Four Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/255)
  • Patent number: 9040544
    Abstract: The invention relates to oxazolopyrimidine compounds of formula I, where A, R1 and R2 are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: May 26, 2015
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Katrin Hiss
  • Publication number: 20150111876
    Abstract: A sulfur-containing bicyclic compound having a PAM action of GABAB, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABAB.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: Astellas Pharma Inc.
    Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
  • Publication number: 20150094305
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: September 25, 2014
    Publication date: April 2, 2015
    Inventors: Donna ROMERO, Craig E. MASSE, Shaughnessy ROBINSON, Jeremy Robert GREENWOOD, Geraldine C. HARRIMAN
  • Patent number: 8980893
    Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: March 17, 2015
    Assignee: Merial, Inc.
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
  • Publication number: 20150050325
    Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to a drug-eluting stent comprising said compounds and methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.
    Type: Application
    Filed: January 16, 2013
    Publication date: February 19, 2015
    Applicant: The Rockefeller University
    Inventors: Barry S. Coller, Craig Thomas, Marta Filizola, Joshua McCoy, Wenwei Huang, Min Shen, Jian-Kang Jiang
  • Publication number: 20150031672
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Patent number: 8921383
    Abstract: The present invention relates to the use of novel thiazolopyrimidine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: December 30, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Cornelius Hermann, Lee Edwin Lowrie, Jr., Matthew C. Lucas, Kin-Chun Thomas Luk, Fernando Padilla, Jutta Wanner, Wenwei Xie, Xiaohu Zhang
  • Patent number: 8921382
    Abstract: The present disclosure relates to thiazolo[5,4-d]pyrimidines and their use as agrochemicals and animal health products.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: December 30, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: William K. Brewster, Carla J. R. Klittich, Brent J. Rieder, Thomas L. Siddall, Chenglin Yao
  • Patent number: 8901133
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: December 2, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Publication number: 20140350034
    Abstract: The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: January 25, 2013
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Trixi Brandl, Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard, Martin Renatus
  • Patent number: 8883833
    Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 11, 2014
    Assignee: Decode Genetics EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
  • Patent number: 8877351
    Abstract: Disclosed are an organometallic complex emitting red light with high color purity. An organometallic complex having a structure represented by the following general formula (G1) is provided. In the formula, of R1 to R13, at least one represents an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms and the other or others represent hydrogen. M represents a central metal, which is a Group 9 or Group 10 element. L represents a monoanionic ligand, and n is 2 when the central metal is a Group 9 element or 1 when the central metal is a Group 10 element.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: November 4, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Satoshi Seo
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20140315885
    Abstract: A series of thiazolo[5,4-d]pyrimidine derivatives of formula (I) or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof: (I) Q represents a group of formula (Qa), (Qb), (Qc), (Qd) or (Qe) are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 23, 2014
    Inventors: Daniel Christopher Brookings, Daniel James Ford, Richard Jeremy Franklin, Anant Ramrao Ghawalkar, Claire Louise Kulisa, Judi Charlotte Neuss, James Thomas Reuberson
  • Publication number: 20140309222
    Abstract: A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
    Type: Application
    Filed: August 15, 2012
    Publication date: October 16, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D, UCB PHARMA S.A.
    Inventors: Daniel Christopher Brookings, Daniel James Ford, Anant Ramrao Ghawalkar, Jean Herman, Qiuya Huang, Claire Louise Kulisa, Thierry Louat, Judi Charlotte Neuss, James Thomas Reuberson, Bart Vanderhoydonck
  • Patent number: 8846692
    Abstract: The present invention relates to oxazolopyrimidine compounds of the formula I, in which A, R1, R2, R3 and X are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: September 30, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Katrin Hiss
  • Patent number: 8846691
    Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2, R3, R4, X and Y are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: September 30, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
  • Patent number: 8846690
    Abstract: Heterocyclic carboxylic acid derivatives comprising a 2,5-substituted oxazolopyrimidine ring as Edg-1 receptor agonists The present invention relates to oxazolopyrimidine compounds of the formula I, in which A, R1, R2, R3, X and Y are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: September 30, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Katrin Hiss
  • Patent number: 8835442
    Abstract: The present invention relates to novel 3-substituted (7-imino-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl of formula 1 wherein R is selected from a group consisting of hydrogen, alkyl having carbon no up to 10, allyl, cycloalkyl, aromatic, substituted aromatics (halogen, OH, COOH, OCH3, alkyl, etc), pyridyl, piperidine, piprazine, morphine. R1 is selected from a group consisting of NH2, NHR, N(R)2 (wherein R could be aliphatic or olefinic group up to 10 carbon), hetrocycles such as furan, thiophene, pyrole, prydyl, piprazine, morphine and R2 is O and S separately. Particularly the present invention relates to (7-Imino-3-substituted-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-urea (15-21) and Furan-2-carboxylic acid (7-imino-3-substituted-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-amide.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: September 16, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Pratibha Mehta Luthra, Chandra Bhushan Mishra
  • Patent number: 8835451
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Grant
    Filed: March 28, 2007
    Date of Patent: September 16, 2014
    Assignee: Novartis AG
    Inventors: Michael H. Serrano-Wu, Young-Shin Kwak, Wenming Liu
  • Publication number: 20140171408
    Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
    Type: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum MacLeod, Steven R. Magnuson, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang
  • Publication number: 20140148433
    Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: August 31, 2011
    Publication date: May 29, 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, Lars Bärfacker, Stefan Weigand
  • Patent number: 8735402
    Abstract: The present invention relates to cycloalkyloxycarboxylic acid derivatives of the formula I in which A, R1, R2a, R2b, R2c, R3 and X are as defined in the claims. The compounds of the formula I are suitable, for example, for wound healing.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Thomas Huebschle, Katrin Hiss, Silke Haag-Diergarten
  • Patent number: 8735387
    Abstract: The present invention relates to oxazolopyrimidine compounds of the formula I in which A, R1, R2 and R3 are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Werngard Czechtizky
  • Patent number: 8728567
    Abstract: The present invention pertains to the double complex salts in optoelectronic components, like organic diodes, organic transistors or organic lasers, in particular an organic solar cell (OSC, OPP) and in particular from oligomers built from charged metal complexes.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: May 20, 2014
    Assignee: Cynora GmbH
    Inventors: Hartmut Yersin, Tobias Fischer, Uwe Monkowius
  • Patent number: 8716297
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, and n are defined in the description. The present invention relates also to compositions containing compounds of formula (I) which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: May 6, 2014
    Assignee: AbbVie Inc.
    Inventors: Keith W. Woods, Chunqui Lai, Thomas D. Penning, Julie M. Miyashiro
  • Patent number: 8703777
    Abstract: Provided herein are substituted bicyclic compounds, e.g., compounds of Formula IV, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for inhibiting phosphatidyl inositol-3 kinase (PI3 kinase), e.g., for the treatment of various diseases and conditions associated with PI3 kinase activity, including but not limited to, cancer, inflammatory disease, immune disease, and respiratory disease.
    Type: Grant
    Filed: January 5, 2009
    Date of Patent: April 22, 2014
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Katrina Chan, Christian Rommel, Liansheng Li
  • Publication number: 20140107098
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
  • Patent number: 8697708
    Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: April 15, 2014
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven R. Magnuson, Vickie H. Tsui, Karen Williams, Birong Zhang
  • Publication number: 20140080842
    Abstract: The present invention relates to the use of compounds which are capable of attenuating skin irritation when they are applied to the skin. Skin irritation can be caused, inter alia, by ingredients of cosmetic or pharmaceutical compositions and/or environmental irritants. In particular, the present invention relates to compounds having the property of antagonizing the activation of the transient receptor potential (TRP) ankyrin 1 (TRPA1) ion channel and the use of said compounds as soothing agents. Such compounds can be used in many fields, particularly in personal-care products, cosmetics, textile and packaging products, pharmaceutical compositions, medical devices, and foodstuffs. The present invention further relates to products and/or pharmaceutical compositions containing said compounds. The present invention also relates to the use of the compounds described herein for the modulation of the taste of a food product.
    Type: Application
    Filed: May 11, 2012
    Publication date: March 20, 2014
    Applicant: B.R.A.I.N. Biotechnology Research and Information Network AG
    Inventors: Michael Krohn, Dirk Sombroek
  • Patent number: 8658791
    Abstract: 6-Amino-4-pyrimidinecarboxylic acids having alkyl, alkenyl or alkynyl substituents in the 5-position and 4-aminopicolinic acids having alkyl, alkenyl or alkynyl substituents in the 3-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: February 25, 2014
    Assignee: Dow AgroSciences, LLC
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, Terry W. Balko, Carla N. Yerkes
  • Patent number: 8637527
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
  • Publication number: 20140024661
    Abstract: A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.
    Type: Application
    Filed: July 19, 2013
    Publication date: January 23, 2014
    Applicant: Cleave Biosciences, Inc.
    Inventors: Han-Jie Zhou, Francesco Parlati
  • Publication number: 20140024659
    Abstract: The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: BASF SE
    Inventors: Ralph Paulini, Carsten Beyer, Henricus Maria Martinus Bastiaans, Nancy B. Rankl
  • Patent number: 8623860
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20130345192
    Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.
    Type: Application
    Filed: October 28, 2011
    Publication date: December 26, 2013
    Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.
    Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
  • Patent number: 8609840
    Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: December 17, 2013
    Assignee: Neuronascent, Inc.
    Inventor: Judith Kelleher-Andersson
  • Publication number: 20130303533
    Abstract: Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: August 31, 2011
    Publication date: November 14, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventors: Qi Chao, Michael J. Hadd, Mark W. Holladay, Martin Rowbottom
  • Publication number: 20130303551
    Abstract: This invention relates to the use of pyrimidinone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of pyrimidinones in the treatment of cancer.
    Type: Application
    Filed: January 10, 2012
    Publication date: November 14, 2013
    Inventors: Nicholas D. Adams, Alexander Joseph Reif, Kenneth Wiggall
  • Patent number: 8580800
    Abstract: The present invention relates to novel 1,4-diarylpyrimido[4,5-d]pyridazine-2,5-dione derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: November 12, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
  • Patent number: 8575178
    Abstract: The present invention is related to novel isothiazolo[3,4-d]pyrimidinedione and isothiazolo[5,4-d]pyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Grant
    Filed: March 22, 2010
    Date of Patent: November 5, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
  • Publication number: 20130281467
    Abstract: Compounds of formula (I), wherein G represents together with the two carbon atoms of the pyrimidine ring to which it is attached, a 5- to 7-membered aliphatic carbocyclic or heterocyclic ring system which contain 0 to 2 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; and wherein said 5- to 7-membered aliphatic carbocyclic or heterocyclic ring system can be mono-, di- or trisubstituted by substituents selected from the group consisting of halogen, keto, C1-C6alkyl, C1-C6alkoxy, C1-C6alkyloximino and C1-C6alkylendioxy; and wherein the other substituents R1, R2, R3, R4, R5 and R6 are as defined in claim 1, and their use as microbicides.
    Type: Application
    Filed: October 28, 2011
    Publication date: October 24, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Stephan Trah, Laura Quaranta, Clemens Lamberth, Martin Pouliot
  • Publication number: 20130266563
    Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.
    Type: Application
    Filed: May 17, 2013
    Publication date: October 10, 2013
    Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
  • Publication number: 20130251761
    Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.
    Type: Application
    Filed: July 15, 2011
    Publication date: September 26, 2013
    Inventors: Barry S. Coller, Craig Thomas, Marta Filizola, Joshua Mccoy, Wenwei Huang, Min Shen
  • Patent number: 8530483
    Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: September 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg, Eric Hostetler
  • Patent number: 8518955
    Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: August 27, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: V. S. Prasada Rao Lingam, Sachin Sundarlal Chaudhari, Abraham Thomas, Neelima Khairatkar-Joshi, Vidya Ganpati Kattige
  • Patent number: 8507491
    Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).
    Type: Grant
    Filed: August 24, 2009
    Date of Patent: August 13, 2013
    Assignee: IRM LLC
    Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
  • Patent number: 8507502
    Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: August 13, 2013
    Assignee: National Health Research Institutes
    Inventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
  • Patent number: 8501750
    Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: August 6, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
  • Publication number: 20130172316
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Inventors: Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH