Double Bonded Divalent Chalcogen Containing Patents (Class 544/130)
-
Publication number: 20120245161Abstract: The present invention discloses and claims a series of substituted indolyl-piperidinyl benzylamines of the formula wherein R1, R2, R4 and R5 are as described herein. More specifically, the compounds of this invention are inhibitors of ?-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted indolyl-piperidinyl benzylamines.Type: ApplicationFiled: June 5, 2012Publication date: September 27, 2012Applicant: SANOFIInventors: Yong Mi CHOI-SLEDESKI, Guyan LIANG, Thaddeus R. NIEDUZAK, Gregory B. POLI, Patrick Wai-Kwok SHUM, Gregory T. STOKLOSA, Zhicheng ZHAO
-
Publication number: 20120245143Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: July 6, 2010Publication date: September 27, 2012Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Elena Casale, Alexander Khvat, Mikhail Yurievitch Krasavin, Paolo Orsini, Helena Posteri, Alessandra Scolaro
-
Publication number: 20120237475Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).Type: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck
-
Publication number: 20120238551Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: ApplicationFiled: December 22, 2011Publication date: September 20, 2012Applicants: Cephalon France, Cephalon, Inc.Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allizon L. Zulli, Christophe Yue
-
Publication number: 20120238574Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.Type: ApplicationFiled: October 26, 2010Publication date: September 20, 2012Applicant: N.V. ORGANONInventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
-
Publication number: 20120238750Abstract: The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group —CH?; R1 represents a group —Z—R6, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.Type: ApplicationFiled: February 29, 2012Publication date: September 20, 2012Inventors: Tae FUKUSHIMA, Shuji Matsumura, Noriaki Takemura, Hideaki Satou, Nobuaki Ito, Takuya Shitsuta, Hironori Tsutsui, Michinori Tanaka, Keizo Kan, Hitoshi Nagao, Kenji Watanabe, Kuninori Tai, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Keisuke Miyajima, Satoshi Yamada, Yutaka Kojima, Koichi Yasumura, Naoto Ohi, Mitsuhiro Okuno, Kazuhisa Sugiyama, Kunihiko Kiyono, Takashi Suzuki, Seiji Akamatsu, Takeshi Kodama, Yasuo Yanagihara, Takumi Sumida
-
Publication number: 20120238573Abstract: The present invention relates to substituted 2-amino-N-(4-fluoro-3-{1-[1-(alkyl)-1H-indole-3-carbonyl]-piperidin-4-yl}-benzyl)-acetamides (compounds of formula I) compositions thereof, and their use in the treatment of inflammatory diseases.Type: ApplicationFiled: June 5, 2012Publication date: September 20, 2012Applicant: SANOFIInventors: Yong Mi CHOI-SLEDESKI, Gregory B. POLI
-
Patent number: 8268996Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.Type: GrantFiled: June 16, 2011Date of Patent: September 18, 2012Assignee: IRM LLCInventors: Hong Liu, David C. Tully, Arnab Chatterjee, Phillip B. Alper, David H. Woodmansee, Daniel Mutnick
-
Publication number: 20120232052Abstract: The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.Type: ApplicationFiled: November 16, 2010Publication date: September 13, 2012Inventors: Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Tadashi Inoue
-
Publication number: 20120225867Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 27, 2010Publication date: September 6, 2012Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
-
Publication number: 20120225868Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: February 27, 2012Publication date: September 6, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
-
Publication number: 20120220564Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).Type: ApplicationFiled: September 17, 2010Publication date: August 30, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
-
Publication number: 20120220563Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: May 19, 2010Publication date: August 30, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Eckhard Bender, Katja Zimmermann, Anja Buchmüller, Christoph Gerdes, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
-
Publication number: 20120214807Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2011Publication date: August 23, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
-
Publication number: 20120214790Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: March 11, 2011Publication date: August 23, 2012Inventors: Megumi Maruyama, Naoya Kinomura, Satoshi Nojima, Masahiro Takamura, Keisuke Kakiguchi, Hiroto Tatamidani
-
Publication number: 20120208815Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: March 3, 2008Publication date: August 16, 2012Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Comelia Bellamacina, Kay Huh, Gordana Atallah, Christopher Mcbride, William Antonios-Mccrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Garcia
-
Publication number: 20120202786Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: April 16, 2012Publication date: August 9, 2012Applicant: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
-
Publication number: 20120201749Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C?O or —C?O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR2, OR1, CN or CO2R; Z1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.Type: ApplicationFiled: August 25, 2010Publication date: August 9, 2012Inventors: Melanie Jayne Crawshaw, Philip Spencer Fallon, Ashley Nicholas Jarvis, Jonathan Raymond Powell, Natalie Louise Winfield, David Selwood, Ian Charles Zachary, Haiyan Jia
-
Patent number: 8222249Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: GrantFiled: January 26, 2012Date of Patent: July 17, 2012Assignee: Celgene CorporationInventors: George W. Muller, Alexander L. Ruchelman
-
Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
-
Publication number: 20120172358Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: February 14, 2012Publication date: July 5, 2012Applicant: Prosidion LimitedInventors: Stuart Edward Bradley, Matthew Colin Thor Fyfe, Lisa Sarah Bertram, William Gattrell, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Chrystelle Marie Rasamison, Philip John Rushworth, Colin Peter Sambrook-Smith, David French Stonehouse, Simon Andrew Swain, Geoffrey Martyn Williams
-
Publication number: 20120157449Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: ApplicationFiled: December 7, 2011Publication date: June 21, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
-
Publication number: 20120149694Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: May 14, 2010Publication date: June 14, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Ulrich Rester, Eckhard Bender, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
-
Publication number: 20120142687Abstract: The present invention provides an indolecarboxylic acid derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1?X2—X3?X4— is a formula of —C(R1)?C(R2)—C(R3)?C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of —Z—R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: February 8, 2012Publication date: June 7, 2012Inventors: Akira KUGIMIYA, Yuki Tachibana
-
Publication number: 20120142690Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: May 18, 2010Publication date: June 7, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Ulrich Rester, Eckhard Bender, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gnoth, Kersten Matthias Gericke, Mario Jeske
-
Publication number: 20120132870Abstract: The present invention relates to indeno-fused naphthopyrans, and in particular indeno[2?,3?:3,4]naphtho[1,2-b]pyrans having certain groups bonded to the 3, 6, 7, 11, and 13 positions thereof. The indeno-fused naphthopyrans of the present invention have an ethylenically unsaturated group selected from (C1-C6 alkyl)acrylate and (C1-C6 alkyl)acrylamide, that is linked to the 11 position or 13 position thereof. The present invention also relates to photochromic articles and photochromic compositions containing such indeno-fused naphthopyrans.Type: ApplicationFiled: December 15, 2011Publication date: May 31, 2012Applicant: TRANSITIONS OPTICAL INC.Inventors: Wenjing Xiao, Barry Van Gemert
-
Publication number: 20120122850Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
-
Publication number: 20120122865Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Inventors: George W. MULLER, Alexander L. Ruchelman
-
Patent number: 8178531Abstract: The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention of organ transplantation rejection, the treatment of immune disorders and inflammation, and treatment of viral (particularly hepatitis C viral) infection.Type: GrantFiled: February 23, 2011Date of Patent: May 15, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Xuri Gao
-
Publication number: 20120115866Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: ApplicationFiled: January 12, 2012Publication date: May 10, 2012Applicant: TYROGENEX, INC.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
-
Publication number: 20120115845Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: November 7, 2011Publication date: May 10, 2012Inventors: Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
-
Patent number: 8168785Abstract: Provided are compounds and their pharmaceutically acceptable salts that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance.Type: GrantFiled: June 17, 2009Date of Patent: May 1, 2012Assignee: Biotie Therapies, Inc.Inventors: Thomas R. Malefyt, Lesley Pickford
-
Publication number: 20120101098Abstract: Compounds according to Formula (I) are described along with compositions containing the same and methods of use thereof for the treatment of viral infections.Type: ApplicationFiled: May 10, 2010Publication date: April 26, 2012Inventors: Kuo-Hsiung Lee, Keduo Qian, Donglei Yu, Chin-Ho Chen, Li Huang, Ibrahim Danlami Bori
-
Patent number: 8163746Abstract: Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.Type: GrantFiled: April 19, 2007Date of Patent: April 24, 2012Assignee: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Matsuzawa, Ryushi Seo, Hironori Harada, Akira Suga, Tomoaki Abe, Hidenori Azami, Shunichiro Matsumoto, Takashi Shin, Masayuki Tanahashi, Toru Watanabe
-
Publication number: 20120088752Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: ApplicationFiled: June 9, 2010Publication date: April 12, 2012Applicant: SIENA BIOTECH S.p.A.Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
-
Publication number: 20120088769Abstract: Provided herein are arylsulfonamide salts, e.g., a salt of a compound of Formula I, which are useful for modulating CCR3 activity, and their pharmaceutical compositions. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: October 10, 2011Publication date: April 12, 2012Applicant: Axikin Pharmaceuticals, Inc.Inventor: Tai Wei LY
-
Patent number: 8153785Abstract: The invention pertains to novel compounds of Formula (I) wherein R1, R2, R3, W, Y, Z, A, m, n, p, and q are defined herein. Such compounds are useful as stabilizing ligands in systems that assist in the determination of protein function.Type: GrantFiled: April 6, 2010Date of Patent: April 10, 2012Assignee: Cheminpharma LLCInventors: Uday Khire, Davoud Asgari
-
Publication number: 20120083604Abstract: Provided are compounds of formula I or II that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods oftreating patients suffering from or susceptible to at least one symptom of abuse of dependence on, or withdrawal from at least one substance.Type: ApplicationFiled: June 16, 2010Publication date: April 5, 2012Applicant: BIOTIE THERAPIES, INC.Inventors: Thomas R. Malefyt, Leslie Pickford
-
Publication number: 20120082702Abstract: Disclosed are nicotinamide compounds of Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. Also disclosed are methods of using such compounds in the treatment of at least one Btk associated condition, such as, for example, inflammatory disease, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: June 10, 2010Publication date: April 5, 2012Inventors: George V. DeLucca, Qing Shi, Chunjian Liu, Jingwu Duan, Andrew J. Tebben
-
Publication number: 20120077812Abstract: The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: November 30, 2011Publication date: March 29, 2012Inventors: JING FANG, Jun Tang, Andrew J. Carpenter, Gregory Peckham, Christopher R. Conlee, Kien S. Du, Subba Reddy Katamreddy
-
Publication number: 20120071467Abstract: Compounds or pharmacologically acceptable salts thereof are provided. In various embodiments the compounds have an antagonistic effect on a neurokinin NK1 receptor, a neurokinin NK2 receptor, and a muscarine M3 receptor. The compounds are useful as therapeutic agents for bronchial asthma, chronic obstructive pulmonary disease, or the like.Type: ApplicationFiled: September 16, 2011Publication date: March 22, 2012Applicant: Daiichi Sankyo Company, LimitedInventors: Takuya Ikeda, Takanori Yamazaki, Hiroshi Tsuchida
-
Publication number: 20120058988Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: ApplicationFiled: December 17, 2009Publication date: March 8, 2012Inventors: Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
-
Patent number: 8129375Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: GrantFiled: October 29, 2009Date of Patent: March 6, 2012Assignee: Celgene CorporationInventors: George W. Muller, Alexander L. Ruchelman
-
Publication number: 20120046268Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use 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 of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: March 12, 2010Publication date: February 23, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
-
Publication number: 20120035164Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Inventors: Jianghe DENG, Jeffrey K. KERNS, Qi JIN, Guoliang LIN, Xichen LIN, Michael LINDENMUTH, Christopher NEIPP, Hong NIE, Sonia M. THOMAS, Katherine L. WIDDOWSON
-
Publication number: 20120035134Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.Type: ApplicationFiled: August 5, 2011Publication date: February 9, 2012Applicant: ASTRAZENECA ABInventors: Robert Bruce DIEBOLD, Thomas GERO, Paul GROVER, Shan HUANG, Stephanos IOANNIDIS, Claude Afona OGOE, Jamal Carlos SAEH, Jeffrey Gilbert VARNES
-
Patent number: 8106191Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.Type: GrantFiled: June 13, 2003Date of Patent: January 31, 2012Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
-
Publication number: 20110319378Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: June 3, 2011Publication date: December 29, 2011Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
-
Publication number: 20110319412Abstract: The present invention discloses novel piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted monocyclic aryl or monocyclic heterocyclyl; X is a single bond or C(?O); Y is a single bond, CR5R6NR7 or C(?O)NR7; R1 and R2 are independently hydrogen or substituted or unsubstituted alkyl; R3 is substituted or unsubstituted aryl or heterocyclyl; R4 is halogen, substituted or unsubstituted alkyl, alkoxy, aryloxy or heterocyclyloxy, etc.; p is an integer of 0 to 2; q is 0 or 1; m is 0 or 1; n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or bicyclic fused hetero ring.Type: ApplicationFiled: March 5, 2010Publication date: December 29, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Masahiro Sakagami, Hitomi Araki, Hiroshi Hashizume, Hiroshi Yari, Kenji Takaya
-
Publication number: 20110312944Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: February 16, 2010Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell