Asymmetrical (e.g., 1, 2, 4-triazines, Etc.) Patents (Class 544/182)
  • Patent number: 10562901
    Abstract: A temozolomide compound according to formula (I) is described, wherein R1, L1, and X are defined herein. The temozolomide compound can be used to prepare polymers comprising temozolomide. Additionally, the polymers comprising temozolomide can be particularly useful in the treatment of certain diseases.
    Type: Grant
    Filed: September 20, 2017
    Date of Patent: February 18, 2020
    Assignee: THE UNIVERSITY OF MASSACHUSETTS
    Inventors: Todd Emrick, Matthew Skinner, Sarah M. Ward, Banishree Saha
  • Patent number: 10376517
    Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.
    Type: Grant
    Filed: April 10, 2018
    Date of Patent: August 13, 2019
    Assignees: Madrigal Pharmaceuticals, Inc., Hoffmann-La Roche Inc.
    Inventors: Rebecca Taub, Charles H. Reynolds, Lianhe Shu, Ping Wang, Duk Soon Choi
  • Patent number: 10329263
    Abstract: This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I]: wherein RA is, for example, a group of the following formula (A-1): wherein ring A1 is, for example, a cycloalkyl group which may be substituted, and RB is, for example, a monocyclic cycloalkyl group, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: June 25, 2019
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Hideki Ushirogochi, Wataru Sasaki, Yuichi Onda, Ryo Sakakibara, Fumihiko Akahoshi
  • Patent number: 10189859
    Abstract: The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: January 29, 2019
    Assignee: Nektar Therapeutics
    Inventors: Pankaj Sharma, Vijay Kumar Khatri, Xuyuan Gu, Yuan Song, Michael Lixin Shen, Jennifer Riggs-Sauthier, Neel K. Anand, Antoni Kozlowski, Aleksandrs Odinecs, Timothy A. Riley, Zhongxu Ren, YongQi Mu, Xiaoming Shen, Xuejun Yuan, Natalia Aurrecoechea, Donogh John Roger O'Mahony, Bo-Liang Deng
  • Patent number: 10112923
    Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocylic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: October 30, 2018
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
  • Patent number: 9988372
    Abstract: The present invention relates to a novel crystalline form of 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulfonate and a pharmaceutical composition containing the same. The novel crystalline form of a compound according to the present invention exhibits excellent stability even in high-temperature and humidity environments, and thus can be favorably used to prevent or treat diseases, such as thrombosis, myocardial infarction, atherosclerosis, inflammation, stroke, angina pectoris, restenosis after angioplasty, and thromboembolism.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: June 5, 2018
    Assignees: GREEN CROSS CORPORATION, LEGOCHEM BIOSCIENCES, INC.
    Inventors: Soongyu Choi, Jungsub Choi, So-Hyun Yoon, Yoo Hoon Kim, Jae Yeon Kim, Suk Ho Lee, Young Lag Cho, Ho Young Song, Dae Yon Lee, Sung Yoon Baek, Sang Eun Chae, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Patent number: 9617228
    Abstract: The invention relates to (among other things) methods for treatment comprising administering oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: April 11, 2017
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
  • Patent number: 9573908
    Abstract: Using a whole-cell high-throughput screen, eleven molecules were identified that activate V. cholerae quorum sensing (QS). Eight molecules are receptor agonists and three molecules are antagonists of LuxO, the central NtrC-type response regulator that controls the global V. cholerae QS cascade. Pro-QS molecules are used for the development of novel anti-infectives.
    Type: Grant
    Filed: February 20, 2013
    Date of Patent: February 21, 2017
    Assignee: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie L. Bassler, Wai-Leung Ng, Lark J. Perez, Jianping Cong, Martin F. Semmelhack
  • Patent number: 9505753
    Abstract: D-amino acid oxidase (DAAO) inhibitors and methods of their use, either alone or in combination with D-serine or D-alanine, to facilitate allosteric activation of NMDA receptor-mediated neurotransmission and methods of their use as therapeutic agents for treating a subject afflicted with one or more cognitive-disorders, such as schizophrenia, including subjects suffering from negative symptoms and cognitive impairments, post-traumatic stress disorder (PTSD), or pain, are disclosed.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: November 29, 2016
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Takashi Tsukamoto, Barbara Stauch Slusher, Dana V. Ferraris, Camilo Rojas, Niyada Hin, Bridget Duvall
  • Patent number: 9416114
    Abstract: This invention relates to 1,2,4-triazine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: August 16, 2016
    Assignees: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE ROUEN, INSTITUT NATIONAL DES SCIENCES APPLIQUEES DE ROUEN (INSA)
    Inventors: Vincent Gembus, Philippe Jubault, Christophe Hoarau, Vincent Levacher, Jean-Francois Bonfanti, David Graig McGowan, Jerome Emile Georges Guillemont
  • Patent number: 9290481
    Abstract: The present invention relates to monocyclic heteroaryl cycloalkyldiamine derivatives of formula (I), to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: March 22, 2016
    Assignee: NOVARTIS AG
    Inventors: Alexander Baxter Smith, Gebhard Thoma, Maurice Van Eis
  • Patent number: 9266845
    Abstract: The invention relates to (among other things) methods for treatment comprising administering oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Grant
    Filed: October 30, 2014
    Date of Patent: February 23, 2016
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
  • Patent number: 9266861
    Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: February 23, 2016
    Assignees: Madrigal Pharmaceuticals, Inc., Hoffmann-La Roche Inc.
    Inventors: D. Keith Hester, II, Robert J. Duguid, Martha J. Kelly, Anna Chasnoff, Gang Dong, Edwin L. Crow, Duk Soon Choi, Lianhe Shu, Ping Wang
  • Patent number: 9249130
    Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, whic
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: February 2, 2016
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
  • Patent number: 9232801
    Abstract: 1,2,4-Triazine-3,5-dione-6-carboxamides of the general formula (I) are described as herbicides. In this formula (I), R1 and R2 are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical. Z and Y are each oxygen or sulfur.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: January 12, 2016
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Ralf Braun, Christian Waldraff, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
  • Patent number: 9040530
    Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 26, 2015
    Assignee: PORTOLA PHARMACEUTICALS, INC.
    Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
  • Patent number: 9040618
    Abstract: A rubber composition for manufacturing tyres is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more 1,2,4-triazine compounds chosen from compounds of formula I and compounds of formula II: Certain specific 1,2,4-triazine derivatives are described.
    Type: Grant
    Filed: April 16, 2012
    Date of Patent: May 26, 2015
    Assignees: COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN, MICHELIN RECHERCHE ET TECHNIQUE S.A.
    Inventors: Anne Veyland, Nicolas Seeboth
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Publication number: 20150126474
    Abstract: Using a whole-cell high-throughput screen, eleven molecules were identified that activate V. cholerae quorum sensing (QS). Eight molecules are receptor agonists and three molecules are antagonists of LuxO, the central NtrC-type response regulator that controls the global V. cholerae QS cascade. Pro-QS molecules are used for the development of novel anti-infectives.
    Type: Application
    Filed: February 20, 2013
    Publication date: May 7, 2015
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie L. Bassler, Wai-Leung Ng, Lark J. Perez, Jianping Cong, Martin F. Semmelhack
  • Patent number: 9024019
    Abstract: Compounds of the formula (I) or (I?), wherein the substituents are as defined in claim 1, are useful as pesticides.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: May 5, 2015
    Assignee: Syngenta Participations AG
    Inventors: Sebastian Rendler, Jurgen Harry Schaetzer, Shuji Hachisu, Peter Maienfisch, Thomas Pitterna, Olivier Jacob, Jerome Yves Cassayre
  • Patent number: 9018224
    Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
  • Publication number: 20150111857
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
  • Publication number: 20150105385
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
  • Patent number: 9000155
    Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula I: in which R1 is a halo-alkyl group and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system, or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: April 7, 2015
    Assignee: University Of Greenwich
    Inventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
  • Publication number: 20150094308
    Abstract: The present application relates to novel substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: January 8, 2013
    Publication date: April 2, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Frank Wunder, Dieter Lang
  • Patent number: 8987256
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Publication number: 20150072986
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Application
    Filed: June 11, 2014
    Publication date: March 12, 2015
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
  • Publication number: 20150065706
    Abstract: The invention relates to (among other things) methods for treatment comprising administering oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Application
    Filed: October 30, 2014
    Publication date: March 5, 2015
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
  • Patent number: 8969554
    Abstract: Disclosed are compounds exhibiting sufficient herbicidal activity at low application dosage when they are applied to soils and foliage, and an agrochemical composition using the same, in particular herbicides. The compounds are triazine derivatives represented by following Formula 1 or salts thereof, and the herbicides containing them: [Chem. 28] wherein in the formula, R1 represents a hydrogen atom; a C1-C12 alkyl group; a C2-C6 alkenyl group, etc., R2 represents a C1-C12 alkyl group, etc., Y and Z represent an oxygen atom or a sulfur atom, and A represents a 5- or 6-membered cyclic group which may contain a nitrogen atom, an oxygen atom, or a sulfur atom.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: March 3, 2015
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Atsushi Shibayama, Ryu Kajiki, Masami Kobayashi, Takashi Mitsunari, Atsushi Nagamatsu
  • Patent number: 8940891
    Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: January 27, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
  • Publication number: 20140378432
    Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140371223
    Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.
    Type: Application
    Filed: June 16, 2014
    Publication date: December 18, 2014
    Applicant: Addex Pharma S.A.
    Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Patent number: 8895553
    Abstract: The invention relates to (among other things) methods for treatment comprising administering oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Grant
    Filed: May 20, 2014
    Date of Patent: November 25, 2014
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
  • Publication number: 20140343038
    Abstract: The present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula R1 represents a hydrogen atom or an optionally substituted C1-C6 alkyl group; A represents a hydrogen atom, an optionally substituted C1-C8 alkyl group, an optionally substituted C2-C6 alkenyl group, an optionally substituted C2-C6 alkynyl group, an optionally substituted C3-C10 cycloalkyl group, an optionally substituted C6-C14 aromatic hydrocarbon group, an optionally substituted 4- to 10-membered unsaturated heterocyclic group, or an optionally substituted 4- to 10-membered saturated heterocyclic group, or optionally forms a 4- to 10-membered unsaturated heterocyclic ring or a 4- to 10-membered saturated heterocyclic ring together with R1 and the nitrogen atom bonded thereto; R2 represents a hydrogen atom or an optionally substituted C1-C6 alkyl group; and B represents an optionally substituted unsaturated heterocyclic group).
    Type: Application
    Filed: September 28, 2012
    Publication date: November 20, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Toshihiro Sakamoto, Takashi Mita, Kazuaki Shibata, Yoshio Ogino, Hideya Komatani
  • Publication number: 20140336186
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Application
    Filed: July 9, 2014
    Publication date: November 13, 2014
    Inventors: Thomas BRETSCHNEIDER, Eva-Maria FRANKEN, Ulrich GÖRGENS, Martin FÜSSLEIN, Achim HENSE, Joachim KLUTH, Hans-Georg SCHWARZ, Adeline KÖHLER, Olga MALSAM, Arnd VOERSTE, Angela BECKER
  • Publication number: 20140329819
    Abstract: Compounds of the formula (I) or (I?), wherein the substituents are as defined in claim 1, are useful as pesticides.
    Type: Application
    Filed: November 20, 2012
    Publication date: November 6, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sebastian Rendler, Jurgen Harry Schaetzer, Shuji Hachisu, Peter Maienfisch, Thomas Pitterna, Olivier Jacob, Jerome Yves Cassayre
  • Publication number: 20140303142
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 9, 2014
    Inventors: John W. Butcher, David Witter, Christopher Dinsmore, June Kim, John Hendrix, Raksha Acharya, Sean P. Ahearn, Joon Jung, Alexey Rivkin, Philip Jones
  • Patent number: 8846669
    Abstract: Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group. In Formula 1, R and Q are the same as defined in the detailed description. In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: September 30, 2014
    Assignee: Legochem Biosciences, Inc.
    Inventors: Young Lag Cho, Sung Yoon Baek, Sang Eun Chae, Sun Young Kim, Hong Bum Lee, Hyang Sook Lee, Kyuman Oh, Hye Jin Heo, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Publication number: 20140275077
    Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.
    Type: Application
    Filed: May 13, 2014
    Publication date: September 18, 2014
    Applicant: Cephalon, Inc.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Patent number: 8822465
    Abstract: The present invention relates to a quinoline derivative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, wherein Ar, R1, R2, R3, X, Y and n have the meanings given in the description. The present invention also relates to the comparatively strong effect of the compound represented by general formula (I) on inhibiting c-Met kinase. The present invention further relates to the use of this compound or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof in the manufacturing of a medicament for treating the disease caused by abnormally over-expressing c-Met kinase, in particular, for treating or preventing cancer.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: September 2, 2014
    Assignee: Wuhan Shengyun Biopharma Co., Ltd.
    Inventor: Hua Xu
  • Publication number: 20140243343
    Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula I: in which R1 is a halo-alkyl group and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system, or a pharmaceutically acceptable salt or solvate thereof.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 28, 2014
    Applicant: University of Greenwich
    Inventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
  • Patent number: 8816079
    Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: August 26, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
  • Patent number: 8809525
    Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, whic
    Type: Grant
    Filed: February 7, 2011
    Date of Patent: August 19, 2014
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
  • Publication number: 20140221362
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
  • Publication number: 20140213590
    Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
    Type: Application
    Filed: January 3, 2014
    Publication date: July 31, 2014
    Applicant: FOCHON PHARMA, INC.
    Inventors: WEIBO WANG, TONGSHUANG LI
  • Patent number: 8779129
    Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: July 15, 2014
    Assignee: Addex Pharma S.A.
    Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
  • Patent number: 8772291
    Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: July 8, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
  • Patent number: 8772479
    Abstract: The invention relates to (among other things) oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: July 8, 2014
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
  • Patent number: 8765943
    Abstract: A 1,2,4-triazine of formula (I): and its process of manufacture and use.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: July 1, 2014
    Assignees: Compagnie Generale des Etablissements Michelin, Michelin Recherche et Technique S.A.
    Inventors: Nicolas Seeboth, Sergey Ivanov, Sergey Molkov