The Additional Chalcogen Containing Hetero Ring Is Part Of A Polycyclo Ring System Patents (Class 514/263.24)
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Patent number: 11466006Abstract: 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: GrantFiled: May 1, 2020Date of Patent: October 11, 2022Assignee: RHIZEN PHARMACEUTICALS AGInventors: Swaroop K. Vakkalanka, Prashant K. Bhavar, Srikant Viswanadha, Govindarajulu Babu
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Patent number: 10953031Abstract: 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: GrantFiled: March 14, 2019Date of Patent: March 23, 2021Assignees: Astrocyte Pharmaceuticals, Inc., The Board of Regents of the University of Texas SystemInventors: William S. Korinek, James D. Lechleiter, Theodore E. Liston
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Patent number: 10851107Abstract: 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: GrantFiled: August 8, 2017Date of Patent: December 1, 2020Assignee: RHIZEN PHARMACEUTICALS SAInventors: Swaroop K. Vakkalanka, Prashant K. Bhavar, Srikant Viswanadha, Govindarajulu Babu
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Patent number: 10532103Abstract: 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: GrantFiled: April 21, 2017Date of Patent: January 14, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
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Patent number: 9926321Abstract: 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: GrantFiled: May 20, 2016Date of Patent: March 27, 2018Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Weilin Sun, Tony Taldone, Pallav Patel, Gabriela Chiosis
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Patent number: 9630965Abstract: 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: GrantFiled: July 1, 2016Date of Patent: April 25, 2017Assignee: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Patent number: 9402832Abstract: 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: GrantFiled: April 8, 2015Date of Patent: August 2, 2016Assignee: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Patent number: 9346808Abstract: 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: GrantFiled: April 5, 2012Date of Patent: May 24, 2016Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Weilin Sun, Tony Taldone, Pallav Patel, Gabriela Chiosis
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Publication number: 20150119406Abstract: 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: ApplicationFiled: September 30, 2014Publication date: April 30, 2015Inventors: Duy H. Hua, Lee-way Jin, Izumi Maezawa, Xinmin Xie
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Publication number: 20150045355Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.Type: ApplicationFiled: December 31, 2011Publication date: February 12, 2015Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
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Publication number: 20140378452Abstract: 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: ApplicationFiled: September 10, 2014Publication date: December 25, 2014Inventor: Gabriela Chiosis
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Publication number: 20140364447Abstract: 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: ApplicationFiled: June 4, 2014Publication date: December 11, 2014Inventors: Swaroop K. V. S. VAKKALANKA, Prashant K. BHAVAR, Srikant VISWANADHA, Govindarajulu BABU
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Publication number: 20140315929Abstract: 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: ApplicationFiled: April 27, 2012Publication date: October 23, 2014Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventor: Gabriela Chiosis
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Publication number: 20140296177Abstract: 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: ApplicationFiled: September 21, 2012Publication date: October 2, 2014Inventors: 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
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Publication number: 20140227183Abstract: 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: ApplicationFiled: April 18, 2014Publication date: August 14, 2014Applicant: MEMORIAL SLOAN KETTERING CANCER CENTERInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
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Publication number: 20140228320Abstract: 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: ApplicationFiled: April 15, 2014Publication date: August 14, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: 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
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Patent number: 8703942Abstract: 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: GrantFiled: November 4, 2010Date of Patent: April 22, 2014Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
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Publication number: 20140088121Abstract: 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: ApplicationFiled: April 5, 2012Publication date: March 27, 2014Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Weilin Sun, Tony Taldone, Pallav Patel, Gabriela Chiosis
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Patent number: 8680076Abstract: 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: GrantFiled: October 20, 2011Date of Patent: March 25, 2014Assignee: Signal Pharmaceuticals, LLCInventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
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Publication number: 20140080827Abstract: 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: ApplicationFiled: November 26, 2013Publication date: March 20, 2014Applicant: Rhizen Pharmaceuticals SAInventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20140045867Abstract: 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: ApplicationFiled: April 5, 2012Publication date: February 13, 2014Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Tony Taldone, Gabriela Chiosis
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Patent number: 8642607Abstract: 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: GrantFiled: November 9, 2011Date of Patent: February 4, 2014Assignee: Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20130303555Abstract: 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: ApplicationFiled: July 23, 2013Publication date: November 14, 2013Inventors: Robert A. Copeland, Victoria M. Richon, Margaret D. Scott, Christopher J. Sneeringer, Kevin W. Kuntz, Sarah K. Knutson, Roy M. Pollock
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Patent number: 8476285Abstract: 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: GrantFiled: June 30, 2009Date of Patent: July 2, 2013Assignee: 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
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Publication number: 20130165427Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: August 24, 2012Publication date: June 27, 2013Applicant: HYDRA BIOSCIENCES, INC.Inventor: Jayhong A. Chong
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Publication number: 20130123283Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.Type: ApplicationFiled: April 11, 2012Publication date: May 16, 2013Inventors: Magdalene M. Moran, Christopher Fanger, Jayhong A. Chong, Colleen McNamara, Xiaoguang Zhen, Josh Mendel-Brehm
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Publication number: 20130109704Abstract: 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: ApplicationFiled: December 19, 2012Publication date: May 2, 2013Applicant: NEUROSEARCH A/SInventor: NeuroSearch A/S
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Publication number: 20130053406Abstract: 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: ApplicationFiled: August 23, 2010Publication date: February 28, 2013Applicant: Myrexis, Inc.Inventors: SE-HO KIM, Herbert L. Ley, III, Ashok Bajji
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Patent number: 8318750Abstract: 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: GrantFiled: August 26, 2011Date of Patent: November 27, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20120295915Abstract: 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: ApplicationFiled: November 22, 2010Publication date: November 22, 2012Inventors: Amita M. Chaudhari, Jason Hallman, Christopher P. Laudeman, David Lee Musso, Cynthia A. Parrish
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Publication number: 20120289496Abstract: 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: ApplicationFiled: May 4, 2012Publication date: November 15, 2012Applicant: Rhizen Pharmaceuticals SAInventors: Dhanapalan NAGARATHNAM, Swaroop Kumar V.S. Vakkalanka, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Prashant K. Bhavar
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Patent number: 8258141Abstract: 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: GrantFiled: April 19, 2007Date of Patent: September 4, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20120202785Abstract: 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: ApplicationFiled: February 8, 2012Publication date: August 9, 2012Inventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
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Patent number: 8217050Abstract: 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: GrantFiled: November 5, 2007Date of Patent: July 10, 2012Assignee: Chroma Therapeutics LimitedInventors: David Festus Charles Moffat, Simon Christopher Hirst, Stuart Thomas Onions
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Publication number: 20120172347Abstract: 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: ApplicationFiled: September 8, 2010Publication date: July 5, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Keiji Aachi, Yoko Nakai, Tomoyuki Furuta, Yuki Fujii
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Publication number: 20120129807Abstract: 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: ApplicationFiled: October 20, 2011Publication date: May 24, 2012Inventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
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Publication number: 20120122810Abstract: 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: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Publication number: 20120122840Abstract: The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.Type: ApplicationFiled: September 23, 2011Publication date: May 17, 2012Applicant: 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
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Patent number: 8153628Abstract: 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: GrantFiled: July 22, 2009Date of Patent: April 10, 2012Assignee: Forest Laboratories Holdings LimitedInventors: Guoquan Wang, Jayson M Rieger, Robert D Thompson
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Publication number: 20120059001Abstract: 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: ApplicationFiled: November 9, 2011Publication date: March 8, 2012Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20120004247Abstract: 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: ApplicationFiled: August 26, 2011Publication date: January 5, 2012Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20120004212Abstract: 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: ApplicationFiled: August 26, 2011Publication date: January 5, 2012Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20110319394Abstract: 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: ApplicationFiled: June 22, 2011Publication date: December 29, 2011Inventors: 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
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Publication number: 20110312980Abstract: Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands.Type: ApplicationFiled: July 6, 2011Publication date: December 22, 2011Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventor: Gabriela Chiosis
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Publication number: 20110301183Abstract: 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: ApplicationFiled: August 19, 2011Publication date: December 8, 2011Inventors: Kyriacos C. Nicolaou, Benjamin Pratt, Stellios Arseniyadis
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Patent number: 8071609Abstract: 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: GrantFiled: August 11, 2006Date of Patent: December 6, 2011Assignee: 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
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Patent number: 8044061Abstract: 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: GrantFiled: December 21, 2007Date of Patent: October 25, 2011Assignee: UCB Pharma GmbHInventors: Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
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Publication number: 20110189255Abstract: Drug eluting stents (DES) useful for the treatment of restenosis are described. The stents comprise biocompatible polymers and adenosine receptor modulators.Type: ApplicationFiled: October 1, 2010Publication date: August 4, 2011Inventors: Michael STUREK, Kinam PARK
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Publication number: 20110172241Abstract: 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: ApplicationFiled: March 23, 2011Publication date: July 14, 2011Applicant: 4SC AGInventors: Thomas HERZ, Rolf KRAUSS, Michael KUBBUTAT, Martin LANG, Christoph SCHAECHTELE, Stefan TASLER, Frank TOTZKE
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Publication number: 20110151018Abstract: 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: ApplicationFiled: December 10, 2010Publication date: June 23, 2011Applicant: BRANDEIS UNIVERSITYInventors: Paul Garrity, KyeongJin Kang