At Least Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 548/360.5)
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Patent number: 12139493Abstract: The present invention relates to novel fused imidazo pyrazole derivatives of formula (I), and formula (II), and methods for preparation thereof, in the presence of a chitosan-Al2O3 nanocomposite film. The invention also relates to pharmaceutical compositions comprising compounds of the invention as active ingredients as well as the use of compounds of the invention for antimicrobial action.Type: GrantFiled: October 16, 2023Date of Patent: November 12, 2024Assignee: Imam Abdulrahman Bin Faisal UniversityInventors: Abir Said Ibrahim Abdel-Naby, Sara Nabil
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Patent number: 12103932Abstract: The present invention relates to novel fused imidazo pyrazole derivatives of formula (I), and formula (II), and methods for preparation thereof, in the presence of a chitosan-Al2O3 nanocomposite film. The invention also relates to pharmaceutical compositions comprising compounds of the invention as active ingredients as well as the use of compounds of the invention for antimicrobial action.Type: GrantFiled: April 2, 2024Date of Patent: October 1, 2024Assignee: Imam Abdulrahman Bin Faisal UniversityInventors: Abir Said Ibrahim Abdel-Naby, Sara Nabil
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Patent number: 11987585Abstract: The present invention relates to novel fused imidazo pyrazole derivatives of formula (I), and formula (II), and methods for preparation thereof, in the presence of a chitosan-Al2O3 nanocomposite film. The invention also relates to pharmaceutical compositions comprising compounds of the invention as active ingredients as well as the use of compounds of the invention for antimicrobial action.Type: GrantFiled: February 9, 2023Date of Patent: May 21, 2024Assignee: Imam Abdulrahman Bin Faisal UniversityInventors: Abir Said Ibrahim Abdel-Naby, Sara Nabil
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Patent number: 11974985Abstract: The present invention relates to a composition of a compound of general formula (A), a pharmaceutically acceptable salt or a prodrug, and a preparation method therefor.Type: GrantFiled: January 30, 2019Date of Patent: May 7, 2024Assignee: HAISCO PHARMACEUTICAL GROUP CO., LTD.Inventors: Yi Mo, Honghu Li, Xing Wan, Fei Ye
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Patent number: 10787460Abstract: The present invention provides novel CDK7 inhibitors and pharmaceutical compositions thereof: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 26, 2019Date of Patent: September 29, 2020Assignee: Eli Lilly and CompanyInventors: David Andrew Coates, Carlos Montero, Bharvin Kumar Rameschandra Patel, David Michael Remick, Yipin Yadav
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Publication number: 20150126371Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.Type: ApplicationFiled: May 29, 2013Publication date: May 7, 2015Inventors: Matthias Witschel, Frank Stelzer, Johannes Hutzler, Tao Qu, Thomas Mietzner, Klaus Kreuz, Klaus Grossmann, Raphael Aponte, Hans Wolfgang Hoeffken, Frederick Calo, Thomas Ehrhardt, Anja Simon, Liliana Parra Rapado
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Patent number: 9012487Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.Type: GrantFiled: March 2, 2007Date of Patent: April 21, 2015Assignee: Nerviano Medical Sciences S.r.l.Inventors: Tiziano Bandiera, Jay Aaron Bertrand, Paolo Pevarello, Ettore Perrone, Andrea Lombardi Borgia, Sten Christian Orrenius, Mauro Angiolini, Daniele Fancelli
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Publication number: 20150099891Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.Type: ApplicationFiled: October 6, 2014Publication date: April 9, 2015Inventors: Itzia Z. Arroyo, Davida Krueger, Ping Chen, Aaron J. Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
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Publication number: 20150065482Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: August 22, 2014Publication date: March 5, 2015Applicant: GENENTECH, INC.Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
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Patent number: 8969341Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: November 28, 2012Date of Patent: March 3, 2015Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20150045327Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: August 5, 2014Publication date: February 12, 2015Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
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Publication number: 20150011590Abstract: The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: February 12, 2013Publication date: January 8, 2015Applicant: Merck Sharp & Dohme CorporationInventors: Ann E. Weber, Tesfaye Biftu
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Publication number: 20140357662Abstract: The present invention provides compounds of formula (I): wherein A, R1, R2, R3 IX, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.Type: ApplicationFiled: November 15, 2012Publication date: December 4, 2014Inventors: Derek Edward John, Basil Hartzoulakis, Simon D. Edwards
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Publication number: 20140350010Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: November 28, 2012Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Patent number: 8895603Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.Type: GrantFiled: June 25, 2012Date of Patent: November 25, 2014Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
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Publication number: 20140315894Abstract: The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same.Type: ApplicationFiled: December 21, 2012Publication date: October 23, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATEInventors: Dan Theodorescu, Michael Fitzpatrick Wempe, David Ross, Samy Meroueh, Martin A. Schwartz, Phillip Reigan
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Patent number: 8853212Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 17, 2011Date of Patent: October 7, 2014Assignee: Merck Sharp & Dohme CorpInventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Patent number: 8809337Abstract: There are provided bicyclic carbonylamino-pyrazoles of formula (I), wherein the variables are as specified in the claims, for use as medicament, in particular for the treatment of diseases due to the malfunctioning of protein kinases (PKs), such as cancer, pharmaceutical compositions comprising such carbamoyl derivatives, and their use as prodrugs of therapeutically active agents. Method of treatment and some new bicyclic carbonylamino-pyrazoles are also object of the present invention.Type: GrantFiled: September 28, 2012Date of Patent: August 19, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Maurizio Pulici, Paolo Polucci
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Publication number: 20140107346Abstract: A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: ApplicationFiled: June 25, 2012Publication date: April 17, 2014Applicants: Merck Sharp & Dohme Ltd., Merck Sharp & Dohme Corp.Inventors: Michael J. Zacuto, Robert F. Dunn, Aaron J. Moment, Jacob M. Janey, David Lieberman, Faye Sheen, Nadine Bremeyer, Jeremy Scott, Jeffrey T. Kuethe
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Publication number: 20140100211Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.Type: ApplicationFiled: October 1, 2013Publication date: April 10, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Publication number: 20140080884Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.Type: ApplicationFiled: June 25, 2012Publication date: March 20, 2014Applicants: Merck Sharp & Dohme Ltd., Merck Sharp & Dohme Corp.Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
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Publication number: 20140051688Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui
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Patent number: 8653127Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: January 14, 2010Date of Patent: February 18, 2014Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Patent number: 8642779Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein A, B, Q, R1, and R2 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT or PDK1 kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds, and methods of utilizing those compositions in the treatment of various disorders.Type: GrantFiled: December 9, 2009Date of Patent: February 4, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Simon Everitt, Francesca Mazzei, Daniel Robinson
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Patent number: 8623876Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: GrantFiled: June 13, 2012Date of Patent: January 7, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ron Ferguson, Helena Posteri
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Patent number: 8592422Abstract: In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: December 16, 2011Date of Patent: November 26, 2013Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James MacDonald, Han Min Tong, Carrie K. Jones, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Chrysa Malosh
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Patent number: 8592371Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 7, 2013Date of Patent: November 26, 2013Assignee: Merck Sharpe & Dohme Corp.Inventors: Tesfaye Biftu, Ann E. Weber
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Patent number: 8563730Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: May 15, 2009Date of Patent: October 22, 2013Assignee: Takeda San Diego, Inc.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
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Patent number: 8557857Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: GrantFiled: July 29, 2008Date of Patent: October 15, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Patent number: 8546442Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.Type: GrantFiled: December 16, 2011Date of Patent: October 1, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Rajashekhar Betageri, Brian Nicholas Cook, Darren DiSalvo, Christian Harcken, Daniel Kuzmich, Pingrong Liu, John Lord, Can Mao, Hossein Razavi
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Patent number: 8541445Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: November 4, 2011Date of Patent: September 24, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Philip Collier
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Patent number: 8481584Abstract: Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: February 24, 2012Date of Patent: July 9, 2013Assignee: Nerviano Medical Sciences S.R.L.Inventors: Daniele Fancelli, Paola Vianello, Mario Varasi, Simona Bindi, Sergio Vioglio, Dania Tesei
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Patent number: 8461193Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: GrantFiled: May 17, 2011Date of Patent: June 11, 2013Assignee: Nerviano Medical Sciences S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Sten Christian Orrenius, Ettore Perrone, Italo Beria, Daniele Fancelli, Arturo Galvani
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Patent number: 8455533Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: August 23, 2010Date of Patent: June 4, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ping Chen, Danqing Feng, Xiaoxia Qian
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Patent number: 8415386Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein all of the variables are defined herein.Type: GrantFiled: October 8, 2009Date of Patent: April 9, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Pratik Devasthale, William N. Washburn, Wei Wang, Andres Hernandez, Saleem Ahmad, Guohua Zhao
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Patent number: 8415297Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 17, 2012Date of Patent: April 9, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ann E. Weber
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Patent number: 8404856Abstract: Heteroaromatic compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein ring A is: (ii-a), (ii-b), (ii-c), (ii-d), or (ii-e); and wherein n, L, M, U, X, Y, Z, RE, RF, R1, R2A, R2B, R2C, R3, R8, R9 and R10 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts and prodrugs are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts and prodrugs can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: November 14, 2008Date of Patent: March 26, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Thomas J. Tucker, Robert Tynebor, John T. Sisko, Neville Anthony, Robert Gomez, Samson M. Jolly
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Publication number: 20130012507Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Publication number: 20120277240Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: February 17, 2011Publication date: November 1, 2012Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20120277248Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: ApplicationFiled: June 13, 2012Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Michele CARUSO, Italo BERIA, Maria Gabriella BRASCA, Ron FERGUSON, Helena POSTERI
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Publication number: 20120214824Abstract: The present invention is directed to compounds of Formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.Type: ApplicationFiled: December 8, 2011Publication date: August 23, 2012Inventors: Bradley Tait, Christopher Borella, Robert Chambers, Matthew Cullen
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Publication number: 20120202815Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Y is a 5-membered, fully or partially unsaturated heterocyclic ring containing 2-4 carbon atoms and 2-3 nitrogen atoms as ring members, the ring substituted with Z on a ring member atom connected through an adjacent single ring member atom to the ring member atom attaching the heterocyclic ring to the phenyl ring of Formula 1, and optionally further substituted with up to 2 substituents independently selected from R5 on carbon atom ring members and from R6 on nitrogen atom ring members; Z is an 8-, 9-, 10- or 11-membered fused heterobicyclic ring system containing ring members selected from carbon atoms and 1 to 4 heteroatoms independently selected from up to 2O, up to 2S and up to 4 N atoms, wherein up to 3 carbon atom ring members are independently selected from C(?O) and C(?S), and the sulfur atom ring members are independently selected from S(?O)u(?NR7)z, the ring system optionally substituted wiType: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Applicant: E.I.DU PONT DE NEMOURS AND COMPANYInventors: John Lawrence Andreassi II, Andrew Edmund Taggi
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Patent number: 8227472Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: GrantFiled: October 9, 2007Date of Patent: July 24, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ron Ferguson, Helena Posteri
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Patent number: 8211926Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: June 16, 2010Date of Patent: July 3, 2012Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Publication number: 20120149734Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: August 23, 2010Publication date: June 14, 2012Inventors: Tesfaye Biftu, Ping Chen, Danqing Feng, Xiaoxia Qian
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Publication number: 20120149637Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: February 17, 2012Publication date: June 14, 2012Inventors: Tesfaye Biftu, Ping Chen, Jason M. Cox, Ann E. Weber
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Patent number: 8183255Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: GrantFiled: February 4, 2008Date of Patent: May 22, 2012Assignee: Pfizer, Inc.Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
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Patent number: 8143289Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 12, 2009Date of Patent: March 27, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ping Chen, Jason M. Cox, Ann E. Weber
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Patent number: 8138217Abstract: Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: February 3, 2005Date of Patent: March 20, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Daniele Fancelli, Paola Vianello, Mario Varasi, Simona Bindi, Sergio Vioglio, Dania Tesei
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Patent number: 8119641Abstract: Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C?O, or —C(?O)NH—; —R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Aurora kinases activity or IGF-1R activity, like cancer.Type: GrantFiled: May 25, 2007Date of Patent: February 21, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Daniele Fancelli, Maurizio Pulici, Jürgen Moll, Tiziano Bandiera