Quinolizines (including Hydrogenated) Patents (Class 514/306)
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Patent number: 7888359Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).Type: GrantFiled: March 22, 2007Date of Patent: February 15, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Rueedi Georg, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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Publication number: 20110028407Abstract: The present invention provides compounds and compositions that enhance the innate immune system. The present invention comprises methods of preventing, treating or ameliorating an infectious disease comprising administering said compounds to a subject. The invention also comprises methods of formulation and administration of said compounds.Type: ApplicationFiled: February 8, 2008Publication date: February 3, 2011Inventors: Mark A. Jutila, Kirk J. Lubick
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Patent number: 7879875Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: GrantFiled: August 8, 2006Date of Patent: February 1, 2011Assignee: Merk Sharp & Dohme Corp.Inventors: Meng-Hsin Chen, James B. Doherty, Robert Tynebor, Swaminathan R. Natarajan, Zhen Li, Soumya P. Sahoo
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Publication number: 20110015201Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.Type: ApplicationFiled: February 12, 2009Publication date: January 20, 2011Inventors: James K. Chen, Joel M. Hyman, Cory A. Ocasio
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Publication number: 20110015180Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the variants R, R9, Z, X, Q and Y are defined in the specification.Type: ApplicationFiled: September 20, 2010Publication date: January 20, 2011Inventors: René Hersperger, Philipp Janser, Emil Pfenninger, Hans Juerg Wuethrich, Wolfgang Miltz
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Publication number: 20110003808Abstract: This invention relates to novel octahydroquinolizines for treatment or prevention of diabetes mellitus and its complications, for treatment or prevention of hyperlipidemia, for treatment of diabetic dyslipidemia, for treatment or prevention of the metabolic syndrome, for treatment of diseases related to metabolic dysfunction, for treatment of obesity or obesity-related diseases. The invention also includes pharmaceutical compositions and kits comprising these compounds alone or in combination with other drugs or compounds aiming towards an improved treatment or prevention of the aforementioned diseases or syndromes in humans or animals.Type: ApplicationFiled: December 17, 2008Publication date: January 6, 2011Applicant: 55PHARMA DRUG DISCOVERY & DEVELOPMENT AGInventors: Immanuel Adorjan, Leonhardt Bauer, Klaus Frobel, Clemens Fuernsinn
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Publication number: 20100324024Abstract: The present invention is directed to compounds of formula (I) (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: February 3, 2009Publication date: December 23, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
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Patent number: 7855203Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: December 13, 2007Date of Patent: December 21, 2010Assignee: Ortho-McNeil-Janssen Pharmaceuticals, Inc.Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Hong Ye, Leonard R. Hecker, David F. McComsey
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Publication number: 20100317690Abstract: Described are various compounds and methods for the treatment of disorders arising from aberrant protein folding, including in particular lysosomal storage diseases. In particular, polyhydroxylated alkaloids and imino sugars which are pharmacoperones of an enzyme and which do not bind to a catalytic site of said enzyme are described.Type: ApplicationFiled: November 20, 2008Publication date: December 16, 2010Inventors: Akane Kawamura, Alan Geoffrey Roach, Francis Xavier Wilson, Jonathon Mark Tinsley, Robert Nash, Richard Storer
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Patent number: 7842702Abstract: N-(1H-tetrazol-5-yl)-1-phenoxy-4H-quinolizin-4-one-3-carboxamide is effective for treating IBS. In addition, IBS may be effectively treated with N-(1H-tetrazol-5-yl)-1-phenoxy-4H-quinolizin-4-one-3-carboxamide when used concomitantly with at least one of various serotonin 5-HT3 receptor antagonists.Type: GrantFiled: February 7, 2008Date of Patent: November 30, 2010Assignee: Astellas Pharma Inc.Inventors: Ryuichi Takezawa, Hitoshi Doihara, Hiroyuki Ito, Jotaro Suzuki
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Patent number: 7842729Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.Type: GrantFiled: June 3, 2005Date of Patent: November 30, 2010Assignees: The United States of America as represented by the Department of Health and Human Services, Sequella, Inc.Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
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Publication number: 20100298372Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).Type: ApplicationFiled: December 9, 2008Publication date: November 25, 2010Inventors: Xianhai Huang, Robert G. Aslanian, Anandan Palani
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Publication number: 20100292170Abstract: Methods for diagnosing a pelvic pain disorder that include analyzing samples for increased levels and/or nuclear accumulation of beta-catenin, which indicates presence of the pelvic pain disorder, particularly interstitial cystitis. Therapeutic treatment of a pelvic pain disorder, particularly interstitial cystitis, includes the administration to a patient of an effective amount of an inhibitor of beta-catenin activity. This can be carried out by direct administration of the therapeutic agent or via gene therapy.Type: ApplicationFiled: November 5, 2008Publication date: November 18, 2010Applicant: UNIVERSITY OF ROCHESTERInventors: Jay E. Reeder, Robert D. Mayer, Mary O'Connell
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Publication number: 20100280003Abstract: The invention provides a pharmaceutical combination comprising: a) at least one agent selected from Bcr-Abl, Flt-3, FAK and RAF kinase inhibitors; and b) at least one JAK kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Nigel Graham Cooke, Paul W. Manley
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Publication number: 20100267766Abstract: The disclosure relates to a compound of formula (I): wherein m, n, Ar, and R are as defined in the disclosure, to compositions containing them and to their therapeutic use. The disclosure also relates to processes for preparing these compounds and to certain intermediate compounds.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: SANOFI-AVENTISInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Maria-Carmen Renones
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Publication number: 20100249124Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20100222355Abstract: The present invention is directed to spiropiperidine 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: October 15, 2008Publication date: September 2, 2010Inventors: Ronald K. Chang, Scott D. Kuduk
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Patent number: 7776880Abstract: The disclosure relates to a compound of formula (I): wherein m, n, Ar, and R are as defined in the disclosure, to compositions containing them and to their therapeutic use. The disclosure also relates to processes for preparing these compounds and to certain intermediate compounds.Type: GrantFiled: March 19, 2009Date of Patent: August 17, 2010Assignee: sanofi-aventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Maria-Carmen Renones
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Patent number: 7745459Abstract: A pharmaceutical agent having an anti-HIV action, particularly, a pharmaceutical agent having an integrase inhibitory action, is provided. The present invention relates to a quinolizinone compound represented by the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing same as an active ingredient. The compound of the present invention has an HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compounds can become a more effective anti-HIV agent. Since the compound has a high inhibitory activity specific for integrases, the compound can provide a safe pharmaceutical agent for human with a fewer side effects.Type: GrantFiled: September 20, 2005Date of Patent: June 29, 2010Assignee: Japan Tobacco Inc.Inventors: Motohide Satoh, Hisateru Aramaki, Hiroshi Nakamura, Masafumi Inoue, Hiroshi Kawakami, Hisashi Shinkai, Yuji Matsuzaki, Kazunobu Yamataka
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Patent number: 7737141Abstract: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.Type: GrantFiled: July 25, 2007Date of Patent: June 15, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Teiji Kimura, Koki Kawano, Noritaka Kitazawa, Nobuaki Sato, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Ikuo Kushida
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Publication number: 20100137230Abstract: The present invention relates to compounds of the formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: January 29, 2010Publication date: June 3, 2010Inventor: Lutz Weber
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Patent number: 7662821Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.Type: GrantFiled: October 12, 2004Date of Patent: February 16, 2010Assignee: Bayer Schering Pharma AGInventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
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Publication number: 20090275605Abstract: The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a proliferative disease or an inflammatory disease, the compound being 3,11b-cis-dihydrotetrabenazine or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 4, 2006Publication date: November 5, 2009Applicant: CAMBRIDGE LABORATORIES (IRELAND) LIMITEDInventors: Andrew John Duffield, Jean Elisabeth Yarrow
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Publication number: 20090275606Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable salts. These compounds can act as potential MEK inhibitors in the treatment of hyperproliferative diseases, like cancer and inflammation. The present invention also reveals methods of preparation thereof.Type: ApplicationFiled: April 21, 2009Publication date: November 5, 2009Inventors: Dinesh Chikkanna, Clive McCarthy, Henrik Moebitz, Chetan Pandit, Ramesh Sistla, Hosahalli Subramanya
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Publication number: 20090258881Abstract: The invention relates to aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description as well as to pharmaceutical compositions and medical treatments employing these compounds.Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Petra LENNIG
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Publication number: 20090258899Abstract: The disclosure relates to a compound of formula (I): wherein m, n, Ar, and R are as defined in the disclosure, to compositions containing them and to their therapeutic use. The disclosure also relates to processes for preparing these compounds and to certain intermediate compounds.Type: ApplicationFiled: March 19, 2009Publication date: October 15, 2009Applicant: SANOFI-AVENTISInventors: Gihad DARGAZANLI, Genevieve ESTENNE-BOUHTOU, Florence MEDAISKO, Maria-Carmen RENONES
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Publication number: 20090258872Abstract: The invention relates to therapeutic use of aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description.Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Petra LENNIG
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Patent number: 7595327Abstract: This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-?, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.Type: GrantFiled: March 16, 2006Date of Patent: September 29, 2009Assignee: WyethInventors: Jeremy I. Levin, Zhong Li, George Diamantidis, Frank E. Lovering, Weiheng Wang, Jeffrey S. Condon, Yang-I Lin, Jerauld S. Skotnicki, Kaapjoo Park
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Publication number: 20090203697Abstract: Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product. (In the formula, Ar1 represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like; Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group or the like; X1 represents —CR3?CR4— (wherein R3 and R4 respectively represent a C1-6 alkyl group or the like); and R1 and R2 respectively represent a C1-6 alkyl group or the like.Type: ApplicationFiled: May 18, 2007Publication date: August 13, 2009Inventors: Teiji Kimura, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Takehiko Miyagawa, Nobuaki Sato, Toshihiko Kaneko, Kogyoku Shin, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Hiroaki Hagiwara
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Patent number: 7569583Abstract: The invention relates to aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description as well as to pharmaceutical compositions and medical treatments employing these compounds.Type: GrantFiled: February 16, 2007Date of Patent: August 4, 2009Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
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Publication number: 20090181945Abstract: The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing A?40 and A?42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? such as Alzheimer's disease or Down's syndrome.Type: ApplicationFiled: March 13, 2009Publication date: July 16, 2009Inventors: Teiji Kimura, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Mamoru Takaishi, Koichi Ito, Toshihiko Kaneko, Takeo Sasaki, Takehiko Miyagawa, Hiroaki Hagiwara, Yu Yoshida
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Publication number: 20090131472Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: ApplicationFiled: August 8, 2006Publication date: May 21, 2009Inventors: Meng-Hsin Chen, James B. Doherty, Robert Tynebor, Swaminathan R. Natarajan, Zhen Li, Soumya P. Sahoo
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Publication number: 20090124595Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: November 7, 2008Publication date: May 14, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: MarK Adams, Qing Dong, Toufike Kanouni, Stephen W. Kaldor, Nicholas Scorah, Michael B. Wallace
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Publication number: 20090062268Abstract: A compound having the structure set forth in Formula (I): wherein the variables Y, R1, R2, R3, R4 and R5 are as defined herein. Compounds described herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of such compounds and pharmaceutical compositions to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: July 25, 2008Publication date: March 5, 2009Applicant: LEAD THERAPEUTICS, INC.Inventor: Daniel CHU
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Publication number: 20090048213Abstract: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.Type: ApplicationFiled: July 25, 2007Publication date: February 19, 2009Inventors: Teiji Kimura, Koki Kawano, Noritaka Kitazawa, Nobuaki Sato, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Ikuo Kushida
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Publication number: 20090017036Abstract: The present invention relates to novel pharmaceutical compositions comprising at least one EGFR kinase inhibitor and at least one additional active compound selected from beta-2 mimetics, steroids, PDE-IV inhibitors, p38 MAP kinase inhibitors, NK1 antagonists and endothelin-antagonists, processes for preparing the compositions and the use thereof as medicament in the treatment of respiratory or gastrointestinal complaints, as well as inflammatory diseases of the joints, the skin or the eyes.Type: ApplicationFiled: September 2, 2008Publication date: January 15, 2009Inventors: Birgit Jung, Frank Himmelsbach
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Patent number: 7473701Abstract: Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particular in oncology.Type: GrantFiled: October 13, 2004Date of Patent: January 6, 2009Assignee: Aventis Pharma S.A.Inventors: Dominique Damour, Jean-Christophe Carry, Patrick Nemecek, Corinne Terrier, Frederico Nardi, Bruno Filoche-Romme, Marie-Pierre Cherrier, Daniel Bezard
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Publication number: 20080306109Abstract: Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of, for example, asthma, chronic obstructive pulmonary disease, rhinitis, allergic airway syndrome, and allergic rhinobronchitis. Formula (I) wherein R1, R2.Type: ApplicationFiled: September 14, 2006Publication date: December 11, 2008Inventors: George Hynd, Nicholas Charles Ray, Harry Finch, John Gary Montana, Michael Colin Cramp, Trevor Keith Harrison, Rosa Arienzo, Paul Blaney, Yann Griffon, David Middlemiss
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Patent number: 7456222Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.Type: GrantFiled: July 1, 2005Date of Patent: November 25, 2008Assignees: Sequella, Inc., The United States of America as represented by the Secretary, Department of Health and Human ServicesInventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
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Publication number: 20080262031Abstract: New 4-aminoquinoline derivatives having the general formula (I) wherein R, M, X, Y and T have the meaning described in the specification, as potent antimalarials active also on chloroquine-resistant Plasmodium falciparum malaria strains.Type: ApplicationFiled: February 1, 2006Publication date: October 23, 2008Applicant: CTG PHARMA S.R.L.Inventor: Fabio Sparatore
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Patent number: 7417055Abstract: The invention is related to phosphorus substituted kinase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: April 26, 2004Date of Patent: August 26, 2008Assignee: Gilead Sciences, Inc.Inventors: Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Manoj Desai, Maria Fardis, Thorsten Kirschberg, Richard L. Mackman, Sundaramoorthi Swaminathan, William J. Watkins
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Publication number: 20080194609Abstract: The present application relates to novel tetrahydroquinoline derivatives, to a process for their preparation, to their use on their own or in combination for treating and/or preventing diseases and to their use for preparing medicaments, in particular as inhibitors of the cholesterol ester transfer protein (CETP) for the treatment and/or prevention of cardiovascular disorders, in particular hypolipoproteinemias, dyslipidemias, hypertriglyceridemias, hyperlipidemias, hypercholesterolemias and arteriosclerosis.Type: ApplicationFiled: December 10, 2005Publication date: August 14, 2008Applicant: Bayer HeathCare AGInventors: Hilmar Bischoff, Heike Gielen-Haertwig, Volkhart Li, Carsten Schmeck, Michael Thutewohl, Martina Wuttke, Alexandros Vakalopoulos, Olaf Weber
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Publication number: 20080188512Abstract: N-(1H-tetrazol-5-yl)-1-phenoxy-4H-quinolizin-4-one-3-carboxamide is effective for treating IBS. In addition, IBS may be effectively treated with N-(1H-tetrazol-5-yl)-1-phenoxy-4H-quinolizin-4-one-3-carboxamide when used concomitantly with at least one of various serotonin 5-HT3 receptor antagonists.Type: ApplicationFiled: February 7, 2008Publication date: August 7, 2008Applicant: Astellas Pharma Inc.Inventors: Ryuichi Takezawa, Hitoshi Doihara, Hiroyuki Ito, Jotaro Suzuki
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Publication number: 20080176833Abstract: This invention provides novel dihydropyridine derivatives of the formula I having protein tyrosine kinase inhibitory activity, to process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions.Type: ApplicationFiled: December 13, 2007Publication date: July 24, 2008Inventors: Marc Adler, Stefan Baeurle, Judi Bryant, Ming Chen, Yuo-Ling Chou, Paul Hrvatin, Seock-Kyu Khim, Monica Kochanny, Wheeseong Lee, Michael Mamounas, Janet Meurer Ogden, Gary Bruce Phillips, Victor Selchau, Christopher West, Bin Ye, Shendong Yuan, Martin Krueger
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Publication number: 20080176860Abstract: The present invention relates to compounds of the formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: January 21, 2008Publication date: July 24, 2008Inventor: Lutz Weber
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Publication number: 20080167318Abstract: The present invention is related to pyrrolidine derivatives of formula I. Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula I are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation.Type: ApplicationFiled: April 9, 2007Publication date: July 10, 2008Applicant: APPLIED RESEARCH SYSTEM ARS HOLDING N.V.Inventors: Serge Halazy, Anna Quattropani, Alexander Scheer, Matthias Schwarz, Russell J. Thomas, Anthony Baxter
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Patent number: 7329657Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: August 2, 2004Date of Patent: February 12, 2008Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Han-Cheng Zhang, Bruce Maryanoff, Bruce Conway, Kimberly White, Hong Ye, Leonard Robert Hecker, David F. McComsey
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Patent number: 7304060Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: July 6, 2004Date of Patent: December 4, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Han-Cheng Zhang, Bruce Maryanoff, Bruce Conway, Kimberly White, Hong Ye, Leonard Robert Hecker, David F. McComsey
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Patent number: 7253182Abstract: Disclosed are enantiomerically pure cyclic aminoalcohol esters of arylcycloalkylhydroxycarboxylic acids with at least 90% enantiomeric excess of the (3R,2?R), (3S,2?R), (3R,2?S), or (3S,2?S) configured enantiomer.Type: GrantFiled: June 23, 2003Date of Patent: August 7, 2007Assignee: Sofotec GmbH & Co. KGInventors: Christian Noe, Ernst Mutschler, Günter Lambrecht, Ruth Irene Elgert, legal representative, Sittah Czeche, Magali Waelbroeck, Michael Elgert, deceased
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Patent number: 7229996Abstract: Novel rifamycin derivatives of formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or their salts, hydrates or prodrugs thereof, wherein: a preferred R comprises hydrogen, acetyl; L is a linker, a preferred linker group elements selected from any combination of 1 to 5 groups shown FIG. 1, provided L is not wherein R1 is H, methyl or alkyl. The inventive compounds exhibit valuable antibiotic properties. Formulations having these compounds can be used in the control or prevention of infectious diseases in mammals, both humans and non-humans. In particular, the compounds exhibit a pronounced antibacterial activity, even against multiresistant strains of microbes.Type: GrantFiled: July 21, 2005Date of Patent: June 12, 2007Assignee: Cumbre Pharmaceuticals Inc.Inventors: Zhenkun Ma, Jing Li, Susan Harran, Yong He, Keith P. Minor, In Ho Kim, Charles Z. Ding, Jamie C. Longgood, Yafei Jin, Keith D. Combrink