The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/127)
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Patent number: 8741932Abstract: The present invention relates to compounds of formula (I), wherein Ra, Rb, Rc, Rd, Re and Rf are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PI3K), mammalian target of rapamycin (mTOR), Signal transducer and activator of transcription 3 (STAT 3), tumor necrosis factor-? (TNF-?), interleukin-6 (IL-6) or a combination thereof particularly in the treatment of cancer and inflammation.Type: GrantFiled: November 4, 2010Date of Patent: June 3, 2014Assignee: Piramal Enterprises LimitedInventors: Sanjay Kumar, Sivaramakrishnan Hariharan, Mandar Bhonde, Nilesh Dagia, Rajiv Sharma, Pallavi Hanmantrao Mane, Pramod Bhaskar Kumar
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Publication number: 20140148430Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: November 26, 2012Publication date: May 29, 2014Applicant: Gilead Connecticut, Inc.Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
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Publication number: 20140148440Abstract: The present invention relates to heterocyclyl compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors, for example cognitive disorders, sleep disorders, obesity and pain.Type: ApplicationFiled: November 15, 2010Publication date: May 29, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Rambabu Namala, Adi Reddy Dwarampudi, Laxman Kota, Murlimohan Gampa, Padmavathi Kodru, Taraka Naga Vinaykumar Tiriveedhi, Vishwottam Nagaraj Kandikere, Nageshwara Rao Muddana, Ramanatha Shrikantha Saralaya, Pradeep Jayarajan, Dhanalakshmi Shanmuganathan, Ishtiyaque Ahmad, Venkateswarlu Jasti
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Publication number: 20140142302Abstract: A 1,5-naphthyridine derivative represented by Formula [1] (in which R1, R2, R3, R4 and R5 represent a hydrogen atom, -L-Z (in which Z represents a non-aromatic heterocyclic group or the like; and L represents a single bond or the like), or the like, R6 represents -L-Z or the like, R7 and R8 represent a hydrogen atom or the like, and Q represents an oxygen atom or the like), or a salt thereof has an excellent inhibitory activity with respect to the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway, and is useful for treatments such as prophylactic treatments and therapeutic treatments of diseases in which the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway are involved.Type: ApplicationFiled: January 28, 2014Publication date: May 22, 2014Applicant: FUJIFILM CorporationInventors: Hidetomo FURUYAMA, Hideki KURIHARA, Kentarou FURUYA, Takahiro TERAO, Shinichirou SEKINE, Daisuke NAKAGAWA
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Publication number: 20140142100Abstract: The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.Type: ApplicationFiled: January 24, 2014Publication date: May 22, 2014Applicant: BASILEA PHARMACEUTICA AGInventors: Johannes Laurenz Kellenberger, Jürg Dreier
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Patent number: 8729074Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: GrantFiled: March 19, 2010Date of Patent: May 20, 2014Assignee: Amgen Inc.Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
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Publication number: 20140128600Abstract: The present invention provides methods of synthesizing compounds of formula (1) and intermediates thereto. The present invention also provides intermediates useful in the synthesis of compounds of formula (1).Type: ApplicationFiled: May 11, 2012Publication date: May 8, 2014Applicant: Bionomics LimitedInventors: Dharam Paul, Andrew John Harvey, Bernard Luke Flynn
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Publication number: 20140128386Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 4, 2013Publication date: May 8, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Ingo HARTUNG, Markus FOLLMANN, Rolf JAUTELAT, Alexander STRAUB, Jorma HAßFELD, Niels LINDNER, Dirk SCHNEIDER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
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Publication number: 20140128385Abstract: The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased ? cell mass and/or function.Type: ApplicationFiled: January 13, 2012Publication date: May 8, 2014Inventor: Heinrich Ruegger
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Publication number: 20140128391Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.Type: ApplicationFiled: November 1, 2013Publication date: May 8, 2014Inventors: John H. van Duzer, Ralph Mazitschek
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Publication number: 20140128372Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: March 7, 2013Publication date: May 8, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva-Maria BECKER, Andreas KNORR
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Patent number: 8710054Abstract: A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: November 20, 2012Date of Patent: April 29, 2014Assignee: UCB Pharma, S.A.Inventors: Rikki Peter Alexander, Pavandeep Singh Aujla, Karen Viviane Lucile Crepy, Anne Marie Foley, Richard Jeremy Franklin
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Patent number: 8703759Abstract: The present disclosure 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 R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: June 30, 2011Date of Patent: April 22, 2014Assignee: Gilead Sciences, Inc.Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Publication number: 20140107118Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: NOVARTIS AGInventors: Sangamesh BADIGER, Murali CHEBROLU, Konstanze HURTH, Sebastien JACQUIER, Rainer Martin LUEOEND, Rainer MACHAUER, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
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Patent number: 8697691Abstract: In one aspect, the invention relates to compounds having a general structure: which are useful as selective allosteric or bitopic agonists of the M1 muscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: December 21, 2010Date of Patent: April 15, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Michael R. Wood, Rocco D. Gogliotti, Colleen M. Niswender, Bruce J. Melancon, Evan P. Lebois
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Patent number: 8691810Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, B, R1, R2, R3, R4a, R5, and Z 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 aurora.Type: GrantFiled: May 12, 2011Date of Patent: April 8, 2014Assignee: AbbVie Inc.Inventors: Michael R. Michaelides, Andrew S. Judd, Shannon R. Fix-Stenzel, Richard F. Clark, Bryan K. Sorensen, Zhiqin Ji
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Patent number: 8685967Abstract: The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.Type: GrantFiled: April 5, 2010Date of Patent: April 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Ginny D. Ho, Elizabeth M. Smith, Eugenia Y. Kiselgof, Kallol Basu, Zheng Tan, Brian McKittrick, Deen Tulshian
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Publication number: 20140088068Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: ApplicationFiled: August 24, 2012Publication date: March 27, 2014Inventors: Sachin Bhagwat, Prasad Keshav Deshpande, Satish Bhawsar, Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Shivaji Sampatrao Pawar, Sunil Bhaginath Jadhav, Sanjay Kisan Dabhade, Vikas Vitthalrao Deshmukh, Bharat Dond, Satish Birajdar, Mohammad Usman Shaikh, Deepak Dekhane, Piyush Ambalal Patel
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Publication number: 20140088080Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
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Publication number: 20140088101Abstract: The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).Type: ApplicationFiled: February 1, 2012Publication date: March 27, 2014Applicant: FibroGen, Inc.Inventors: Danny Ng, Michael P. Arend, Lee A. Flippin
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Patent number: 8680089Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: GrantFiled: January 17, 2011Date of Patent: March 25, 2014Assignee: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Patent number: 8680096Abstract: The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3.Type: GrantFiled: December 3, 2010Date of Patent: March 25, 2014Assignee: Sanofi-AventisInventors: Florian Auger, Luc Even
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Patent number: 8680098Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: GrantFiled: February 25, 2011Date of Patent: March 25, 2014Assignee: Janssen Pharmaceutica, NVInventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
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Publication number: 20140080804Abstract: The invention provides novel substituted 6-arylamino pyridone carboxamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, poly-morph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.Type: ApplicationFiled: November 1, 2011Publication date: March 20, 2014Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Shixin Wang, Rong Yu, Wei Hu, Zhi Liang, Xijie Liu, Quan Hu
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Publication number: 20140073635Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: November 8, 2013Publication date: March 13, 2014Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
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Publication number: 20140065095Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: June 5, 2013Publication date: March 6, 2014Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
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Publication number: 20140057894Abstract: Disclosed herein is a compound of Formula I: wherein X, R1, R2, and R3 are as defend herein, or a pharmaceutically acceptable salt thereof to allow the drug to penetrate the cell membrane; or a prodrug, or the compound is labeled with a detectable label or an affinity tag thereof. Also disclosed is a pharmaceutical composition, a method of treating a disorder mediated by melanocortin-4 receptors, and a method of treating obesity using the compounds described.Type: ApplicationFiled: January 26, 2012Publication date: February 27, 2014Applicant: Universite De MontrealInventors: Michel Bouvier, Anne Marinier, Rejean Ruel, Patricia René, Yves Chantigny, Philippe Dagneau, Stéphane Gingras
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Publication number: 20140057891Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl 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.Type: ApplicationFiled: November 4, 2013Publication date: February 27, 2014Applicant: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20140051677Abstract: Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.Type: ApplicationFiled: April 26, 2012Publication date: February 20, 2014Inventors: Christel Jeanne Marie Menet, Alastair James Hodges, Huw David Vater
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Publication number: 20140045839Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.Type: ApplicationFiled: September 18, 2013Publication date: February 13, 2014Applicant: Bionomics LimitedInventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Phillip Street, Nurul Quazi, Chinh Thien Bui
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Publication number: 20140038936Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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.Type: ApplicationFiled: May 7, 2013Publication date: February 6, 2014Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
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Publication number: 20140038955Abstract: Heteroaryl amide analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: October 2, 2013Publication date: February 6, 2014Applicant: H. Lundbeck A/SInventors: David C. IHLE, Qin GUO, Kevin HODGETTS, Jun YUAN
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Publication number: 20140038960Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: October 4, 2013Publication date: February 6, 2014Applicant: MERCK PATENT GMBHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20140038939Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.Type: ApplicationFiled: October 9, 2013Publication date: February 6, 2014Applicant: Genentech, Inc.Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Christopher Hurley, Jun Liang, Wendy Liu, Joseph P. Lyssikatos
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Patent number: 8642595Abstract: This invention relates to novel annellated 4-(indazolyl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: GrantFiled: May 29, 2009Date of Patent: February 4, 2014Assignee: Bayer Intellectual Property GmbHInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Karen Engel
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Publication number: 20140031339Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1, A2, L1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 16, 2013Publication date: January 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael Jason BURKE, Thomas Martin KIRRANE, JR., Chuk Chui MAN, Daniel Richard MARSHALL, Anil Kumar PADYANA, Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Roger John SNOW, Ronald John SORCEK, Hidenori TAKAHASHI, Steven John TAYLOR, Michael Robert TURNER, Erick Richard Roush YOUNG, Qiang ZHANG, Yunlong ZHANG, Renee M. ZINDELL
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Publication number: 20140030191Abstract: A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN? groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.Type: ApplicationFiled: April 20, 2012Publication date: January 30, 2014Applicant: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Sylvain Routier, Franck Suzenet, Frederic Pin, Sylvie Chalon, Johnny Vercouillie, Denis Guilloteau
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Patent number: 8637509Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: GrantFiled: May 5, 2011Date of Patent: January 28, 2014Assignee: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis LaFrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
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Publication number: 20140024646Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, R5, Z1 and Z2 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: July 16, 2013Publication date: January 23, 2014Applicant: Janssen Pharmaceutica NVInventors: Chaozhong Cai, David F. MCCOMSEY, Zhihua Sui, Fu-An Kang
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Publication number: 20140018345Abstract: Compounds of formula (I): wherein R1, R2, R3, R5, R6, A1, A2, A3, A4 assume meanings as defined in formula (I) are inhibitors of neutrophil elastase.Type: ApplicationFiled: July 12, 2013Publication date: January 16, 2014Applicant: CHIESI FARMACEUTICI S.p.AInventors: Carmelida Capaldi, Robert Andrew Heald, Nicholas Charles Ray, Jonathan Mark Sutton
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Publication number: 20140018533Abstract: To provide a novel furanone derivative, and a medicine including the same.Type: ApplicationFiled: March 30, 2012Publication date: January 16, 2014Applicants: CARNA BIOSCIENCES, INC., SBI BIOTECH CO., LTD.Inventors: Takayuki Irie, Ayako Sawa, Masaaki Sawa, Tokiko Asami, Yoko Funakoshi, Chika Tanaka
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Publication number: 20140011806Abstract: This invention describes substituted pyrazole derivatives of Formula I and methods of making and using the compounds. These compounds have utility in the treatment of conditions or diseases in which modification of the activity of ERK would have a positive therapeutic outcome, for instance various cancers, psoriasis and actinic keratosis.Type: ApplicationFiled: January 3, 2012Publication date: January 9, 2014Applicant: KINENTIA BIOSCIENCES LLCInventors: David Fairfax, Russell Joseph Deorazio
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Publication number: 20140011807Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.Type: ApplicationFiled: March 15, 2012Publication date: January 9, 2014Applicants: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD., MITSUBISHI TANABE PHARMA CORPORATIONInventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie
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Publication number: 20140005383Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.Type: ApplicationFiled: September 5, 2013Publication date: January 2, 2014Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Publication number: 20140005170Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: September 6, 2013Publication date: January 2, 2014Applicant: Samumed, LLCInventors: John Hood, David Mark Wallace, Sunil Kumar KC
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Publication number: 20130345218Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: June 14, 2013Publication date: December 26, 2013Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Marion W. Wannamaker, Tiansheng Wang, Francesco G. Salituro
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Publication number: 20130345181Abstract: The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them.Type: ApplicationFiled: March 14, 2012Publication date: December 26, 2013Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Vassilios Bavetsias, Butrus Atrash, Sébastien Gaston André Naud, Peter William Sheldrake, Julian Blagg
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Publication number: 20130345192Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.Type: ApplicationFiled: October 28, 2011Publication date: December 26, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
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Patent number: 8609648Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: December 17, 2013Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
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Publication number: 20130331378Abstract: A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as a therapeutic agent for lower urinary tract symptoms (LUTS), particularly, overactive bladder syndrome (OABs), or a prophylactic agent therefor and furthermore, is also useful in the treatment, prevention, or suppression of various pathological conditions in which the EP1 receptor is involved, such as inflammatory disease, pain disease, osteoporosis, and cancer. [A is a benzene ring or the like, Y1 is C1-6 alkylene, R1 is —C(?O)—OZ1 or the like, Z1 is H or the like, R2 is a branched C3-6 alkyl group or the like, R3 is H or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like].Type: ApplicationFiled: January 25, 2012Publication date: December 12, 2013Applicants: KISSEI PHARMACEUTICAL CO., LTD., KYORIN PHARMACEUTICAL CO., LTD.Inventors: Shigeki Seto, Kentaro Umei, Yosuke Nishigaya, Asao Tanioka, Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura