The Additional Hetero Ring Is Attached Indirectly To The Morpholine Ring By An Acyclic Chain Having A Hetero Atom As A Chain Member Patents (Class 514/237.2)
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Publication number: 20100298328Abstract: 1-Heterocyclylamino-2-hydroxy-3-amino-?-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.Type: ApplicationFiled: March 30, 2007Publication date: November 25, 2010Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
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Publication number: 20100279986Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Yue-Mei ZHANG, Bangping Xiang, Shyh-Ming Yang, Kenneth Rhodes, Robert Scannevin, Paul Jackson, Davraj Chakravarty, Xiaodong Fan, Lawrence J. Wilson, Prabha Karnachi
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Patent number: 7825152Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: April 9, 2007Date of Patent: November 2, 2010Assignee: Novartis AGInventors: Trixi Brandl, Jiping Fu, Francois Lenoir, David Thomas Parker, Michael Patane, Branko Radetich, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic, Aregahegn Yifru, Rui Zheng
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Patent number: 7825115Abstract: The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.Type: GrantFiled: January 10, 2008Date of Patent: November 2, 2010Assignee: Aventis Pharma S.A.Inventors: Marcel Patek, Anil Nair, Augustin Hittinger, Conception Nemecek, Daniel Bond, Greg Harlow, Herve Bouchard, Jacques Mauger, Jean-Luc Malleron, Mark Palermo, Fahad Al-Obeidi, Thomas Faitg, Hartmut Strobel, Sven Ruf, Kurt Ritter, Youssef El-Ahmad, Dominique Lesuisse, Didier Bénard
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Publication number: 20100273799Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: ApplicationFiled: June 24, 2010Publication date: October 28, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
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Publication number: 20100273797Abstract: The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions medicated by cytokines such as arthritis.Type: ApplicationFiled: July 2, 2010Publication date: October 28, 2010Inventors: Erik Boman, Susana Conde Ceide, Russell Dahl, Nancy G. J. Delaet, Justin Ernst, Antonio Garrido Montalban, Jeffrey Kahl, Christopher Larson, Stephen Miller, Hiroshi Nakanishi, Edward Roberts, Eddine Saiah, Robert Sullivan, Zhijun Wang
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Patent number: 7820661Abstract: Therapeutic compounds, compositions, medicaments, and methods are disclosed herein.Type: GrantFiled: April 22, 2009Date of Patent: October 26, 2010Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Publication number: 20100267726Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: DOMPE PHA.R.MA S.P.A.Inventors: Alessio MORICONI, Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Francesco Colotta
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Patent number: 7812023Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.Type: GrantFiled: November 5, 2009Date of Patent: October 12, 2010Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzèn, William Patrick Watson
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Publication number: 20100256147Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: April 14, 2008Publication date: October 7, 2010Inventor: David G. Hangauer, JR.
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Publication number: 20100222319Abstract: The disclosure relates to compounds of formula (I): wherein A, Z, Z?, L, R2 and R3 are as defined in the disclosure, to compositions comprising said compounds, and to methods for the manufacture and therapeutic use thereof.Type: ApplicationFiled: March 26, 2010Publication date: September 2, 2010Applicant: SANOFI-AVENTISInventors: Claude BERNHART, Monsif BOUABOULA, Pierre CASELLAS, Samir JEGHAM, Jèrome ARIGON, Romain COMBET, Sandrine HILAIRET, Pierre FRAISSE
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Publication number: 20100216792Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: October 14, 2009Publication date: August 26, 2010Applicant: Bayer CropScience AGInventors: Ulrich Görgens, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Publication number: 20100204200Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: wherein Q is an optionally substituted azetidinyl, pyrrolidinyl, piperidyl, and indolinyl; or Q is NR25R26; and A, R5, R6, R7, R8, R9, R25, R26 and Ar are substituents.Type: ApplicationFiled: April 21, 2010Publication date: August 12, 2010Applicant: IRM LLCInventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
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Publication number: 20100204211Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.Type: ApplicationFiled: December 22, 2009Publication date: August 12, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: John Edward PARK, Gerald Juergen ROTH, Armin HECKEL, Nveed CHAUDHARY, Trixi BRANDL, Georg DAHMANN, Matthias GRAUERT
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Publication number: 20100197564Abstract: The present invention provides compounds having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, which are useful as CB1 receptor antagonists. The compounds of the invention may be useful in treating diseases, disorders, or conditions responsive to CB1 receptor antagonists, including, but not limited to, metabolic syndrome, obesity, waist circumference, dyslipidemia, insulin sensitivity, neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.Type: ApplicationFiled: April 17, 2008Publication date: August 5, 2010Inventors: Jack D. Scott, Andrew Stamford
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Publication number: 20100183606Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Inventors: ROBERT M BORZILLERI, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Publication number: 20100179118Abstract: The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or —C(R6)(R7)—, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.Type: ApplicationFiled: September 7, 2007Publication date: July 15, 2010Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Michinori Ozawa, Tomoya Shiro, Takaaki Sumiyoshi, Mari Itoh
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Publication number: 20100172974Abstract: Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques are disclosed.Type: ApplicationFiled: March 12, 2010Publication date: July 8, 2010Inventors: Benjamin Oshlack, Mark Chasin, Hua-Pin Huang
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Publication number: 20100160299Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.Type: ApplicationFiled: September 30, 2009Publication date: June 24, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: James R. Baker, JR., Xue-min Cheng, Abraham F.L. Van Der Spek, Baohua Mark Huang, Thommey P. Thomas
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Publication number: 20100160326Abstract: A novel pesticide is provided. The present invention provides a pesticide containing, as an active ingredient, a pyridyl-methanamine derivative represented by the formula (I) or its salt: wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, a heterocyclic group, etc.; each of R2 and R3 which are independent of each other, is hydrogen, halogen, cyano, nitro, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, a heterocyclic group, etc.; R4 is trifluoromethyl or chlorodifluoromethyl; R5 is hydrogen, halogen, cyano, nitro, alkyl, etc.; each of R6 and R7 which are independent of each other, is hydrogen, cyano, alkyl, haloalkyl, etc.; R8 is alkyl, cycloalkyl, alkoxyalkyl, alkoxyalkoxyalkyl, hydroxyalkyl, halogen, haloalkyl, cyano, nitro, etc.; and n is an integer of from 0 to 4.Type: ApplicationFiled: July 20, 2007Publication date: June 24, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Hirohiko Kimura, Masayuki Morita, Kazuhiro Yamamoto, Toshihiko Ueki, Kumiko Azuma, Taku Hamamoto
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Publication number: 20100152190Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, R5, R6 and R7 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: ApplicationFiled: February 9, 2010Publication date: June 17, 2010Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Jing Zhang, Zhuming Zhang
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Publication number: 20100152138Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: ApplicationFiled: December 18, 2009Publication date: June 17, 2010Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Publication number: 20100130472Abstract: Provided herein are methods of utilizing bile acid transport inhibitors for the treatment of obesity and diabetes.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: SATIOGEN PHARMACEUTICALS, INC.Inventors: Andrew A. YOUNG, Bronislava GEDULIN, Howard E. GREENE
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Patent number: 7705146Abstract: The invention relates to compounds of formula (I) wherein R?, R2, R3, R4, R5, R6, Y, n and m are as defined herein. The compounds are useful for the treatment and prevention of hepatitis C viral infections in mammals by inhibiting HCV NS3 protease. The invention further relates to azalactone compounds of the formula (III) which can be reacted with an amide anion to produce the compounds of formula (I).Type: GrantFiled: June 22, 2005Date of Patent: April 27, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Murray D. Bailey, Punit Bhardwaj, Pasquale Forgione, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Montse Llinas-Brunet, Marc-Andre Poupart, Jean Rancourt
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Patent number: 7705001Abstract: Disclosed herein is a compound comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, X, R and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: March 17, 2009Date of Patent: April 27, 2010Assignee: Allergan, IncInventor: David W. Old
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Publication number: 20100093692Abstract: The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient.Type: ApplicationFiled: February 27, 2008Publication date: April 15, 2010Applicant: Schering Corporation Sechering-Plough CorporationInventors: Robert G. Aslanian, Jean E. Lachowicz, Michael Y. Berlin, Joyce J. Hwa
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Publication number: 20100093695Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, —C(O)—Y, —X—C(O)—Y, -alkylene-X—C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-X—C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-X—C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-X—C(O)—Y, -cycloalkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-X—C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heterType: ApplicationFiled: December 8, 2009Publication date: April 15, 2010Inventors: Hubert B. Josien, John W. Clader, Thomas A. Bara, Ruo Xu, Hongmei Li, Dmitri A. Pissarnitski, Zhiqiang Zhao
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Publication number: 20100087425Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, —C(O)—Y, —X—C(O)—Y, -alkylene-X—C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-X—C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-X—C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-X—C(O)—Y, -cycloalkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-X—C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heterType: ApplicationFiled: December 8, 2009Publication date: April 8, 2010Inventors: Hubert B. Josien, John W. Clader, Thomas A. Bara, Ruo Xu, Hongmei Li, Dmitri A. Pissarnitaki, Zhiqiang Zhao
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Publication number: 20100075971Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: ApplicationFiled: December 1, 2009Publication date: March 25, 2010Inventors: Jacques DUMAS, Wendy Lee, Yuanwei Chen, Lila Adnane, William J. Scott, Sharad Verma, Jianqing Chen, Zhi Chen, Lin Yi
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Publication number: 20100063045Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.Type: ApplicationFiled: March 28, 2008Publication date: March 11, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20100048571Abstract: The present disclosure relates to XIAP inhibitor compound of the formula I:Type: ApplicationFiled: December 7, 2007Publication date: February 25, 2010Inventors: Zhuoliang Chen, Run-Ming Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
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Publication number: 20100029652Abstract: The invention provides a method of treating hepatitis C, by providing compound of Formula I (shown below) in combination with a second active agent to a patient infected with the hepatitis C virus. Also provided herein are pharmaceutical combinations comprising a compound of Formula I and a second active agent. The pharmaceutical combination may be a unit dosage form or a packaged pharmaceutical composition. Packaged pharmaceutical combinations include a compound of Formula I and a second active agent in a package with instructions for using the formulation to treat a hepatitis C infection.Type: ApplicationFiled: December 17, 2007Publication date: February 4, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Mingjun Huang, Joanne Fabrycki, Wengang Yang, Xingtie Nie, Avinash Phadke, Milind Deshpande
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Publication number: 20100022546Abstract: The present invention provides adamantyl-diamide derivatives of formula (1): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: ApplicationFiled: July 17, 2009Publication date: January 28, 2010Applicant: H. LUNDBECK A/SInventors: Hermogenes N. Jimenenz, Guiying Li, Dario Doller, Michel Grenon, Andrew D. White, Gil Ma, Maojun Guo
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Publication number: 20100016291Abstract: The present invention is concerned with novel tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes. Formula (I).Type: ApplicationFiled: October 22, 2007Publication date: January 21, 2010Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Ten Holte, Guuske Frederike Busscher
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Publication number: 20100009971Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: August 19, 2009Publication date: January 14, 2010Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
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Publication number: 20100009968Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: June 28, 2007Publication date: January 14, 2010Applicant: High Point Pharmaceuticals, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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SELECTED CGRP ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS
Publication number: 20100004228Abstract: The present invention relates to the CGRP antagonists of general formula I wherein R1, R2, R3 and R4 are as defined in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: ApplicationFiled: June 17, 2009Publication date: January 7, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Dirk STENKAMP, Kirsten ARNDT, Henri DOODS -
Publication number: 20090318452Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Applicant: Vertex Pharmaceuticals IncorporatedInventors: John Cochran, Vincent Galullo, Guy W. Bemis
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Patent number: 7632835Abstract: The present invention relates to morpholine and thiomorpholine derivatives or the general formula I or pharmaceutically acceptable salts thereof and their use.Type: GrantFiled: January 28, 2009Date of Patent: December 15, 2009Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornoe, Mario Rottlander, Nikolay Khanzhin, Andreas Ritzen, William Patrick Watson
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Publication number: 20090306134Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.Type: ApplicationFiled: September 30, 2008Publication date: December 10, 2009Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Publication number: 20090306077Abstract: The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group, or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.Type: ApplicationFiled: December 26, 2007Publication date: December 10, 2009Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Patent number: 7625896Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: November 8, 2006Date of Patent: December 1, 2009Assignee: Hoffman-La Roche Inc.Inventors: Lothar Kling, Ulrike Reiff, Manfred Schwaiger, Georg Tiefenthaler, Wolfgang von der Saal, Thomas von Hirschheydt
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Publication number: 20090281089Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: April 8, 2009Publication date: November 12, 2009Applicant: Genentech, Inc.Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca L. LaLonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina
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Publication number: 20090264432Abstract: Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.Type: ApplicationFiled: April 5, 2007Publication date: October 22, 2009Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh
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Publication number: 20090264431Abstract: The invention is directed to compounds according to Formula I: wherein R1, R2a, R2b, R2c, R3, and n are defined below, and to pharmaceutically-acceptable salts thereof. They are cathepsin C inhibitors and can be used in the treatment of diseases mediated by the cathepsin C enzyme, such as COPD.Type: ApplicationFiled: August 18, 2008Publication date: October 22, 2009Inventors: Michael R. Palovich, Haibo Xie, Jianghe Deng, Dramane Ibrahim Laine
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Publication number: 20090253700Abstract: The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, n and Ar are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.Type: ApplicationFiled: April 15, 2005Publication date: October 8, 2009Inventors: Clive Leslie Branch, David John Nash, Howard Marshall, Roderick Porter
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Publication number: 20090239866Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: July 28, 2006Publication date: September 24, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jeffrey Michael Axten, Jesus R. Medina
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Publication number: 20090239867Abstract: Disclosed herein is a compound comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, X, R and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: March 17, 2009Publication date: September 24, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
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Publication number: 20090227569Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.Type: ApplicationFiled: February 25, 2009Publication date: September 10, 2009Applicant: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu