Polycyclo Ring System Having The Additional Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/252.04)
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Publication number: 20110166124Abstract: The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.Type: ApplicationFiled: July 21, 2009Publication date: July 7, 2011Inventors: Kevin D. McCormick, Robert G. Aslanian, Pietro Mangiaracina, Michael Y. Berlin, Manuel De Lera Ruiz, Christopher W. Boyce, Jianhua Chao, Pauline C. Ting, Junying Zheng, Stuart B. Rosenblum
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Publication number: 20110160220Abstract: The present disclosure generally relates to a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form, as well of methods of using a crystalline form in the treatment of depression and other conditions and methods for obtaining such crystalline form.Type: ApplicationFiled: June 4, 2009Publication date: June 30, 2011Inventors: Jun Qiu, Qi Gao, Shuang Liu, Min Hu, Yuh-Lin Allen Yang, Matthew Isherwood, Rasidul Amin
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Publication number: 20110160183Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: March 11, 2011Publication date: June 30, 2011Applicant: Merck & Co., Inc.Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
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Publication number: 20110160209Abstract: Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: June 18, 2009Publication date: June 30, 2011Inventors: Congxin Liang, Zhigang Li
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Publication number: 20110152282Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: August 24, 2009Publication date: June 23, 2011Applicant: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Patent number: 7960383Abstract: The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis or irritable bowel disease.Type: GrantFiled: June 13, 2005Date of Patent: June 14, 2011Assignee: Laboratorios Almirall SAInventors: Antonia Maria Buil Albero, Vittorio Dal Piaz, Yolanda Garrido Rubio, Jordi Gracia Ferrer, Lluis Miquel Pages Santacana, Joan Taltavull Moll
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Publication number: 20110136800Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: ApplicationFiled: November 5, 2010Publication date: June 9, 2011Inventors: Matthias Eckhardt, Stefan Peters, Herbert Nar, Frank Himmelsbach, Linghang Zhuang
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Publication number: 20110130406Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: September 5, 2008Publication date: June 2, 2011Applicants: Array BioPharma Inc., Genentech, Inc.Inventors: Jason DeMeese, John Gaudino, Alicia Tarin Neitzel, Paul Lunghofer, Jeongbeob Seo, Hongqi Tian, Wendy B. Young, Daniel P. Sutherlin
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Publication number: 20110118252Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: November 12, 2010Publication date: May 19, 2011Applicant: Amgen Inc.Inventors: Tae-Seong Kim, David Bauer, Steven Bellon, Alessandro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
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Publication number: 20110118230Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: June 10, 2009Publication date: May 19, 2011Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum Macleod, Karen Williams
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Publication number: 20110082099Abstract: The present invention relates to methods and compositions to treat subjects having cystic fibrosis. These compositions comprise the class of isothiocyanates. Isothiocyanates, absorbed by a cell are conjugated with glutathione GSH by glutathione-s-tranferase (GST). The conjugates are substrates of the multi-drug resistance associated (MRP)/multi-drug resistance (MDR) proteins. These proteins are functionally redundant to the cystic fibrosis transmembrane conductance regulator (CFTR), allowing for the substrate conjugates to be exported from the cell. The export of GSH conjugates restores intracellular and extracellular levels of GSH to normal levels. Normalizing both extracellular and intracellular GSH via the increased conjugation of isothiocyanates with GSH, and subsequent export, can significantly rectify numerous enzymatic processes and correct the pathologies that are typical of patients suffering from cystic fibrosis.Type: ApplicationFiled: June 14, 2010Publication date: April 7, 2011Inventor: Melanie Childers
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Publication number: 20110082135Abstract: The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: May 27, 2009Publication date: April 7, 2011Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Yoshio Ogino, Yu Onozaki, Michael A. Rossi, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
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Publication number: 20110077220Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: April 23, 2009Publication date: March 31, 2011Inventors: Scott D. Kuduk, Christina Ng Di Marco, William D. Shipe
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Publication number: 20110053931Abstract: Compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: June 8, 2007Publication date: March 3, 2011Inventors: John Gaudino, Steven Armen Boyd, Allison L. Marlow, Tomas Kaplan, Kin Chiu Fong, Jeongbeob Seo, Hongqi Tian, James Blake, Kevin Koch
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Publication number: 20110046110Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: April 30, 2009Publication date: February 24, 2011Inventors: Chi B. Vu, Jeremy S. Disch, Stephanic K. Springer, Charles A. Blum, Robert B. Perni
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Patent number: 7888351Abstract: The present invention relates to compounds of the formula; and their use in therapy.Type: GrantFiled: April 10, 2007Date of Patent: February 15, 2011Assignee: Novartis AGInventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
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Publication number: 20110034475Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.Type: ApplicationFiled: October 19, 2010Publication date: February 10, 2011Inventors: Dominik FEUERBACH, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
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Publication number: 20110021521Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: July 26, 2010Publication date: January 27, 2011Applicant: Gilead Palo Alto, Inc.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Publication number: 20110003798Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
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Publication number: 20100331339Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.Type: ApplicationFiled: January 9, 2009Publication date: December 30, 2010Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter Robert GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG, Mark Hadden, James Grabowski, Alexander Usyatinsky
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Publication number: 20100324060Abstract: This invention relates to combinations of Compound 1 and Compound 2 which are useful for treating hepatitis C virus infection.Type: ApplicationFiled: June 18, 2010Publication date: December 23, 2010Applicant: Gilead Sciences, Inc.Inventors: William E. Delaney, Hongmei Mo, Weidong Zhong
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Publication number: 20100324043Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: ApplicationFiled: June 16, 2010Publication date: December 23, 2010Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Publication number: 20100324059Abstract: This invention relates to combinations of Compound 1 and Compound 2 which are useful for treating hepatitis C virus infection.Type: ApplicationFiled: June 18, 2010Publication date: December 23, 2010Applicant: Gilead Sciences, Inc.Inventors: William E. Delaney, Hongmei Mo, Weidong Zhong
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Patent number: 7846932Abstract: A subject of the invention is the compounds of formula (I); in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.Type: GrantFiled: August 14, 2009Date of Patent: December 7, 2010Assignee: Galapagos SASInventors: Jean-Michel Lefrancois, Bertrand Heckmann
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Publication number: 20100298332Abstract: The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.Type: ApplicationFiled: July 29, 2010Publication date: November 25, 2010Applicant: Cephalon, Inc.Inventors: Reddeppa reddy Dandu, Robert L. Hudkins, Babu G. Sundar
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Publication number: 20100292242Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
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Publication number: 20100292212Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, m, A, R1 and R2 have the significance given in the description. The compounds are useful as HSL inhibitors and may be used in the treatment or prophylaxis of diabetes, dyslipidemia, atherosclerosis or obesity.Type: ApplicationFiled: May 3, 2010Publication date: November 18, 2010Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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Patent number: 7825119Abstract: A subject of the invention is the compounds of formula (I): in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.Type: GrantFiled: May 13, 2005Date of Patent: November 2, 2010Assignee: Galapagos SASInventors: Jean-Michel Lefrancois, Bertrand Heckmann
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Publication number: 20100267709Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: December 9, 2008Publication date: October 21, 2010Inventors: Jonathan R. Young, Jongwon Lim, Michelle R. Machacek, Brandon Mitsuo Taoka, Ryan D. Otte
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Publication number: 20100261701Abstract: The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKK? inhibiting activity and the like and is useful for the prevention and/or treatment of IKK?-associated diseases or symptoms and the like.Type: ApplicationFiled: October 1, 2009Publication date: October 14, 2010Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Shunsuke Kaneko, Kenichiro Sato, Daisuke Shikanai, Rintaro Yamada, Katsuhiko Sakurada
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Publication number: 20100261728Abstract: Tetrahydroisoquinoline compounds of formula (I), and compositions containing them, for the treatment of acute, inflammatory and neurophatic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neurophatic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceratType: ApplicationFiled: December 4, 2008Publication date: October 14, 2010Applicant: Amgen Inc.Inventors: Mark H. Norman, Yunxin Y. Bo, Vijay K. Gore, Daniel Horne, Matthew Kaller, Vu Van Ma, Holger Monenschein, Thomas Nguyen, Nobuko Nishimura, Nuria Tamayo
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Publication number: 20100240610Abstract: This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.Type: ApplicationFiled: February 10, 2010Publication date: September 23, 2010Inventors: JENNIFER R. ALLEN, KAUSTAV BISWAS, ROLAND BURLI, JENNIFER DAO, MICHAEL J. FROHN, JENNIFER E. GOLDEN, RANDALL W. HUNGATE, ROBERT KURZEJA, STEPHANIE J. MERCEDE, KRISTINE M. MULLER, SUSANA C. NEIRA, TANYA A. N. PETERKIN, CHRISTOPHER M. TEGLEY, VIOLETA YU
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Publication number: 20100227869Abstract: This invention relates to novel enantiopure azabicyclo pyridazinyloxy derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: February 13, 2007Publication date: September 9, 2010Inventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring
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Publication number: 20100222321Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: June 7, 2006Publication date: September 2, 2010Inventors: Donna J. Armstrong, Essa H. Hu, Michael J. Kelly, III, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang
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Publication number: 20100216793Abstract: The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.Type: ApplicationFiled: February 16, 2010Publication date: August 26, 2010Inventors: Daniela Alberati, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rose Maria Rodriguez Sarmiento, Mark Rogers-Evans, Markus Rudolph
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Publication number: 20100209345Abstract: The invention provides fluorinated compounds of formula (I): The compounds may be used in diagnosis or treatment of a disorder in a mammal characterised by an abnormal density of peripheral benzodiazepine receptors.Type: ApplicationFiled: August 24, 2007Publication date: August 19, 2010Inventors: Andrew Katsifis, Christopher John Reginald Fookes, Tien Quoc Pham, Ivan Damir Greguric, Maria Filomena Pereira Soares Mattner
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Publication number: 20100210590Abstract: The present invention relates to therapeutic and/or prophylactic uses of pyridazine compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disorder characterized by conduction disturbances, electroconvulsions and/or seizures, in particular epilepsy, more particularly pediatric epilepsy. In an aspect of the invention, the pyridnsine compound has the Formula (Ia) or (Ib) wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the description.Type: ApplicationFiled: February 29, 2008Publication date: August 19, 2010Applicant: NORTHWESTERN UNIVERSITYInventors: Martin D. Watterson, Linda J. Van Eldik, Mark S. Wainwright
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Publication number: 20100197651Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: February 4, 2010Publication date: August 5, 2010Inventors: Takahiko Taniguchi, Akira Kawada, Mitsuyo Kondo, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
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Publication number: 20100197698Abstract: To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and/or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases caused by pathological blood clots such as ischemic heart diseases (myocardial infarction, angina), intraatrial thrombus, pulmonary embolism, deep venous thrombosis, disseminated intravascular coagulation, ischemic cerebral diseases (cerebral infarction, cerebral bleeding) and arteriosclerosis and the like. To provide a pharmaceutical drug comprising a 5-phenyl-3-pyridazinone derivative represented by the following general formula (I): and an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, useful for preventing and/or treating disease conditions or symptoms mediated by plasminogen activator inhibitor-1.Type: ApplicationFiled: June 19, 2008Publication date: August 5, 2010Applicant: KOWA COMPANY, LTD.Inventors: Noriaki Gomi, Shinji Ina, Kenjirou Yamana, Yoshio Kaneko
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Patent number: 7763617Abstract: Novel pyrazolopyridine-4-yl pyridazinone derivatives serve as phosphodiesterase inhibitors and are useful compounds for use in pharmaceutical products. Specifically, the compounds of the present invention are pyrazolopyridine-4-yl pyridazinone derivatives represented by the following general formula (1): (Example: 6-(2-ethyl-7-methoxy-pyrazolo[1,5-a]pyridine-4-yl)-5-methyl-4, 5-dihydro-3(2H)-pyridazinone).Type: GrantFiled: March 6, 2006Date of Patent: July 27, 2010Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasushi Kohno, David Roger Adams, Naoki Ando
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Publication number: 20100184758Abstract: Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.Type: ApplicationFiled: July 15, 2008Publication date: July 22, 2010Inventors: Peter H. Dobbelaar, Wu Du, Liangqin Guo, William K. Hagmann, Shuwen He, Tianying Jian, Jian Liu, Ravi P. Nargund, Alexander Pasternak, Shrenik K. Shah, Quang T. Truong, Zhixiong Ye, James Deliureficio, Raman Bakshi
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Publication number: 20100184775Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.Type: ApplicationFiled: March 26, 2010Publication date: July 22, 2010Inventors: Mathias FREDERIKSEN, Dominik Feuerbach, Konstanze Hurth, Manuel Koller, Bernard Lucien Roy
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Publication number: 20100184763Abstract: This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HW molecule.Type: ApplicationFiled: February 10, 2010Publication date: July 22, 2010Inventors: Jennifer R. Allen, Kaustav Biswas, Roland Burli, Jennifer Dao, Michael J. Frohn, Jennifer E. Golden, Randall W. Hungate, Robert Kurzeja, Stephanie J. Mercede, Kristine M. Muller, Susana C. Neira, Tanya A. N. Peterkin, Christopher M. Tegley, Violeta Yu
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Publication number: 20100179152Abstract: The present invention is concerned with the use of PDE5 inhibitors in medicine.Type: ApplicationFiled: January 4, 2010Publication date: July 15, 2010Applicant: NYCOMED GmbHInventors: Torsten Dunkern, Christian Schudt, Friedrich Grimminger, Hossein Ardeschir Ghofrani, Manfred Kaps, Bernhard Rosengarten
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Publication number: 20100179160Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: ApplicationFiled: March 26, 2010Publication date: July 15, 2010Inventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY, Beatrix WAGNER
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Publication number: 20100179148Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 2, 2008Publication date: July 15, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Patent number: 7754720Abstract: A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections Methods of making and formulating compound (1) are provided.Type: GrantFiled: July 6, 2007Date of Patent: July 13, 2010Assignees: Gilead Sciences, Inc., K.U. Leuven Research & Development, Gerhard PuerstingerInventors: Steven S. Bondy, Terrence C. Dahl, David A. Oare, Reza Oliyai, Winston C. Tse, Vahid Zia
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Publication number: 20100160309Abstract: The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.Type: ApplicationFiled: March 10, 2008Publication date: June 24, 2010Inventors: Tony Siu, Jonathan Young, Micheal Altman, Alan Northrup, Ekaterina Kozina, Christopher Dinsmore, David J. Guerin, Kevin A. Keenan, Joon O. Jung, Solomon Kattar, Rachel N. MacCoss
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Publication number: 20100160335Abstract: It is to provide a novel pyridazinone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1 represents H or C1-6 alkyl, each of R2 and R3 represents H, X, C1-6 alkoxy, Z represents O or S, and A represents AA or BB, wherein AA represents: and BB represents: wherein R4 represents H or C1-6 alkyl, and each of R5 and R6 represents C1-6 alkyl.Type: ApplicationFiled: June 18, 2008Publication date: June 24, 2010Inventors: Yasushi Kohno, Koji Ochiai, Satoshi Takita, Akihiko Kojima, Tomohiko Eiraku, Tetsuya Kishi
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Publication number: 20100152193Abstract: The present invention is concerned with novel pyridazinones of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of CNS disorders.Type: ApplicationFiled: November 30, 2009Publication date: June 17, 2010Inventors: Daniela Alberati, Luca Gobbi, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento, Mark Rogers-Evans, Markus Rudolph