The Additional Hetero Ring Is Six-membered And Contains Nitrogen Patents (Class 540/481)
  • Patent number: 10851087
    Abstract: 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: Grant
    Filed: May 3, 2019
    Date of Patent: December 1, 2020
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Anjali Pandey, Arvinder Sran, Ying Chen, Daniele Poggiali, Tiziano Fumagalli
  • Publication number: 20140249135
    Abstract: 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: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: 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
  • Patent number: 8822451
    Abstract: 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: Grant
    Filed: May 22, 2006
    Date of Patent: September 2, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Anna R. Hazlewood, Peter D. J. Grootenhuis, Ashvani Kumar Singh, Thomas Cleveland, Frederick F. Van-Goor
  • Patent number: 8772478
    Abstract: 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: Grant
    Filed: June 28, 2010
    Date of Patent: July 8, 2014
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlène Schuppli
  • Patent number: 8765941
    Abstract: 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: Grant
    Filed: February 4, 2009
    Date of Patent: July 1, 2014
    Assignee: Kino Pharma, Inc.
    Inventors: Hiroshi Onogi, Masatoshi Hagiwara, Masaaki Suzuki, Hiroko Koyama, Takamitsu Hosoya, Toshiyuki Hiramatsu
  • Patent number: 8524894
    Abstract: 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: Grant
    Filed: June 4, 2010
    Date of Patent: September 3, 2013
    Assignee: Laboratorios Salvat, S.A.
    Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleo Mas
  • Patent number: 8389560
    Abstract: 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: Grant
    Filed: September 15, 2009
    Date of Patent: March 5, 2013
    Assignee: 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
  • Publication number: 20120309742
    Abstract: 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: Application
    Filed: August 8, 2012
    Publication date: December 6, 2012
    Inventors: Ralf GLATTHAR, Donald JOHNS, Daniel UMBRICHT
  • Publication number: 20120232062
    Abstract: Azaindazole compounds are useful for treating Flaviviridae virus infection, including HCV infection.
    Type: Application
    Filed: October 19, 2010
    Publication date: September 13, 2012
    Applicant: EIGER BIOPHARMACEUTICALS, INC.
    Inventors: Wenjin Yang, Ingrid Choong
  • Publication number: 20120172347
    Abstract: 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: Application
    Filed: September 8, 2010
    Publication date: July 5, 2012
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Keiji Aachi, Yoko Nakai, Tomoyuki Furuta, Yuki Fujii
  • Publication number: 20120165309
    Abstract: [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: Application
    Filed: February 10, 2010
    Publication date: June 28, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Fumie Takahashi, Sunao Imada, Masahiko Shiwaku, Yasumasa Shiwaku, Atsuko Shiwaku, Koji Kato, Hidehiko Fukahori
  • Publication number: 20120156219
    Abstract: 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: Application
    Filed: February 22, 2012
    Publication date: June 21, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
  • Publication number: 20120121727
    Abstract: 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: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: 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
  • Publication number: 20120116072
    Abstract: 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: Application
    Filed: June 28, 2010
    Publication date: May 10, 2012
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlene Schuppli
  • Publication number: 20120083602
    Abstract: 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: Application
    Filed: September 28, 2011
    Publication date: April 5, 2012
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
  • Publication number: 20120071466
    Abstract: 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: Application
    Filed: June 4, 2010
    Publication date: March 22, 2012
    Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleomas
  • Publication number: 20110288074
    Abstract: 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: Application
    Filed: January 25, 2010
    Publication date: November 24, 2011
    Applicant: DOMAIN THERAPEUTICS
    Inventors: Stephan Schann, Stanislas Mayer
  • Patent number: 8063036
    Abstract: 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: Grant
    Filed: April 7, 2010
    Date of Patent: November 22, 2011
    Assignee: 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
  • Publication number: 20110229500
    Abstract: 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: Application
    Filed: August 7, 2009
    Publication date: September 22, 2011
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Patent number: 7973028
    Abstract: 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: Grant
    Filed: April 17, 2009
    Date of Patent: July 5, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hajime Mizuno, Akio Manabe
  • Patent number: 7943605
    Abstract: 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: Grant
    Filed: October 25, 2006
    Date of Patent: May 17, 2011
    Assignee: UCB Pharma S.A.
    Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
  • Publication number: 20110092488
    Abstract: 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: Application
    Filed: October 27, 2006
    Publication date: April 21, 2011
    Inventors: Geoffrey Dow, Tiffany Heady, Kirsten Smith
  • Publication number: 20110077395
    Abstract: 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: Application
    Filed: December 2, 2010
    Publication date: March 31, 2011
    Inventors: James J. Li, Lawrence G. Hamann, Zheming Ruan, Christopher B. Cooper, Shung C. Wu, Ligaya M. Simpkins, Haixia Wang, Akbar Nayeem, Stanley R. Krystek
  • Publication number: 20110059950
    Abstract: 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: Application
    Filed: February 4, 2009
    Publication date: March 10, 2011
    Applicant: KinoPharma, Inc.
    Inventors: Hiroshi Onogi, Masatoshi Hagiwara, Masaaki Suzuki, Hiroko Koyama, Takamitsu Hosoya, Toshiyuki Hiramatsu
  • Publication number: 20110039832
    Abstract: 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: Application
    Filed: February 6, 2009
    Publication date: February 17, 2011
    Applicant: N.V. Organon
    Inventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lar Anders van der Veen, Willem Frederik Johan Karstens
  • Publication number: 20100324010
    Abstract: 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: Application
    Filed: October 14, 2008
    Publication date: December 23, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Amano
  • Publication number: 20100305097
    Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.
    Type: Application
    Filed: July 28, 2010
    Publication date: December 2, 2010
    Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
  • Publication number: 20100305085
    Abstract: 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: Application
    Filed: October 12, 2007
    Publication date: December 2, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: 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
  • Publication number: 20100298284
    Abstract: 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: Application
    Filed: April 7, 2010
    Publication date: November 25, 2010
    Inventors: Bing-Yan ZHU, Penglie ZHANG, Lingyan WANG, Wenrong HUANG, Erick A. GOLDMAN, Wenhao LI, Jingmei ZUCKETT, Yonghong SONG, Robert M. SCARBOROUGH
  • Publication number: 20100261706
    Abstract: 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: Application
    Filed: December 8, 2009
    Publication date: October 14, 2010
    Applicant: INOTEK PHARMACEUTICALS CORPORATION
    Inventors: Prakash JAGTAP, Duy-Phong Pham-Huu, Frederick COHEN, Huiyong HU, Xiaojing WANG
  • Publication number: 20100261705
    Abstract: 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: Application
    Filed: November 3, 2009
    Publication date: October 14, 2010
    Inventors: Takeshi Kuroda, Takahito Yamauchi, Tomoichi Shinohara, Kunio Oshima, Chiharu Kitajima, Hitoshi Nagao, Tae Fukushima, Takahiro Tomoyasu, Hironobu Ishiyama, Ohta Kazuhide, Masaaki Takano, Takumi Sumida
  • Publication number: 20100249089
    Abstract: 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: Application
    Filed: December 2, 2008
    Publication date: September 30, 2010
    Applicant: KABUSHIKI KAISHA YAKULT HONSHA
    Inventors: Ryuta Yamazaki, Hiroshi Hatano, Takashi Yaegashi, Yoshiaki Igarashi, Oh Yoshida, Yoshikazu Sugimoto
  • Publication number: 20100221259
    Abstract: 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: Application
    Filed: May 10, 2010
    Publication date: September 2, 2010
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
  • Patent number: 7709466
    Abstract: 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: Grant
    Filed: October 24, 2006
    Date of Patent: May 4, 2010
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Guenter Mueller, Martin Bossart
  • Publication number: 20100075953
    Abstract: 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: Application
    Filed: September 18, 2009
    Publication date: March 25, 2010
    Applicant: Glaxo Group Limited
    Inventors: Rachael Ancliff, Colin David Eldred, Ashley Paul Hancock, Thomas Daniel Heightman, Heather Hobbs, Simon Teanby Hodgson, David Matthew Wilson
  • Patent number: 7589085
    Abstract: 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: Grant
    Filed: August 6, 2004
    Date of Patent: September 15, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Lihu Yang, Stephen D. Goble
  • Publication number: 20090176980
    Abstract: 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: Application
    Filed: March 3, 2008
    Publication date: July 9, 2009
    Inventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zhihong Guo, Peter Hrnciar
  • Patent number: 7544677
    Abstract: 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: Grant
    Filed: August 19, 2005
    Date of Patent: June 9, 2009
    Assignee: 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
  • Patent number: 7544675
    Abstract: 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: Grant
    Filed: March 29, 2003
    Date of Patent: June 9, 2009
    Assignee: UCB, S.A.
    Inventors: Laurent Provins, Berend Jan Van Keulen, John Surtees, Patrice Talaga, Bernard Christophe
  • Publication number: 20080300236
    Abstract: 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: Application
    Filed: July 16, 2008
    Publication date: December 4, 2008
    Inventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
  • Patent number: 7452992
    Abstract: 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: Grant
    Filed: December 12, 2003
    Date of Patent: November 18, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: Christopher Joseph Aquino, Pek Yeng Chong, Maosheng Duan, Wieslaw Mieczyslaw Kazmierski
  • Patent number: 7423030
    Abstract: 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: Grant
    Filed: October 11, 2006
    Date of Patent: September 9, 2008
    Assignee: Sanofi-Aventis
    Inventors: Jean Michel Augereau, Michel Geslin, Gilles Courtemanche
  • Publication number: 20080081803
    Abstract: 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: Application
    Filed: October 15, 2004
    Publication date: April 3, 2008
    Inventors: Gabor Butora, Stephen D. Goble, Alexander Pastemak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
  • Patent number: 7276524
    Abstract: 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 immunosuppression
    Type: Grant
    Filed: October 10, 2003
    Date of Patent: October 2, 2007
    Assignee: Astellas Deutschland GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
  • Patent number: 7214714
    Abstract: 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: Grant
    Filed: April 26, 2002
    Date of Patent: May 8, 2007
    Assignee: Taisho Pharmaceutical Co. Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
  • Patent number: 7186827
    Abstract: Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:
    Type: Grant
    Filed: October 27, 2004
    Date of Patent: March 6, 2007
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Carl Alan Busacca, Nizar Haddad, Suresh R. Kapadia, Lana Smith Keenan, Jon Charles Lorenz, Chris Hugh Senanayake, Xudong Wei
  • Patent number: 7173033
    Abstract: 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: Grant
    Filed: July 28, 2005
    Date of Patent: February 6, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Susumu Igarashi, Ryo Naito, Yoshinori Okamoto, Noriyuki Kawano, Issei Tsukamoto, Ippei Sato, Makoto Takeuchi, Hiroyuki Kanoh, Masato Kobori
  • Patent number: 7157451
    Abstract: 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: Grant
    Filed: September 12, 2003
    Date of Patent: January 2, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Karnail S. Atwal, Wayne Vaccaro, John Lloyd, Heather Finlay, Lin Yan, Rao S. Bhandaru
  • Patent number: 7026310
    Abstract: 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: Grant
    Filed: April 14, 2005
    Date of Patent: April 11, 2006
    Assignee: Zentaris GmbH
    Inventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
  • Patent number: RE39112
    Abstract: 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: Grant
    Filed: December 24, 1998
    Date of Patent: May 30, 2006
    Assignee: 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