The -c(=x)- Group Is Bonded Directly To The Thiazole Ring Patents (Class 548/188)
  • Patent number: 9598383
    Abstract: Provided herein are ROS-sensitive prodrug compositions and methods of treating ROS-associated diseases by administering the ROS-sensitive prodrug compositions.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: March 21, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Seth M. Cohen, Jean-Philippe Monserrat, Christian Perez
  • Publication number: 20150133470
    Abstract: Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Michael Neary, James Nieman, Steven Tanis, Daniel Lawton, Garry Smith
  • Publication number: 20150119571
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: September 4, 2014
    Publication date: April 30, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Patent number: 8987306
    Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: March 24, 2015
    Assignee: The Trustees Of The University of Pennsylvania
    Inventors: William F. DeGrado, Meredith W. Miller, Sandeep Basra, Joel S. Bennett, Sungwook Choi
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Publication number: 20150031733
    Abstract: The present invention provides a compound having an excellent efficacy for controlling pests. A tetrazolinone compound of a formula (1): [wherein, R1 represents an C6-C16 aryl group, an C1-C12 alkyl group, a C3-C12 cycloalkyl group or an adamantyl group, etc., which each optionally be substituted; R2 represents a hydrogen atom, an C1-C12 alkyl group, or a halogen atom, etc.; R4 and R5 represent independently of each other a hydrogen atom or an C1-C3 alkyl group, etc.; R6, R7, R8 and R9 represent independently of each other a hydrogen atom, a halogen atom, an C1-C12 alkyl group, a C1-C12 haloalkyl group, an C2-C12 alkenyl group, a C3-C12 cycloalkyl group, an C1-C12 alkoxy group or a C1-C12 haloalkoxy group, etc.; X and Y represent independently of each other a sulfur atom or an oxygen atom; Q represents an oxygen atom or a sulfur atom; and R10 represents an C1-C6 alkyl group, etc.] shows an excellent controlling efficacy on pests.
    Type: Application
    Filed: April 26, 2013
    Publication date: January 29, 2015
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yuya Yoshimoto, Teruki Takahashi, Daisuke Oohira, Shuhei Azuma
  • Publication number: 20150005352
    Abstract: Provided herein are ROS-sensitive prodrug compositions and methods of treating ROS-associated diseases by administering the ROS-sensitive prodrug compositions.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 1, 2015
    Inventors: Seth M. Cohen, Jean-Philippe Monserrat, Christian Perez
  • Publication number: 20140371276
    Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.
    Type: Application
    Filed: December 19, 2012
    Publication date: December 18, 2014
    Inventors: Alessio Moriconi, Gianluca Bianchini, Sandro Colagioia, Laura Brandolini, Andrea Aramini, Chiara Liberati, Silvia Bovolenta
  • Patent number: 8871792
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: October 28, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Patent number: 8835467
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: September 16, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20140243292
    Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 11, 2014
    Publication date: August 28, 2014
    Applicant: Sanofi
    Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary McCORT
  • Publication number: 20140171387
    Abstract: Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 19, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuyuki OHMOTO, Akihiro Kinoshita, Hidekazu Matsuya, Hiroki Okada
  • Publication number: 20140148468
    Abstract: The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
    Type: Application
    Filed: November 27, 2013
    Publication date: May 29, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder
  • Patent number: 8716490
    Abstract: Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: May 6, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Hidekazu Matsuya, Hiroki Okada
  • Publication number: 20140114068
    Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: April 24, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
  • Patent number: 8686160
    Abstract: Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: April 1, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Hidekazu Matsuya, Hiroki Okada
  • Patent number: 8680339
    Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: March 25, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Patent number: 8653115
    Abstract: The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: February 18, 2014
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Haijun Chen, Guifeng Wang, Min Gu, Fenghua Zhu, Wei Tang
  • Publication number: 20140011997
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
  • Publication number: 20130330365
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130184236
    Abstract: Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder.
    Type: Application
    Filed: March 4, 2013
    Publication date: July 18, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventor: ONO PHARMACEUTICAL CO., LTD.
  • Publication number: 20130143934
    Abstract: An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.
    Type: Application
    Filed: January 25, 2013
    Publication date: June 6, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventor: ONO PHARMACEUTICAL CO., LTD.
  • Patent number: 8404859
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: March 26, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
  • Publication number: 20130065859
    Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 12, 2011
    Publication date: March 14, 2013
    Applicant: SANOFI
    Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary MCCORT
  • Patent number: 8383653
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: June 30, 2004
    Date of Patent: February 26, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20130005767
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicant: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 8309582
    Abstract: Bcl-xL/Bcl-2 binding inhibitors useful in the treatment of unwanted proliferating cells, including cancers and precancers, in subjects in need of such treatment. Also provided are methods of treating a subject having unwanted proliferating cells comprising administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject in need of such treatment. Also provided are methods of preventing the proliferation of unwanted proliferating cells, such as cancers and precancers, in a subject comprising the step of administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject at risk of developing a condition characterized by unwanted proliferating cells.
    Type: Grant
    Filed: January 5, 2010
    Date of Patent: November 13, 2012
    Assignee: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Chung-Wai Shiau
  • Patent number: 8278328
    Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
    Type: Grant
    Filed: September 18, 2008
    Date of Patent: October 2, 2012
    Assignee: Glaxo Group Limited
    Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
  • Publication number: 20120238569
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.
    Type: Application
    Filed: February 17, 2012
    Publication date: September 20, 2012
    Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
  • Publication number: 20120202773
    Abstract: A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).
    Type: Application
    Filed: April 23, 2012
    Publication date: August 9, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Toru Maruyama, Kaoru Kobayashi, Tohru Kambe, Takayuki Maruyama, Hideyuki Yoshida, Akio Nishiura, Nobutaka Abe
  • Publication number: 20120115916
    Abstract: The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: June 11, 2010
    Publication date: May 10, 2012
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20120088805
    Abstract: Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder.
    Type: Application
    Filed: June 9, 2010
    Publication date: April 12, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Hidekazu Matsuta, Hiroki Okada
  • Publication number: 20120059007
    Abstract: This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.
    Type: Application
    Filed: September 15, 2010
    Publication date: March 8, 2012
    Inventors: Jeffrey D. Laskin, Diane E. Heck, Carl Jeffrey Lacey, Erik Aponte, Mou-Tuan Huang, Ned D. Heindel
  • Publication number: 20120028800
    Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: January 25, 2010
    Publication date: February 2, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20110263556
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Application
    Filed: October 20, 2010
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
  • Publication number: 20110263545
    Abstract: The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.
    Type: Application
    Filed: May 20, 2009
    Publication date: October 27, 2011
    Inventors: Naweed Muhammad, Keith R. Bley, Jeffrey Tobias
  • Publication number: 20110237630
    Abstract: A compound represented by the formula (I) wherein R1 and R2 are each a hydrogen atom, an alkyl group and the like, R3 is a hydrogen atom, an alkyl group and the like, R4 is a hydrogen atom, an alkyl group and the like, m is an integer of 0 to 3, X is a bond, an oxygen atom or a sulfur atom, Y is a carbonyl group, a hydroxymethylene group and the like, and Z is a halogen atom, an alkyl group, an aryl group, a heteroaryl group and the like, or a pharmaceutically acceptable salt thereof has a superior PPAR? agonist action and a lipid-lowering action, and is useful as a prophylactic or therapeutic drug for hyperlipidemia and the like.
    Type: Application
    Filed: December 1, 2009
    Publication date: September 29, 2011
    Inventor: Naoko Ando
  • Publication number: 20110178102
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: June 30, 2004
    Publication date: July 21, 2011
    Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Vern L Schramm, Anthony A. Suave
  • Publication number: 20110152318
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
    Type: Application
    Filed: July 2, 2009
    Publication date: June 23, 2011
    Applicant: Amorepacific Corporation
    Inventors: Byoung Young Woo, Sun-Young Kim, Yeonjoon Kim, Song Seok Shin, Jin Kwan Kim, Ki-Wha Lee, Dong Hyun Kim, Kyung Min Lim, Joo-Hyun Moh, Yeon Su Jeong, Jin Kyu Choi, Hyun Ju Koh, Jeongho Lee, Hyuk Kim, Jeong Hoon Yoon, Funan Li, Jee-Suk Kim, Young-Ger Suh
  • Publication number: 20110059920
    Abstract: An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.
    Type: Application
    Filed: November 11, 2010
    Publication date: March 10, 2011
    Applicant: ONO PHARMACEUTICAL CO., LTD
    Inventors: Kazuyuki OHMOTO, Akihiro KINOSHITA, Hidekazu Matsuya
  • Publication number: 20110059939
    Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.
    Type: Application
    Filed: May 4, 2009
    Publication date: March 10, 2011
    Applicant: ALLERGAN ,INC
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20110039705
    Abstract: A method of producing a granular agrochemical composition having excellent handling properties, wherein a powdered agrochemical wettable composition or powdered agrochemical water-soluble composition is converted in form to a granular agrochemical composition, without altering the formulation thereof. The method of producing a granular agrochemical composition includes: treating a powdered agrochemical wettable composition or powdered agrochemical water-soluble composition by (1) a step of adding water, kneading, extruding and drying, (2) a step of adding water, granulating by stirring and drying, (3) a step of adding water, kneading and spray-drying, (4) a step of adding water and performing fluidized bed granulation, or (5) a step of pressure molding the powdered agrochemical wettable composition or powdered agrochemical water-soluble composition; followed by (a) a step of performing microgranulation by grinding, and if necessary, (b) a step of performing grain size regulation by sieving.
    Type: Application
    Filed: April 23, 2009
    Publication date: February 17, 2011
    Inventors: Yoshihisa Endo, Satoru Yamamura
  • Publication number: 20110015238
    Abstract: It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and, therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
    Type: Application
    Filed: September 24, 2010
    Publication date: January 20, 2011
    Applicant: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Yoshihisa Kamanaka, Hidekazu Matsuya
  • Patent number: 7858650
    Abstract: A medicinal composition for inhalation containing a continuous-release type prodrug of an EP2 agonist topically exhibits a prolonged bronchodilating and antiinflammatory effects. Namely, the medicinal composition for inhalation containing a continuous-release type prodrug of an EP2 agonist is useful as a safe preventive and/or a remedy for respiratory diseases (for example, asthma, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, adult respiratory distress syndrome, cystic fibrosis, pulmonary hypertension or the like) without causing any systemic effect such as lowering blood pressure. Thus, a safe and useful remedy for respiratory diseases is provided.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: December 28, 2010
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Shigeki Yamamoto, Tsutomu Shiroya, Michiaki Kadode, Toru Maruyama, Kousuke Tani, Toshihiko Nagase
  • Publication number: 20100305131
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 27, 2010
    Publication date: December 2, 2010
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 7786117
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J, B, Y, G and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: August 31, 2010
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Publication number: 20100113388
    Abstract: An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof.
    Type: Application
    Filed: January 7, 2010
    Publication date: May 6, 2010
    Applicant: Ono Pharmaceutical Co., Ltd.
    Inventors: Kousuke Tani, Kaoru Kobayashi, Toru Maruyama, Tohru Kambe, Mikio Ogawa, Tsutomu Shiroya
  • Publication number: 20090233968
    Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.
    Type: Application
    Filed: June 7, 2006
    Publication date: September 17, 2009
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: William F. Degrado, Joel S. Bennett, Seth Elliott Snyder, Sungwook Choi
  • Patent number: 7589213
    Abstract: Therapeutic compounds, compositions, medicaments, and methods are disclosed herein.
    Type: Grant
    Filed: March 17, 2008
    Date of Patent: September 15, 2009
    Inventor: David W. Old
  • Publication number: 20090227644
    Abstract: An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.
    Type: Application
    Filed: June 2, 2006
    Publication date: September 10, 2009
    Applicant: ONO PHARMACEUTICAL CO., LTD
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Hidekazu Matsuya