Additional Hetero Ring Attached Directly Or Indirectly To The Diazole Ring By Nonionic Bonding (e.g., 1,3-dioxolan-2-yl Methyl-imidazole, Etc.) Patents (Class 548/311.1)
  • Patent number: 10329268
    Abstract: The present invention provides a compound of formula N wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group, wherein N is in the form of the individual R- and S-enantiomer or a mixture of the (R)- and (S)-enantiomer. The present invention also provides a compound of formula MA. The present invention also provides processes for preparing the above compounds, and processes involving their use. The compounds are particularly useful as intermediates in the synthesis of peripherally-selective inhibitors of dopamine-?-hydroxylase.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: June 25, 2019
    Assignee: Bial-Portela & CA, S.A.
    Inventors: Domenico Russo, Jorge Wahnon, William Maton, Beat T. Weber, Paula Jeronimo, Luisa Sousa, Pedro Barrocas, Rita Pires, Ricardo Lima, Teofilo Vasconcelos
  • Patent number: 10201483
    Abstract: The present invention relates to a composition for dyeing human keratin fibres, such as the hair, which is free of oxidizing agent other than atmospheric oxygen and which is in cream form, comprising: (a) at least one oxidation dye precursor; (b) at least one ionic surfactant; (c) at least one oil; (d) optionally at least one solid fatty alcohol in a content of not more than 0.5% by weight relative to the weight of the composition; (e) at least one thickening polymer. The invention also relates to a process for dyeing human keratin fibres, in which this composition is applied to the said fibres, in the presence of at least one oxidizing agent other than atmospheric oxygen, and also to a multi-compartment device that is suitable for performing this process.
    Type: Grant
    Filed: August 2, 2013
    Date of Patent: February 12, 2019
    Assignee: L'OREAL
    Inventors: Delphine Charrier, Geraldine Fack
  • Patent number: 10081620
    Abstract: There is provided a labeling precursor compound represented by the following general formula (2): wherein R1 represents an alkynyl group, an alkynyloxy group, an azide group, an azidoalkyl group, an arylazide group, a monocyclic or condensed polycyclic aryl group or a nitrogen-containing heterocycle; R2 and R3 each independently represent an alkyl group or a hydroxyalkyl group which hydroxy group may be protected with a protecting group, and n is an integer of 1 or 2; R6 represents an alkyl group or —CONR11R12 wherein R11 and R12 each independently represent an alkyl group or a monocyclic or condensed polycyclic aryl group; and R4, R5, R7 and R8 each independently represent a hydrogen atom, an alkyl group or an alkoxy group.
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: September 25, 2018
    Assignees: NIHON MEDI-PHYSICS CO., LTD., TOKYO INSTITUTE OF TECHNOLOGY
    Inventors: Masahito Toyama, Masato Kiriu, Hiroshi Tanaka
  • Patent number: 9676752
    Abstract: Imidazolidine-2,4-dione derivatives of formula (I): The compounds have anti-proliferative activity and are useful for treating pathological states and diseases linked to an abnormal cell proliferation such as cancer.
    Type: Grant
    Filed: December 31, 2013
    Date of Patent: June 13, 2017
    Assignee: IPSEN PHARMA S.A.S.
    Inventors: Serge Auvin, Christophe Lanco, Qi Chao, Kaichun Gu
  • Patent number: 9260382
    Abstract: A method of reducing virulence in a bacterium comprising at least one of a GacS/GacA-type system, a HrpX/HrpY-type system, a T3SS-type system, and a Rsm-type system, the method comprising contacting the bacterium with an effective amount of a compound described herein.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: February 16, 2016
    Assignees: UWM Research Foundation, Duke University
    Inventors: Ching-Hong Yang, Xin Chen, Eric J. Toone
  • Patent number: 9173887
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: November 3, 2015
    Assignee: AbbVie Inc.
    Inventors: Clarence J. Maring, John K. Pratt, William A. Carroll, Dachun Liu, David A. Betebenner, Douglas K. Hutchinson, Michael D. Tufano, Todd W. Rockway, Uwe Schoen, Axel Pahl, Adreas Witte
  • Publication number: 20150133431
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 14, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventor: Gary C. Look
  • Patent number: 9024036
    Abstract: Provided are a white-emitting monomolecular compound using excited-state intramolecular proton transfer (ESIPT) characteristics, and an organic electroluminescence device and a laser device comprising same. The white-emitting monomolecular compound according to the present invention is prepared by covalently bonding at least two types of molecules which produce different colors and have excited-state intramolecular proton transfer (ESIPT) characteristics. The white-emitting monomolecular compound according to the present invention achieves white luminescence irrespective of the concentration thereof and of the state of the materials thereof, and therefore can be used in a variety of fields including an organic electroluminescence device and a laser device.
    Type: Grant
    Filed: September 12, 2013
    Date of Patent: May 5, 2015
    Assignees: Dongwoo Fine-Chem Co. Ltd., SNU R&DB Foundation
    Inventors: Soo Young Park, Sang Hyuk Park, Ji Eon Kwon
  • Publication number: 20150105354
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20150051225
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 19, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus, Maria Gijsen, Mark Wall
  • Patent number: 8957222
    Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral transition metal catalyst and a source of hydrogen, wherein X is CH2, oxygen, or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino, or dialkylamino group; and R4 is alkyl or aryl, wherein the transition metal catalyst comprises a chiral ligand having the formula wherein p is from 1 to 6, and Ar means aryl group; wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means an aromatic or heteroaromatic group, optionally substituted by alkyloxy, halogen, or nitro group; and the term halogen means fluorine, chlorine, bromine, or iodine.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: February 17, 2015
    Assignee: Bial-Portela & CA, S.A.
    Inventors: Alexander Beliaev, David Alexander Learmonth, Wenge Li
  • Patent number: 8927709
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20140378457
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
  • Patent number: 8895584
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
  • Publication number: 20140336232
    Abstract: The present invention relates to novel 2-iodoimidazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Application
    Filed: November 23, 2012
    Publication date: November 13, 2014
    Inventors: Hendrik Helmke, Sebastian Hoffmann, Carl Friedrich Nising, Alexander Sudau, Tomoki Tsuchiya, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Stephane Brunet, Marie-Claire Grosjean-Cournoyer, Hélène Lachaise, Philippe Rinolfi
  • Publication number: 20140315945
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Patent number: 8859611
    Abstract: The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: October 14, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventor: Xicheng Sun
  • Patent number: 8859602
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: October 14, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Bruce E. Tomczuk, Mark Wall, Kenneth Wilson
  • Patent number: 8835480
    Abstract: The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: September 16, 2014
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Nicholas G. Nickols
  • Publication number: 20140243382
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: May 12, 2014
    Publication date: August 28, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
  • Patent number: 8785488
    Abstract: The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: July 22, 2014
    Assignee: Exelixis Patent Company LLC
    Inventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt, Tie-Lin Wang, Richard Martin, Xiao-Hui Gu
  • Publication number: 20140200245
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Carl R. ILLIG, Jinsheng CHEN, Renee Louise DESJARLAIS, Kenneth WILSON
  • Publication number: 20140178349
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
    Type: Application
    Filed: December 16, 2013
    Publication date: June 26, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
  • Patent number: 8759384
    Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: June 24, 2014
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Charles Erec Stabbins, Vincent A. Fischetti
  • Patent number: 8729101
    Abstract: The present invention relates to a group of novel 1H-imidazole derivatives, to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component. These 1H-imidazole derivatives are potent cannabinoid-CB1 receptor agonists, partial agonists or antagonists, useful for the treatment of psychiatric and neurological disorders, as well as and other diseases involving cannabinoid neurotransmission. The compounds have the general formula (I), wherein R and R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: September 2, 2008
    Date of Patent: May 20, 2014
    Assignee: Solvay Pharmaceuticals, B.V.
    Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Arnoldus H. J. Herremans, Herman H. Van Stuivenberg
  • Patent number: 8722718
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: May 13, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Jinsheng Chen, Renee Louise DesJarlais, Kenneth Wilson
  • Patent number: 8637560
    Abstract: The present invention features imidazolidinone compounds and pharmaceutical compositions of imidazolidinone compounds. The compounds of the invention are utilized in methods of treating a deubiquitination-related disorder in a subject and inhibiting p97-associated deubiquitination.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: January 28, 2014
    Assignee: The United States of America as Represented by the Secretary of the Department of Health and Human Services
    Inventors: William Trenkle, Adrian Wiestner, Qiuyan Wang, Yihong Ye, Helena Mora-Jensen
  • Patent number: 8624037
    Abstract: The subject matter of the present application is novel imidazolidine-2,4-dione derivatives. These products have an antiproliferative activity. They are particularly advantageous for treating pathological conditions and diseases associated with abnormal cell proliferation, such as cancers. The invention also relates to pharmaceutical compositions containing said products and to the use thereof for preparing a medicament.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: January 7, 2014
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Dennis Bigg, Serge Auvin, Christophe Lanco, Grégoire Prevost
  • Patent number: 8623898
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: January 7, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Akito Yasuhara, Shuji Yamamoto, Hiroshi Ohta, Yoshihisa Shirasaki, Kazunari Sakagami, Masato Hayashi, Tsuyoshi Shibata, Youichi Shimazaki, Yuko Araki, Kumi Abe, Xiang-Min Sun
  • Patent number: 8592454
    Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: November 26, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
  • Patent number: 8586624
    Abstract: The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: November 19, 2013
    Assignee: N30 Pharmaceuticals, Inc.
    Inventor: Xicheng Sun
  • Patent number: 8569336
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: October 29, 2013
    Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K. C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Publication number: 20130281475
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: June 13, 2013
    Publication date: October 24, 2013
    Inventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
  • Patent number: 8563586
    Abstract: The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds in hydrophilic or lipophilic form, which are useful as angiotensin II ATI receptor antagonists suitable for transdermal delivery. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: October 22, 2013
    Assignee: Eldrug S.A.
    Inventors: John Matsoukas, Michael Maragoudakis, Dimitrios Vlaxakos
  • Publication number: 20130230501
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
    Type: Application
    Filed: July 16, 2012
    Publication date: September 5, 2013
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
  • Patent number: 8501798
    Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: August 6, 2013
    Assignee: Theravance, Inc.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8492556
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: July 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20130172522
    Abstract: There is provided an epoxy compound that provides properties of cured products combining high transparency with high flexural strength by being thermally cured while maintaining advantageous handling properties in a liquid state thereof. An epoxy compound of Formula (1): (where n1 and n2 are independently an integer of 2 to 6; n3 and n4 are individually an integer of 2; n5 and n6 are individually an integer of 1; R4-R7 are independently a hydrogen atom or a C1-10 alkyl group; and X1 is a group of Formula (2)-(4): (where R1-R3 are independently a hydrogen atom, a C1-10 alkyl group, or the like)); and a curable composition comprising the epoxy compound and a curing agent.
    Type: Application
    Filed: July 29, 2011
    Publication date: July 4, 2013
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Mikio Kasai, Toshiaki Takeyama, Yuki Endo
  • Patent number: 8455528
    Abstract: The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Linus S. Lin, Marc D. Chioda, Ping Liu, Ravi P. Nargund
  • Patent number: 8450498
    Abstract: Ionic liquid epoxide monomers capable of reacting with cross-linking agents to form polymers with high tensile and adhesive strengths. Ionic liquid epoxide monomers comprising at least one bis(glycidyl) N-substituted nitrogen heterocyclic cation are made from nitrogen heterocycles corresponding to the bis(glycidyl) N-substituted nitrogen heterocyclic cations by a method involving a non-nucleophilic anion, an alkali metal cation, epichlorohydrin, and a strong base.
    Type: Grant
    Filed: May 14, 2011
    Date of Patent: May 28, 2013
    Assignee: AZ Technology, Inc.
    Inventor: Mark S. Paley
  • Patent number: 8450355
    Abstract: This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: May 28, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael K. C. Wong, Wensheng Yu, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Joseph A. Kozlowski, Seong Heon Kim, Guowei Zhou, De-Yi Yang, Razia K. Rizvi, Lei Chen, Aneta Maria Kosinzki, Kristin E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Patent number: 8445523
    Abstract: SOAT-1 inhibitors of general formula (I) and cosmetic and pharmaceutical compositions containing such a compound are described.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: May 21, 2013
    Assignee: Galderma Research & Development
    Inventors: Laurence Dumais, Cédric Poinsard, Thibaud Portal
  • Publication number: 20130123493
    Abstract: A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof, Formula (II): Formula (I): the process comprising the reaction of a carbamate of Formula (II?): or formula (I?): with a primary or secondary amine of the formula: R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
    Type: Application
    Filed: July 28, 2011
    Publication date: May 16, 2013
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Brian Broadbelt, Jorge Bruno Reis Wahnon
  • Patent number: 8436035
    Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase (CYP11B2), and/or 11 beta-hydroxylase (CYP11B1), and/or aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase, aromatase, or CYP11B1. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: May 7, 2013
    Assignee: Novartis AG
    Inventors: Christopher Adams, Qi-Ying Hu, Gary Michael Ksander, Julien Papillon
  • Publication number: 20130102614
    Abstract: Described herein are methods of inhibiting angiogenesis, and treating and preventing disorders associated with angiogenesis by administering anti-angiogenesis compounds to a subject.
    Type: Application
    Filed: April 11, 2012
    Publication date: April 25, 2013
    Inventors: Jun O. Liu, Curtis R. Chong, Jing Xu, Juu Lu, Shridhar Bhat
  • Patent number: 8420684
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(he
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: April 16, 2013
    Assignee: Probiodrug AG
    Inventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
  • Patent number: 8420681
    Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions containing such a compound are described.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: April 16, 2013
    Assignee: Galderma Research & Development
    Inventor: Cédric Poinsard
  • Patent number: 8420680
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3?R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: April 16, 2013
    Assignees: Emory University, NeurOp, Inc.
    Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Yesim Altas Tahirovic, Scott J. Myers
  • Patent number: 8420682
    Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions including such a compound are described.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: April 16, 2013
    Assignee: Galderma Research & Development
    Inventors: Cédric Poinsard, Thibaud Portal
  • Patent number: 8410155
    Abstract: The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, R3, R4, R8a, R11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: April 2, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Donald J. P. Pinto