Triazine Ring Patents (Class 544/112)
  • Patent number: 11235316
    Abstract: The present invention is directed to reaction mixtures comprising a water-surfactant mixture, wherein the catalyst comprises a compound with solubilizing groups. This technology improves the solubility of the reaction components in the water-surfactant mixture and thereby, greatly increases the productivity and selectivity of the chemical reaction.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: February 1, 2022
    Assignee: Novartis AG
    Inventors: Fabrice Gallou, Pengfei Guo, Jianguang Zhou, Michael Parmentier
  • Patent number: 11040048
    Abstract: A medicament characterized in that (A) a compound represented by the formula (I): its pharmaceutically acceptable salt, or a solvate thereof, wherein P is hydrogen or a group to form a prodrug; A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is each independently CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A4 is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A are each independently hydrogen, halogen, alkyl, or the like; R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle; n is any integer of 1 to 2; and R1 is or the like, is combined
    Type: Grant
    Filed: December 14, 2016
    Date of Patent: June 22, 2021
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Takao Shishido, Takeshi Noshi, Atsuko Yamamoto, Mitsutaka Kitano
  • Patent number: 9913861
    Abstract: Described herein is a pharmaceutical composition comprising atropine or a salt thereof; aconitine; and mercury cyanide. The composition is useful in a method for treating a viral infection.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: March 13, 2018
    Assignee: Medice Arzneimittel Puettere GMBH & Co. KG
    Inventors: Sigurd Puetter, Richard Ammer, Michael Schmidbauer
  • Patent number: 9724352
    Abstract: The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: August 8, 2017
    Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.
    Inventors: Chunhao Yang, Linghua Meng, Yanhong Chen, Xiang Wang, Cun Tan, Jiapeng Li, Jian Ding, Yi Chen
  • Patent number: 9453000
    Abstract: Disclosed is a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by A?, wherein Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; X1 represents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: September 27, 2016
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Teiji Kimura, Noritaka Kitazawa, Toshihiko Kaneko, Nobuaki Sato, Koki Kawano, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Yu Yoshida, Toshiyuki Uemura, Takashi Doko, Daisuke Shinmyo, Daiju Hasegawa, Takehiko Miyagawa, Hiroaki Hagiwara
  • Patent number: 9447101
    Abstract: The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.
    Type: Grant
    Filed: April 23, 2013
    Date of Patent: September 20, 2016
    Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.
    Inventors: Chunhao Yang, Linghua Meng, Yanhong Chen, Xiang Wang, Cun Tan, Jiapeng Li, Jian Ding, Yi Chen
  • Publication number: 20150141644
    Abstract: The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.
    Type: Application
    Filed: April 23, 2013
    Publication date: May 21, 2015
    Applicants: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.
    Inventors: Chunhao Yang, Linghua Meng, Yanhong Chen, Xiang Wang, Cun Tan, Jiapeng Li, Jian Ding, Yi Chen
  • Publication number: 20150111887
    Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
    Type: Application
    Filed: October 15, 2014
    Publication date: April 23, 2015
    Inventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
  • Publication number: 20150111854
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 23, 2015
    Inventors: Chika TAKAHASHI, Hindenori MIKAMIYAMA, Toshiyuki AKIYAMA, Kenji TOMITA, Yoshiyuki TAODA, Makoto KAWAI, Kosuke ANAN, Masayoshi MIYAGAWA, Naoyuki SUZUKI
  • Patent number: 8987441
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: March 24, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Chika Takahashi, Hidenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa, Naoyuki Suzuki
  • Publication number: 20150080371
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: December 11, 2012
    Publication date: March 19, 2015
    Inventors: Marie-Pierre Collin, Dirk Brohm, Melanie Heroult, Mario Lobell, Walter Hübsch, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer, Niels Lindner
  • Publication number: 20150065465
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Patent number: 8957081
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 17, 2015
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Publication number: 20150031676
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: February 20, 2013
    Publication date: January 29, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Mario Lobell, Walter Hübsch, Hartmut Schirok, Mélanie Héroult, Dirk Brohm, Marie-Pierre Collin, Sylvia Grünewald, Klemens Lustig, Ulf Bömer, Verena Vöhringer, Niels Lindner
  • Patent number: 8940736
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: January 27, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Publication number: 20140378451
    Abstract: The present invention relates to cannabinoid-2-receptor (CB2R) agonist compounds. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of diseases or conditions in which CB2R stimulation is beneficial (especially inflammatory conditions).
    Type: Application
    Filed: September 19, 2012
    Publication date: December 25, 2014
    Inventors: Ivy Christou, Rebecca Lillian Cross, Matteo Gianella-Borradori, David Robert Greaves, Angela Jane Russell, Graham Michael Wynne
  • 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: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Publication number: 20140336173
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(?O)—NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR2R10, —C(?O)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: December 10, 2012
    Publication date: November 13, 2014
    Inventors: Dirk Brohm, Melanie Heroult, Marie-Pierre Collin, Walter Hübsch, Mario Lobell, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer
  • Patent number: 8841288
    Abstract: Compounds of Formula (I): able to inhibit kinase activity, in particular Phosphatidylinositol 3-Kinases activity. The disclosure also relates to the use of compounds of Formula (I) for treatment of pathological conditions associated to alterations in Phosphatidylinositol 3-Kinases activity.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: September 23, 2014
    Assignees: Universtà Degli Studi di Torino, Università Degli Studi del Piemonte Orientale “Amedeo Avogadro”
    Inventors: Giovanni Sorba, Gian Cesare Tron, Ubaldina Galli, Alberto Massarotti, Emilio Hirsch, Elisa Ciraolo, Tracey Pirali
  • Publication number: 20140275072
    Abstract: The invention relates to compounds of the formula (I) in which R1, L and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into a salt thereof.
    Type: Application
    Filed: October 30, 2012
    Publication date: September 18, 2014
    Applicant: Merck Patent GmbH
    Inventors: Werner Mederski, Thomas Fuchss, Ulrich Emde, Hans-Peter Buchstaller
  • Publication number: 20140256718
    Abstract: This invention relates to novel 5-[(hydroxymethyl)aryl]-substituted pyrrolo[2,1-f][1,2,4]triazin-4-amines of formula (I), to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating angiogenesis-related disorders, in particular angiogenesis-related ocular disorders.
    Type: Application
    Filed: June 26, 2012
    Publication date: September 11, 2014
    Applicants: BAYER INTELLECTUAL PROPERTY GmbH, BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Jürgen Klar, Verena Vöhringer, Joachim Telser, Mario Lobell, Frank Süssmeier, Volkhart Min-Jian Li, Michael Böttger, Stefan Golz, Dieter Lang, Karl-Heinz Schlemmer, Thomas Schlange, Andreas Schall, Wenlang Fu
  • Publication number: 20140256719
    Abstract: A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, maintaining normal sinus rhythm, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 11, 2014
    Inventors: Heather Finlay, Ashok Kumar Adisechan, Naveen Kumar Dhondi, Kavitha Govindrajulu, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
  • 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
  • Patent number: 8679773
    Abstract: This invention pertains to methods, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: March 25, 2014
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Darryl J. C. Pappin, Michael Bartlett-Jones
  • Publication number: 20140018319
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: July 12, 2013
    Publication date: January 16, 2014
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Publication number: 20130345191
    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: Application
    Filed: March 15, 2013
    Publication date: December 26, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
  • Publication number: 20130345219
    Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 28, 2013
    Publication date: December 26, 2013
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Chi-Wan Lee, Teresa Prezewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
  • Patent number: 8557808
    Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: October 15, 2013
    Assignees: North Carolina Central University, The University of North Carolina at Chapel Hill, Albert Einstein College of Medicine of Yeshiva University
    Inventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
  • Publication number: 20130252958
    Abstract: The present invention relates to a quinoline deravative 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: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Inventor: Hua XU
  • Publication number: 20130225809
    Abstract: This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.
    Type: Application
    Filed: December 20, 2012
    Publication date: August 29, 2013
    Applicant: Bayer HealthCare LLC
    Inventor: Bayer HealthCare LLC
  • Patent number: 8512421
    Abstract: A polyurethane derivative and a composition thereof are disclosed. The polyurethane derivative of the present invention has a structure of formula (I). The polyurethane derivative and the composition thereof can be used for increasing light fastness.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: August 20, 2013
    Assignee: Everlight Chemical Industrial Corporation
    Inventors: Hsin-Ying Lu, Sheue-Rong Lee, Tzu-Heng Ko, Hsiang-Lin Chiang, Der-Gun Chou
  • Publication number: 20130197219
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: September 21, 2011
    Publication date: August 1, 2013
    Inventors: Chika Takahashi, Hidenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa, Naoyuki Suzuki
  • Publication number: 20130196972
    Abstract: This invention relates to novel compounds of reverse-turn mimetics, having pyrazino-triazinone as a basic framework, and a method of preparing the same, and the use thereof to treat diseases such as cancer, in particular, acute myeloid leukemia.
    Type: Application
    Filed: October 14, 2011
    Publication date: August 1, 2013
    Applicant: JW PHARMACEUTICAL CORPORATION
    Inventors: Jae-Uk Chung, Mi-Jung Kim, Yong-Sil Lee, Sang-Ho Ma, Young-Seok Cho, Sang-Hak Lee, Young-Jun Na, Myoung-Joo Kang, Woul-Seong Park
  • Publication number: 20130150369
    Abstract: Benzotriazine doxides are disclosed as drugs targeting mycobacterium tuberculosis, including novel compounds of formula I:
    Type: Application
    Filed: December 23, 2012
    Publication date: June 13, 2013
    Applicant: SRI INTERNATIONAL
    Inventors: Peter Madrid, Sidharth Chopra, Kenneth Ryan, Gary Koolpe
  • Publication number: 20130096109
    Abstract: An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Application
    Filed: April 11, 2011
    Publication date: April 18, 2013
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Kazunari Hattori, Kenji Tomita
  • Publication number: 20130096114
    Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof.
    Type: Application
    Filed: December 7, 2012
    Publication date: April 18, 2013
    Applicant: SURFACE LOGIX, INC.
    Inventor: SURFACE LOGIX, INC.
  • Patent number: 8399450
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: March 19, 2013
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Publication number: 20130059844
    Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.
    Type: Application
    Filed: March 26, 2012
    Publication date: March 7, 2013
    Applicant: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jorg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
  • Publication number: 20130029963
    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: Application
    Filed: February 7, 2011
    Publication date: January 31, 2013
    Applicant: HEPTARES THERAPEUTICS LIMITED
    Inventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
  • Publication number: 20130023514
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) pyrrolotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: March 30, 2011
    Publication date: January 24, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventors: Jay A. Markwalder, Brian E. Fink, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Steven P. Seitz
  • Patent number: 8338414
    Abstract: A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: December 25, 2012
    Assignee: Zenyaku Kogyo KabushikiKaisha
    Inventors: Kazuhiko Haruta, Shinichi Yaguchi, Toshiyuki Matsuno, Yoshio Tsuchida, Tetsuo Watanabe, Kimitomo Yoshioka, Ryogo Yui
  • Publication number: 20120322797
    Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.
    Type: Application
    Filed: December 9, 2010
    Publication date: December 20, 2012
    Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, NORTH CAROLINA CENTRAL UNIVERSITY, ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
  • Publication number: 20120289493
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 8, 2012
    Publication date: November 15, 2012
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20120232054
    Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has a Btk inhibitory activity, and is useful as a method for preventing and/or treating a rheumatoid arthritis, an autoimmune disease, a B cell lymphoma of cancer, and the like.
    Type: Application
    Filed: April 28, 2010
    Publication date: September 13, 2012
    Applicant: LOCUS PHARMACEUTICALS, INC.
    Inventors: Kevin J. Moriarty, Dora Do-York Wong, Zenon Konteatis, Kristofer Moffett, Younghee Lee, Wenchun Chao
  • Publication number: 20120220584
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Application
    Filed: September 23, 2011
    Publication date: August 30, 2012
    Applicant: TargeGen, Inc.
    Inventors: Wolfgang WRASIDLO, Elena Dneprovskaia
  • Publication number: 20120184734
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: June 14, 2010
    Publication date: July 19, 2012
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20120165314
    Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.
    Type: Application
    Filed: March 7, 2012
    Publication date: June 28, 2012
    Applicant: Bayer HealthCare LLC
    Inventors: Julie Dixon, Barton Phillips, Yamin Wang, Tindy Li, Kyle Parcella, Jason Newcom, Harold C.E. Kluender, Zhenqiu Hong, Brent Chandler, Zhonghua Zhang, Steven Magnuson, Kristen M. Allegue, Zheng Liu
  • Publication number: 20120010172
    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 31, 2009
    Publication date: January 12, 2012
    Applicant: McDERMOTT WILL & EMERY LLP
    Inventors: Mette Knak Christensen, Fredrik Bjorkling