Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
Type:
Application
Filed:
July 25, 2014
Publication date:
January 29, 2015
Applicant:
GENENTECH, INC.
Inventors:
Joachim Rudolph, Lewis J. Gazzard, James J. Crawford, Chudi Ndubaku, Joy Drobnick, Wendy Lee
Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
Type:
Application
Filed:
January 22, 2013
Publication date:
January 22, 2015
Applicant:
MERCK PATENT GMBH
Inventors:
Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
Abstract: The present application relates to novel substituted azabicycles, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
Type:
Application
Filed:
March 5, 2013
Publication date:
January 22, 2015
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
Abstract: A heterocyclic compound represented by the general formula (In the formula, R1, R2 and R3 may be the same or different, and each represents a hydrogen atom, a halogen atom, or this general formula (X1—Y1—R4) (in the formula: X1 represents this general formula (NR5) (in the formula, R5 represents a hydrogen atom, etc.) or the like; Y1 represents an optionally substituted C1-6 alkylene group or the like; and R4 represents an optionally substituted aryl group or the like), and Z represents a nitrogen atom or this general formula (CR6) (in the formula, R6 represents a hydrogen atom, a halogen atom, or an optionally substituted C1-12 alkyl group or the like)), or a salt thereof, exhibits excellent anti-HIV activity and is useful as an anti-HIV agent.
Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
Type:
Application
Filed:
March 7, 2013
Publication date:
January 15, 2015
Inventors:
Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
Abstract: Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde or a derivative thereof, b) forming an anhydro dimer of the provided salicylaldehyde compound, c) performing one or more chemical transformations on the anhydro dimer and d) hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a).
Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.
Type:
Grant
Filed:
June 9, 2011
Date of Patent:
December 16, 2014
Assignee:
Afraxis Holdings, Inc.
Inventors:
David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
Abstract: The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
Type:
Application
Filed:
August 20, 2014
Publication date:
December 4, 2014
Applicant:
FAB PHARMA S.A.S.
Inventors:
Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
Abstract: This invention relates to piperidino-pyhmidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
Type:
Application
Filed:
February 7, 2013
Publication date:
November 27, 2014
Inventors:
David Craig Mc Gowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Mourad Daoubi Khamlichi
Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Application
Filed:
August 8, 2014
Publication date:
November 27, 2014
Applicant:
NOVARTIS AG
Inventors:
Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian HURLEY, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
Abstract: The present application relates to novel fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
Type:
Application
Filed:
July 5, 2011
Publication date:
November 27, 2014
Applicant:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Walter Kroh, Lars Bärfacker
Abstract: Compounds useful as antiproliferative agents according to Formula (I), wherein n, A, R1, R2, and Ar1 are as defined herein, and salts thereof; antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.
Type:
Grant
Filed:
December 17, 2010
Date of Patent:
November 18, 2014
Assignee:
Temple University—Of The Commonwealth System Of Higher Education
Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119.
Type:
Application
Filed:
November 9, 2012
Publication date:
November 6, 2014
Inventors:
Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
Abstract: A compound represented by Formula 1. An organic electric element includes a first electrode, a second electrode, and an organic material layer between the first electrode and the second electrode. The organic material layer includes the compound represented by Formula 1. When the organic electric element includes the compound in the organic material layer, luminous efficiency, stability, and life span can be improved.
Type:
Application
Filed:
November 13, 2012
Publication date:
November 6, 2014
Inventors:
Junghwan Park, Sunhee Lee, Soungyun Mun, Daesung Kim, Hwasoon Jung, Wonsam Kim, Jihun Byun, Bumsung Lee
Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).
Type:
Grant
Filed:
March 15, 2013
Date of Patent:
November 4, 2014
Assignees:
Genosco, Oscotec, Inc.
Inventors:
Hong Woo Kim, Hee Kyu Lee, Ho-Juhn Song, Jaekyoo Lee, Jong Sung Koh, Jung-Ho Kim, Se Won Kim, In Yong Lee
Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders using such compounds.
Type:
Application
Filed:
April 30, 2014
Publication date:
October 30, 2014
Applicant:
GENENTECH, INC.
Inventors:
James J. CRAWFORD, Wendy LEE, Joachim RUDOLPH
Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
Type:
Application
Filed:
April 30, 2014
Publication date:
October 30, 2014
Applicant:
AFRAXIS HOLDINGS, INC.
Inventors:
Sergio DURÓN, David CAMPBELL, Chudi NDUBAKU, Joachim RUDOLPH
Abstract: Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.
Type:
Application
Filed:
November 12, 2012
Publication date:
October 23, 2014
Inventors:
Meizhong Jin, Mridula Kadalbajoo, An-Hu Li, Mark J. Mulvihill, Kam W. Siu, Arno G. Steinig, Jing Wang
Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
Abstract: Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, respiratory conditions, and others.
Type:
Grant
Filed:
March 1, 2010
Date of Patent:
October 14, 2014
Assignee:
Evotec AG
Inventors:
Michael G. Kelly, John Kincaid, Carl J. Kaub
Abstract: The present invention relates to 1.5 hydrate of of 1-{(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl]-4-oxobutyl}-5,5-difluoropiperidin-2-one tartrate, a process for preparing the same, and a pharmaceutical composition for inhibiting DPP-IV, which comprises said compound as the active component.
Type:
Grant
Filed:
October 31, 2011
Date of Patent:
October 14, 2014
Assignee:
LG Life Sciences Ltd.
Inventors:
Ki Sook Park, Jung Min Yun, Bong Chan Kim, Kyu Young Kim, Ji Hye Lee
Abstract: 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:
Grant
Filed:
February 17, 2011
Date of Patent:
October 7, 2014
Assignee:
Merck Sharp & Dohme Corp
Inventors:
Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
Abstract: The present invention relates to methods for synthesizing energetic compounds and intermediates thereof. Specifically, the present invention relates to methods for synthesizing adamantanes and intermediates that are useful in such synthesis. Synthesized intermediates are useful in the synthesis of bicyclic and tricyclic substituted adamantanes. Examples of various intermediates are: acyclic 2-nitromalonaldehyde intermediates, 2,6,9-tri-substituted-4,8-dinitro-2,6,9-triazabicyclo[3.3.1]nona-3,7-dienes and 2,6-dinitro-4,8,9,10-tetra-aza-4,8,9,10-tetra-substituted adamantanes. Intermediates synthesized according to the methods of the present invention are useful toward the synthesis of tetraaza-adamantanes, which can serve as precursors to potentially superior new high-energy-density compounds (HEDCs). The tricyclic intermediate compound has a structure of Formula III: where R is one of a benzyl, 4-methoxybenzyl, acetyl, nitro, formyl, allyl, and a carboethoxyl group.
Type:
Grant
Filed:
February 25, 2011
Date of Patent:
October 7, 2014
Assignee:
The United States of America as Represented by the Secretary of the Navy
Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4 and A1 to A5 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
Type:
Application
Filed:
March 26, 2014
Publication date:
October 2, 2014
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Christian SMETHURST, Harald ENGELHARDT, Davide GIANNI, Ulrich REISER
Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
Type:
Application
Filed:
March 14, 2014
Publication date:
October 2, 2014
Applicants:
Sanofi, Celgene Avilomics Research, Inc.
Inventors:
Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
July 19, 2012
Date of Patent:
September 30, 2014
Assignee:
Novartis AG
Inventors:
Christopher Michael Adams, Veronique Darsigny, Alec Nathanson Flyer, Christine Fang Gelin, Timothy Brian Hurley, Nan Ji, Rajeshri Ganesh Karki, Toshio Kawanami, Erik Meredith, Chang Rao, Michael H. Serrano-Wu, Catherine Fooks Solovay
Abstract: The present invention is directed to a compound of Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
Type:
Application
Filed:
March 14, 2014
Publication date:
September 18, 2014
Applicant:
JANSSEN PHARMACEUTICA NV
Inventors:
Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Michael A. Letavic, Dale A. Rudolph, Brock T. Shireman, Brice M. Stenne, Jeannie M. Ziff
Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
Type:
Grant
Filed:
October 8, 2010
Date of Patent:
September 16, 2014
Assignee:
GlaxoSmithKline LLC
Inventors:
Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
Abstract: Certain 2-aminopyrimidine compounds of formula (I) are serotonin receptor modulators useful in the treatment of diseases mediated by serotonin receptors.
Type:
Grant
Filed:
October 29, 2009
Date of Patent:
September 9, 2014
Assignee:
Janssen Pharmaceutica NV
Inventors:
Nicholas I. Carruthers, Gregor J. MacDonald, Brock T. Shireman, Vi T. Tran
Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.
Type:
Application
Filed:
February 26, 2014
Publication date:
September 4, 2014
Inventors:
Andrew TASKER, Ryan WURZ, Liping H. PETTUS, Bradley J. HERBERICH
Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
September 8, 2010
Date of Patent:
August 19, 2014
Assignee:
Novartis AG
Inventors:
Karen Miller-Moslin, Bakary-Barry Toure, Michael Scott Visser, Naeem Yusuff
Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.
Type:
Application
Filed:
August 2, 2013
Publication date:
August 14, 2014
Applicants:
University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
Inventors:
Sandhya Kortagere, Eldo V. Kuzhikandahil
Abstract: Compounds of the formula I in which Het, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of RON and can be employed, for the treatment of cancer
Type:
Application
Filed:
June 15, 2012
Publication date:
August 14, 2014
Applicant:
MERCK PATENT GMBH
Inventors:
Wolfgang Stahle, Oliver Schadt, Christine Knuehl, Manja Friese-Hamim, Bayard Huck, Andreas Goutopoulos, Nadia Brugger
Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
Type:
Grant
Filed:
July 11, 2013
Date of Patent:
August 12, 2014
Assignee:
Blueprint Medicines Corporation
Inventors:
Neil Bifulco, Jr., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
Abstract: The present invention provides compounds of formula 1 as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula 1 can be employed as therapeutics in human and veterinary medicine, where they can be used, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
Type:
Application
Filed:
January 30, 2014
Publication date:
August 7, 2014
Applicant:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
Type:
Grant
Filed:
June 4, 2012
Date of Patent:
August 5, 2014
Assignee:
Exelixis Patent Company LLC
Inventors:
Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
Type:
Grant
Filed:
October 8, 2010
Date of Patent:
August 5, 2014
Assignee:
GlaxoSmithKline LLC
Inventors:
Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
Abstract: A phosphorescent metal complex is provided, which comprises a metallic central atom M and at least one ligand coordinated by the metallic central atom M, wherein the one metallic central atom M and the ligand form a six-membered metallacyclic ring. Additionally specified are a radiation-emitting component comprising a metal complex, and a process for preparing the metal complex.
Type:
Application
Filed:
March 14, 2014
Publication date:
July 31, 2014
Applicant:
OSRAM Opto Semiconductors GmbH
Inventors:
Jürgen ADLER, Andreas KANITZ, Günter SCHMID, Oksana FREYDENZON, Anna MALTENBERGER
Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
Type:
Application
Filed:
September 4, 2013
Publication date:
July 31, 2014
Applicant:
ABBVIE INC.
Inventors:
David A. DEGOEY, Pamela L. DONNER, Warren M. KATI, Charles W. HUTCHINS, Allan C. KRUEGER, John T. RANDOLPH, Christopher E. MOTTER, Preethi KRISHNAN, Neeta C. MISTRY, Tami J. PILOT-MATIAS, Sachin V. PATEL, Xiaoyan LI, Todd N. SOLTWEDEL, Lissa T. NELSON
Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
Type:
Application
Filed:
September 9, 2013
Publication date:
July 31, 2014
Applicant:
ABBVIE INC.
Inventors:
David A. DEGOEY, Pamela L. DONNER, Warren M. KATI, Charles W. HUTCHINS, Mark A. MATULENKO, Tammie K. JINKERSON, Ryan G. KEDDY
Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
Type:
Application
Filed:
April 16, 2014
Publication date:
July 31, 2014
Applicant:
Celgene Avilomics Research, Inc.
Inventors:
Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
Abstract: The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
Type:
Grant
Filed:
May 31, 2011
Date of Patent:
July 29, 2014
Assignee:
Merck Patent GmbH
Inventors:
Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
Abstract: The invention relates to compounds of formula (I) wherein X, R1, R2, T, m, n, o have the meaning as cited in the description and the claims. The compounds of formula (I) are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
Type:
Grant
Filed:
March 12, 2010
Date of Patent:
July 22, 2014
Assignee:
Cellzome Limited
Inventors:
Rosemary Lynch, Andrew David Cansfield, Helen Sarah Niblock, Daniel Hardy, Jane Elizabeth Scanlon, Rita Adrego, Nigel Ramsden
Abstract: The present invention provides compounds of the Formula I: wherein X is a bond or CH2; R is selected from the group consisting of R1 and R2 are each independently selected from the group consisting of CH and N; R3 is H or CH3; R4 is H or CH3; L is selected from the group consisting of —O(CH2)3—, —C(O)NH(CH2)2—, —CH2C(O)NH(CH2)2—, —(CH2)3N(C(O)CH3)CH2—, —(CH2)2N(C(O)CH3)CH2—, —(CH2)3NH—, (CH2)2OCH2—, —(CH2)4—, —(CH2)2NHCH2—, —(CH2)3O—, and —CH2O(CH2)2—; or a pharmaceutically acceptable salt thereof. Compounds of this invention are autotaxin inhibitors.
Type:
Application
Filed:
January 7, 2014
Publication date:
July 17, 2014
Applicant:
Eli Lilly and Company
Inventors:
Thomas James Beauchamp, Yen Dao, Spencer Brian Jones, Bryan Hurst Norman, Lance Allen Pfeifer