Nitrogen Bonded Directly At 2- And 4-positions Patents (Class 544/291)
  • Patent number: 11124487
    Abstract: This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: September 21, 2021
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Gregory Chin, Richard L. Mackman, Michael R. Mish, Jeff Zablocki
  • Patent number: 10370342
    Abstract: This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: August 6, 2019
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Gregory Chin, Richard L. Mackman, Michael R. Mish, Jeff Zablocki
  • Publication number: 20150126492
    Abstract: The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 7, 2015
    Applicant: NOVARTIS AG
    Inventors: Michael Dechantsreiter, Jonathan E. Grob, Aengus Macsweeney, Wolfgang Miltz, Stefan Andreas Randl, Richard Sedrani, Holger Sellner, Finton Sirockin, Eric Valeur
  • Publication number: 20150080409
    Abstract: Embodiments of the present disclosure, in one aspect, relate to a 2,4-diaminoquinazoline compound, pharmaceutical compositions including a 2,4-diaminoquinazoline compound, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
    Type: Application
    Filed: October 31, 2014
    Publication date: March 19, 2015
    Applicant: University of South Florida (A Florida Non-Profit Corporation)
    Inventors: Roman Manetsch, Lindsey Neil Shaw, Kurt Steven Van Horn, Whittney Nicole Burda
  • Publication number: 20150057263
    Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 26, 2015
    Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
  • Publication number: 20140363588
    Abstract: Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Aiko YAMAMOTO, Satoshi TANAKA, Teruki NIORI, Masato NAGURA, Masaki NORO, Aiko YOSHIDA, Nobutaka FUKAGAWA, Yasukazu KUWAYAMA
  • Patent number: 8865708
    Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: October 21, 2014
    Assignees: California Institute of Technology, The University of Kansas, Cleave Biosciences, Inc.
    Inventors: Raymond J. Deshaies, Tsui-Fen Chou, Frank J. Schoenen, Kelin Li, Kevin J. Frankowski, Jeffrey Aube, Samuel W. Gerritz, Han-Jie Zhou
  • Patent number: 8859571
    Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: October 14, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp
  • Publication number: 20140294764
    Abstract: This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods of generating epigenetically altered cells comprising mixing isolated cells with compositions disclosed herein under conditions such that epigenetically altered cells are formed. In certain embodiments, the disclosure contemplates inducing cells, such as adult somatic cells or cells that are not naturally pluripotent, into cells with chemically induce pluripotency. In certain embodiments, the disclosure contemplates certain compounds disclosed herein, compounds disclosed herein optionally substituted with one or more substituents, derivatives, or salts thereof, for these purposes.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 2, 2014
    Applicants: ISTITUTO PASTEUR - FONDAZIONE CENCI BOLOGNETTI, EMORY UNIVERSITY
    Inventors: Young-Sup Yoon, Xiaodong Cheng, Ji Woong Han, Antonello Mai
  • Patent number: 8716476
    Abstract: A process for preparing alfuzosin or a salt thereof comprising: (a) condensing 4-amino-2-chloro-6,7-dimethoxyquinazoline with 3-methylaminopropionitrile in the presence of a polar aprotic solvent selected from the group consisting of diglyme, dimethyl formamide, t-butanol, hexamethylphosphoramide or mixtures thereof to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine (b) hydrogenating the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine using a hydrogenating agent under a pressure of less than 10 kg/cm2 to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine and optionally converting the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine to an acid addition salt thereof; and (c) converting tetrahydrofuroic acid to an intermediate form and condensing the intermediate form with the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine or with the acid addition salt to yield alfuzosin base, and optionally converting alfuzosin base to a
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: May 6, 2014
    Assignee: Cipla Limited
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Dilip Birari
  • Publication number: 20140080848
    Abstract: A series of mono- and di-substituted quinazoline and pyrimidine derivatives based on the skeleton of erlotinib (an EGFR inhibitor) were synthesized and their bioactivities against hepatocellular carcinoma and human lung adenocarcinoma were evaluated.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Applicants: National Taiwan University, National Yang-Ming University
    Inventors: Chung-Wai SHIAU, Kuen-Feng CHEN
  • Publication number: 20140073642
    Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.
    Type: Application
    Filed: May 18, 2012
    Publication date: March 13, 2014
    Applicant: Janssen R&D Ireland
    Inventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
  • Patent number: 8658652
    Abstract: The present invention provides combinations of active agents, such combinations comprising one or more antifolate compounds. The particularly can include methotrexate and one or more further antifolate compounds. In specific embodiments, the combinations are useful for treating certain conditions, such as rheumatoid arthritis. The invention also provides articles useful to provide the combinations in desirable dosage forms and combinations. The combinations further may be useful in the treatment of further conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: February 25, 2014
    Assignee: Chelsea Therapeutics, Inc.
    Inventors: Michael J. Roberts, Gerry Rowse
  • Publication number: 20130296327
    Abstract: The present invention relates to substituted heterocyclic compounds of Formula I or XI: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.
    Type: Application
    Filed: July 8, 2013
    Publication date: November 7, 2013
    Inventors: Jincong Zhuo, Thomas P. Maduskuie, Ding-quan Qian, Wenqing Yao
  • Publication number: 20130261139
    Abstract: Disclosed is a use of a quinazoline compound of Formula I having 2,4-diaminoquinazoline as a parent nucleus in preparation of a medicament for treating diseases caused by flaviviridae infection, especially a use in combating Hepatitis C virus infection and Dengue fever virus infection.
    Type: Application
    Filed: December 2, 2011
    Publication date: October 3, 2013
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Jianping Zuo, Youhong Hu, Wei Tang, Bo Chao, Xiankun Tong, Dewen Li, Feihong Ji, Peilan He
  • Patent number: 8530653
    Abstract: The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GAR, FPGS, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: September 10, 2013
    Assignee: Chelsea Therapeutics, Inc.
    Inventor: Michael J. Roberts
  • Patent number: 8471011
    Abstract: A process for the preparation of an acid addition salt of an organic base comprising exposing the organic base in solid form to a gaseous acid, with the proviso that ziprasidone, its acid addition salts and intermediates thereof are excluded.
    Type: Grant
    Filed: June 29, 2005
    Date of Patent: June 25, 2013
    Assignee: Apotex PharmaChem Inc.
    Inventors: Allan W. Rey, Lotfi Derdour, K. S. Keshava Murthy, Probal Kanti Datta, Martin Ehlert, Stephen E. Horne
  • Patent number: 8426590
    Abstract: The present invention relates to a process for the preparation of doxazosin or salts thereof.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: April 23, 2013
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Dilip Ramdas Birari
  • Publication number: 20130029942
    Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Application
    Filed: October 4, 2012
    Publication date: January 31, 2013
    Applicant: Myrexis, Inc.
    Inventor: Myrexis, Inc.
  • Patent number: 8309562
    Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: November 13, 2012
    Assignee: Myrexis, Inc.
    Inventors: Mark B. Anderson, J. Adam Willardsen, Warren S. Weiner, Ashantai Yungai, Robert J. Halter, Yevgeniya Klimova, Kazuyuki Suzuki, Matthew Reeder
  • Publication number: 20120197016
    Abstract: Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADR?1 receptors, and determining based on the binding interaction of the test agent with the ADR?1 receptors whether the test agent is an effective ADR?1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADR?1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.
    Type: Application
    Filed: October 21, 2011
    Publication date: August 2, 2012
    Applicant: THE PROCTER & GAMBLE COMPANY
    Inventors: Leo Timothy Laughlin, II, Tomohiro Hakozaki, Wenzhu Zhao, Jiazhen Wang, John Crist Bierman
  • Publication number: 20120136014
    Abstract: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.
    Type: Application
    Filed: June 2, 2011
    Publication date: May 31, 2012
    Applicant: TRIUS THERAPEUTICS, INC.
    Inventors: Zhiyong Chen, Christopher J. Creghton, Mark Cunningham, John Finn, Mark Hilgers, Michael Jung, Lucy Aguirre Kohnen, Thanh Lam, Xiaoming Li, Mark Stidham, Les Tari, Michael Trzoss, Junhu Zhang
  • Publication number: 20120095006
    Abstract: This invention relates to the use of certain cyclic guanosine 3?,5?-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.
    Type: Application
    Filed: December 16, 2011
    Publication date: April 19, 2012
    Inventors: Ghazwan Saleem Butrous, Timothy Michael Lukas, Ian Machin
  • Publication number: 20120041199
    Abstract: The present invention relates to a process for the preparation of doxazosin or salts thereof.
    Type: Application
    Filed: March 23, 2010
    Publication date: February 16, 2012
    Applicant: CIPLA LIMITED
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Dilip Ramdas Birari
  • Patent number: 8093384
    Abstract: The invention relates to processes for the preparation of alfuzosin or pharmaceutically acceptable salts thereof in high purity. More particularly, it relates to the preparation of pure crystalline alfuzosin base. The invention also relates to pharmaceutical compositions that include the pure alfuzosin or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 14, 2006
    Date of Patent: January 10, 2012
    Assignee: Wockhardt Ltd.
    Inventors: Pankaj Kumar Nathani, Sunil Dnyaneshwar Narode, Mohammad Jaweed Mukarram Siddiqui
  • Publication number: 20110288082
    Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate.
    Type: Application
    Filed: May 6, 2011
    Publication date: November 24, 2011
    Inventors: Raymond J. Deshaies, Tsui-Fen Chou, Frank J. Schoenen, Kelin Li, Kevin J. Frankowski, Jeffrey Aube, Samuel W. Gerritz, Han-Jie Zhou
  • Publication number: 20110224155
    Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
    Type: Application
    Filed: June 3, 2008
    Publication date: September 15, 2011
    Applicant: SENOMYX INC.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
  • Patent number: 7989462
    Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: August 2, 2011
    Assignee: Myrexis, Inc.
    Inventors: Sui Xiong Cai, Mark B. Anderson, Adam Willardsen, Nilantha Sudath Sirisoma, Hong Zhang, Kazuyuki Suzuki
  • Patent number: 7985755
    Abstract: 2,4-Diaminoquinazolines of formula (I) are provided herein and are useful for treating spinal muscular atrophy (SMA).
    Type: Grant
    Filed: August 1, 2007
    Date of Patent: July 26, 2011
    Assignee: Families of Spinal Muscular Atrophy
    Inventors: Jasbir Singh, Mark E. Gurney
  • Publication number: 20110124650
    Abstract: The present invention provides stable crystalline polymorphic forms of antifolate compounds, particularly (S)-2-{4-[2-(2,4-diamino-quinazolin-6-yl)-ethyl]-benzoylamino}-4-methylene-pentanedioic acid, dipotassium salt, and methods of preparation thereof The polymorphs may be in the form of hydrates. The invention further provides pharmaceutical compositions comprising the polymorphs and methods of treatment using the polymorphs. The polymorphs are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis, and the polymorphs may be administered alone in or combination with on or more further active agents.
    Type: Application
    Filed: July 7, 2010
    Publication date: May 26, 2011
    Inventors: Harish K. Pimplaskar, Mikhail Lebedev, Karol Horvath
  • Publication number: 20110112126
    Abstract: The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GAR, FPGS, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation.
    Type: Application
    Filed: November 4, 2010
    Publication date: May 12, 2011
    Inventor: Michael J. Roberts
  • Patent number: 7888366
    Abstract: 2,4-Diaminoquinazolines of formulae I-IV and VI are useful for treating spinal muscular atrophy (SMA).
    Type: Grant
    Filed: June 7, 2005
    Date of Patent: February 15, 2011
    Assignee: Families of Spinal Muscular Atrophy
    Inventors: Jasbir Singh, Mark E. Gurney
  • Publication number: 20110034477
    Abstract: Crystalline Form IV of doxazosin mesylate, a process for its preparation and uses thereof.
    Type: Application
    Filed: July 10, 2008
    Publication date: February 10, 2011
    Applicant: CIPLA LIMITED
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Manish Gopaldas Gangrade, Shrikant Suresh Mudgal
  • Publication number: 20110015201
    Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.
    Type: Application
    Filed: February 12, 2009
    Publication date: January 20, 2011
    Inventors: James K. Chen, Joel M. Hyman, Cory A. Ocasio
  • Publication number: 20100256370
    Abstract: A process for preparing alfuzosin or a salt thereof comprising: (a) condensing 4-amino-2-chloro-6,7-dimethoxyquinazoline with 3-methylaminopropionitrile in the presence of a polar aprotic solvent selected from the group consisting of diglyme, dimethyl formamide, t-butanol, hexamethylphosphoramide or mixtures thereof to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine (b) hydrogenating the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine using a hydrogenating agent under a pressure of less than 10 kg/cm2 to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine and optionally converting the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine to an acid addition salt thereof; and (c) converting tetrahydrofuroic acid to an intermediate form and condensing the intermediate form with the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine or with the acid addition salt to yield alfuzosin base, and optionally converting alfuzosin base to a
    Type: Application
    Filed: August 1, 2008
    Publication date: October 7, 2010
    Applicant: CIPLA LIMITED
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Dilip Birari
  • Publication number: 20100221259
    Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.
    Type: Application
    Filed: May 10, 2010
    Publication date: September 2, 2010
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
  • Publication number: 20100150896
    Abstract: The present invention relates to new diaminoquinazoline inhibitors of dihydrofolate reductase activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 11, 2009
    Publication date: June 17, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20100143299
    Abstract: This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR?R? and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene; n is 0, 1 or 2; and R6 is selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-?/-oxide, a solvate or a pro-drug thereof.
    Type: Application
    Filed: July 20, 2007
    Publication date: June 10, 2010
    Applicant: Gilead Sciences, Inc.
    Inventors: Ling-Jie Gao, Piet André Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
  • Publication number: 20100144731
    Abstract: Novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided.
    Type: Application
    Filed: September 3, 2009
    Publication date: June 10, 2010
    Applicant: Dr. Reddy's Laboratories Ltd.
    Inventors: Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti
  • Publication number: 20100130476
    Abstract: The present invention relates to compounds and compositions for inducing the expansion of pancreatic ?-cells. The invention further relates to a use of these expanded pancreatic ?-cells to reversibly expand pancreatic ?-cells and other quiescent cells to overcome deficits associated with degenerative and/or autoimmune diseases.
    Type: Application
    Filed: November 12, 2009
    Publication date: May 27, 2010
    Applicant: The Scripps Research Institute
    Inventors: Weidong Wang, Peter G. Schultz
  • Publication number: 20100099658
    Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.
    Type: Application
    Filed: July 4, 2008
    Publication date: April 22, 2010
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Yutaka Kondoh, Kazuhiko Iikubo, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani, Itsuro Shimada, Takahiro Matsuya, Kazuo Kurosawa, Akio Kamikawa, Hiroyuki Mano
  • Publication number: 20100068197
    Abstract: Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Application
    Filed: July 9, 2009
    Publication date: March 18, 2010
    Applicant: Myriad Pharmaceuticals, Inc.
    Inventors: MARK B. ANDERSON, J. Adam Willardsen, Warren S. Weiner, Kazuyuki Suzuki, Robert J. Halter, In Chul Kim, Matthew Reeder, Ashantai Yungai
  • Publication number: 20100069383
    Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Application
    Filed: July 10, 2009
    Publication date: March 18, 2010
    Applicant: Myriad Pharmaceuticals, Incorporated
    Inventors: MARK B. ANDERSON, J. Adam Willardsen, Warren S. Weiner, Ashantai Yungai, Robert J. Halter, Yevgeniya Klimova, Kazuyuki Suzuki, Matthew Reeder
  • Publication number: 20100016293
    Abstract: Compounds that interact with the histamine H4 receptor, and which may be useful for treating or preventing disorders and conditions mediated by the histamine H4 receptor, e.g. inflammation, are of formula (I) wherein Q is CR1 or N; X is CR2 or N, provided that Q and X are not both N; Y is CR3 or N; Z is CH or N; R1, R2, R3, R4, R5 and R6 are independently H, F, Cl, Br, I, or a hydrocarbon group which optionally contains one or more heteroatoms; and R7 is a heterocyclic radical including one or more N atoms; or a pharmaceutically acceptable salt, ester or solvate thereof.
    Type: Application
    Filed: July 3, 2007
    Publication date: January 21, 2010
    Inventors: Rogier Adriaan Smits, Herman Dirnawan Lim, Regorius Leurs, Iwan Jozef Philomena De Esch
  • Publication number: 20090312351
    Abstract: The invention relates to processes for the preparation of alfuzosin or pharmaceutically acceptable salts thereof in high purity. More particularly, it relates to the preparation of pure crystalline alfuzosin base. The invention also relates to pharmaceutical compositions that include the pure alfuzosin or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 14, 2006
    Publication date: December 17, 2009
    Inventors: Pankaj Kumar Nathani, Sunil Dnyaneshwar Narode, Mohammed Jaweed Mukarram Siddiqui
  • Patent number: 7601713
    Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.
    Type: Grant
    Filed: December 15, 2006
    Date of Patent: October 13, 2009
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
  • Publication number: 20090253719
    Abstract: The present invention provides methods of preparing antifolate compounds. The inventive methods can particularly be use for preparing compounds exhibiting improved bioavailability, making the compound particularly useful in pharmaceutical compositions. The compounds prepared according to the inventive methods are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.
    Type: Application
    Filed: April 7, 2009
    Publication date: October 8, 2009
    Inventors: Harish K. Pimplaskar, Mikhail Lebedev, Karol Horvath
  • Publication number: 20090233949
    Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.
    Type: Application
    Filed: March 9, 2009
    Publication date: September 17, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Henning STEINHAGEN, Markus FOLLMANN, Jochen GOERLITZER, Herman SCHREUDER
  • Patent number: 7544690
    Abstract: The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression.
    Type: Grant
    Filed: September 30, 2002
    Date of Patent: June 9, 2009
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Yoshinori Sekiguchi, Kosuke Kanuma, Katsunori Omodera, Thuy-Anh Tran, Bryan Aubrey Kramer, Nigel Robert Arnold Beeley
  • Publication number: 20090118311
    Abstract: Compounds of formula (I) or (II) are dihydrofolate reductase inhibitors, useful for the treatment of, for example, cell proliferative diseases: wherein A and D are independently —CHR7— or —NR7—; E and G are independently ?CR7— or ?N—; each R6 independently represents hydrogen or —OR7; R7 is hydrogen or C1-C6 alkyl; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid which does not contain a carboxyl, or carboxyl ester group; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, and Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—, —NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R
    Type: Application
    Filed: April 24, 2007
    Publication date: May 7, 2009
    Inventor: Alan Hornsby Davidson