, 2007
    Date of Patent: June 26, 2012
    Assignee: Merck Patent GmbH
    Inventors: Markus Klein, Rolf Gericke, Norbert Beier, Florian Lang
  • Patent number: 8110572
    Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: February 7, 2012
    Assignee: Abbott Laboratories
    Inventors: Yujia Dai, Zhiqin Ji, Michael R. Michaelides
  • Publication number: 20120022253
    Abstract: 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: Application
    Filed: September 29, 2011
    Publication date: January 26, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
  • Publication number: 20120015932
    Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: February 24, 2010
    Publication date: January 19, 2012
    Inventors: Heather Hobbs, Simon Teanby Hodgson, Yannick Maurice LaCroix, Deborah Needham, Nigel James Parr, Panayiotis Alexandrou Procopiou, Timothy John Ritchie, Michael David Woodrow
  • Publication number: 20110306592
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: June 9, 2011
    Publication date: December 15, 2011
    Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
  • Patent number: 8067457
    Abstract: 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: Grant
    Filed: October 26, 2006
    Date of Patent: November 29, 2011
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
  • Publication number: 20110281843
    Abstract: 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: Application
    Filed: December 15, 2009
    Publication date: November 17, 2011
    Applicant: NERVIANO MEDICAL SCIENCES S.r.l.
    Inventors: Maria Menichincheri, Jay Aaron Bertrand, Chiara Marchionni, Marcella Nesi, Paolo Orsini, Achille Panzeri
  • Publication number: 20110237783
    Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
    Type: Application
    Filed: December 23, 2010
    Publication date: September 29, 2011
    Applicant: Valocor Therapeutics, Inc.
    Inventors: Zaihui Zhang, Timothy S. Daynard, Mikhail A. Chafeev, Shisen Wang, Gregory B. Chopiuk, Serguei V. Sviridov
  • Publication number: 20110196010
    Abstract: 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: Application
    Filed: April 18, 2011
    Publication date: August 11, 2011
    Applicant: ABBOTT LABORATORIES
    Inventor: Thomas B. Borchardt
  • Patent number: 7994208
    Abstract: 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: Grant
    Filed: October 15, 2008
    Date of Patent: August 9, 2011
    Assignee: Abbott Laboratories
    Inventor: Thomas B. Borchardt
  • Patent number: 7968583
    Abstract: Substituted pyrrolo-pyrazole 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 dysregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: June 28, 2011
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Sten Christian Orrenius, Ettore Perrone, Italo Beria, Daniele Fancelli, Arturo Galvani
  • Patent number: 7960564
    Abstract: 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: Grant
    Filed: October 15, 2008
    Date of Patent: June 14, 2011
    Assignee: Abbott Laboratories
    Inventors: Thomas B. Borchardt, Michael J. Rozema
  • Patent number: 7956185
    Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 7, 2011
    Assignee: Abbott Laboratories
    Inventors: Robert B. Diebold, Stevan W. Djuric, Vincent L. Giranda, Laura A. Hexamer, Nan-Horng Lin, Julie M. Miyashiro, Thomas D. Penning, Magdalena Przytulinska, Thomas J. Sowin, Gerard M. Sullivan, Zhi-Fu Tao, Yunsong Tong, Anil Vasudevan, Le Wang, Keith W. Woods, Zhiren Xia, Henry Q. Zhang
  • Patent number: 7947843
    Abstract: 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: Grant
    Filed: October 15, 2008
    Date of Patent: May 24, 2011
    Assignee: Abbott Laboratories
    Inventors: Thomas B. Borchardt, Michael J. Rozema, Shailendra V. Bordawekar, Alexander F. Chu-Kung
  • Patent number: 7943651
    Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament, particularly for the treatment of inflammation and/or allergic conditions.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: May 17, 2011
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Anthony William James Cooper, David House, Iain McFarlane McLay
  • Patent number: 7943782
    Abstract: 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: Grant
    Filed: October 15, 2008
    Date of Patent: May 17, 2011
    Assignee: Abbott Laboratories
    Inventor: Rodger F. Henry
  • Publication number: 20110112161
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Application
    Filed: October 13, 2010
    Publication date: May 12, 2011
    Inventors: David Robert Bolin, Matthew Michael Hamilton, Lee Apostle McDermott, Lin Yi
  • Publication number: 20110065702
    Abstract: The present invention is directed to a compound is represented by Structural Formula (A):or a pharmaceutically acceptable salt therof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 19, 2008
    Publication date: March 17, 2011
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • Patent number: 7884126
    Abstract: The invention relates to novel indazole derivatives as cited in claim 1, which are inhibitors of CHK1, CHK2 and SGK kinases and can be used to treat cancer and other diseases.
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: February 8, 2011
    Assignee: Merck Patent GmbH
    Inventors: Markus Klein, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang