Four Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 544/184)
  • Patent number: 10287293
    Abstract: The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: June 27, 2016
    Date of Patent: May 14, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Michael P. Dwyer, Christopher J. Sinz, Jonathan E. Wilson, Daniel V. Paone, Yili Chen, Shimin Xu
  • Patent number: 10179785
    Abstract: The present invention relates to a novel imidazotriazinone or imidazopyrazinone derivative, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating a tankyrase-related disease, which contains the same as an active ingredient.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: January 15, 2019
    Assignee: ST PHARM CO., LTD.
    Inventors: Jung Nyoung Heo, Hwan Jung Lim, Kwang Rok Kim, Kyung Jin Kim, Uk Il Kim, Hyung Tae Bang, Ji Hye Yoon
  • Patent number: 10005788
    Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: June 26, 2018
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, David M. Burns
  • Patent number: 9988387
    Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.
    Type: Grant
    Filed: October 21, 2015
    Date of Patent: June 5, 2018
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Jincong Zhuo, Chunhong He, Wenqing Yao
  • Patent number: 9981975
    Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
    Type: Grant
    Filed: March 27, 2017
    Date of Patent: May 29, 2018
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Xiaozhao Wang, Chunhong He
  • Patent number: 9708333
    Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: July 18, 2017
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, David M. Burns
  • Patent number: 9598419
    Abstract: The present invention provides thiazole compounds of Formula I wherein X, Y, Z, X1, X2, X3, X4, X5, R1, R2, R4, R5, R6, R7, and W, are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug, ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Grant
    Filed: June 23, 2015
    Date of Patent: March 21, 2017
    Assignee: UNIVERSITE DE MONTREAL
    Inventors: Alain Martel, Francois Tremblay
  • Patent number: 9505786
    Abstract: The present application relates to novel substituted fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: November 29, 2016
    Assignees: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder, Walter Hübsch, Alexandros Vakalopoulos, Adrian Tersteegen
  • Patent number: 9296761
    Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.
    Type: Grant
    Filed: August 19, 2015
    Date of Patent: March 29, 2016
    Assignee: Pfizer Inc.
    Inventors: Thomas Allen Chappie, Christopher John Helal, Bethany Lyn Kormos, Jamison Bryce Tuttle, Patrick Robert Verhoest
  • Patent number: 9273057
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: March 1, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann, Yong Zhang, Libing Chen, Bin Chen, John S. Tokarski, Ashvinikumar V. Gavai
  • Patent number: 9216978
    Abstract: The present application relates to novel fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: December 22, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Walter Kroh, Lars Bärfacker
  • Patent number: 9174998
    Abstract: A compound represented by formula (1) or pharmaceutically acceptable salt thereof: wherein R1 is a C1-6 alkyl group; R2 and R3 are the same or different from each other and each is a hydrogen atom or a C1-6 alkyl group; X2, X3 and X4 are the same or different from each other and each is a hydrogen atom or a halogen atom; and X5 is a hydrogen atom or —P(?O)(OH)2 has a Wnt Pathway modulating activity.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: November 3, 2015
    Assignees: Eisai R&D Management Co., Ltd., PRISM Pharma Co., Ltd.
    Inventors: Satoshi Inoue, Yuji Yamamoto, Kentaro Iso
  • Patent number: 9145427
    Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: September 29, 2015
    Assignee: Pfizer Inc.
    Inventors: Thomas Allen Chappie, Christopher John Helal, Bethany Lyn Kormos, Jamison Byrce Tuttle, Patrick Robert Verhoest
  • Patent number: 9115053
    Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: August 25, 2015
    Assignees: Massachusetts Institute of Technology, The General Hospital Corporation
    Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Publication number: 20150133453
    Abstract: Compounds of the formula I in which X, R1 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Application
    Filed: April 6, 2013
    Publication date: May 14, 2015
    Applicant: Merck Patent GmbH
    Inventors: Dieter Dorsch, Hans-Peter Buchstaller
  • Publication number: 20150080401
    Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.
    Type: Application
    Filed: November 21, 2014
    Publication date: March 19, 2015
    Inventors: Thomas Allen Chappie, Christopher John Helal, Bethany Lyn Kormos, Jamison Bryce Tuttle, Patrick Robert Verhoest
  • Patent number: 8981088
    Abstract: A compound comprising a boron subphthalocyanine moiety, a plurality of solubilizing substituents positioned on peripheral cyclic groups of the boron subphthalocyanine moiety and an axial substituent positioned on the boron atom. The plurality of solubilizing substituents comprise an oxygen or sulfur containing functional group and a substituted or unsubstituted, linear, branched or cyclic, aliphatic or aromatic terminal hydrocarbyl group that is 8 or more carbon atoms in length, the hydrocarbyl group optionally containing one or more heteroatoms. The axial substituent is a cyclic group selected from the group consisting of heterocyclic amine groups, diaryl ketone groups, benzotriazole groups, benzyl alcohol groups and polycyclic aromatic hydrocarbon groups, the cyclic group being bonded to the boron atom by an oxygen containing linking moiety, the cyclic group optionally being substituted with one or more additional substituents.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: March 17, 2015
    Assignee: Xerox Corporation
    Inventors: Jeffrey H. Banning, Wolfgang G. Wedler, Stephan V. Drappel
  • Publication number: 20150065465
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Publication number: 20150057283
    Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
    Type: Application
    Filed: March 28, 2014
    Publication date: February 26, 2015
    Applicant: CHOONGWAE PHARMA CORPORATION
    Inventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
  • Publication number: 20150045348
    Abstract: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).
    Type: Application
    Filed: January 25, 2013
    Publication date: February 12, 2015
    Applicant: H. Lundbeck A/S
    Inventors: Niels Svenstrup, Klaus Bæk Simonsen, Lars Kyhn Rasmussen, Karsten Juhl, Morten Langgärd, Kate Wen, Yazhou Wang
  • Patent number: 8940736
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: January 27, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Patent number: 8933224
    Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: January 13, 2015
    Assignee: Pfizer Inc.
    Inventors: Thomas Allen Chappie, Christopher John Helal, Bethany Lyn Kormos, Jamison Bryce Tuttle, Patrick Robert Verhoest
  • Publication number: 20150005232
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 1, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
  • Publication number: 20140378451
    Abstract: The present invention relates to cannabinoid-2-receptor (CB2R) agonist compounds. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of diseases or conditions in which CB2R stimulation is beneficial (especially inflammatory conditions).
    Type: Application
    Filed: September 19, 2012
    Publication date: December 25, 2014
    Inventors: Ivy Christou, Rebecca Lillian Cross, Matteo Gianella-Borradori, David Robert Greaves, Angela Jane Russell, Graham Michael Wynne
  • Publication number: 20140357637
    Abstract: The present application relates to novel substituted fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: January 10, 2013
    Publication date: December 4, 2014
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder, Walter Hübsch, Alexandros Vakalopoulos, Adrian Tersteegen
  • Patent number: 8901123
    Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: December 2, 2014
    Assignee: Incyte Corporation
    Inventors: Lingkai Weng, Lei Qiao, Jiacheng Zhou, Pingli Liu, Yongchun Pan
  • Publication number: 20140350020
    Abstract: The present application relates to novel fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: July 5, 2011
    Publication date: November 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Walter Kroh, Lars Bärfacker
  • Publication number: 20140329820
    Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.
    Type: Application
    Filed: April 30, 2014
    Publication date: November 6, 2014
    Applicant: Pfizer Inc.
    Inventors: Thomas Allen Chappie, Christopher John Helal, Bethany Lyn Kormos, Jamison Bryce Tuttle, Patrick Robert Verhoest
  • Publication number: 20140330014
    Abstract: The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 6, 2014
    Inventors: Richard CHESWORTH, Gerhard KOENIG, Amy RIPKA, Gideon SHAPIRO
  • Patent number: 8853394
    Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: October 7, 2014
    Assignee: Surface Logix, Inc.
    Inventors: Stewart Campbell, David Duffy, Michael Grogan, Steven Kates, Emanuele Ostuni, Olivier Schueller, Paul Sweetnam
  • Patent number: 8841446
    Abstract: The invention relates to a method for producing medicaments that contain vardenafil hydrochloride, essentially as trihydrate in solid form, and to medicaments that can be obtained according to this method.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: September 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Peter Serno, Alfons Grunenberg, Andreas Ohm, Rainer Bellinghausen, Elmer Vollers, Jan-Olav Henck
  • Publication number: 20140271847
    Abstract: There is disclosed a formulation for creating a rapid penile erection within 30 minutes. In an embodiment, a lozenge has a preparation configured to create a rapid penile erection. The preparation is effective to create the rapid penile erection with sildenafil citrate in a range of 50-100 mg. The preparation is effective to create the rapid penile erection with tadalafil in a range of 5-40 mg. The preparation is effective to create the rapid penile erection with vardenafil hydrochloride in a range of 5-40 mg. In various embodiments, the formulation includes a solvent configured to permeate skin. Other embodiments are also disclosed.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Ray L. Hauser, BoLin Zheng
  • Publication number: 20140256718
    Abstract: This invention relates to novel 5-[(hydroxymethyl)aryl]-substituted pyrrolo[2,1-f][1,2,4]triazin-4-amines of formula (I), to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating angiogenesis-related disorders, in particular angiogenesis-related ocular disorders.
    Type: Application
    Filed: June 26, 2012
    Publication date: September 11, 2014
    Applicants: BAYER INTELLECTUAL PROPERTY GmbH, BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Jürgen Klar, Verena Vöhringer, Joachim Telser, Mario Lobell, Frank Süssmeier, Volkhart Min-Jian Li, Michael Böttger, Stefan Golz, Dieter Lang, Karl-Heinz Schlemmer, Thomas Schlange, Andreas Schall, Wenlang Fu
  • Patent number: 8809328
    Abstract: An object of the present invention is to provide a compound that can regulate plant growth. The compound selected from the group consisting of (A) and (B): (A) 3H-imidazo[4,5-d][1,2,3]triazin-4,6(5H,7H)-dione; and (B) 3-methyl-3H-imidazo[4,5-d][1,2,3]triazin-4,6(5H,7H)-dione; has a plant growth regulating action.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: August 19, 2014
    Assignee: National University Corporation Shizuoka University
    Inventors: Hirokazu Kawagishi, Jae-Hoon Choi
  • Publication number: 20140228366
    Abstract: The present application relates to novel heteroaryl-substituted pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: July 5, 2012
    Publication date: August 14, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder
  • Publication number: 20140221333
    Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Application
    Filed: July 19, 2012
    Publication date: August 7, 2014
    Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
  • Publication number: 20140200219
    Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Applicant: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center
    Inventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
  • Publication number: 20140171434
    Abstract: The present application relates to novel substituted imidazopyridines and imidazopyridazines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: May 2, 2012
    Publication date: June 19, 2014
    Applicants: BAYER PHARMA AKTIENGESSELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder, Volkhart Min-Jian Li
  • Patent number: 8754211
    Abstract: The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein the variables are defined herein.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: June 17, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, William N. Washburn, Kishore V. Renduchintala, Radhakrishnan Sridhar
  • Publication number: 20140148598
    Abstract: An object of the present invention is to provide a compound that can regulate plant growth. The compound selected from the group consisting of (A) and (B): (A) 3H-imidazo[4,5-d][1,2,3]triazin-4,6(5H,7H)-dione; and (B) 3-methyl-3H-imidazo[4,5-d][1,2,3]triazin-4,6(5H,7H)-dione; has a plant growth regulating action.
    Type: Application
    Filed: April 24, 2012
    Publication date: May 29, 2014
    Inventors: Hirokazu Kawagishi, Jae-Hoon Choi
  • Patent number: 8729262
    Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: May 20, 2014
    Assignee: Choongwae Pharma Corporation
    Inventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
  • Publication number: 20140134133
    Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: November 10, 2013
    Publication date: May 15, 2014
    Applicants: Calitor Sciences, LLC
    Inventor: Ning Xi
  • Publication number: 20140100229
    Abstract: The present application relates to novel fluoroalkyl-substituted pyrazolopyridines, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: April 20, 2012
    Publication date: April 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Itasch, Gorden Redlich, Nils Griebenow, Frank Wunder, Volkhart Min-Jian Li, Dieter Lang
  • Publication number: 20140080756
    Abstract: The present invention provides a compound of Formula (I) a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.
    Type: Application
    Filed: November 18, 2013
    Publication date: March 20, 2014
    Applicant: Pfizer Inc.
    Inventors: Samit K. Bhattacharya, Kimberly O. Cameron, Dilinie P. Fernando, Kim F. McClure, Daniel W. Kung, Allyn T. Londregan, Suvi T.M. Orr
  • Publication number: 20140066622
    Abstract: The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.
    Type: Application
    Filed: November 1, 2013
    Publication date: March 6, 2014
    Applicant: Pfizer Inc.
    Inventors: Christopher John Helal, Thomas Allen Chappie, John Michael Humphrey, Patrick Robert Verhoest, Eddie Yang
  • Publication number: 20140051706
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Application
    Filed: February 27, 2012
    Publication date: February 20, 2014
    Applicant: PRISM PHARMA CO., LTD.
    Inventors: Hiroyuki Kouji, Takenao Odagami
  • Publication number: 20140038967
    Abstract: Provided herein are compounds for use in the treatment of central nervous system (CNS)-trauma related disorders like spinal cord injuries. Pharmaceutical compositions, single unit dosage forms, and kit suitable for use for the treatment of (CNS)-trauma related disorders are also disclosed.
    Type: Application
    Filed: March 12, 2012
    Publication date: February 6, 2014
    Applicant: ALGIAX PHARMACEUTICALS GMBH
    Inventors: Guido Koopmans, Birgit Hasse
  • Publication number: 20140018319
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: July 12, 2013
    Publication date: January 16, 2014
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Publication number: 20130345224
    Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.
    Type: Application
    Filed: June 12, 2013
    Publication date: December 26, 2013
    Applicant: INCYTE CORPORATION
    Inventors: Jincong Zhuo, Chunhong He, Wenqing Yao