The Additional Hetero Ring Contains Ring Nitrogen Patents (Class 514/210.2)
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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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Publication number: 20140343029Abstract: The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: September 12, 2012Publication date: November 20, 2014Applicant: MERCK PATENT GMBHInventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Lizbeth Celeste Deselm, Hui Qiu, Constantin Neagu, Donald Bankston, Christopher Charles Victor Jones
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Publication number: 20140343030Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: May 16, 2014Publication date: November 20, 2014Applicant: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, Ding-Quan Qian, Song Mei, Ganfeng Cao, Yongchun Pan, Qun Li, Zhongjiang Jia
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Publication number: 20140343031Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Applicant: Pfizer Inc.Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joesph Melnick, Justin Ian Montgomery, Usa Reilly
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Patent number: 8889665Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R3 and L are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: GrantFiled: July 1, 2008Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Steffen Steurer, Irene Waizenegger
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Publication number: 20140336165Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.Type: ApplicationFiled: November 14, 2012Publication date: November 13, 2014Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
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Publication number: 20140329797Abstract: The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 16, 2012Publication date: November 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Unterschemmann
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Patent number: 8877741Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: January 22, 2014Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
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Publication number: 20140323460Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
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Publication number: 20140323463Abstract: [Problem] A compound which is useful as an inhibitor on EGFR T790M mutation kinase activity is provided. [Means for Solution] The present inventors have investigated a compound having an inhibitory action on an EGFR T790M mutation kinase, and have found that a pyrazinecarboxamide compound has an inhibitory action on an EGFR T790M mutation kinase, thereby completing the present invention.Type: ApplicationFiled: January 15, 2013Publication date: October 30, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Takahiro Matsuya, Yutaka Kondoh, Itsuro Shimada, Shigetoshi Kikuchi, Maiko Iida, Kenichi Onda, Hiroki Fukudome, Yukihiro Takemoto, Nobuaki Shindou, Hideki Sakagami, Hisao Hamaguchi
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Publication number: 20140323448Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: April 29, 2014Publication date: October 30, 2014Applicant: Ironwood Pharmaceuticals Inc.Inventors: Charles KIM, Takashi NAKAI, Thomas Wai-Ho LEE, Joel MOORE, Nicholas Robert PERL, Jason ROHDE, Rajesh R. IYENGAR, Ara MERMERIAN, Angelika FRETZEN
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Publication number: 20140323461Abstract: Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep.Type: ApplicationFiled: November 9, 2012Publication date: October 30, 2014Inventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar, Venkata M. Yenugonda, Edward D. Levin, Amir H. Rezvani
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Publication number: 20140315879Abstract: The present invention relates to sulfonamide derivatives, of formula (I): or a pharmaceutically acceptable salts thereof, wherein X, Z, R1a, R1b, R2, R3, R4 and R5 are as defined in the description, and to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. The compounds of formula (I) are Nav1.7 inhibitors useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: December 6, 2012Publication date: October 23, 2014Applicant: PFIZER LIMITEDInventors: David James Rawson, Robert Ian Storer, Nigel Alan Swain
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Publication number: 20140315881Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.Type: ApplicationFiled: July 27, 2012Publication date: October 23, 2014Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
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Publication number: 20140315878Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or a pharmaceutically acceptable salt thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes, and to methods of treatment, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.Type: ApplicationFiled: April 17, 2014Publication date: October 23, 2014Applicant: PFIZER LIMITEDInventors: Robert Ian Storer, Nigel Alan Swain, Robert McKenzie Owen
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Publication number: 20140309206Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: June 27, 2014Publication date: October 16, 2014Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
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Publication number: 20140303139Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.Type: ApplicationFiled: August 31, 2012Publication date: October 9, 2014Inventors: Chiyou Ni, Laykea Tafesse, Jiangcho Yao, Mark Youngman, Minnie Park, Bin Shao
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Publication number: 20140301999Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: June 23, 2014Publication date: October 9, 2014Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Publication number: 20140303137Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: April 5, 2013Publication date: October 9, 2014Inventors: Michael Mortimore, Julian Golec, Daniel Robinson, John Studley
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Publication number: 20140303138Abstract: The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.Type: ApplicationFiled: December 3, 2013Publication date: October 9, 2014Inventors: Wilfried Braje, Astrid Netz, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Patent number: 8853196Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: GrantFiled: August 3, 2012Date of Patent: October 7, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
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Patent number: 8853197Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: GrantFiled: June 3, 2014Date of Patent: October 7, 2014Assignee: Wockhardt Ltd.Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
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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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Patent number: 8846655Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.Type: GrantFiled: October 28, 2010Date of Patent: September 30, 2014Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
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Publication number: 20140288049Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.Type: ApplicationFiled: June 9, 2014Publication date: September 25, 2014Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
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Publication number: 20140288044Abstract: The invention relates to compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders.Type: ApplicationFiled: April 12, 2012Publication date: September 25, 2014Applicant: Alzheimer's Institute of America, Inc.Inventors: Ryan Holcomb, Paul R. Sebahar, Kazuyuki Suzuki, Donald A. McLeod, David M. Dastrup, Christophe Hoarau, Robert J. Halter, Matthew Gregory Bursavich, Mark D. Shenderovich, Burt Richards, Paul L. Bartel
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Publication number: 20140288041Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: May 12, 2014Publication date: September 25, 2014Applicant: EPIZYME, INC.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
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Patent number: 8841287Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: June 11, 2009Date of Patent: September 23, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
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Publication number: 20140275006Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Mitsukane Yoshinaga, Takeshi Kuwada, Naoki Miyakoshi, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki
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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: 20140271662Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ? with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: February 14, 2014Publication date: September 18, 2014Applicants: Astex Therapeutics Ltd, Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer HospitalInventors: Valerio BERDINI, Gordon SAXTY, Marinus Leendert VERDONK, Steven John WOODHEAD, Paul Graham WYATT, Robert George BOYLE, Hannah Fiona SORE, David Winter WALKER, Ian COLLINS, Robert DOWNHAM, Robin Arthur Ellis CARR
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Publication number: 20140275002Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.Type: ApplicationFiled: March 7, 2014Publication date: September 18, 2014Applicant: Eli Lilly and CompanyInventors: Gary G. DENG, Danwen HUANG, Joshua O. ODINGO
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Publication number: 20140275012Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Todd BOSANAC, Michael J. BURKE, Darren DISALVO, Wang MAO, John WESTBROOK
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Publication number: 20140275003Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Applicant: NOVARTIS AGInventors: Paul A. Barsanti, Matthew Burger, Yan Lou, Gisele Nishiguchi, Valery Polyakov, Savithri Ramurthy, Alice Rico, Lina Setti, Aaron Smith, Benjamin Taft, Huw Tanner, Alan DiPesa, Naeem Yusuff
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Publication number: 20140256703Abstract: 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: ApplicationFiled: March 13, 2013Publication date: September 11, 2014Inventors: Juan-Miguel Jimenez, Philip Collier, Andrew Miller
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Publication number: 20140256708Abstract: The present invention is directed to substituted azetidinecompounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 1, 2012Publication date: September 11, 2014Inventors: Christopher D. Cox, Douglas C. Beshore, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen
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Publication number: 20140256699Abstract: Substituted cyclopropyl compounds of the formula I and the pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. Another aspect of the invention that is of interest relates to compounds of formula Ia.Type: ApplicationFiled: September 24, 2012Publication date: September 11, 2014Inventors: Michael W. Miller, Andrew W. Stamford, Kallol Basu, Scott Edmondson, Zhiqiang Guo, William B. Geiss
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Publication number: 20140256701Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins, Sean Turner
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Patent number: 8828987Abstract: The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is —O—, —O(C1-C3 alkyl)-; —(C1-C3 alkyl)O—; —C(O)—; —C(?N—O(C1-C3 alkyl))-; —NH— or —NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, —NH(C1-C3alkyl)-; —N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is covalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-memberType: GrantFiled: December 10, 2010Date of Patent: September 9, 2014Assignee: Rottapharm Biotech S.R.L.Inventors: Manuela Borriello, Lucio Rovati, Luigi Piero Stasi, Benedetta Buzzi, Fabrizio Colace
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Patent number: 8828986Abstract: Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and Hepatitis C.Type: GrantFiled: April 20, 2012Date of Patent: September 9, 2014Assignee: Prosetta Antiviral Inc.Inventors: Clarence Hurt, Andy Atuegbu, Anatoliy Kitaygorodskyy, Beverly Freeman, Vishwanath Lingappa
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Publication number: 20140249128Abstract: The present disclosure provides substituted triazine carboxamides of Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein A1, X, A2, E, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.Type: ApplicationFiled: February 26, 2014Publication date: September 4, 2014Applicant: Purdue Pharma L.P.Inventors: Dawit Tadesse, Jianming Yu
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Publication number: 20140249127Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: February 14, 2014Publication date: September 4, 2014Applicants: Genentech, Inc., Array BioPharma Inc.Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
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Patent number: 8822449Abstract: 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: GrantFiled: August 25, 2009Date of Patent: September 2, 2014Assignee: SanofiInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Patent number: 8822450Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: GrantFiled: August 24, 2012Date of Patent: September 2, 2014Assignee: Wockhardt Ltd.Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
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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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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: 20140243290Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: April 17, 2014Publication date: August 28, 2014Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon D. Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric T. Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Publication number: 20140235440Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: March 24, 2014Publication date: August 21, 2014Applicant: DOW AGROSCIENCES LLCInventors: Erich W. Baum, Gary D. Crouse, William H. Dent, III, Thomas C. Sparks, Lawrence C. Creemer
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Publication number: 20140235606Abstract: There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: AstraZeneca ABInventors: Britt Anne Ingela Gullberg, Thomas Peter Larsson, Jeffrey Paul Stonehouse
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Publication number: 20140235609Abstract: The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for treating diseases connected to tehinhibition of H3 receptor.Type: ApplicationFiled: October 8, 2012Publication date: August 21, 2014Inventors: Tie-Lin Wang, Xuechun Zhang