At Least Three Ring Nitrogens In The Two Rings Which Form The Spiro Patents (Class 546/20)
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Patent number: 9487517Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.Type: GrantFiled: September 17, 2015Date of Patent: November 8, 2016Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
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Patent number: 9156840Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.Type: GrantFiled: February 19, 2014Date of Patent: October 13, 2015Assignee: ALTOS THERAPEUTICS, LLCInventors: Gary W. Luehr, Arathi Sundaram, Priyadarshini Jaishankar, Philip W Payne, Pascal Druzgala
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Patent number: 9045480Abstract: The disclosure concerns sterically hindered amine light stabilizers (HALS) with low basicity at the nitrogen atom and high thermal stability. They are characterized by their spiro-substitution in the 4-position of the tetramethylpiperidine ring (Spiro-NOR-HALS). These compounds are useful in stabilizing polymers, especially thermoplastic polyolefins, against the deleterious effects of oxidative, thermal and actinic radiation. The compounds are also useful in stabilizing acid catalyzed and ambient cured coatings systems. They are particularly useful when high processing temperatures are additional required.Type: GrantFiled: June 1, 2010Date of Patent: June 2, 2015Assignee: BASF SEInventors: Kai-Uwe Schöning, Adriana Edenharter, Stefan Hauck
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Publication number: 20150099730Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.Type: ApplicationFiled: September 6, 2013Publication date: April 9, 2015Applicant: Janssen Pharmaceutica, NVInventor: Peter J. Connolly
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Publication number: 20150045347Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: February 12, 2015Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
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Publication number: 20150011532Abstract: Compounds having the following formula: wherein A is, or; and X is N or C—R7, or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: January 8, 2015Inventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banejee, Ramesh Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
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Patent number: 8921555Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: June 7, 2010Date of Patent: December 30, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Patent number: 8901108Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.Type: GrantFiled: September 11, 2013Date of Patent: December 2, 2014Assignee: AbbVie Bahamas LimitedInventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A. M. Rensink, Jennifer Venhorst, Martina A. W. Van Der Neut, Martin De Hann, Cornelis G. Kruse
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Publication number: 20140350005Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.Type: ApplicationFiled: February 19, 2014Publication date: November 27, 2014Inventors: GARY W. LUEHR, ARATHI SUNDARAM, PRIYADARSHINI JAISHANKAR, PHILIP W. PAYNE, PASCAL DRUZGALA
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Publication number: 20140336158Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: ApplicationFiled: July 25, 2014Publication date: November 13, 2014Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
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Publication number: 20140303372Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: ApplicationFiled: March 28, 2014Publication date: October 9, 2014Applicant: ABBVIE BHAMAS LTD.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A.W. Van Der Neut, Cornelis G. Kruse
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Patent number: 8802690Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: July 11, 2013Date of Patent: August 12, 2014Assignee: Pfizer Inc.Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Patent number: 8778957Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: GrantFiled: March 8, 2010Date of Patent: July 15, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley
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Publication number: 20140171439Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: February 21, 2014Publication date: June 19, 2014Applicant: Janssen Pharmaceutica, N.V.Inventors: Kristof VAN EMELEN, Marc Gustaaf Celine VERDONCK, Sven Franciscus Anna VAN BRANDT, Patrick Rene ANGIBAUD, Lieven MEERPOEL, Alexey Borisovich DYATKIN
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Patent number: 8742111Abstract: An improved process or method of synthesis of carfentanil and other potent opioid analgesics of the N-alkyl 4-substituted 4-piperidinylamide class which can be used as morphine substitutes.Type: GrantFiled: February 21, 2013Date of Patent: June 3, 2014Assignee: The United States of America as Represented by the Secretary of the ArmyInventors: Andrew J Walz, Fu-Lian Hsu
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Patent number: 8722887Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: GrantFiled: February 16, 2010Date of Patent: May 13, 2014Assignee: Abbvie Bahamas, Ltd.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
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Publication number: 20140113895Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.Type: ApplicationFiled: December 20, 2013Publication date: April 24, 2014Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Patent number: 8697717Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: May 6, 2013Date of Patent: April 15, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Patrick Rene Angibaud, Lieven Meerpoel, Alexey Borisovich Dyatkin
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Patent number: 8691836Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.Type: GrantFiled: June 17, 2011Date of Patent: April 8, 2014Assignee: Altos Therapeutics, LLCInventors: Gary W. Luehr, Arathi Sundaram, Priyadarshini Jaishankar, Philip W. Payne, Pascal Druzgala
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Publication number: 20140011775Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.Type: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: Abbott Healthcare Products B.V.Inventors: Arnold van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A.M. Rensink, Jennifer Venhorst, Martina A.W. Van Der Neut, Martin De Hann, Cornelis G. Kruse
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Publication number: 20130331369Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.Type: ApplicationFiled: August 8, 2013Publication date: December 12, 2013Applicant: Novartis AGInventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
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Patent number: 8580809Abstract: A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within.Type: GrantFiled: March 8, 2010Date of Patent: November 12, 2013Assignee: Pain Therapeutics, Inc.Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Patent number: 8563723Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.Type: GrantFiled: March 17, 2009Date of Patent: October 22, 2013Assignee: Abbott Healthcare Products, B.V.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A. M. Rensink, Jennifer Venhorst, Martina A. W. Van Der Neut, Martin De Haan, Cornelis G. Kruse
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Patent number: 8563570Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: January 20, 2012Date of Patent: October 22, 2013Assignee: Incyte CorporationInventors: Wenqing Yao, Chunhong He, David M. Burns, Jincong Zhuo, Meizhong Xu, Colin Zhang, Ding-Quan Qian, Brian Metcalf
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Publication number: 20130245034Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: May 6, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica, N.V.Inventors: Kristof VAN EMELEN, Marc Gustaaf Celine VERDONCK, Sven Franciscus Anna VAN BRANDT, Patrick Rene ANGIBAUD, Lieven MEERPOEL, Alexey Borisovich DYATKIN
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Publication number: 20130131041Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: December 19, 2012Publication date: May 23, 2013Applicant: Merck Sharp & Dohme Corp.Inventor: Merck Sharp & Dohme Corp.
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Publication number: 20130123242Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
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Publication number: 20130116269Abstract: The present invention relates to novel cyclic N,N?-diarylureas and N,N?-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.Type: ApplicationFiled: July 1, 2011Publication date: May 9, 2013Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin
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Patent number: 8415369Abstract: A compound of the formula (I) wherein the substituents are as defined in the claims, is useful as a pesticide.Type: GrantFiled: October 13, 2008Date of Patent: April 9, 2013Assignee: Syngenta Crop Protection LLCInventors: Werner Zambach, Ottmar Franz Hueter, Jean Wenger, Marcela Goeghova, Thomas Pitterna, Peter Maienfisch, Michel Muehlebach
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Patent number: 8394811Abstract: A method of identification of compounds that modulate thyroid hormone activity, and the use of such compounds and compositions thereof for such purposes are disclosed. The compounds may be selected from the group consisting of: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to aberrant thyroid hormone activity, such as hyperthyroidism and thyrotoxicosis.Type: GrantFiled: April 18, 2008Date of Patent: March 12, 2013Assignees: Molsoft LLC, New York University School of MedicineInventors: Herbert H. Samuels, Ruben Abagyan, Matthieu Schapira, Maxim Totrov, Bruce M. Raaka, Stephen R. Wilson, Li Fan, Zhiguo Zhou
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Patent number: 8377954Abstract: The present invention is directed to bicyclic spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that 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: GrantFiled: December 28, 2007Date of Patent: February 19, 2013Assignee: Merck, Sharp & Dohme, CorpInventors: Shaun R. Stauffer, Samuel L. Graham
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Publication number: 20130012434Abstract: The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: Michael K. Wong, Brian J. Lavey, Wensheng Yu, Joseph A. Kozlowski, Duanc E. DeMong, Xing Dai, Andrew W. Stamford, Michael W. Miller, Guowei Zhou, De-Yi Yang, William J. Greenlee
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Publication number: 20120328691Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 29, 2007Publication date: December 27, 2012Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory Poker, Timothy J. Guzi
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Publication number: 20120316162Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.Type: ApplicationFiled: August 22, 2012Publication date: December 13, 2012Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Kai SCHIEMANN, Melanie SCHULTZ, Andree BLAUKAT, Ingo KOBER
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Publication number: 20120302540Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
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Patent number: 8318762Abstract: The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: May 18, 2009Date of Patent: November 27, 2012Assignee: Pfizer Inc.Inventors: Jeffrey W. Corbett, Richard Elliott, Kevin Freeman-Cook, David A. Griffith, Dennis P. Phillion
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Publication number: 20120270838Abstract: The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2010Publication date: October 25, 2012Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Toru Esaki, Yoshikazu Nishimura, Yoshiaki Isshiki, Naoki Okamoto, Yoshiyuki Furuta, Akemi Mizutani, Masateru Ohta, Wayne Wen Lai, Tomoya Kotake
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Patent number: 8293759Abstract: The present invention is directed to spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that 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: GrantFiled: October 29, 2007Date of Patent: October 23, 2012Assignee: Merck, Sharp & Dohme, Corp.Inventors: Shaun R. Stauffer, Ivory D. Hills, Ashley Nomland
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Publication number: 20120197016Abstract: Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADR?1 receptors, and determining based on the binding interaction of the test agent with the ADR?1 receptors whether the test agent is an effective ADR?1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADR?1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.Type: ApplicationFiled: October 21, 2011Publication date: August 2, 2012Applicant: THE PROCTER & GAMBLE COMPANYInventors: Leo Timothy Laughlin, II, Tomohiro Hakozaki, Wenzhu Zhao, Jiazhen Wang, John Crist Bierman
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Publication number: 20120122858Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: January 20, 2012Publication date: May 17, 2012Applicant: Incyte CorporationInventors: Wenqing Yao, Chunhong He, David M. Burns, Jincong Zhuo, Meizhong Xu, Colin Zhang, Ding-Quan Qian, Brian Metcalf
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Publication number: 20120095001Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: June 7, 2010Publication date: April 19, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Publication number: 20120045500Abstract: Compounds of general formula (I): and cosmetic and pharmaceutical compositions including such a compound are described.Type: ApplicationFiled: February 26, 2010Publication date: February 23, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Thibaud Portal, Jean-Claude Pascal
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Patent number: 8119652Abstract: The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: May 14, 2007Date of Patent: February 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher Hamblett, Solomon Kattar, Dawn Mampreian, Joey Methot, Thomas Miller, Paul Tempest
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Publication number: 20110319363Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.Type: ApplicationFiled: December 20, 2010Publication date: December 29, 2011Inventors: Michael N. Greco, Harold R. Almond, JR., Michael J. Hawkins, Eugene Powell
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Patent number: 8076349Abstract: Compounds according to formula (I): wherein A, R1 and R2 are as defined herein, and the pharmaceutically acceptable salts, hydrates and solvates thereof are useful for the modulation of CCR5 chemokine receptor activity.Type: GrantFiled: December 9, 2005Date of Patent: December 13, 2011Assignee: Virochem Pharma Inc.Inventors: Laval Chan Chun Kong, Christophe Moinet, Marc Courchesne, Louis Vaillancourt, Monica Bubenik
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Publication number: 20110275657Abstract: Melanocortin receptor modulators, processes for preparing them and use thereof in human medicine and cosmetics are described. Melanocortin receptor modulators corresponding to formula (I): compositions containing them, processes for their preparation and their use in pharmaceutical or cosmetic compositions are also described.Type: ApplicationFiled: November 4, 2009Publication date: November 10, 2011Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Claire Bouix-Peter, Itaru Suzuki, Isabelle Pelisson, Pascal Collette, Samuel Tabet, Guillaume Lafitte
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Patent number: 8039624Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.Type: GrantFiled: December 20, 2007Date of Patent: October 18, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 8026365Abstract: This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: April 29, 2008Date of Patent: September 27, 2011Assignee: Hoffman-La Roche Inc.Inventors: Andreas Christ, Rainer Martin, Peter Mohr
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Publication number: 20110178080Abstract: Melanocortin receptor-specific compounds of formula I below: wherein the variables are as defined in the specification, and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders.Type: ApplicationFiled: March 29, 2011Publication date: July 21, 2011Applicant: PALATIN TECHNOLOGIES, INC.Inventors: Yi-Qun Shi, John H. Dodd, Elizabeth G. Rowley, Gary L. Olson, Axel Metzger
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Patent number: 7981904Abstract: The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula wherein the variables are as defined herein. In particular, the present invention relates to ACC1 and/or ACC2 inhibitors, compositions of matter, kits and articles of manufacture comprising these compounds, methods for inhibiting ACC1 and/or ACC2, and methods of making the inhibitors.Type: GrantFiled: March 19, 2009Date of Patent: July 19, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Tracy Duong, Angie Vassar