Nitrogen Bonded Directly At 2-position Patents (Class 544/292)
  • Publication number: 20150141442
    Abstract: Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described.
    Type: Application
    Filed: September 19, 2014
    Publication date: May 21, 2015
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson
  • Publication number: 20150119405
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: October 23, 2014
    Publication date: April 30, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Publication number: 20150099882
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Applicant: Pfizer Inc.
    Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
  • Publication number: 20150087664
    Abstract: Compounds having the formula (I) wherein R1, R2, R3 and Ar as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
    Type: Application
    Filed: August 3, 2012
    Publication date: March 26, 2015
    Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.
    Inventors: James F. Blake, Huifen Chen, Mark Joseph Chicarelli, Jason Demeese, Rustam Ferdinand Garrey, John Gaudino, Lewis Gazzard, Robert J. Kaus, Samuel Kintz, Peter J. Mohr, David A. Moreno, Jacob Schwartz, Christopher S. Siedem, Eli M. Wallace
  • Publication number: 20150080392
    Abstract: A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production.
    Type: Application
    Filed: July 21, 2012
    Publication date: March 19, 2015
    Applicants: HANGZHOU MINSHENG PHARMACEUTICAL CO. LTD, HANGZHOU MINSHENG INSTITUTES FOR PHARMA RESEARCH
    Inventors: Shulong Wang, Jian Cai, Qiufu Ge, Dianwu Guo, Lan Yang, Binnan Huang, Zhenhua Liu, Zhonghua Peng, Ximing Shen, Feiyu Feng
  • Publication number: 20150045363
    Abstract: Hedgehog pathway inhibitors, such as small molecules, are used to prevent, slow, block the formation of cartilage tumors as well as exostosis or enchondromas.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 12, 2015
    Inventors: Wentian Yang, Benjamin G. Neel
  • Publication number: 20140350248
    Abstract: Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described.
    Type: Application
    Filed: December 23, 2013
    Publication date: November 27, 2014
    Applicant: Intellikine, LLC.
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson
  • Publication number: 20140296233
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicants: Sanofi, Celgene Avilomics Research, Inc.
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
  • Publication number: 20140291646
    Abstract: A pyrene-based compound and an organic light-emitting diode including the same, the pyrene-based compound being represented by Formula 1, below:
    Type: Application
    Filed: March 25, 2014
    Publication date: October 2, 2014
    Applicant: Samsung Display Co., Ltd.
    Inventors: Dong-Woo SHIN, O-Hyun KWON, Mie-Hwa PARK, Seul-Ong KIM, Byoung-Ki CHOI
  • Patent number: 8816076
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: August 26, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8802697
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 12, 2014
    Assignee: Blueprint Medicines Corporation
    Inventors: Neil Bifulco, Jr., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
  • Publication number: 20140221371
    Abstract: The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.
    Type: Application
    Filed: December 23, 2013
    Publication date: August 7, 2014
    Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Franciso Javier Garcia-Ladona, Wolfgang Wernet
  • Publication number: 20140187559
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: December 26, 2013
    Publication date: July 3, 2014
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventor: Chandrasekhar V. Miduturu
  • Publication number: 20140135338
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: July 12, 2012
    Publication date: May 15, 2014
    Applicant: PFIZER INC.
    Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu
  • Patent number: 8716285
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: May 6, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
  • Publication number: 20140100195
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: October 5, 2012
    Publication date: April 10, 2014
    Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
  • Publication number: 20140088100
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: July 11, 2013
    Publication date: March 27, 2014
    Applicant: BLUEPRINT MEDICINES
    Inventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
  • Publication number: 20140077179
    Abstract: Provided are a novel compound for an organic electronic material and an organic electroluminescent device using the same. The compound for an organic electronic material according to the present invention has high electron transport efficiency, thereby preventing crystallization at the time manufacturing of a device, and allows a layer to be easily formed, thereby improving current characteristics of the device, and thus an OLED device having a lowered driving voltage and improved power efficiency as well as superior luminous efficiency and lifespan characteristics as compared with the existing material can be manufactured.
    Type: Application
    Filed: November 16, 2011
    Publication date: March 20, 2014
    Applicant: Rohm and Haas Electronic Materials Korea Ltd.
    Inventors: Hyo Nim Shin, Chi Sik Kim, Su Hyun Lee, Hong Yoep Na, Seok-Keun Yoon, Soo Jin Yang, Soo Yong Lee, Young Jun Cho, Kyoung-Jin Park, Kyung Joo Lee, Bong Ok Kim
  • Publication number: 20140061609
    Abstract: Provided are novel compounds in accordance with Formula I for an organic electronic material and an organic electroluminescent device using same. The compound for an organic electronic material disclosed herein exhibits high electron transport efficiency and thus prevents crystallization upon manufacturing a device, and also facilitates the formation of a layer, thus improving current properties of the device. Thereby, OLED devices having improved power efficiency as well as reduced operating voltage can be manufactured.
    Type: Application
    Filed: October 13, 2011
    Publication date: March 6, 2014
    Inventors: Nam Kyun Kim, Seok-Keun Yoon, Jin Hee Kim, Hyo Jung Lee, Mi Ja Lee, Hee Choon Ahn, Doo-Hyeon Moon, Jung-Eun Yang, Hee Sook Kim, Soo-Jin Hwang, Young Jun Cho, Kyung Joo Lee, Hyuck Joo Kwon, Bong Ok Kim
  • Patent number: 8664388
    Abstract: The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: March 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Fuchs, Niklas Heine, Christian Eickmeier, Sandra Handschuh, Cornelia Dorner-Ciossek, Stefan Hoerer
  • Publication number: 20130331570
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: August 14, 2013
    Publication date: December 12, 2013
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20130289044
    Abstract: The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: October 5, 2011
    Publication date: October 31, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: R. Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Publication number: 20130289057
    Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.
    Type: Application
    Filed: January 12, 2012
    Publication date: October 31, 2013
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
  • Publication number: 20130261123
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Patent number: 8546425
    Abstract: Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: October 1, 2013
    Assignees: Purdue Research Foundation, Endocyte, Inc.
    Inventors: Christopher Paul Leamon, Iontcho Radoslavov Vlahov, Philip Stewart Low
  • Publication number: 20130253186
    Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 26, 2013
    Applicant: Amgen Inc.
    Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
  • Patent number: 8541577
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: September 24, 2013
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20130234118
    Abstract: Embodiments of the present invention include an amine-based compound represented by Formula 1, an organic light-emitting diode including the amine-based compound, and an organic light-emitting apparatus including the amine-based compound.
    Type: Application
    Filed: December 5, 2012
    Publication date: September 12, 2013
    Applicant: SAMSUNG DISPLAY CO. LTD.
    Inventors: O-Hyun Kwon, Dong-Woo Shin, Kyul Han, Seul-Ong Kim, Byoung-Ki Choi
  • Publication number: 20130225596
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 29, 2013
    Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
  • Patent number: 8513269
    Abstract: A compound represented by the formula (I), salt thereof, or hydrate thereof has an excellent anti-pruritic effect and an excellent effect in terms of metabolism. The topical formulation of the present invention has excellent skin absorption properties of the compound represented by the formula (I), salt thereof, or hydrate thereof. Furthermore, the topical formulation of the present invention is excellent in stability because ingredients are hardly bled after long-term storage. wherein R represents hydroxyl, C1-6 alkoxy optionally substituted with C1-6 alkoxy, or amino optionally substituted with C1-6 alkyl.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: August 20, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Chiharu Kimura, Maho Sakurai
  • Publication number: 20130123271
    Abstract: The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder.
    Type: Application
    Filed: June 22, 2011
    Publication date: May 16, 2013
    Applicant: FOVEA PHARMACEUTICALS
    Inventors: David Middlemiss, Caroline Leriche
  • Publication number: 20130123496
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: November 5, 2012
    Publication date: May 16, 2013
    Applicant: ALLERGAN, INC.
    Inventor: Allergan, Inc.
  • Patent number: 8436006
    Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE.
    Type: Grant
    Filed: August 4, 2005
    Date of Patent: May 7, 2013
    Assignee: Jansssen Pharmaceutica N.V.
    Inventors: Francois Paul Bischoff, Mirielle Braeken, Serge Maria Aloysius Pieters, Mark Hubert Mercken, Hans Louis Jos De Winter, Didier Jean-Claude Berthelot
  • Patent number: 8426429
    Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE.
    Type: Grant
    Filed: August 4, 2005
    Date of Patent: April 23, 2013
    Assignee: Jansssen Pharmaceutica N.V.
    Inventors: Ellen Baxter, Robert Boyd, Steven J. Coats, Alfonzo D. Jordan, Allen B. Reitz, Charles H. Reynolds, Mark Schulz, Malcolm Scott
  • Patent number: 8394807
    Abstract: There is provided a dihydroquinazoline compound of the formula or a pharmaceutically acceptable salt thereof, wherein the values of the radicals are defined herein, as well as a pharmaceutical composition containing the compound, and a method of using the compound for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: March 12, 2013
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Patent number: 8383637
    Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE.
    Type: Grant
    Filed: August 4, 2005
    Date of Patent: February 26, 2013
    Assignee: Jansssen Pharmaceutica N.V.
    Inventors: Ellen Baxter, Francois Paul Bischoff, Robert E. Boyd, Mirielle Braeken, Steve Coats, Yifang Huang, Alfonzo D. Jordan, Chi Luo, Marc Hubert Mercken, Serge Maria Aloysius Pieters, Allen B. Reitz, Charles H. Reynolds, Tina Morgan Ross, Brett A. Tounge, Mark J. Schulz, Hans Louis Jos De Winter
  • Patent number: 8343981
    Abstract: The invention relates to heterocyclyl-substituted dihydroquinazolines of formula (I), to processes for their preparation, to medicaments containing them, and to methods for the treatment and/or prophylaxis of diseases, in particular, for use as anti-viral agents, in particular, against cytomegaloviruses.
    Type: Grant
    Filed: April 28, 2004
    Date of Patent: January 1, 2013
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Tobias Wunberg, Judith Baumeister, Mario Jeske, Peter Nell, Susanne Nikolic, Frank Suessmeier, Holger Zimmermann, Rolf Grosser, Kerstin Henninger, Guy Hewlett, Joerg Keldenich, Dieter Lang
  • Patent number: 8304420
    Abstract: This invention relates to the discovery of prodrugs of 3-or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets. An example of a compound of the present invention is methyl 2-(2-amino-5,6- dichloroquinazolin-3 (4H)-yl)-2-methylpropanoate or the 3,3-demethyl anagrelide open-ringed analog.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: November 6, 2012
    Assignee: Shire LLC
    Inventors: Richard Franklin, Bernard T. Golding, Peter A. Cicala
  • Publication number: 20120263670
    Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
    Type: Application
    Filed: June 29, 2011
    Publication date: October 18, 2012
    Applicant: Ardelyx, Inc.
    Inventors: Dominique Charmot, Jeffrey W. Jacobs, Michael Robert Leadbetter, Marc Navre, Christopher Carreras, Noah Bell
  • Publication number: 20120238582
    Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R4 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Application
    Filed: October 26, 2010
    Publication date: September 20, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER hAFTUNG
    Inventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
  • Patent number: 8222264
    Abstract: The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Grant
    Filed: July 3, 2008
    Date of Patent: July 17, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Fuchs, Niklas Heine, Christian Eickmeier, Sandra Handschuh, Cornelia Dorner-Ciossek, Stefan Hoerer
  • Publication number: 20120156219
    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: February 22, 2012
    Publication date: June 21, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
  • Publication number: 20120130072
    Abstract: The present invention relates to a process for the preparation of dihydroquinazolines, which are used for the production of medicaments.
    Type: Application
    Filed: November 30, 2011
    Publication date: May 24, 2012
    Applicant: AiCuris GmbH & Co. KG
    Inventors: Kãthe Gooßen, Oliver Kuhn, Mathias Berwe, Joachim Krüger, Hans-Christian Militzer
  • Patent number: 8178544
    Abstract: This invention provides 2,3-diamino-quinazolinone compounds of Formula (I) stereoisomers thereof, pharmaceutically-acceptable addition salts thereof, and N-oxides thereof, wherein the variables are as defined in the specification. The 2,3-diamino-quinazolinone compounds have medical utility. The 2,3-diamino-quinazolinone compounds can be used for the manufacture of medicaments, including pharmaceutical compositions. This invention also provides methods of treating disorders, diseases, or conditions which are responsive to activation of Kv7 channels.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: May 15, 2012
    Assignee: Neurosearch A/S
    Inventors: Carsten Jessen, William Dalby Brown, Joachim Demnitz, Dorte Strøbæk, Mads P. G. Korsgaard, Palle Christophersen
  • Patent number: 8168646
    Abstract: Disclosed are 3,4-dihydroquinazoline derivatives of formula (I), a process of preparing them and a pharmaceutical composition including them.
    Type: Grant
    Filed: May 6, 2008
    Date of Patent: May 1, 2012
    Assignee: Dongwoo Syntech Co., Ltd.
    Inventors: Jae Yeol Lee, Dong Joon Choo, Young Deuk Kim, Chun Rim Oh
  • Publication number: 20120065204
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.
    Type: Application
    Filed: September 7, 2011
    Publication date: March 15, 2012
    Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
  • Publication number: 20120035194
    Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).
    Type: Application
    Filed: August 8, 2011
    Publication date: February 9, 2012
    Applicant: Pfizer Inc.
    Inventors: Liming Huang, Song Liu, Elizabeth A. Lunney, Simon P. Planken
  • Publication number: 20120004210
    Abstract: The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted quinazoline compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder, In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.
    Type: Application
    Filed: December 18, 2009
    Publication date: January 5, 2012
    Inventors: Caroline Leriche, Eric Auclair, Jacques Le Roux, David Middlemiss
  • Patent number: 8063055
    Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: November 22, 2011
    Assignee: Amgen Inc.
    Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
  • Patent number: 8053434
    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: September 1, 2009
    Date of Patent: November 8, 2011
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland