The Additional Hetero Ring Is Six-membered And Contains Nitrogen Patents (Class 540/481)
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Patent number: 10851087Abstract: The present disclosure provides processes for the preparation of cerdulatinib, which is of formula I: or a salt thereof. The disclosure also provides intermediates and processes for the preparation of the intermediates useful in the preparation of cerdulatinib or a salt thereof.Type: GrantFiled: May 3, 2019Date of Patent: December 1, 2020Assignee: Portola Pharmaceuticals, Inc.Inventors: Anjali Pandey, Arvinder Sran, Ying Chen, Daniele Poggiali, Tiziano Fumagalli
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Publication number: 20140249135Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: May 9, 2014Publication date: September 4, 2014Applicant: NOVARTIS AGInventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
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Patent number: 8822451Abstract: 4-amido-pyrimidine compounds, derivatives and compositions thereof, and synthetic methods described herein are useful for modulating ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: May 22, 2006Date of Patent: September 2, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Anna R. Hazlewood, Peter D. J. Grootenhuis, Ashvani Kumar Singh, Thomas Cleveland, Frederick F. Van-Goor
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Patent number: 8772478Abstract: Benzenesulfonamide compounds having a structure of the following general formula (I) are described. Also described, are methods for synthesizing the compounds, and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: June 28, 2010Date of Patent: July 8, 2014Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlène Schuppli
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Patent number: 8765941Abstract: Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.Type: GrantFiled: February 4, 2009Date of Patent: July 1, 2014Assignee: Kino Pharma, Inc.Inventors: Hiroshi Onogi, Masatoshi Hagiwara, Masaaki Suzuki, Hiroko Koyama, Takamitsu Hosoya, Toshiyuki Hiramatsu
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Patent number: 8524894Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: GrantFiled: June 4, 2010Date of Patent: September 3, 2013Assignee: Laboratorios Salvat, S.A.Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleo Mas
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Patent number: 8389560Abstract: This invention relates to macrocyclic compounds of formula (I) shown in the specification. These compounds can be used to treat hepatitis C virus infection.Type: GrantFiled: September 15, 2009Date of Patent: March 5, 2013Assignee: TaiGen Biotechnology Co., Ltd.Inventors: Chen-Fu Liu, Kuang-Yuan Lee, Pei-Chin Cheng, Yo-Chin Liu, Pin Lo, Kuo-Feng Tseng, Chih-Ming Chen, Chi-Hsin Richard King, Chu-Chung Lin
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Publication number: 20120309742Abstract: The invention concerns the use an mGluR modulator, e.g. an mGluR5 modulator, for the treatment, prevention or delay of progression of cognitive dysfunction.Type: ApplicationFiled: August 8, 2012Publication date: December 6, 2012Inventors: Ralf GLATTHAR, Donald JOHNS, Daniel UMBRICHT
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Publication number: 20120232062Abstract: Azaindazole compounds are useful for treating Flaviviridae virus infection, including HCV infection.Type: ApplicationFiled: October 19, 2010Publication date: September 13, 2012Applicant: EIGER BIOPHARMACEUTICALS, INC.Inventors: Wenjin Yang, Ingrid Choong
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Publication number: 20120172347Abstract: The present invention provides a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof (wherein W represents a hydrogen atom, a halogen atom, or the others; A represents an alkyl group optionally substituted by aryl group or the others, an aryl group, or the others; and one of X and Y represents a di-substituted alkylaminocarbonyl group, or the others, and the other represents a hydrogen atom, an alkyl group, an alkylcarbonyl group, or the others); a medicament or a pharmaceutical composition for treatment or prophylaxis of FAAH-related diseases such as depression, anxiety disorder or pains, comprising the compound or the like as an active ingredient; a use of the compound or the like; and a method for treatment or prophylaxis using the compound or the like.Type: ApplicationFiled: September 8, 2010Publication date: July 5, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Keiji Aachi, Yoko Nakai, Tomoyuki Furuta, Yuki Fujii
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Publication number: 20120165309Abstract: [Object] A novel and excellent method for preventing or treating rejection in the transplantation of various organs, allergy diseases, autoimmune diseases, hematologic tumor, or the like, based on a PI3K?-selective inhibitory action and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), is provided [Means for Solution] It was found that a 3-substituted triazine or 3-substituted pyrimidine derivative exhibits a PI3K?-selective inhibitory action, and/or an IL-2 production inhibitory action, and/or a B cell proliferation inhibitory action (including an activation inhibitory action), and can be an agent for preventing or treating rejection in the transplantation of various organs, allergy diseases (asthma, atopic dermatitis, etc.), autoimmune diseases (rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus, etc.), hematologic tumor (leukemia etc.Type: ApplicationFiled: February 10, 2010Publication date: June 28, 2012Applicant: Astellas Pharma Inc.Inventors: Fumie Takahashi, Sunao Imada, Masahiko Shiwaku, Yasumasa Shiwaku, Atsuko Shiwaku, Koji Kato, Hidehiko Fukahori
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Publication number: 20120156219Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: February 22, 2012Publication date: June 21, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Publication number: 20120121727Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Kai THEDE, Ingo FLAMME, Felix OEHME, Jens-Kerim ERGÜDEN, Friederike STOLL, Joachim SCHUHMACHER, Hanno WILD, Peter KOLKHOF, Hartmut BECK, Jörg KELDENICH, Metin AKBABA, Mario JESKE
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Publication number: 20120116072Abstract: Benzenesulfonamide compounds having a structure of the following general formula (I) are described. Also described, are methods for synthesizing the compounds, and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: June 28, 2010Publication date: May 10, 2012Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlene Schuppli
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Publication number: 20120083602Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: September 28, 2011Publication date: April 5, 2012Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20120071466Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type I (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: ApplicationFiled: June 4, 2010Publication date: March 22, 2012Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleomas
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Publication number: 20110288074Abstract: The present invention provides new compounds with high affinity for adenosine A2A receptors. It also provides antagonists of adenosine A2A receptors and their use as medicaments for the treatment and/or prophylaxis of diseases and disorders where the partial or total inactivation of adenosine A2A receptors signalling pathways could be beneficial such as Alzheimer's disease, Parkinson's disease, attention deficit and hyperactivity disorders (ADHD), Huntington's disease, neuroprotection, schizophrenia, anxiety and pain.Type: ApplicationFiled: January 25, 2010Publication date: November 24, 2011Applicant: DOMAIN THERAPEUTICSInventors: Stephan Schann, Stanislas Mayer
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Patent number: 8063036Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 7, 2010Date of Patent: November 22, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20110229500Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: ApplicationFiled: August 7, 2009Publication date: September 22, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
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Patent number: 7973028Abstract: The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a hydrogen atom, halogen atom or C1-C3 alkyl; X represents C7 polymethylene, in which a CH2—CH2 may be replaced with a CH?CH, optionally substituted with at least one substituent selected from the group consisting of halogen atoms, trifluoromethyl and C1-C4 alkyls. This pyrimidine compound has an excellent activity of controlling pests.Type: GrantFiled: April 17, 2009Date of Patent: July 5, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Hajime Mizuno, Akio Manabe
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Patent number: 7943605Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.Type: GrantFiled: October 25, 2006Date of Patent: May 17, 2011Assignee: UCB Pharma S.A.Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
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Publication number: 20110092488Abstract: Malaria is responsible for 1-2 million deaths and 300-500 million clinical cases annually and is an ever present problem for the military, tourists and business travelers. Mefloquine is known and used for malaria prophylaxis. However it is associated with neurological effects. The present invention is directed to providing new and novel quinoline analogs that are less neurotoxic than mefloquine without compromising efficacy. The present invention is also directed to the prevention and treatment of other microbial, parasitic, protozoan, bacterial and fungal diseases.Type: ApplicationFiled: October 27, 2006Publication date: April 21, 2011Inventors: Geoffrey Dow, Tiffany Heady, Kirsten Smith
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Publication number: 20110077395Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R6, R7, and R8 are defined herein.Type: ApplicationFiled: December 2, 2010Publication date: March 31, 2011Inventors: James J. Li, Lawrence G. Hamann, Zheming Ruan, Christopher B. Cooper, Shung C. Wu, Ligaya M. Simpkins, Haixia Wang, Akbar Nayeem, Stanley R. Krystek
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Publication number: 20110059950Abstract: Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.Type: ApplicationFiled: February 4, 2009Publication date: March 10, 2011Applicant: KinoPharma, Inc.Inventors: Hiroshi Onogi, Masatoshi Hagiwara, Masaaki Suzuki, Hiroko Koyama, Takamitsu Hosoya, Toshiyuki Hiramatsu
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Publication number: 20110039832Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-a]isoquinoline and pyrrolo[2,1-a]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: February 6, 2009Publication date: February 17, 2011Applicant: N.V. OrganonInventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lar Anders van der Veen, Willem Frederik Johan Karstens
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Publication number: 20100324010Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: October 14, 2008Publication date: December 23, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Amano
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Publication number: 20100305097Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.Type: ApplicationFiled: July 28, 2010Publication date: December 2, 2010Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
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Publication number: 20100305085Abstract: The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds.Type: ApplicationFiled: October 12, 2007Publication date: December 2, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
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Publication number: 20100298284Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: April 7, 2010Publication date: November 25, 2010Inventors: Bing-Yan ZHU, Penglie ZHANG, Lingyan WANG, Wenrong HUANG, Erick A. GOLDMAN, Wenhao LI, Jingmei ZUCKETT, Yonghong SONG, Robert M. SCARBOROUGH
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Publication number: 20100261706Abstract: Provided herein are tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analogs and derivatives, compositions comprising an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog and/or derivative and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, a reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, an ocular or opthalmologic disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, contrast induced nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of a tetracyclic 1H-indeno[1,2-b]pyridine-2(5H)-one analog or derivative.Type: ApplicationFiled: December 8, 2009Publication date: October 14, 2010Applicant: INOTEK PHARMACEUTICALS CORPORATIONInventors: Prakash JAGTAP, Duy-Phong Pham-Huu, Frederick COHEN, Huiyong HU, Xiaojing WANG
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Publication number: 20100261705Abstract: The present invention provides a carbostyril compound represented by General Formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R4 and R5 each represent a hydrogen atom; the bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; R1 is a hydrogen atom, etc; R2 is a hydrogen atom, etc; and R3 is a hydrogen atom, etc. The carbostyril compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.Type: ApplicationFiled: November 3, 2009Publication date: October 14, 2010Inventors: Takeshi Kuroda, Takahito Yamauchi, Tomoichi Shinohara, Kunio Oshima, Chiharu Kitajima, Hitoshi Nagao, Tae Fukushima, Takahiro Tomoyasu, Hironobu Ishiyama, Ohta Kazuhide, Masaaki Takano, Takumi Sumida
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Publication number: 20100249089Abstract: The present invention relates to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The invention provides an acrylonitrile derivative represented by formula (1): (wherein A represents an optionally substituted 3- to 8-membered heterocyclic ring) or a salt thereof.Type: ApplicationFiled: December 2, 2008Publication date: September 30, 2010Applicant: KABUSHIKI KAISHA YAKULT HONSHAInventors: Ryuta Yamazaki, Hiroshi Hatano, Takashi Yaegashi, Yoshiaki Igarashi, Oh Yoshida, Yoshikazu Sugimoto
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Publication number: 20100221259Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Patent number: 7709466Abstract: The present invention relates to pyridazinone compounds and their derivatives according to the general formula (I), with the substituents X, R1 and R2 defined herein, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK-3? (glycogen synthase kinase-3?) which are useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovary syndrome and syndrome X or immunodeficiency.Type: GrantFiled: October 24, 2006Date of Patent: May 4, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Guenter Mueller, Martin Bossart
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Publication number: 20100075953Abstract: The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.Type: ApplicationFiled: September 18, 2009Publication date: March 25, 2010Applicant: Glaxo Group LimitedInventors: Rachael Ancliff, Colin David Eldred, Ashley Paul Hancock, Thomas Daniel Heightman, Heather Hobbs, Simon Teanby Hodgson, David Matthew Wilson
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Patent number: 7589085Abstract: The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.Type: GrantFiled: August 6, 2004Date of Patent: September 15, 2009Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Lihu Yang, Stephen D. Goble
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Publication number: 20090176980Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: ApplicationFiled: March 3, 2008Publication date: July 9, 2009Inventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zhihong Guo, Peter Hrnciar
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Patent number: 7544677Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: August 19, 2005Date of Patent: June 9, 2009Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Nicholas D. P. Cosford, John C. Hartnett, Yiwei Li, Jun Liang, Peter J. Manley, Lou Anne Neilson, Tony Siu, Zhicai Wu
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Patent number: 7544675Abstract: The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: March 29, 2003Date of Patent: June 9, 2009Assignee: UCB, S.A.Inventors: Laurent Provins, Berend Jan Van Keulen, John Surtees, Patrice Talaga, Bernard Christophe
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Publication number: 20080300236Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to quinoline-derived amides that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.Type: ApplicationFiled: July 16, 2008Publication date: December 4, 2008Inventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
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Patent number: 7452992Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: GrantFiled: December 12, 2003Date of Patent: November 18, 2008Assignee: SmithKline Beecham CorporationInventors: Christopher Joseph Aquino, Pek Yeng Chong, Maosheng Duan, Wieslaw Mieczyslaw Kazmierski
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Patent number: 7423030Abstract: A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments using the compounds of formula (I).Type: GrantFiled: October 11, 2006Date of Patent: September 9, 2008Assignee: Sanofi-AventisInventors: Jean Michel Augereau, Michel Geslin, Gilles Courtemanche
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Publication number: 20080081803Abstract: The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: ApplicationFiled: October 15, 2004Publication date: April 3, 2008Inventors: Gabor Butora, Stephen D. Goble, Alexander Pastemak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
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Patent number: 7276524Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppressionType: GrantFiled: October 10, 2003Date of Patent: October 2, 2007Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
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Patent number: 7214714Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.Type: GrantFiled: April 26, 2002Date of Patent: May 8, 2007Assignee: Taisho Pharmaceutical Co. Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Patent number: 7186827Abstract: Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:Type: GrantFiled: October 27, 2004Date of Patent: March 6, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Carl Alan Busacca, Nizar Haddad, Suresh R. Kapadia, Lana Smith Keenan, Jon Charles Lorenz, Chris Hugh Senanayake, Xudong Wei
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Patent number: 7173033Abstract: As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.Type: GrantFiled: July 28, 2005Date of Patent: February 6, 2007Assignee: Astellas Pharma Inc.Inventors: Susumu Igarashi, Ryo Naito, Yoshinori Okamoto, Noriyuki Kawano, Issei Tsukamoto, Ippei Sato, Makoto Takeuchi, Hiroyuki Kanoh, Masato Kobori
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Patent number: 7157451Abstract: Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: GrantFiled: September 12, 2003Date of Patent: January 2, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Karnail S. Atwal, Wayne Vaccaro, John Lloyd, Heather Finlay, Lin Yan, Rao S. Bhandaru
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Patent number: 7026310Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: April 14, 2005Date of Patent: April 11, 2006Assignee: Zentaris GmbHInventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Patent number: RE39112Abstract: The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, or —CH?CH— or —C?C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R5 and R6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R2 is an amino group, etc.Type: GrantFiled: December 24, 1998Date of Patent: May 30, 2006Assignee: Eisai Co., Ltd.Inventors: Osamu Asano, Hitoshi Harada, Yorihisa Hoshino, Seiji Yoshikawa, Takashi Inoue, Tatsuo Horizoe, Nobuyuki Yasuda, Kaya Ohashi, Junsaku Nagaoka, Manabu Murakami, Seiichi Kobayashi