Bicyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/235)
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Patent number: 12215069Abstract: In one aspect, compounds modulating sirtuin activity are described herein. Sirtuin modulation by compounds described herein includes sirtuin activation and sirtuin inhibition. Modulation of sirtuin activity includes sirtuin activation and/or sirtuin inhibition. In some embodiments, a sirtuin modulating compound and/or salt thereof is of Formula I described herein.Type: GrantFiled: January 24, 2024Date of Patent: February 4, 2025Assignee: CODAGEN BIOSCIENCES, INC.Inventors: Célina Reverdy, Gaetan Gitton, Xiangying Guan, Indranil Adhya, Rama Krishna Dumpati, Samir Roy, Santu Chall, Anisha Ghosh, Gauthier Errasti, Thomas Delacroix, Raj Chakrabarti
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Patent number: 12012370Abstract: In one aspect, compounds modulating sirtuin activity are described herein. Sirtuin modulation by compounds described herein includes sirtuin activation and sirtuin inhibition. Modulation of sirtuin activity includes sirtuin activation and/or sirtuin inhibition. In some embodiments, a sirtuin modulating compound and/or salt thereof is of Formula I described herein.Type: GrantFiled: December 29, 2022Date of Patent: June 18, 2024Assignee: CODAGEN BIOSCIENCES, INC.Inventors: Célina Reverdy, Gaetan Gitton, Xiangying Guan, Indranil Adhya, Rama Krishna Dumpati, Samir Roy, Santu Chall, Anisha Ghosh, Gauthier Errasti, Thomas Delacroix, Raj Chakrabarti
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Patent number: 11673899Abstract: Disclosed are a crystal form of a thieno[2,3-c]pyridazine-4(1H)-one compound, a preparation method therefor and the use thereof in the preparation of a drug as an inhibitor of ACC1 and ACC2.Type: GrantFiled: December 4, 2020Date of Patent: June 13, 2023Assignees: ZHANGZHOU PIEN TZE HUANG PHARMACEUTICAL CO., LTD., MEDSHINE DISCOVERY INC.Inventors: Juan Yu, Zhiliang Chen, Shicong Wang, Tingting Yin, Kaili Jian, Xiaoping Zheng, Zhigan Jiang, Haiying He
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Patent number: 11053250Abstract: A compound of Formula (I): pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof are disclosed.Type: GrantFiled: August 9, 2019Date of Patent: July 6, 2021Assignee: Gilead Sciences, Inc.Inventors: Stephen Ammann, Elizabeth M. Bacon, Gediminas Brizgys, Elbert Chin, Chienhung Chou, Jeromy J. Cottell, Marilyn Ndukwe, James G. Taylor, Nathan E. Wright, Zheng-Yu Yang, Sheila M. Zipfel
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Patent number: 10647794Abstract: The invention provides a polymerizable compound of formula (I), polymerizable composition, polymer, and optically anisotropic article capable of obtaining an optical film having a low melting point, excellent solubility, being manufactured at low cost, and of uniform polarized light conversion across a broad wavelength region. In formula (I): Y1 to Y6 are independently a chemical single bond, —O—, —O—C(?O)—, —C(?O)—O—; G1 and G2 are independently a divalent C1-C20 aliphatic group; Z1 and Z2 are independently a C2-C10 alkenyl group substituted with a halogen atom; Ax is a C2-C30 organic group that includes at least one aromatic ring of an aromatic hydrocarbon ring or an aromatic hetero ring; Ay is H, a C1-C20 alkyl group, a C2-C20 alkenyl group, a C3-C12 cycloalkyl group; A1 is a trivalent aromatic group; A2 and A3 are independently a divalent C6-C30 aromatic group; and Q1 is H, or a C1-C6 alkyl group.Type: GrantFiled: October 22, 2015Date of Patent: May 12, 2020Assignee: ZEON CORPORATIONInventors: Kei Sakamoto, Kumi Okuyama
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Patent number: 10450288Abstract: Disclosed are compounds having the formula: wherein R1, R2 and R3 are as defined herein, and methods of making and using the same, including use as inhibitors of BMP1, TLL1 and/or TLL2 and in treatment of diseases associated with BMP1, TLL1 and/or TLL2 activity.Type: GrantFiled: January 9, 2015Date of Patent: October 22, 2019Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Sarah E. Dowdell, Hilary Schenck Eidam, Mark Elban, Ryan Michael Fox, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Lara Kallander, Brian Griffin Lawhorn, Sharada Manns, Joanne Philp, David G. Washburn, Guosen Ye
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Patent number: 9364481Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: GrantFiled: November 18, 2015Date of Patent: June 14, 2016Assignee: Nivalis Therapeutics, Inc.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Patent number: 9174947Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: GrantFiled: October 26, 2006Date of Patent: November 3, 2015Assignee: Exelixus, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
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Patent number: 9133200Abstract: New imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: GrantFiled: November 24, 2011Date of Patent: September 15, 2015Assignee: Almirall, S.A.Inventors: Jacob Gonzalez Rodriguez, Bernat Vidal Juan, Laura Vidal Gispert, Jordi Bach Taña
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Patent number: 9120723Abstract: The present disclosure relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is selected from OH, NHCH2CH2F, NHCH(Me)CH2OH and NHCH2CH2OH; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is phenyl or pyridyl; and B is (CH2)n where n is 0; with the proviso that: (i) when A is phenyl, and Z is OH, X—Y is other than C?C—(CH2)2CO2H, C?C—(CH2)2CO2Me, (CH2)4CO2H. Uses of such compounds as medicaments for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors are provided.Type: GrantFiled: October 18, 2012Date of Patent: September 1, 2015Assignee: CANBEX THERAPEUTICS LIMITEDInventors: Masahiro Okuyama, David Selwood, Cristina Visintin, David Baker, Gareth Pryce
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Publication number: 20150126513Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.Type: ApplicationFiled: July 13, 2012Publication date: May 7, 2015Applicant: Novartis AGInventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
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Publication number: 20150126487Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, a sleep disorder and the like. The present invention relates to a compound represented by the formula (I): wherein R1 is an optionally substituted amino group or an optionally substituted cyclic amino group, R2 and R3 are each independently a hydrogen atom or a substituent, X is —CH? or —N?, and ring A is an optionally substituted 5- to 10-membered ring, or a salt thereof.Type: ApplicationFiled: February 28, 2013Publication date: May 7, 2015Inventors: Hiroki Sakamoto, Takahiro Sugimoto
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Publication number: 20150111894Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.Type: ApplicationFiled: May 9, 2013Publication date: April 23, 2015Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
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Publication number: 20150099277Abstract: Provided herein, inter alia, are compositions and methods of synthesis and detection of tetrazines and diazonorcaradienes.Type: ApplicationFiled: October 6, 2014Publication date: April 9, 2015Inventors: Neal K. Devaraj, Jun Yang, Jolita Seckute
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Publication number: 20150087043Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.Type: ApplicationFiled: April 11, 2014Publication date: March 26, 2015Applicants: Coferon, Inc, Cornell UniversityInventors: Lee Daniel Arnold, Maneesh Pingle, Douglas S. Werner
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Patent number: 8987273Abstract: The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacture and their use for the treatment of benign and malignant neoplasia.Type: GrantFiled: July 27, 2011Date of Patent: March 24, 2015Assignee: Bayer Intellectual Property GmbHInventors: Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
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Patent number: 8987268Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.Type: GrantFiled: March 16, 2012Date of Patent: March 24, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Stephen T. Wrobleski, Jagabandhu Das, Jingwu Duan, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Zhonghui Lu, William J. Pitts, Steven H. Spergel, Hong Wu, Bingwei Vera Yang
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Patent number: 8980871Abstract: Provided herein are methods of treating hemolysis by administering an active compound in an amount sufficient to treat said hemolysis. It has been found that nitroxyl donors or similar compounds preferentially react with cell-free OxyHb, as compared to OxyHb encapsulated in a red blood cell, and reacts with MetHb to form iron-nitrosyl Hb or nitrite bound MetHb. It has also been found that such compounds reduce cell-free Hb and hemolysis. Active compounds are also contemplated for use in combination therapies, for example, in combination with the administration of red blood cells and/or an agent that promotes hematopoiesis, or in combination with the administration of a nitric oxide donor.Type: GrantFiled: September 19, 2008Date of Patent: March 17, 2015Assignees: Wake Forest University Health Sciences, The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Daniel B. Kim-Shapiro, S. Bruce King, Daniel A. Sweeney, Mark T. Gladwin
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Publication number: 20150072987Abstract: Novel compound having the following formula: wherein Y is N, O, or S. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.Type: ApplicationFiled: July 17, 2014Publication date: March 12, 2015Inventor: Zhanggui WU
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Publication number: 20150065501Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.Type: ApplicationFiled: March 27, 2013Publication date: March 5, 2015Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
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Patent number: 8962626Abstract: The present invention relates to thienopyridazine compounds of formula (I), their pharmaceutically acceptable salts or hydrates, wherein R1 and R2 are independently H or C1-4 alkyl, R3 is a saturated or unsaturated 5- or 6-membered ring containing N, S or O, or its optical isomers, R4 is a halophenyl monosubstituted or disubstituted at any position. The present invention provides the preparation methods of these compounds, pharmaceutical compositions containing these compounds and the uses of these compounds, particularly in treating cancer.Type: GrantFiled: January 7, 2009Date of Patent: February 24, 2015Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical FactoryInventor: Zhanggui Wu
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Patent number: 8957073Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: May 11, 2011Date of Patent: February 17, 2015Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
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Publication number: 20150038510Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined in the specification. The compounds are inhibitors of Bruton's tyrosine kinase (BTK). This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with BTK.Type: ApplicationFiled: March 25, 2013Publication date: February 5, 2015Inventors: John David Lawson, Mark Sabat, Christopher Smith, Haixia Wang, Young K. Chen, Toufike Kanouni
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Publication number: 20150031686Abstract: Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.Type: ApplicationFiled: March 6, 2013Publication date: January 29, 2015Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
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Publication number: 20150018309Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: February 23, 2013Publication date: January 15, 2015Inventors: Craig W Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, James C. Tarr, James M. Salovich
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Publication number: 20150004100Abstract: Pyridazinone compounds of Formula I: (I) wherein: R? is alkyl or Ar, optionally substituted with at least one alkyl, halogen, hydroxyl, alkoxy, haloalkoxy, acid, ester, amino, nitro, amide, or alkoxyhalo; 2 R is independently alkyi, alkynyl, ester, amino, amide, acid, aryl, heteroaryl, aminoalkyl, —C(=0)alkyl, —C(=0)aryl, —C(=0)heteroaryl, —C(=0)heterocycloalkyl, —C(=0)heterocycloalkylAr, —C(=0)(CH2)nhalo, —C(?O)(CH2)nheterocyclyl, or —SC?Ar, optionally substituted with at least one alkyi, alkylhalo, halogen, nitro, aryl, heteroaryl, or heteroaryl(CH2)nhalo; R3 and R4 are independently hydrogen, alkyi, alkenyl, alkynyl, aryl, heteroaryl; Ar is an aryl, heteroaryl, cycloalkyl, heterocycloalkyl group; n is an integer from 0-10; or a radiolabeled derivative thereof. The compounds are useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.Type: ApplicationFiled: December 13, 2012Publication date: January 1, 2015Applicant: GE HEALTHCARE LIMITEDInventors: Clare Jones, Matthias Eberhard Glaser, Duncan Wynn, James Nairne, Umamaheshwar P. Mokkapati, Ian Martin Newington, Chitralekha Rangswamy, Jinto Jose, Saga Johansson
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Patent number: 8921368Abstract: Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.Type: GrantFiled: March 16, 2012Date of Patent: December 30, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Stephen T. Wrobleski, Gregory D. Brown, Lidia M. Doweyko, Jingwu Duan, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Zhonghui Lu, Steven H. Spergel, John S. Tokarski, Hong Wu, Bingwei Vera Yang
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Patent number: 8916554Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: July 22, 2013Date of Patent: December 23, 2014Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Publication number: 20140364431Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.Type: ApplicationFiled: December 7, 2012Publication date: December 11, 2014Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
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Patent number: 8883786Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: GrantFiled: February 13, 2012Date of Patent: November 11, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch
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Patent number: 8883787Abstract: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: GrantFiled: June 10, 2013Date of Patent: November 11, 2014Assignee: Eisai Inc.Inventors: Weizheng Xu, Greg Delahanty, Jie Zhang
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Patent number: 8865709Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: September 24, 2013Date of Patent: October 21, 2014Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Patent number: 8865719Abstract: The present invention is related to heterocycles represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs and/or GABAA receptors. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs and negative allosteric modulation of GABAA receptors in a mammal by administering an effective amount of a compound of Formula I.Type: GrantFiled: March 9, 2010Date of Patent: October 21, 2014Assignee: The Regents of the University of CaliforniaInventors: Timothy B. C. Johnstone, Derk J. Hogenkamp, Kelvin W. Gee
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Patent number: 8859549Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: May 8, 2012Date of Patent: October 14, 2014Assignee: AbbVie, Inc.Inventors: Brian S. Brown, Tongmei Li, Sridhar Peddi, Arturo Perez-Medrano, David DeGoey
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Publication number: 20140303150Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.Type: ApplicationFiled: December 22, 2011Publication date: October 9, 2014Applicant: LEO Laboratories LimitedInventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
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Publication number: 20140288052Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 19, 2012Publication date: September 25, 2014Inventors: Charles A. Blum, Jeremy S. Disch, Stephanie K. Springer
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Publication number: 20140283218Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.Type: ApplicationFiled: June 27, 2012Publication date: September 18, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Roger Graham Hall, Andrew Edmunds, Andre Jeanguenat, Thomas Pitterna, Sebastian Rendler
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Publication number: 20140275069Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: February 25, 2014Publication date: September 18, 2014Inventors: Katja JANTOS, Michael OCHSE, Hervé GENESTE, Jayne FROGGETT, Clarissa JAKOB, Karla DRESCHER, Jürgen DINGES
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Publication number: 20140249151Abstract: [Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating 11?-hydroxysteroid dehydrogenase type 1-related diseases such as dementia, schizophrenia, depression, pain (particularly, neuropathic pain or fibromyalgia), diabetes (particularly, type II diabetes mellitus), insulin resistance and the like. [Means for Solution] A bicyclic heterocyclic compound (the bicyclic heterocycle is formed when a cyclohexane ring is fused with a 5- to 6-membered monocyclic heterocycle that has only a nitrogen atom as a hetero atom) substituted with an acylamino group such as a (hetero)aroylamino group or the like or a pharmaceutically acceptable salt thereof was found to have an excellent selective inhibitory action against 11?-HSD1.Type: ApplicationFiled: October 17, 2012Publication date: September 4, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Shimpei Kawakami, Minoru Sakurai, Noriyuki Kawano, Takayuki Suzuki, Nobuyuki Shiraishi, Wataru Hamaguchi, Ryuichi Sekioka, Hiroyuki Moritomo, Ayako Motitomo
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Publication number: 20140235855Abstract: Compounds of formula (I), wherein A1 represents —O—, —S— or —CH2—; A2 represents —CH2— or —O—; A3 represents C3-C8-cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, —C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; m is 0 or 1; n is 1; the —(CH2)n— group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.Type: ApplicationFiled: June 11, 2012Publication date: August 21, 2014Inventors: Berangere Gaucher, Franck Hubert Danel, Tong Xie, Lin Xu
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Patent number: 8809427Abstract: Provided is a phthalocyanine compound which is halogen-free and which has a green hue, excellent resistance to organic solvents and acids, and high chroma. Also provided are a metal-free phthalocyanine compound or a metal phthalocyanine compound represented by specified general formula (1-1) or (1-2) and having a N,N?-disubstituted imidazolone structure or piperazinedione structure introduced therein, and a coloring composition including the compound and a synthetic resin. The phthalocyanine compound of the present invention exhibits a clear green color and is halogen-free, and is thus useful as a clear green pigment for coloring materials such as a coating material, plastic, a printing ink, rubber, leather, textile printing, a color filter, a jet ink, a heat transfer ink, etc.Type: GrantFiled: August 6, 2010Date of Patent: August 19, 2014Assignee: DIC CorporationInventors: Hitoshi Kondou, Yoshiyuki Sano, Yutaka Tachikawa
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Patent number: 8785643Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: GrantFiled: December 16, 2011Date of Patent: July 22, 2014Assignee: N30 Pharmaceuticals, Inc.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Patent number: 8765691Abstract: The present invention relates to the use of osmolytes for treating allergic or viral respiratory diseases, e.g. allergic rhinitis (hay fever) as well as rhinovirus and/or adenovirus infections. The invention also relates to a medicament preparation containing one or more compounds from the group of osmolytes. The group of osmolytes used in the invention comprises various low-molecular substances, more specifically ectoine, 4,5,6,7-tetrahydro-2-methyl-1H-[1,3]-diazepine-4-S-carboxylic acid (homoectoine), hydroxyectoine, di-myo-inositol-phosphate (DIP), to cyclic 2,3-diphosphoglycerate (cDPG), 1,1-diglycerol phosphate (DGP), ?-mannosylglycerate (firoin), ?-mannosylglyceramide (firoin-A), dimannosyl-diinositol phosphate (DMIP), glucosylglycerol, taurine, betaine, citrulline, and/or a derivative, e.g. an acid, salt, or ester of said compounds.Type: GrantFiled: August 25, 2008Date of Patent: July 1, 2014Assignee: Bitop AGInventors: Jean Krutmann, Georg Lentzen, Thomas Schwarz
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Patent number: 8759539Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.Type: GrantFiled: November 11, 2009Date of Patent: June 24, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
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Patent number: 8754082Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: GrantFiled: May 9, 2013Date of Patent: June 17, 2014Assignee: Siga Technologies, Inc.Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
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Publication number: 20140163035Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: July 20, 2012Publication date: June 12, 2014Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Kurt Hilpert, Francis Hubler, Thierry Kimmerlin, Dorte Renneberg, Simon Stamm, Mark Murphy
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Publication number: 20140155404Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.Type: ApplicationFiled: February 10, 2014Publication date: June 5, 2014Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Genfeng Cao, Taisheng Huang, Lihua Chen, Ke Zhang, Anlai Wang, David J. Meloni, Rajan Anand, Joseph Glenn, Brian W. Metcalf
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Publication number: 20140142088Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.Type: ApplicationFiled: November 18, 2013Publication date: May 22, 2014Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Alison L. Zulli
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Publication number: 20140114068Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.Type: ApplicationFiled: June 18, 2012Publication date: April 24, 2014Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
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Patent number: RE47047Abstract: The present invention relates to compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: GrantFiled: March 24, 2016Date of Patent: September 18, 2018Assignees: ASTRAZENECA AB, BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Berger, Hartmut Rehwinkel, Thomas Zollner, Ekkehard May, Jorma Hassfeld, Heike Schaecke