Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/350)
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Publication number: 20140357640Abstract: The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. 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: September 18, 2012Publication date: December 4, 2014Applicant: SANOFIInventors: Marc Nazare, Nis Halland, Friedemann chmidt, Tilo Weiss, Uwe Dietz, Armin Hofmeister
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Publication number: 20140357641Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.Type: ApplicationFiled: January 11, 2013Publication date: December 4, 2014Applicant: NOVARTIS AGInventors: Gurdip Bhalay, Steven Carl Chatlton, Mark Patrick Healy, Catherine Leblanc, Stephen Carl McKeown
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Publication number: 20140357642Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: January 11, 2013Publication date: December 4, 2014Applicant: NOVARTIS AGInventors: Steven Carl Chatlton, Catherine Leblanc, Stephen Carl McKeown
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Patent number: 8901302Abstract: The object of the present invention is to provide a compound which is useful as a production intermediate of pyrazine carboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazine carboxamide. The present invention provides a pyrazino[2,3-d]isoxazole derivative represented by the formula (I): wherein X represents a halogen atom, a hydroxyl group or a sulfamoyloxy group, and Y represents —C(?O)R or —CN; wherein R represents a hydrogen atom, an alkoxy group an aryloxy group, an alkyl group, an aryl group or an amino group.Type: GrantFiled: May 3, 2013Date of Patent: December 2, 2014Assignees: FUJIFILM Corporation, Toyama Chemical Co., Ltd.Inventors: Kouki Nakamura, Takeshi Murakami, Hiroyuki Naitou, Naoyuki Hanaki, Katsuyuki Watanabe
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Patent number: 8901125Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: June 19, 2013Date of Patent: December 2, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
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Publication number: 20140350023Abstract: The present invention claims amorphous solid state forms of sitagliptin salts, processes for their preparation, and pharmaceutical compositions thereof. As salt forming anions are claimed: The maleate, fumarate, besylate, mesylate and succinate.Type: ApplicationFiled: December 7, 2012Publication date: November 27, 2014Inventors: Suresh Babu Jayachandra, Jigar Bhaskarbhai Shah, Chiguru Sailu, Sandeep Thakaji Kanawade
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Publication number: 20140349986Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.Type: ApplicationFiled: July 24, 2014Publication date: November 27, 2014Applicant: SANOFIInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Patent number: 8895740Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: July 27, 2012Date of Patent: November 25, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Luca Settimo, Damien Fraysse, Guy Brenchley, Christopher John Davis, Andrew W. Miller
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Publication number: 20140343066Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.Type: ApplicationFiled: December 20, 2013Publication date: November 20, 2014Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha H.M. Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn M. George, Lu Wang, Biqin Li, Nigel S. Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
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Patent number: 8889686Abstract: L malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are disclosed for decreasing the bitterness of eszopiclone dosage formsType: GrantFiled: July 1, 2013Date of Patent: November 18, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
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Patent number: 8889684Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: GrantFiled: January 27, 2012Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Heinz Stadtmueller
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Patent number: 8889685Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful for treating sleep disorders.Type: GrantFiled: June 27, 2013Date of Patent: November 18, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
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Patent number: 8889664Abstract: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.Type: GrantFiled: April 28, 2011Date of Patent: November 18, 2014Assignee: Exelixis, Inc.Inventors: William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
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Publication number: 20140336196Abstract: The present invention relates to novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, and polymorphs, hydrates and solvates thereof, which are potent inhibitors of dipeptidyl peptidase-IV useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The present invention also relates to the process for preparing the novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, as well as pharmaceutical compositions containing the novel phosphoric acid salts, and methods of use thereof for the treatment of diabetes, obesity, and high blood pressure.Type: ApplicationFiled: May 22, 2012Publication date: November 13, 2014Applicant: Merck Sharp & Dohme Corp.Inventor: Jerry L. Atwood
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Publication number: 20140336177Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.Type: ApplicationFiled: December 11, 2012Publication date: November 13, 2014Inventors: Barbara Pio, Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Shawn Walsh
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Patent number: 8883784Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: August 12, 2013Date of Patent: November 11, 2014Assignee: AbbVie Inc.Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
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Patent number: 8877761Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: GrantFiled: April 18, 2012Date of Patent: November 4, 2014Assignee: Pfizer Inc.Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
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Patent number: 8877757Abstract: The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: August 31, 2011Date of Patent: November 4, 2014Assignee: Merck Serono SAInventors: Pascale Gaillard, Anna Quattropani, Vincent Pomel, Thomas Rueckle, Jasna Klicic, Dennis Church
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Publication number: 20140323485Abstract: A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, Ra, A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: September 14, 2012Publication date: October 30, 2014Applicant: NOVARTIS AGInventors: Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Darren Mark LeGrand, Roger John Taylor
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Patent number: 8871929Abstract: The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined herein. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and methods of using the compound of Formula (I) to treat microbial infections.Type: GrantFiled: July 28, 2011Date of Patent: October 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Tin-Yau Chan, Henry M. Vaccaro
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Publication number: 20140315908Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.Type: ApplicationFiled: April 16, 2014Publication date: October 23, 2014Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Anil Menon, Darshan K. Parikh, Dora Visky, Matthew Michael Kreilein, Nathan Boersen, Thomas Lee, Ying Li, Jean Xu, Xiaozhang Liang, William Wei-Hwa Leong, Benjamin Cohen
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Publication number: 20140315909Abstract: The present invention relates to compounds described by Formula I: salts thereof, their synthesis, and their use as ITK and JAK3 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such disease associated with abnormal cell growth such as autoimmune, inflammation, rheumatoid arthritis, systemic lupus erythematosus, atherosclerosis, ulcerative colitis, psoriatic arthritis, psoriasis, Crohn's, metabolic and cancer diseases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions and processes for preparing the compounds of the invention.Type: ApplicationFiled: April 16, 2014Publication date: October 23, 2014Applicant: ARRIEN PHARMACEUTICALS LLCInventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy, Paramareddy Gangireddy, Rajendra P. Appalaneni
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Patent number: 8865711Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: February 3, 2012Date of Patent: October 21, 2014Assignee: H. Lundbeck A/SInventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
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Patent number: 8865713Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: September 3, 2013Date of Patent: October 21, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Patent number: 8865715Abstract: The invention relates to compounds the formula (I): and pharmaceutically usable salts, tautomers and stereoisomers thereof, wherein R1, R2 and R3 are defined herein. The compounds of formula (I) and their pharmaceutically usable salts, tautomers and stereoisomers are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.Type: GrantFiled: October 12, 2011Date of Patent: October 21, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Margarita Wucherer-Plietker, Thomas J. J. Mueller, Eugen Merkul
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Patent number: 8859550Abstract: The present invention relates to salts, hydrates, and polymorphs of bicyclic heteroaryl compounds, and pharmaceutical compositions thereof, which may be useful as inhibitors of H4R for the treatment or prevention of diseases including allergic rhinitis.Type: GrantFiled: September 7, 2012Date of Patent: October 14, 2014Assignee: Kalypsys, Inc.Inventors: Pingyun Chen, Stephen A. R. Carino, Ricky Wayne Couch, Daniel S. Kinder, Beth A. Norton
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Publication number: 20140303171Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
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Publication number: 20140303366Abstract: Provided is a method of treating myasthenia gravis in a patient by administering to the patient an effective amount of a skeletal muscle troponin activator, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 7, 2014Publication date: October 9, 2014Inventors: Aaron Hinken, Fady Malik, Malar Pannirselvam, Alan Russell
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Publication number: 20140302539Abstract: Coelenterazine analogs having luminescence properties different from those of known coelenterazine analogs are desired for various luciferases. The invention provides compounds represented by general formula (1) below.Type: ApplicationFiled: April 4, 2014Publication date: October 9, 2014Applicant: JNC CORPORATIONInventors: Satoshi INOUYE, Junichi SATO, Yuiko MIURA
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Publication number: 20140303158Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: May 9, 2014Publication date: October 9, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Patent number: 8853212Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 17, 2011Date of Patent: October 7, 2014Assignee: Merck Sharp & Dohme CorpInventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20140296521Abstract: There has been a need for coelenterazine analogs that exhibit luminescence properties different from those of known coelenterazine analogs. The present invention provides the compound represented by general formula (1).Type: ApplicationFiled: May 21, 2014Publication date: October 2, 2014Inventors: Satoshi INOUYE, Yuiko SAHARA, Rie IIMORI, Takamitsu HOSOYA
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Publication number: 20140296066Abstract: A compound of formula (I) (I), wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has one or more substituents at least one of which is, for example, a 5 membered heterocycle; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.Type: ApplicationFiled: October 31, 2012Publication date: October 2, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Thomas Pitterna, Olivier Loiseleur, Anthony Cornelius O'Sullivan, Torsten Luksch
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Patent number: 8846916Abstract: The present invention relates to novel processes for the preparation of enantiomerically enriched ?-amino acid derivatives such as ?-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.Type: GrantFiled: May 10, 2010Date of Patent: September 30, 2014Assignee: Generics [UK] LimitedInventors: Vinayak Govind Gore, Maheshkumar Gadakar, Priyanka Bhosle, Suresh Shinde
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Patent number: 8846672Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: September 30, 2014Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
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Patent number: 8846664Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: November 12, 2009Date of Patent: September 30, 2014Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Wei-Sheng Huang, R. Mathew Thomas
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Publication number: 20140288053Abstract: The invention relates to new pyridopyrazine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: October 26, 2012Publication date: September 25, 2014Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Gordon Saxty, Patrick Rene Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet, Bruno Roux, Lieven Meerpoel
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Publication number: 20140288062Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
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Publication number: 20140288302Abstract: A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R1R2)—C(?O)—NR3R4 and a group represented by formula: —R5, a broken line represents presence or absence of a bond, Z is —NR6—, ?N—, —O—, or —S—, R6 is halogen or substituted or unsubstituted alkyl, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen or substituted or unsubstituted alkyl, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: Shionogi & Co., Ltd.Inventors: Koji MASUDA, Shiro KIDA, Kyohei HAYASHI, Manabu KATOU, Naoki YOSHIKAWA, Akira KUGIMIYA, Mado NAKAJIMA, Nobuyuki TANAKA
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Publication number: 20140288083Abstract: The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. 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 9, 2014Publication date: September 25, 2014Applicant: SANOFIInventors: Marc Nazare, Nis Halland, Friedemann Schmidt, Tilo Weiss, Uwe Dietz, Armin Hofmeister, Jean-Christophe Carry
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Publication number: 20140288082Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: June 4, 2014Publication date: September 25, 2014Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Publication number: 20140288084Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 28, 2012Publication date: September 25, 2014Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
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Patent number: 8841299Abstract: There are provided compounds of the formula wherein R1 and R2 are as described herein. The compounds are useful as anticancer agents.Type: GrantFiled: June 19, 2013Date of Patent: September 23, 2014Assignee: Genentech, Inc.Inventors: Johannes Hermann, Ann Catherine Petersen, Jutta Wanner, Lin Yi
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Patent number: 8841298Abstract: Substituted pyrazines of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the pyrazines of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one pyrazine compound of the formula I to act on plants, their seed and/or their habitat.Type: GrantFiled: May 31, 2010Date of Patent: September 23, 2014Assignee: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Anna Aleksandra Michrowska, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Bernd Sievernich, Anja Simon, Ricarda Niggeweg
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Publication number: 20140275020Abstract: This invention relates to compounds of Formula I having the following general structure: 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 18, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
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Publication number: 20140275097Abstract: The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.Type: ApplicationFiled: October 3, 2012Publication date: September 18, 2014Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme L. Fraser, Marie-Odile Roy, Mohamed El Bousmaqui, Frederic Batt
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Publication number: 20140275061Abstract: 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: September 18, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
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Publication number: 20140275096Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
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Publication number: 20140256736Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Applicant: XENON PHARMACEUTICALS INC.Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
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Publication number: 20140249129Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: February 20, 2014Publication date: September 4, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF