Spiro Ring System Patents (Class 514/278)
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Publication number: 20140315902Abstract: 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.Type: ApplicationFiled: April 18, 2014Publication date: October 23, 2014Inventors: Yaping Sun, Liang Lu, Wenqing Yao, Jincong Zhuo, Liangxing Wu, Meizhong Xu, Ding-Quan Qian, Chunhong He, Fenglei Zhang
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Patent number: 8865741Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: GrantFiled: February 18, 2012Date of Patent: October 21, 2014Assignee: Asana Biosciences, LLCInventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
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Patent number: 8865702Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.Type: GrantFiled: July 23, 2008Date of Patent: October 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Patent number: 8865641Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.Type: GrantFiled: June 14, 2012Date of Patent: October 21, 2014Assignee: The Feinstein Institute for Medical ResearchInventors: Valentin A. Pavlov, Kevin J. Tracey
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Patent number: 8865701Abstract: The present invention is directed to spiropyrrolidine 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: February 20, 2010Date of Patent: October 21, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
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Patent number: 8865911Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: GrantFiled: March 15, 2013Date of Patent: October 21, 2014Assignee: Astrazeneca ABInventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
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Publication number: 20140309251Abstract: The use of ORL-1 receptor antagonists of the formula: for the treatment of alcohol use disorders is described.Type: ApplicationFiled: November 29, 2012Publication date: October 16, 2014Applicant: Eli Lilly and CompanyInventor: Linda Rorick Kehn
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Publication number: 20140309220Abstract: The invention relates to benzoxazines useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: November 2, 2012Publication date: October 16, 2014Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Corey Anderson, Joseph Pontillo, Edward Adam Kallel, Mehdi Michael Djamel Numa, Bryan A. Frieman, Jason McCartney, Jennings Franklin Worley, III, Vijayalaksmi Arumugam, Johnny Uy, Nicole Hilgraf, Brian Richard Bear
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Publication number: 20140308282Abstract: Benzimidazoles of formula (I): wherein: A is 5- to 12-membered aryl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, —(CH2)p—, —X—, —CH2—X—, or —X—CH2—; X is —O—, —S—, —N(R2)—, >C?O, >S(?O), >S(?O)2, —O—C(?O)—, —C(?O)—O—, N(R2)—C(?O)—, or —C(?O)—N(R2)—; each L is independently a single bond, C1-3alkylene, C2-3alkenylene or C2-3alkynylene; R1 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, each of which is unsubstituted or substituted; each Z is independently —N(R2)2, —OR2, —SR2, —S(?O)R2, —S(?O)2R2; each R2 is independently hydrogen, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.Type: ApplicationFiled: November 12, 2012Publication date: October 16, 2014Applicant: re: Viral LtdInventors: Stuart Cockerill, Christopher Pilkington, James Lumley, Richard Angell, Neil Mathews
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Publication number: 20140309227Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
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Publication number: 20140309207Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.Type: ApplicationFiled: October 18, 2012Publication date: October 16, 2014Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
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Patent number: 8859773Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is 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 an acetyl-CoA carboxylase enzyme(s) in an animal.Type: GrantFiled: October 27, 2011Date of Patent: October 14, 2014Assignee: Pfizer Inc.Inventors: David A. Griffith, Robert L. Dow, Scott W. Bagley, Aaron Smith
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Patent number: 8859462Abstract: Disclosed is a pest control composition comprising at least one pyripyropene derivative of formula (I) or agriculturally and horticulturally acceptable salt thereof and at least one other pest control agent as active ingredients. The combined use of the two ingredients can provide a better insecticidal effect.Type: GrantFiled: March 10, 2008Date of Patent: October 14, 2014Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Ryo Horikoshi, Kazuhiko Oyama, Mitsuyuki Yabuzaki
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Patent number: 8859608Abstract: A spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, halogen, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridyl, pyrimidyl, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 15, 2010Date of Patent: October 14, 2014Assignee: Rottapharm Biotech S.R.L.Inventors: Luigi Piero Stasi, Lucio Rovati
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Patent number: 8859577Abstract: The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 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: September 20, 2011Date of Patent: October 14, 2014Assignee: Pfizer Inc.Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
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Publication number: 20140296134Abstract: Embodiments include methods for generating a metabolite profile of a stool sample and methods of assessing the status of a subject using the metabolic profile derived from a stool sample.Type: ApplicationFiled: November 8, 2012Publication date: October 2, 2014Applicant: The Board of Regents of the University of Texas SystemInventors: Tor Savidge, Sara Dann
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Publication number: 20140296272Abstract: The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Dorothée Bardiot, Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
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Publication number: 20140296169Abstract: The present disclosure relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 18, 2014Publication date: October 2, 2014Inventors: Hauke SZILLAT, Thomas LEEUW, Martin LORENZ
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Publication number: 20140296214Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: October 2, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
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Publication number: 20140296196Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.Type: ApplicationFiled: June 13, 2014Publication date: October 2, 2014Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
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Publication number: 20140296200Abstract: The present invention provides compounds of the formula: which are useful as inhibitors of PHD, pharmaceutical compositions thereof, methods for treatment of conditions associated with HIF, processes for making the compounds and intermediates thereof.Type: ApplicationFiled: March 26, 2014Publication date: October 2, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Jason W. Brown, Melinda Davis, Anthony Ivetac, Benjamin Jones, Andre A. Kiryanov, Jon Kuehler, Marion Lanier, Joanne Miura, Sean Murphy, Xiaolun Wang
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Publication number: 20140288110Abstract: 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections.Type: ApplicationFiled: March 24, 2014Publication date: September 25, 2014Applicant: EVOLVA SAInventors: Karsten KRISTIANSEN, Prathama S. MAINKAR, Jean-Philippe MEYER, Alexandra Santana SORENSEN
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Publication number: 20140288111Abstract: 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: ApplicationFiled: May 9, 2014Publication date: September 25, 2014Applicant: Pfizer Inc.Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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Publication number: 20140288076Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.Type: ApplicationFiled: June 4, 2014Publication date: September 25, 2014Applicant: NOVARTIS AGInventors: Paul A. Barsanti, Cheng Hu, Jeff Jin, Robert Keyes, Robert Kucejko, Xiaodong Lin, Yue Pan, Keith B. Pfister, Martin Sendzik, James Sutton, Lifeng Wan
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Publication number: 20140288091Abstract: Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: ApplicationFiled: October 10, 2012Publication date: September 25, 2014Applicants: ASTRAZENECA AB, ASTRAZENECA ABInventors: Anna Minidis, Fredrik Rahm, Jenny Viklund
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Publication number: 20140288106Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.Type: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Applicant: SanofiInventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
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Publication number: 20140286931Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventor: Chengzhi Zhang
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Publication number: 20140288109Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventors: Tjeerd Andries BARF, Arthur OUBRIE, Carsten SCHULTZ-FADERMRECHT, Eduard Willem ZWART, Niels HOOGENBOOM, Sander Martijn DE WILDE, Allard KAPTEIN
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Publication number: 20140288042Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: September 25, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
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Patent number: 8841296Abstract: This invention provides novel substituted 1,4-dioxa-8-azaspiro[4,5]decane compounds of the general formula (1), wherein R1 is selected from phenethyl, 4,6-dimethoxypyrimidin-2-yl and (2-chloro-5-thiazolyl)methyl and R2 is selected from the group consisting of hydroxy, 4-bromo-2-chlorophenoxy, morpholin-4-yl, (2-chloro-5-thiazolyl)methyloxy, benzyloxy, phenylsulfanyl, benzotriazol and 5-chloro-2-fluoroanilino. The present invention also relates to a process for the preparation of novel substituted 1,4-dioxa-8-azaspiro[4,5]decanes of general formula (1). The novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1) has fungicidal activity.Type: GrantFiled: March 23, 2010Date of Patent: September 23, 2014Assignee: Council of Scientific and Industrial Research, Anusandhan Bhawan, Rafi MargInventors: Mukund Vinayak Deshpande, Sunita Ranjan Deshpande, Fazal Shirazi, Preeti Madhukar Chaudhary, Nelavelli Malleswara Rao, Baidyanath Mohanty, Nageshwar Nath Sharma, Anand Kumar Bachhawat, Ganesan Kaliannan, Sanjoy Paul, Raj Kumar, Bommena Vittal Rao, Bhimrao Bodhanrao Gawali, Vaddu Venkata Narayana Reddy, Jhillu Singh Yadav
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Publication number: 20140275017Abstract: 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: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
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Publication number: 20140275036Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.Type: ApplicationFiled: May 29, 2014Publication date: September 18, 2014Applicant: Chase Pharmaceuticals CorporationInventors: Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
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Publication number: 20140275025Abstract: 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: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
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Publication number: 20140275048Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Alkermes Pharma Ireland LimitedInventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
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Publication number: 20140275005Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: ApplicationFiled: May 5, 2014Publication date: September 18, 2014Applicant: SanofiInventor: Zhongli GAO
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Publication number: 20140275019Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHDInventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
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Publication number: 20140275080Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Michael D. Kaufman, William C. Patt, Thiwanka Samarakoon, Lakshminarayana Vogeti, Karen M. Yates
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Publication number: 20140256712Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: March 12, 2014Publication date: September 11, 2014Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
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Publication number: 20140249170Abstract: The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial FabI and can be used for the treatment of Staphylococcal infections.Type: ApplicationFiled: September 18, 2012Publication date: September 4, 2014Inventors: Radha Rangarajan, Rajinder Kumar, BV Prabhakar, P Chandrasekhar, P Mallikarjuna, Ankita Banerjee
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Patent number: 8822486Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.Type: GrantFiled: November 19, 2010Date of Patent: September 2, 2014Assignee: Eli Lilly and CompanyInventors: Chafiq Hamdouchi, Jayana Pankaj Lineswala, Pranab Maiti
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Patent number: 8822495Abstract: The invention relates to azacyclyl-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the azacyclyl-substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.Type: GrantFiled: August 14, 2008Date of Patent: September 2, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
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Patent number: 8822448Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: GrantFiled: March 7, 2013Date of Patent: September 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
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Publication number: 20140243309Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 28, 2014Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
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Publication number: 20140243303Abstract: The present invention relates to spirocyclic compounds of formula I, namely spirocyclic (1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fiuorophenyl)ethoxy)pyridin-2-amines having protein kinase inhibitory activity, and methods of synthesizing and using such compounds. Preferred compounds are c-Met and/or ALK inhibitors useful for the treatment of abnormal cell growth, such as cancers.Type: ApplicationFiled: July 26, 2012Publication date: August 28, 2014Applicant: Beta Pharma Canada Inc.Inventors: Zhaoyin Wang, Lianhai Li, Zhigang Wang
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Patent number: 8815869Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: March 10, 2011Date of Patent: August 26, 2014Assignee: AbbVie Inc.Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
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Publication number: 20140234402Abstract: Compositions and methods for treating systemic diseases by intravenous administration of formulations of synthesized curcumin (diferuloylmethane) and concomitantly a calcium channel blocker to human subjects with neoplastic and neurodegenerative diseases are disclosed herein. The diseases are treated by prolonged administration of sub-optimal doses of liposomal curcumin or polymeric nanocurcumin or the sustained release curcumin from PLGA nanocurcumin at dosages below systemic hemolytic thresholds concomitantly with or without calcium channel blockers.Type: ApplicationFiled: April 30, 2014Publication date: August 21, 2014Applicant: SignPath Pharma Inc.Inventor: Lawrence Helson
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Publication number: 20140235634Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.Type: ApplicationFiled: February 14, 2014Publication date: August 21, 2014Applicant: Kala Pharmaceuticals, Inc.Inventors: Winston Zapanta ONG, Pawel Wojciech NOWAK, Ben C. ASKEW, Jinsoo KIM
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Publication number: 20140235593Abstract: In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. 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: ApplicationFiled: August 24, 2012Publication date: August 21, 2014Applicants: ST. JUDE CHILDREN'S RESEARCH HOSPITAL, RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, MMV MEDICINES FOR MALARIA VENTUREInventors: Rodney Kiplin Guy, Fangyi Zhu, Wendyam Armand Guiguemde, David Floyd, Spencer Knapp, Philip Stein, Steve Castro
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Patent number: 8809361Abstract: The present invention relates to compounds of general formula I, wherein the groups R1 and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: May 6, 2013Date of Patent: August 19, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Matthias Eckhardt
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Publication number: 20140228333Abstract: In one aspect, the invention relates to methods for treating muscle atrophy by providing to an animal in need thereof an effective amount of a compound. The compound can modulate the expression levels of multiple mRNA of a muscle atrophy signature. 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: ApplicationFiled: June 6, 2012Publication date: August 14, 2014Applicants: UNIVERSITY OF IOWA RESEARCH FOUNDATION, The United States of America as Represented by the Department of Veterans AffairsInventors: Christopher M. Adams, Steven D. Kunkel, Michael Welsh