Additional Hetero Ring Containing Patents (Class 546/125)
  • Patent number: 8999975
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2 and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are inhibitors of Cathepsin C.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters, Doris Riether, Wolfgang Wienen
  • Patent number: 8987249
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Florian Binder, Matthias Grauert, Marc Grundl, Peter Wilhelm Haebel, Thorsten Oost, Alexander Pautsch, Stefan Peters, Viktor Vintonyak
  • Patent number: 8981102
    Abstract: Provided herein are compounds and methods of preparation of compounds that are capable of functioning as agonists or antagonists of a nicotinic receptor. Also provided are pharmaceutical compositions comprising one or more of these compounds, which may further comprise one or more additional therapeutic agents. Further provided are methods of treatment of various conditions that may be responsive to such activity at the nicotinic receptors, such as nicotine dependence.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: March 17, 2015
    Assignee: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Pauline Wanjiku Ondachi
  • Patent number: 8921544
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: December 30, 2014
    Assignee: Sareum Limited
    Inventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
  • Patent number: 8853241
    Abstract: The invention relates to biaryl substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: October 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Jianguo Ji, Tao Li, Kevin B. Sippy, Chih-Hung Lee, Murali Gopalakrishnan
  • Patent number: 8846675
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: September 30, 2014
    Assignee: Cymabay Therapeutics, Inc.
    Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
  • Publication number: 20140221420
    Abstract: Compounds that modulate the CCR5 chemokine receptor, pharmaceutical compositions containing them, and uses therefor in the treatment of HIV and related diseases are described.
    Type: Application
    Filed: March 18, 2011
    Publication date: August 7, 2014
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Venkateswararao Kalapala, Jianfeng Li
  • Patent number: 8779143
    Abstract: The present invention provides novel crystalline forms of maraviroc phosphate, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides novel process for the preparation of maraviroc amorphous form and pharmaceutical composition comprising it.
    Type: Grant
    Filed: August 30, 2010
    Date of Patent: July 15, 2014
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Kesireddy Subash Chander Reddy, Bandi Vamsi Krishna
  • Patent number: 8772277
    Abstract: The present invention provides a novel compound having a superior activity as an ERR-? modulator and useful as an agent for the prophylaxis or treatment of ERR-? associated diseases. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: July 8, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shigemitsu Matsumoto, Koji Ono, Yusuke Tominari, Taisuke Katoh, Kazuhiro Miwa, Atsushi Hasuoka, Shinichi Imamura
  • Publication number: 20140171404
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
  • Patent number: 8754220
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: June 17, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang
  • Patent number: 8748457
    Abstract: The present invention is related to novel 2-Amino-2-[8-(dimethyl carbamoyl)-8-aza-bicyclo[3.2.1]oct-3-yl]-exo-ethanoyl derivatives of the general formula (A), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors, which are useful in the treatment or prevention of diseases particularly Type II diabetes, other complications related to diabetes and other pathogenic conditions in which DPP IV enzyme is involved.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: June 10, 2014
    Assignee: Lupin Limited
    Inventors: Neelima Sinha, Prathap Nair, Navnath Karche, Nabendu Saha, Rajan Goel, Rajender Kumar Kamboj
  • Patent number: 8697691
    Abstract: In one aspect, the invention relates to compounds having a general structure: which are useful as selective allosteric or bitopic agonists of the M1 muscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. 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: Grant
    Filed: December 21, 2010
    Date of Patent: April 15, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Michael R. Wood, Rocco D. Gogliotti, Colleen M. Niswender, Bruce J. Melancon, Evan P. Lebois
  • Publication number: 20140093518
    Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
    Type: Application
    Filed: August 26, 2013
    Publication date: April 3, 2014
    Applicant: The Scripps Research Institute
    Inventor: Carlos F. Barbas, III
  • Publication number: 20140030191
    Abstract: A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN? groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.
    Type: Application
    Filed: April 20, 2012
    Publication date: January 30, 2014
    Applicant: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Sylvain Routier, Franck Suzenet, Frederic Pin, Sylvie Chalon, Johnny Vercouillie, Denis Guilloteau
  • Publication number: 20130331349
    Abstract: The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
    Type: Application
    Filed: November 30, 2011
    Publication date: December 12, 2013
    Inventors: David C. Tully, Paul Vincent Rucker, Phillip B. Alper, Daniel Mutnick, Donatella Chianelli
  • Patent number: 8604195
    Abstract: In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Unmesh Shah, Craig D. Boyle, Samuel Chackalamannil
  • Publication number: 20130281428
    Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.
    Type: Application
    Filed: January 30, 2013
    Publication date: October 24, 2013
    Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
  • Publication number: 20130261129
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Application
    Filed: March 29, 2013
    Publication date: October 3, 2013
    Applicant: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Wei, Lijuan Jane Wang
  • Patent number: 8536340
    Abstract: Cyclic amine compounds represented by formula (1) or salts thereof or N-oxides thereof, wherein Cy1 represents an unsubstituted or substituted aromatic ring; X represents oxygen, sulfur, unsubstituted or substituted nitrogen, sulfinyl, or sulfonyl; R1a and R2a, R1a and R4a, R2a and R3a, or R3a and R4a form saturated rings together; R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, and R5 which do not form the saturated rings are each independently hydrogen, hydroxyl, halogen, unsubstituted or substituted amino, nitro, or an organic group; Cy2 represents an unsubstituted or substituted aromatic ring with a proviso that Cy2 is an unsubstituted or substituted heteroaromatic ring when R1a and R2a form a saturated ring together and Cy1 is an unsubstituted or substituted phenyl, and Cy2 is a substituted pyridin-2-yl having one or more cyano as a substituent when Cy1 is an unsubstituted or substituted phenyl and Cy2 is a pyridin-2-yl.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: September 17, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Masahiro Kawaguchi, Daisuke Hanai, Takao Iwasa
  • Publication number: 20130211091
    Abstract: The present invention provides novel crystalline forms of maraviroc phosphate, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides novel process for the preparation of maraviroc amorphous form and pharmaceutical composition comprising it.
    Type: Application
    Filed: August 30, 2010
    Publication date: August 15, 2013
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Kesireddy Subash Chander Reddy, Bandi Vamsi Krishna
  • Publication number: 20130203987
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 8, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rigel Pharmaceuticals, Inc.
  • Publication number: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • Publication number: 20130197217
    Abstract: The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.
    Type: Application
    Filed: September 30, 2011
    Publication date: August 1, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Takeshi Kuwada, Mitsukane Yoshinaga, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki, Naoki Miyakoshi
  • Publication number: 20130197027
    Abstract: In one aspect, the invention relates to compounds which are useful as allosteric or bitopic agonists of the M1 muscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. 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: Application
    Filed: March 10, 2011
    Publication date: August 1, 2013
    Inventors: Craig Lindsley, P. Jeffrey Conn, Colleen M. Niswender, Michael R. Wood, Brian Chauder, Evan P. Lebois
  • Patent number: 8481524
    Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: July 9, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Lauffer, Pan Li, Nathan Waal, Kira Mcginty, Qing Tang, Steven Ronkin, Luc Farmer, Dean Shannon, Dylan Jacobs
  • Publication number: 20130172327
    Abstract: Disclosed are N-1-cyano-2-(phenyl)ethyl)-2-azabicyclo[2.2.1]heptane-3-carboxamides of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory diseases.
    Type: Application
    Filed: September 14, 2012
    Publication date: July 4, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Doris RIETHER, Wolfgang WIENEN
  • Patent number: 8466170
    Abstract: Novel 7-azaindole derivatives of the formula (I), in which U, L, R, Y, X1, X2 and X3 have the meanings indicated in Claim (1), are kinase inhibitors and can be used for the treatment of diseases and conditions such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in any type of fibroses, inflammatory processes, tumors and tumor diseases.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: June 18, 2013
    Assignee: Merck Patent GmbH
    Inventor: Markus Klein
  • Publication number: 20130123268
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1).
    Type: Application
    Filed: March 10, 2011
    Publication date: May 16, 2013
    Applicant: THE UNIVERSITY OF EDINBURGH
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Patent number: 8410094
    Abstract: The present invention pertains to the field of pharmaceutical chemistry and discloses 8-(3-aminopropyl)-3-exo-8-azabicyclo[3.2.1]octane-3-amino amide compounds represented by formula I, the pharmaceutical compositions, the preparation method and the use thereof. Such compounds or pharmaceutically acceptable salts thereof can be used as an antagonist of CCR5 in preparing medicaments for treating diseases mediated by CCR5, particularly HIV infection, asthma, rheumatoid arthritis, autoimmune diseases and chronic obstructive pulmonary diseases (COPD).
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: April 2, 2013
    Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Targetdrug Co., Ltd.
    Inventors: Yaqiu Long, Xing Fan, Dongzhi Feng, Li Chen, Renhai Chen
  • Publication number: 20130072467
    Abstract: The present invention provides a novel compound having a superior activity as an ERR-? modulator and useful as an agent for the prophylaxis or treatment of ERR-? associated diseases. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: August 3, 2012
    Publication date: March 21, 2013
    Inventors: Shigemitsu MATSUMOTO, Koji Ono, Yusuke Tominari, Taisuke Katoh, Kazuhiro Miwa, Atsushi Hasuoka, Shinichi Imamura
  • Publication number: 20130053364
    Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: April 23, 2012
    Publication date: February 28, 2013
    Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
  • Publication number: 20130040986
    Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.
    Type: Application
    Filed: October 15, 2012
    Publication date: February 14, 2013
    Inventors: Hayley Binch, Lev T.D. Fanning, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
  • Patent number: 8367698
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: February 5, 2013
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8362008
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: January 29, 2013
    Assignee: The University Of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Patent number: 8338614
    Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: December 25, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
  • Publication number: 20120322804
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Application
    Filed: May 3, 2012
    Publication date: December 20, 2012
    Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
  • Publication number: 20120251447
    Abstract: The present invention provides novel radio iodinated tropanes incorporating triazole or isoxazole rings. Also provided are methods of preparation of said tropanes from functionalised tropane precursors, using click cycloaddition chemistry, as well as radiopharmaceutical compositions comprising such radio iodinated tropanes. The invention also provides in vivo imaging methods using the radio iodinated tropanes.
    Type: Application
    Filed: December 21, 2010
    Publication date: October 4, 2012
    Inventors: Michelle Emma Avory, Harry John Wadsworth, Robert James Domett Nairne
  • Publication number: 20120238600
    Abstract: The present invention discloses and claims a series of substituted tropinone benzylamines of formula (I): The compounds of this invention are inhibitors of ?-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted tropinone benzylamines.
    Type: Application
    Filed: June 5, 2012
    Publication date: September 20, 2012
    Applicant: SANOFI
    Inventors: Yong Mi CHOI-SLEDESKI, Guyan LIANG, Patrick Wai-Kwok SHUM
  • Publication number: 20120232109
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Application
    Filed: May 23, 2012
    Publication date: September 13, 2012
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20120214805
    Abstract: The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Application
    Filed: October 28, 2010
    Publication date: August 23, 2012
    Inventors: Joel M. Harris, Andrew Stamford, William J. Greenlee, Santhosh Francis Neelamkavil
  • Publication number: 20120172393
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Application
    Filed: September 14, 2010
    Publication date: July 5, 2012
    Applicant: THE UNIVERSITY OF EDINBURGH
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Patent number: 8207176
    Abstract: The present invention is directed to novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds, compositions, and use in therapy as CSBP/RK/p38 kinase inhibitors of Formulas (V) and (Va) wherein inter alia, G5 and G6 are nitrogen and CH, provided that only one of G5 or G6 is nitrogen and the other is CH; R1 is C(Z)N(R10?)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10?)C(Z)(CR10R20)vRb, N(R10?)C(Z)N(R10?)(CR10R20)vRb, or N(R10?)OC(Z)(CR10R20)vRb; R1? is independently selected at each occurrence from halogen, C1-4 alkyl, halo-substituted-C1-4 alkyl, cyano, nitro, (CR10R20)v?NRdRd?, (CR10R20)v?C(O)R12, SR5, S(O)R5, S(O)2R5, or (CR10R20)v?OR13; Rb is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or heterocyclylC1-10 alkyl moiety, which moieties, excluding hydrogen, may all be optionally substituted; X is R2, OR2?, S(O)mR2?, (CH2)n?N(R10?)S(O)mR2?, (CH2)n?N(R10?)C(O)R2?, (CH2)n?NR4R14, (CH2)
    Type: Grant
    Filed: March 24, 2006
    Date of Patent: June 26, 2012
    Assignee: Glaxo Group Limited
    Inventors: James F. Callahan, Jeffrey C. Boehm, Anthony William James Cooper, Stefano Livia, Paul Bamborough, Neysa Nevins, Zehong Wan, Beth A. Norton, Xichen Lin
  • Patent number: 8188280
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Grant
    Filed: February 4, 2009
    Date of Patent: May 29, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20120028970
    Abstract: The present invention relates to a compound represented by a formula (I): wherein X is a group represented by or the like; Y is a group represented by or the like; and Ar1 is a group represented by or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2010
    Publication date: February 2, 2012
    Applicant: MSD K.K.
    Inventors: Minoru Kameda, Kensuke Kobayashi, Chisato Nakama, Makoto Ando, Nagaaki Sato
  • Publication number: 20120020881
    Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
    Type: Application
    Filed: December 4, 2009
    Publication date: January 26, 2012
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
  • Publication number: 20110311516
    Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
    Type: Application
    Filed: February 10, 2010
    Publication date: December 22, 2011
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventor: Carlos F. Barbas, III
  • Publication number: 20110306597
    Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.
    Type: Application
    Filed: June 12, 2009
    Publication date: December 15, 2011
    Inventors: James Michael Crawforth, Paul Alan Glossop, Bruce Cameron Hamper, Wei Huang, Bradley Elwood Neal, Simon John Mantell, Kirk Olson, Atli Thorarensen, Steve Ronald Turner
  • Patent number: 8063045
    Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
    Type: Grant
    Filed: February 1, 2010
    Date of Patent: November 22, 2011
    Assignee: Sanofi-Aventis
    Inventors: Peter Aranyi, Laszlo Balazs, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Karoly Kanai, Zoltan Kapui, Edit Susan, Tibor Szabo, Lajos T. Nagy, Katalin Urban-Szabo, Marton Varga
  • Patent number: RE45364
    Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: February 3, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa