The Additional Chalcogen Containing Hetero Ring Is Part Of A Polycyclo Ring System Patents (Class 514/263.24)
  • Patent number: 11466006
    Abstract: The present invention relates to dual delta (?) and gamma (?) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: October 11, 2022
    Assignee: RHIZEN PHARMACEUTICALS AG
    Inventors: Swaroop K. Vakkalanka, Prashant K. Bhavar, Srikant Viswanadha, Govindarajulu Babu
  • Patent number: 10953031
    Abstract: The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: March 23, 2021
    Assignees: Astrocyte Pharmaceuticals, Inc., The Board of Regents of the University of Texas System
    Inventors: William S. Korinek, James D. Lechleiter, Theodore E. Liston
  • Patent number: 10851107
    Abstract: The present invention relates to dual delta (?) and gamma (?) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: August 8, 2017
    Date of Patent: December 1, 2020
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Swaroop K. Vakkalanka, Prashant K. Bhavar, Srikant Viswanadha, Govindarajulu Babu
  • Patent number: 10532103
    Abstract: The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 9 (CDK9), the present application also relates to methods for the targeted degradation of CDK9 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK9 which can be utilized in the treatment of disorders modulated by CDK9.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: January 14, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
  • Patent number: 9926321
    Abstract: The disclosure relates to Compounds of Formulae (IA) and (IB), and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Xd, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and (IB) in which X2 is a leaving for introducing a radiolabeled atom, such as 124I or 131I and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: March 27, 2018
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Weilin Sun, Tony Taldone, Pallav Patel, Gabriela Chiosis
  • Patent number: 9630965
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: April 25, 2017
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Patent number: 9402832
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Grant
    Filed: April 8, 2015
    Date of Patent: August 2, 2016
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Patent number: 9346808
    Abstract: The disclosure relates to Compounds of Formulae (IA) and (IB): and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Xd, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and IB) in which X2 is a leaving for introducing a radiolabeled atom, such as 124I or 131I and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: May 24, 2016
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Weilin Sun, Tony Taldone, Pallav Patel, Gabriela Chiosis
  • Publication number: 20150119406
    Abstract: Tricyclic pyrone compounds having high oral bioavailability, excellent blood-brain barrier permeability, and low toxicity are presented. Administration of the compounds to Alzheimer's Disease transgenic models resulted in substantially reduced soluble and insoluble A? species in the brain without affecting general behavior and motor coordination. Furthermore, in addition to blocking the toxicity and formation of both intraneuronal and extracellular A? aggregates, the compounds also increase cellular cholesterol efflux, restore axonal trafficking, and enhance hippocampal synaptic plasticity.
    Type: Application
    Filed: September 30, 2014
    Publication date: April 30, 2015
    Inventors: Duy H. Hua, Lee-way Jin, Izumi Maezawa, Xinmin Xie
  • Publication number: 20150045355
    Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
    Type: Application
    Filed: December 31, 2011
    Publication date: February 12, 2015
    Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
  • Publication number: 20140378452
    Abstract: Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are other wise delivered to the brain.
    Type: Application
    Filed: September 10, 2014
    Publication date: December 25, 2014
    Inventor: Gabriela Chiosis
  • Publication number: 20140364447
    Abstract: The present invention relates to dual delta (?) and gamma (?) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.
    Type: Application
    Filed: June 4, 2014
    Publication date: December 11, 2014
    Inventors: Swaroop K. V. S. VAKKALANKA, Prashant K. BHAVAR, Srikant VISWANADHA, Govindarajulu BABU
  • Publication number: 20140315929
    Abstract: This invention concerns a method for selecting an inhibitor of a cancer-implicated pathway or of a component of a cancer-implicated pathway for coadministration, with an inhibitor of HSP90, to a subject suffering from a cancer which comprises the following steps: (a) contacting a sample containing cancer cells from a subject with an inhibitor of HSP90 or an analog, homolog or derivative of an inhibitor of HSP90 under conditions such that one or more cancer pathway components present in the sample bind to the HSP90 inhibitor or the analog, homolog or derivative of the HSP90 inhibitor; (b) detecting pathway components bound to the HSP90 inhibitor or to the analog, homolog or derivative of the HSP90 inhibitor; (c) analyzing the pathway components detected in step (b) so as to identify a pathway which includes the components detected in step (b) and additional components of such pathway; and (d) selecting an inhibitor of the pathway or of a pathway component identified in step (c).
    Type: Application
    Filed: April 27, 2012
    Publication date: October 23, 2014
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventor: Gabriela Chiosis
  • Publication number: 20140296177
    Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 2, 2014
    Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
  • Publication number: 20140228320
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):
    Type: Application
    Filed: April 15, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
  • Publication number: 20140227183
    Abstract: Hsp90 inhibitors having are provided having the formula: (I) with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.
    Type: Application
    Filed: April 18, 2014
    Publication date: August 14, 2014
    Applicant: MEMORIAL SLOAN KETTERING CANCER CENTER
    Inventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
  • Patent number: 8703942
    Abstract: The present disclosure provides inhibitors of Hsp90 and methods of making and using the same. Such compounds are useful as radioimaging ligands and for the treatment of cancer and other conditions where cell growth or maintenance depend on Hsp90 activity.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: April 22, 2014
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
  • Publication number: 20140088121
    Abstract: The disclosure relates to Compounds of Formulae (IA) and (IB): and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Xd, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (IA) and/or (IB), and methods to treat or prevent a condition, such cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (IA) or (IB). The disclosure further relates to compounds of Formulae (IA) and IB) in which X2 is a leaving for introducing a radiolabeled atom, such as 124I or 131I and to methods of using such compounds in the preparation of radiolabeled compounds, particularly for use in imaging.
    Type: Application
    Filed: April 5, 2012
    Publication date: March 27, 2014
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Weilin Sun, Tony Taldone, Pallav Patel, Gabriela Chiosis
  • Patent number: 8680076
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: March 25, 2014
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
  • Publication number: 20140080827
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 20, 2014
    Applicant: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
  • Publication number: 20140045867
    Abstract: The disclosure relates to Compounds of Formula (1) : and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof, and methods to treat or prevent a condition, such as cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: February 13, 2014
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Tony Taldone, Gabriela Chiosis
  • Patent number: 8642607
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: February 4, 2014
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
  • Publication number: 20130303555
    Abstract: The invention relates to determining the presence of an EZH2 gene mutation in a sample from a subject and inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono-through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
    Type: Application
    Filed: July 23, 2013
    Publication date: November 14, 2013
    Inventors: Robert A. Copeland, Victoria M. Richon, Margaret D. Scott, Christopher J. Sneeringer, Kevin W. Kuntz, Sarah K. Knutson, Roy M. Pollock
  • Patent number: 8476285
    Abstract: The invention relates to compounds of Formulae I-III: and therapeutic uses thereof, wherein A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group; B is chosen from a substituted or unsubstituted piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group; R1 is chosen from hydro, alkyl, aryl, heteroaryl, amino, or halo; and L1, L2, are as defined herein.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: July 2, 2013
    Assignee: Myrexis, Inc.
    Inventors: Ashok C. Bajji, Se-Ho Kim, Benjamin Markovitz, Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A. Vanecko
  • Publication number: 20130165427
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: August 24, 2012
    Publication date: June 27, 2013
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventor: Jayhong A. Chong
  • Publication number: 20130123283
    Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.
    Type: Application
    Filed: April 11, 2012
    Publication date: May 16, 2013
    Inventors: Magdalene M. Moran, Christopher Fanger, Jayhong A. Chong, Colleen McNamara, Xiaoguang Zhen, Josh Mendel-Brehm
  • Publication number: 20130109704
    Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
    Type: Application
    Filed: December 19, 2012
    Publication date: May 2, 2013
    Applicant: NEUROSEARCH A/S
    Inventor: NeuroSearch A/S
  • Publication number: 20130053406
    Abstract: The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders such as cancer.
    Type: Application
    Filed: August 23, 2010
    Publication date: February 28, 2013
    Applicant: Myrexis, Inc.
    Inventors: SE-HO KIM, Herbert L. Ley, III, Ashok Bajji
  • Patent number: 8318750
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: November 27, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120295915
    Abstract: Disclosed are compounds having Formula (I), wherein R1, R2, R3, R4, Ra, Rb, X, Y, m, and n are defined herein and methods of using the same.
    Type: Application
    Filed: November 22, 2010
    Publication date: November 22, 2012
    Inventors: Amita M. Chaudhari, Jason Hallman, Christopher P. Laudeman, David Lee Musso, Cynthia A. Parrish
  • Publication number: 20120289496
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: May 4, 2012
    Publication date: November 15, 2012
    Applicant: Rhizen Pharmaceuticals SA
    Inventors: Dhanapalan NAGARATHNAM, Swaroop Kumar V.S. Vakkalanka, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Prashant K. Bhavar
  • Patent number: 8258141
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Grant
    Filed: April 19, 2007
    Date of Patent: September 4, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120202785
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: February 8, 2012
    Publication date: August 9, 2012
    Inventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
  • Patent number: 8217050
    Abstract: The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: July 10, 2012
    Assignee: Chroma Therapeutics Limited
    Inventors: David Festus Charles Moffat, Simon Christopher Hirst, Stuart Thomas Onions
  • Publication number: 20120172347
    Abstract: The present invention provides a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof (wherein W represents a hydrogen atom, a halogen atom, or the others; A represents an alkyl group optionally substituted by aryl group or the others, an aryl group, or the others; and one of X and Y represents a di-substituted alkylaminocarbonyl group, or the others, and the other represents a hydrogen atom, an alkyl group, an alkylcarbonyl group, or the others); a medicament or a pharmaceutical composition for treatment or prophylaxis of FAAH-related diseases such as depression, anxiety disorder or pains, comprising the compound or the like as an active ingredient; a use of the compound or the like; and a method for treatment or prophylaxis using the compound or the like.
    Type: Application
    Filed: September 8, 2010
    Publication date: July 5, 2012
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Keiji Aachi, Yoko Nakai, Tomoyuki Furuta, Yuki Fujii
  • Publication number: 20120129807
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.
    Type: Application
    Filed: October 20, 2011
    Publication date: May 24, 2012
    Inventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
  • Publication number: 20120122840
    Abstract: The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.
    Type: Application
    Filed: September 23, 2011
    Publication date: May 17, 2012
    Applicant: Myrexis, Inc.
    Inventors: Dange Vijay Kumar, Ian A. McAlexander, Matthew Gregory Bursavich, Christophe Hoarau, Paul M. Slattum, David A. Gerrish, Jeffrey W. Lockman, Weston R. Judd, Michael Saunders, Daniel P. Parker, Daniel Feodore Zigar, In Chul Kim, J. Adam Willardsen, Kraig M. Yager, Mark D. Shenderovich, Brandi L. Williams, Keith D. Tardif
  • Publication number: 20120122810
    Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
  • Patent number: 8153628
    Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted xanthines of formula I: or pharmaceutically acceptable salts thereof, wherein: Z is selected from the group consisting of oxazoyl, isoxazoyl, thiazolyl, and isothiazoyl; and Z1 is a 5-14 member substituted or unsubstituted heteroaryl ring; which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: April 10, 2012
    Assignee: Forest Laboratories Holdings Limited
    Inventors: Guoquan Wang, Jayson M Rieger, Robert D Thompson
  • Publication number: 20120059001
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: November 9, 2011
    Publication date: March 8, 2012
    Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
  • Publication number: 20120004212
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: August 26, 2011
    Publication date: January 5, 2012
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120004247
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: August 26, 2011
    Publication date: January 5, 2012
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20110319394
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.
    Type: Application
    Filed: June 22, 2011
    Publication date: December 29, 2011
    Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
  • Publication number: 20110312980
    Abstract: Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands.
    Type: Application
    Filed: July 6, 2011
    Publication date: December 22, 2011
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventor: Gabriela Chiosis
  • Publication number: 20110301183
    Abstract: A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 8, 2011
    Inventors: Kyriacos C. Nicolaou, Benjamin Pratt, Stellios Arseniyadis
  • Patent number: 8071609
    Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: December 6, 2011
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
  • Patent number: 8044061
    Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: October 25, 2011
    Assignee: UCB Pharma GmbH
    Inventors: Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
  • Publication number: 20110189255
    Abstract: Drug eluting stents (DES) useful for the treatment of restenosis are described. The stents comprise biocompatible polymers and adenosine receptor modulators.
    Type: Application
    Filed: October 1, 2010
    Publication date: August 4, 2011
    Inventors: Michael STUREK, Kinam PARK
  • Publication number: 20110172241
    Abstract: The present invention relates to compounds of the general formulas (I), (Ia) and (II) and salts and physiologically functional derivatives thereof, wherein the substituents —Y are attached to the 5- or 6-position of the benzazole.
    Type: Application
    Filed: March 23, 2011
    Publication date: July 14, 2011
    Applicant: 4SC AG
    Inventors: Thomas HERZ, Rolf KRAUSS, Michael KUBBUTAT, Martin LANG, Christoph SCHAECHTELE, Stefan TASLER, Frank TOTZKE
  • Publication number: 20110151018
    Abstract: The present invention is directed towards methods of inhibiting thermo- and chemo-sensing in insects and pests by inhibiting TRPA1 ion gated channel or family members. The present invention is also directed towards methods of insect control by modulating the TRPA1 ion gated channel or family members. The methods are applicable to a wide variety of insects and pests including agricultural and horticultural pests.
    Type: Application
    Filed: December 10, 2010
    Publication date: June 23, 2011
    Applicant: BRANDEIS UNIVERSITY
    Inventors: Paul Garrity, KyeongJin Kang