Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
  • Patent number: 10961216
    Abstract: Provided herein are compounds useful for modulating the activity of an androgen receptor, or a variant thereof, and related compositions and methods. Compounds of the invention are useful for antagonizing the androgen receptor splice variant AR-v7, and for the treatment of castration-resistant prostate cancer.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: March 30, 2021
    Assignee: Massachusetts Institute of Technology
    Inventors: David Freeman, Nicholas B. Struntz, Shelby K. Doyle, Andre Richters, Angela N. Koehler
  • Patent number: 10919914
    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: June 7, 2017
    Date of Patent: February 16, 2021
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Catherine A. Evans, Martin R. Tremblay
  • Patent number: 10906899
    Abstract: Disclosed herein are compounds and compositions for treating or inhibiting RSV and related members of the pneumovirus and paramyxovirus families such as human metapneumovirus, mumps virus, human parainfluenzaviruses, and Nipah and hendra virus, and methods of treatment or prevention thereof.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: February 2, 2021
    Assignee: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
    Inventors: Richard K. Plemper, Eddy Lee, John Vernachio, Elyse Bourque
  • Patent number: 10849886
    Abstract: Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect. An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: December 1, 2020
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromi Muraoka, Akira Kanoh
  • Patent number: 10842793
    Abstract: The present invention relates to compounds that have the capability of inhibiting the secretion of fibroblast growth factor 2 (FGF2) by tumor cells, as well as uses of said compound in medicine, in particular in the prevention and/or treatment of cancerous or inflammatory diseases.
    Type: Grant
    Filed: February 7, 2017
    Date of Patent: November 24, 2020
    Assignees: Universitat Heidelberg, European Molecular Biology Laboratory
    Inventors: Walter Nickel, Joe Lewis
  • Patent number: 10792283
    Abstract: The present disclosure provides selective phosphoinositide 3-kinase inhibitors of formula (A), or pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of conditions mediated by one or more P13K isoforms, such as PI3K delta (PI3K?). The present disclosure further provides methods of inhibiting phosphoinositide 3-kinase inhibitors using these compounds for treatment of disorders related to phosphatidylinositol 3-kinase activity.
    Type: Grant
    Filed: February 28, 2017
    Date of Patent: October 6, 2020
    Assignee: HANGZHOU ZHENGXIANG PHARMACEUTICALS CO., LTD.
    Inventor: Xiaolin Hao
  • Patent number: 10696688
    Abstract: The present invention relates to fused pyrimidines of formulae I and II wherein, R1, R2 are as herein described. The present invention particularly relates to isoform selective PI3K? inhibition and their medicinal use as anticancer agents.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: June 30, 2020
    Assignee: Council of Scientific & Industrial Research
    Inventors: Sandip Bibishan Bharate, Shashi Bhushan, Shabber Mohammed, Santosh Kumar Guru, Sonali Sandip Bharate, Vikas Kumar, Girish Mahajan, Mubashir Javed Mintoo, Dilip Manikrao Mondhe, Ram Vishwakarma
  • Patent number: 10640502
    Abstract: Disclosed are methods for treating cancers associated with rearrangements in the mixed lineage leukemia gene (MLL-r), including MLL-r leukemia. The methods typically include administering a therapeutic amount of one or more therapeutic agents that inhibit the biological activity of one or more members of the interleukin-1 signaling pathway such inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4).
    Type: Grant
    Filed: July 9, 2018
    Date of Patent: May 5, 2020
    Assignee: Northwestern University
    Inventors: Ali Shilatifard, Kaiwei Liang, Edwin Richard Smith, Gary E. Schiltz
  • Patent number: 10633382
    Abstract: The present invention provides compounds according to formula (I) below that are PDE1 enzyme inhibitors and their use as medicaments, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: April 28, 2020
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Lars Kyhn Rasmussen, Morten Langgård, Mikkel Jessing, Paulo Jorge Vieira Vital, Karsten Juhl
  • Patent number: 10632114
    Abstract: Described herein are methods for using compounds that activate pyruvate kinase.
    Type: Grant
    Filed: April 27, 2018
    Date of Patent: April 28, 2020
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Shin-San Michael Su, Lenny Dang
  • Patent number: 10604524
    Abstract: The present invention relates to compounds of formulae I, or pharmaceutically acceptable salts or esters thereof, wherein: R1 is selected from H and CO—NR8R9, wherein R8 and R9 are each independently selected from H, alkyl, cycloalkyl and mono or bicyclic heterocycloalkyl, wherein said alkyl group is optionally substituted by one or more R12 groups, and said heterocycloalkyl is optionally substituted by R10 or R12; or R8 and R9 are linked, together with the nitrogen to which they are attached, to form a heterocycloalkyl group optionally containing one or more additional heteroatoms, and optionally substituted by one or more groups select from R10 and (CH2)mR12; R2 is selected from H and alkyl, wherein said alkyl group is optionally substituted by one or more R12 groups; R3 is selected from alkyl, cycloalkyl and heterocycloalkyl, each of which may be optionally substituted by halo, OH or alkoxy; Z1, Z2, Z3 and Z4 are all C; R4, R5, R6 and R7 are each independently selected from H, alkyl, CN, NO2, OH, alkoxy, N
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: March 31, 2020
    Assignee: LIFE ARC
    Inventors: Jon James Winter-Holt, Edward Giles Mciver, Stephen Lewis, Joanne Osborne
  • Patent number: 10577382
    Abstract: Provided is a compound represented by the following formula, or a salt thereof: [wherein each symbol is as defined herein].
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: March 3, 2020
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Youichi Kawakita, Takuto Kojima, Noriyuki Nii, Yoshiteru Ito, Nobuki Sakauchi, Hiroshi Banno, Xin Liu, Koji Ono, Keisuke Imamura, Shinichi Imamura
  • Patent number: 10564168
    Abstract: Certain embodiments include methods of assessing male fertility.
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: February 18, 2020
    Inventors: Amina El Jamali, Veronique Barnes
  • Patent number: 10526327
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: January 7, 2020
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 10472360
    Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
    Type: Grant
    Filed: August 3, 2017
    Date of Patent: November 12, 2019
    Assignee: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
    Inventors: Soo Yei Ho, Stephanie Eliane Blanchard, Athisayamani Jeyaraj Duraiswamy, Jenefer Alam, Vikrant Arun Adsool
  • Patent number: 10442815
    Abstract: The invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof and/or stereoisomers thereof. The compounds of the invention are useful in therapy.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: October 15, 2019
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen J. Shuttleworth, Franck A. Silva, Alexander R. L. Cecil, Rikki P. Alexander, Alice E. Gatland, Daniel J. Finnemore
  • Patent number: 10435375
    Abstract: Provided herein are small molecule modulators of CXCR4 activity (e.g., agonists, antagonists, inverse agonists, partial agonists), and methods of use thereof (e.g., for the treatment of disease).
    Type: Grant
    Filed: May 5, 2016
    Date of Patent: October 8, 2019
    Assignee: Northwestern University
    Inventors: Gary E. Schiltz, Richard J. Miller, Rama K. Mishra
  • Patent number: 10406140
    Abstract: Provided is a compound which is useful as an AMPK activator, represented by formula: wherein the symbols are defined in the specification.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: September 10, 2019
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Yuusuke Tamura, Toshihiro Wada
  • Patent number: 10342814
    Abstract: This disclosure demonstrates that inhibition of Sirt5 can suppress malignant transformation of cells. Therefore, methods of treating cancer based on inhibition of Sirt5 are disclosed.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: July 9, 2019
    Assignee: CORNELL UNIVERSITY
    Inventors: Hening Lin, Richard Cerione
  • Patent number: 10336770
    Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: July 2, 2019
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Chenggeng Qian
  • Patent number: 10328069
    Abstract: Methods are provided for treating a lymphoproliferative malignancy to a patient in need of such treatment, comprising administering to the patient an effective amount of compound A as described herein.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: June 25, 2019
    Assignee: EXELIXIS, INC.
    Inventors: Arthur DeCillis, Joanne Lager
  • Patent number: 10266535
    Abstract: Provided in the present invention is a novel inhibitor of FLT3 kinase, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, ester, acid, metabolite or prodrug thereof. Also provided in the present invention are a pharmaceutical composition comprising a compound of formula (I) and a use and method for preventing or treating cell proliferative conditions and/or FLT3-related conditions, in particular for conditions responding to the inhibition of FLT3 kinase (especially FLT3/ITD mutant kinases).
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: April 23, 2019
    Assignees: HEFEI INSTITUTES OF PHYSICAL SCIENCE, CHINESE ACADEMY OF SCIENCES, HEFEI COSOURCE PHARMACEUTICAL CO., LTD.
    Inventors: Jing Liu, Qingsong Liu, Xixiang Li, Aoli Wang, Hong Wu, Cheng Chen, Wenchao Wang, Chen Hu, Zheng Zhao, Jiaxin Wu, Juan Liu, Kailin Yu, Wei Wang, Li Wang, Beilei Wang
  • Patent number: 10253028
    Abstract: The compound 3,3,3-trifluoro-N-((1,4-trans)-4-((3-((S)-2-methylmorpholino)-IH-pyrazolo[3,4-d]pyrimidin-6-yl)amino)cyclohexyl)propane-1-sulfonamide having the Formula (I) or a salt thereof, its opposite enantiomer, compositions comprising the compound and its use in the treatment or prevention of leishmaniasis, particularly visceral leishmaniasis.
    Type: Grant
    Filed: January 21, 2016
    Date of Patent: April 9, 2019
    Assignees: GlaxoSmithKline Intellectual Property Development Limited, University of Dundee
    Inventors: Timothy James Miles, Michael George Thomas
  • Patent number: 10239863
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: October 20, 2017
    Date of Patent: March 26, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ning Shao, Scott D. Edmondson, Santhosh Neelamkavil, Zhuyan Guo, Eric Mertz, Yi Zang, Jiafang He
  • Patent number: 10189856
    Abstract: The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: January 29, 2019
    Assignee: Adverio Pharma GMBH
    Inventors: Claudia Hirth-Dietrich, Peter Sandner, Johannes-Peter Stasch, Andreas Knorr, Georges Von Degenfeld, Michael Hahn, Markus Follmann
  • Patent number: 10167313
    Abstract: The present invention relates to compounds of Formula I, IA, II, IIA, III, or IIIA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: January 1, 2019
    Assignee: Genesis Technologies Limited
    Inventors: Jan-Eric Ahlfors, Khalid Mekouar
  • Patent number: 10160762
    Abstract: The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone compounds of formula (I) 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 hypo-function or basal ganglia dysfunction.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: December 25, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Michael P. Dwyer, Christopher J. Sinz, Deping Wang, Shawn J. Stachel, Daniel V. Paone, Ashley Forster, Richard Berger, Yili Chen, Yimin Qian, Shimin Xu, Chunmei Hu, William D. Shipe, Jianmin Fu, Zhigang Guo, Haitang Li, Yingjian Bo
  • Patent number: 10155767
    Abstract: The present invention provides a therapeutic agent of acute myeloid leukemia containing a 1,3,7-trisubstituted 3,4-dihydropyrimido[4,5-d]pyrimidine-2(1H)-one compound as an active ingredient, which has proliferation inhibitory activity for a human acute myeloid leukemia cell line OCI-AML3 having a NRAS mutant gene while having low inhibitory activity for wild type NRAS and has activity of inhibiting GCK and ACK1 protein kinases at the same time.
    Type: Grant
    Filed: August 9, 2017
    Date of Patent: December 18, 2018
    Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Tae Bo Sim, Han Na Cho, Eun Hye Ju, Woo Young Hur, Ho Jong Yoon, Chi Man Song
  • Patent number: 10118904
    Abstract: The invention relates to triazole compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: November 6, 2018
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Robert J. Davies, Jingrong Cao, Meghan Elise Cockerill, Philip Noel Collier, Elisabeth Doyle, James Daniel Frantz, Huai Gao, Brian Anthony Goldman, Ronald Lee Grey, Jr., Anne-Laure Grillot, Wenxin Gu, James A. Henderson, Raul Eduardo Krauss Irarrazaval, Adrianne Lynn Kolpak, Yusheng Liao, Sanjay Shivayogi Magavi, David Messersmith, Albert Charles Pierce, Emanuele Perola, Elizabeth Jin-Sun Ryu, Joshua Syken, Jian Wang, Michael Paul DeNinno, Francois Maltais
  • Patent number: 10111864
    Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
    Type: Grant
    Filed: April 25, 2017
    Date of Patent: October 30, 2018
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Chenggeng Qian
  • Patent number: 10106536
    Abstract: Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related to seizures, pain, neurotransmitter release, etc.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: October 23, 2018
    Assignee: Knopp Biosciences LLC
    Inventors: Lynn Resnick, George T. Topalov, Charles A. Flentge, James S. Hale, David A. Mareska
  • Patent number: 10064868
    Abstract: Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.
    Type: Grant
    Filed: June 3, 2015
    Date of Patent: September 4, 2018
    Assignee: MEI PHARMA, INC.
    Inventors: S. David Brown, David J. Matthews
  • Patent number: 10053465
    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 25, 2016
    Date of Patent: August 21, 2018
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, David M. Burns, Hao Feng, Joseph Glenn, Chunhong He, Taisheng Huang, Song Mei, Jun Pan, Xiaozhao Wang, Yingda Ye
  • Patent number: 10039846
    Abstract: Bradykinin B1 receptor (B1R) targeting peptides and compounds are radiolabelled with radioisotopes that are suitable for imaging and/or radiotherapy. The radiolabelled peptides and compounds have utility in imaging tissues expressing or overexpressing B1R and/or treating diseases or conditions in which B1R is expressed or overexpressed, including cancer.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: August 7, 2018
    Assignee: BRITISH COLUMBIA CANCER AGENCY BRANCH
    Inventors: Kuo-shyan Lin, Francois Benard, Jinhe Pan, Felix Mesak, Zhengxing Zhang
  • Patent number: 10022461
    Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: July 17, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Abbas M. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
  • Patent number: 9994562
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: June 12, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
  • Patent number: 9980961
    Abstract: Described herein are methods for using compounds that activate pyruvate kinase.
    Type: Grant
    Filed: May 1, 2017
    Date of Patent: May 29, 2018
    Assignee: AGIOS PHARMACEUTICALS, INC.
    Inventors: Shin-San Michael Su, Lenny Dang
  • Patent number: 9969731
    Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: May 15, 2018
    Assignee: Lupin Limited
    Inventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9949981
    Abstract: The present invention relates to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-(3-morpholinophenyl)-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine or N-(1-(3-(3-(4-(1-aminocyclobutyl)phenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-5-yl)phenyl)piperidin-4-yl)-N-methylacetamide. The methods of the present invention can also relate to methods of treating cell proliferative disorders, such as cancer or Proteus syndrome, by utilizing the above compounds in combination with ((R)-6-(2-fluorophenyl)-N-(3-(2-((2-methoxyethyl)amino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine).
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: April 24, 2018
    Assignee: ArQule, Inc.
    Inventors: Daniel T. Dransfield, Sudharshan Eathiraj, Jean-Marc Lapierre, Brian Schwartz, Yi Yu
  • Patent number: 9938291
    Abstract: The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is alkyl; A is absent or present, and when present is —C(O)— or —C(O)NH—; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is —C(O)—, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: April 10, 2018
    Assignee: THE TRUSTESS OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Nicoleta Dobri, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
  • Patent number: 9938281
    Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: April 10, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Abdelghani Abe Achab, Michael D. Altman, Yongqi Deng, Solomon Kattar, Jason D. Katz, Joey L. Methot, Hua Zhou, Meredeth McGowan, Matthew P. Christopher, Yudith Garcia, Neville John Anthony, Francesc Xavier Fradera Llinas, Liping Yang, Changwei Mu, Xiaona Wang, Feng Shi, Baijun Ye, Sixing Zhang, Xiaoli Zhao, Rong Zhang, Kin Chiu Fong, Xiansheng Leng
  • Patent number: 9932324
    Abstract: The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, wherein R1, R2, R3, R4, X, and Z have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: April 3, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Kley, Joerg P. Hehn, Armin Heckel
  • Patent number: 9926324
    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: Grant
    Filed: November 10, 2013
    Date of Patent: March 27, 2018
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventor: Ning Xi
  • Patent number: 9868729
    Abstract: Provided are methods of treating inflammatory disorders, autoimmune disorders, or a hematological malignancies using compounds of formula I and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof. Such disorders and conditions include leukemia and Non Hodgkin's Lymphoma.
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: January 16, 2018
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Shawn M. Bauer, Anjali Pandey
  • Patent number: 9850232
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: December 26, 2017
    Assignee: PFIZER INC.
    Inventors: David Lawrence Firman Gray, Lei Zhang, Michael Aaron Brodney, Michael Eric Green, Chakrapani Subramanyam
  • Patent number: 9834554
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jian Liu, Ronald M. Kim, Joseph Kozlowski, Deodialsingh Guiadeen, Arto D. Krikorian, Younong Yu
  • Patent number: 9737522
    Abstract: This disclosure relates to NMDA modulators and used related thereto such as for treatment of central nervous system disorders. In certain embodiments, compounds disclosed herein are NR2C subunit-selective NMDA potentiators. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiments, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof. In certain embodiments, the disclosure relates to methods of treating or preventing nervous system disorders comprising administering an effective amount of a composition comprising compound disclosed herein to a subject in need thereof.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: August 22, 2017
    Assignee: Emory University
    Inventors: Stephen F. Traynelis, Praseeda Mullasseril, Ethel C Garnier, Dennis C. Liotta, Sommer Zimmerman
  • Patent number: 9708318
    Abstract: The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 and/or FGFR4 enzyme and are useful in the treatment of FGFR-associated diseases.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: July 18, 2017
    Assignee: Incyte Corporation
    Inventors: Liang Lu, Bo Shen, Alexander Sokolsky, Xiaozhao Wang, Liangxing Wu, Wenqing Yao, Yingda Ye
  • Patent number: 9694001
    Abstract: Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect. An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: July 4, 2017
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromi Muraoka, Akira Kanoh
  • Patent number: RE46856
    Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyperproliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: January 5, 2017
    Date of Patent: May 22, 2018
    Assignee: Bayer Intellectual Property GMBH
    Inventors: Martin Hentemann, Jill Wood, William Scott, Martin Michels, Ann-Marie Campbell, Ann-Marie Bullion, Bruce R. Rowley, Aniko Redman