Tricyclo Ring System Having The Oxazine Ring As One Of The Cyclos Patents (Class 544/101)
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Patent number: 11979405Abstract: Disclosed is a method for processing network resource access requests. The method comprises: receiving a resource access request and acquiring resource access request information; extracting user information and target resource information from the resource access request information, and requiring to establish a corresponding access mediator instance according to the user information and the target resource information; establishing the access mediator instance; and initiating an access to a target resource correspondingly by using the access mediator instance according to the resource access request information received by the access mediator instance. The network security is improved greatly.Type: GrantFiled: January 28, 2022Date of Patent: May 7, 2024Assignee: Hangzhou Jindoutengyun Technologies Co., Ltd.Inventor: Yang Yang
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Patent number: 11807648Abstract: The present invention provides a process for preparing a compound of the formula (II): wherein R2 is unsubstituted alkyl, characterized by reacting a compound of the formula (I): wherein R1 is hydrogen or a protecting group other than unsubstituted alkyl, with a compound of the formula: R2—OH, wherein R2 is as defined above, in the presence of a sodium salt and/or a magnesium salt.Type: GrantFiled: January 19, 2022Date of Patent: November 7, 2023Assignee: SHIONOGI & CO., LTD.Inventor: Setsuya Shibahara
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Patent number: 11518772Abstract: The present disclosure provides certain fused tricyclic ring derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: September 18, 2020Date of Patent: December 6, 2022Assignee: NIKANG THERAPEUTICS, INC.Inventors: Jiping Fu, Yan Lou, Yigang He
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Patent number: 11498926Abstract: The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: December 11, 2020Date of Patent: November 15, 2022Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr., James D. Rodgers
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Patent number: 11459340Abstract: The present disclosure provides certain tri-substituted heteroaryl derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: September 17, 2019Date of Patent: October 4, 2022Assignee: NIKANG THERAPEUTICS, INC.Inventors: Jiping Fu, Yan Lou, Yigang He
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Patent number: 11261198Abstract: The present invention provides a process for preparing a compound of the formula (II): wherein R2 is unsubstituted alkyl, characterized by reacting a compound of the formula (I): wherein R1 is hydrogen or a protecting group other than unsubstituted alkyl, with a compound of the formula: R2—OH, wherein R2 is as defined above, in the presence of a sodium salt and/or a magnesium salt.Type: GrantFiled: June 19, 2017Date of Patent: March 1, 2022Assignee: SHIONOGI & CO., LTD.Inventors: Setsuya Shibahara, Kosuke Anan
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Patent number: 11034705Abstract: The present disclosure provides certain fused tricyclic ring derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: October 19, 2020Date of Patent: June 15, 2021Assignee: Nikang Therapeutics, Inc.Inventors: Jiping Fu, Yan Lou, Yigang He
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Patent number: 10919912Abstract: The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: September 27, 2019Date of Patent: February 16, 2021Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr., James D. Rodgers
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Patent number: 10894797Abstract: The present disclosure provides certain fused tricyclic ring derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: May 12, 2020Date of Patent: January 19, 2021Assignee: Nikang Therapeutics, Inc.Inventors: Jiping Fu, Yan Lou, Yigang He
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Patent number: 10618910Abstract: The present disclosure relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: February 1, 2019Date of Patent: April 14, 2020Assignee: Incyte CorporationInventors: Andrew P. Combs, Richard B. Sparks
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Patent number: 10570149Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of ATR, and can be employed for the treatment of diseases such as cancer.Type: GrantFiled: May 22, 2017Date of Patent: February 25, 2020Assignee: MERCK PATENT GMBHInventors: Lars Burgdorf, Dieter Dorsch, Christos Tsaklakidis
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Patent number: 10464947Abstract: The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: February 27, 2018Date of Patent: November 5, 2019Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr., James D. Rodgers
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Patent number: 10392406Abstract: The present invention provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is 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 A1, 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 and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.Type: GrantFiled: April 27, 2016Date of Patent: August 27, 2019Assignee: SHIONOGI & CO., LTD.Inventor: Makoto Kawai
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Patent number: 10259770Abstract: The invention provides an improved process for preparing Ethacrynic acid of formula I, including the steps of: (a) reacting 4-butyryl-2,3-dichloro-phenoxy acetic acid of formula II with dimethylamine or its salt to obtain [2,3-dichloro-4-(2-dimethylaminomethylbutyryl)phenoxy] acetic acid of formula III or its salt; (b) hydrolyzing [2,3-dichloro-4-(2-dimethylaminomethylbutyryl)phenoxy] acetic acid hydrochloride of formula III obtained in step a) with t-butyl amine to obtain t-butyl amine salt of Ethacrynic acid; (c) acidifying the t-butyl amine salt of Ethacrynic acid formed in step b) to obtain Ethacrynic acid of formula I; and (d) optionally purifying the obtained Ethacrynic acid with a solvent mixture of alkyl acetate and hydrocarbon solvent. The invention also provides crystalline t-butylamine salt of Ethacrynic acid and process thereof. Also provide compound Ethacrynic acid having a purity of greater than or equal to 99% and a composition including the compound.Type: GrantFiled: October 23, 2017Date of Patent: April 16, 2019Assignee: Strides Shasun LimitedInventors: Sankar Arjunan, Dhanapal Ramu, Sasidaran Manjiny
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Patent number: 10227359Abstract: The present disclosure relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: November 2, 2017Date of Patent: March 12, 2019Assignee: Incyte CorporationInventors: Andrew P. Combs, Richard B. Sparks
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Patent number: 10106508Abstract: The present invention relates to an N-substituted-phenyl-5-substituted-alkoxy-2,3-dihydro-[1,4]dioxane[2,3-f]quinazolin-10-amine (I) or 4-substituted-arylamino-6-substituted-alkyl-6H-[1,4]oxazino[3,2-g]quinazoline-7(8H)-one (II) type compounds, a preparation method thereof and an application thereof as an inhibitor for epidermal growth factor receptor (EGFR) (comprising some mutant forms of EGFR) to treat cancer. These compounds and salts thereof can be used to treat or prevent various cancer diseases.Type: GrantFiled: January 12, 2016Date of Patent: October 23, 2018Assignee: BEIJING SCITECH-MQ PHARMACEUTICALS LIMITEDInventors: Wang Sheng, Leifu Yang, Zhiyong Pan
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Patent number: 10106557Abstract: A preparation method for a high-purity benzoxazoleoxazine ketone compound, a crystal form thereof, and an intermediate compound for preparing a compound of formula (I), and a preparation method therefor.Type: GrantFiled: September 23, 2015Date of Patent: October 23, 2018Assignee: NORTH CHINA PHARMACEUTICAL NEW DRUG R&D CO., LTD.Inventors: Shuhui Chen, Zhaozhong Ding, Gangli Gong, Xiaobing Yan, Wei Huang, Feng Guo, Baoling Duan, Renlong Gao, Pingfan Zhou, Xinhua Lu, Guimin Dong
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Patent number: 9938294Abstract: The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: January 5, 2017Date of Patent: April 10, 2018Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr., James D. Rodgers
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Patent number: 9925141Abstract: In one aspect, a dry formulation for the effective administration of multiple medications simultaneously for one or more ailments may be provided. The dry formulations include one or more of the following actives in combination with pharmaceutically acceptable excipients or additives: a) at least one antibiotic; b) at least one anti-inflammatory steroid; and c) at least one antifungal agent.Type: GrantFiled: October 17, 2016Date of Patent: March 27, 2018Assignee: CMPD LICENSING LLCInventor: Jay Richard Ray, II
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Patent number: 9834565Abstract: The present disclosure relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: November 18, 2016Date of Patent: December 5, 2017Assignee: Incyte CorporationInventors: Andrew P. Combs, Richard B. Sparks
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Patent number: 9812648Abstract: Spirobifluroene compounds of the formula (1) which are suitable for use in electronic devices, and in particular organic electroluminescent devices, and to electronic devices that include the spirobifluorene compounds.Type: GrantFiled: January 21, 2013Date of Patent: November 7, 2017Assignee: Merck Patent GmbHInventors: Elvira Montenegro, Amir H. Parham, Philipp Stoessel, Teresa Mujica-Fernaud, Frank Voges, Arne Buesing
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Patent number: 9643982Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1-R8, A, X and n are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.Type: GrantFiled: April 18, 2014Date of Patent: May 9, 2017Assignee: MERCK SHARP & DOHME CORP.Inventors: Paul J. Coleman, Timothy J. Hartingh, Izzat T. Raheem, John Schreier, John Sisko, John Wai, Thomas H. Graham, Lihong Hu, Xuanjia Peng
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Patent number: 9624241Abstract: The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: October 26, 2015Date of Patent: April 18, 2017Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr.
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Patent number: 9548456Abstract: Disclosed are a novel organic compound and an organic light emitting diode device using the same. More particularly, a novel organic compound having electrical stability, high charge transport capability, and light emitting performance, high glass transition temperature and being capable of preventing crystallization, and an organic light emitting diode device including an organic layer including the same are disclosed.Type: GrantFiled: August 2, 2013Date of Patent: January 17, 2017Assignee: Samsung Display Co., Ltd.Inventors: Eun-Young Lee, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jun-Ha Park, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
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Patent number: 9527864Abstract: The present disclosure relates to tricyclic heterocycles of Formula I, which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: September 14, 2015Date of Patent: December 27, 2016Assignee: Incyte CorporationInventors: Andrew P. Combs, Richard B. Sparks
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Patent number: 9512142Abstract: The present invention relates to new tricyclic triazolic compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.Type: GrantFiled: April 21, 2014Date of Patent: December 6, 2016Assignee: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: José-Luís Díaz-Fernández, Carmen Almansa-Rosales, Félix Cuevas-Cordobés
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Patent number: 9416144Abstract: Disclosed are a benzoxazine oxazolidinone compound shown by a general formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, a preparation method thereof, and an application thereof in preparing a drug for treating an infectious disease and in particular, an infectious disease caused by multidrug resistant bacteria.Type: GrantFiled: December 25, 2013Date of Patent: August 16, 2016Assignees: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, ZHE JIANG JUTAI PHARMACEUTICAL CO., LTD.Inventors: Yushe Yang, Bin Guo
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Patent number: 9382265Abstract: The present invention relates to the field of a pharmaceutical compound, and more specifically, relates to a new oxazolidone compound, an enantiomer, a diastereoisomer and a raceme thereof, and a mixture thereof, and a pharmaceutically acceptable salt thereof, a preparation method thereof, an application thereof as a bioactive substance in a drug. The compound in the present invention has strong anticoagulant activity, does not affect the activity of thrombin, and can reduce the risk of hemorrhage. A pharmacokinetics experiment shows that the compound in the present invention further has good metabolic characteristics, and has a far better oral bioavailability than a positive contrastive agent rivaroxaban.Type: GrantFiled: December 30, 2013Date of Patent: July 5, 2016Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhe Jiang Jutai Pharmaceutical Co., Ltd.Inventors: Yushe Yang, Tao Xue, Shi Ding, Bin Guo
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Patent number: 9290514Abstract: The present invention relates to tricyclic heterocycles of Formula (I), which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: July 7, 2014Date of Patent: March 22, 2016Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Thomas P. Maduskuie, Jr.
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Patent number: 9227985Abstract: The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: GrantFiled: March 14, 2014Date of Patent: January 5, 2016Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, James D. Rodgers
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Patent number: 9045496Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m are defined in the specification. 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 inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3K?.Type: GrantFiled: June 24, 2014Date of Patent: June 2, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Tony Gibson, Bohan Jin, Nicholas Scorah, Qing Dong
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Publication number: 20150126502Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: January 14, 2015Publication date: May 7, 2015Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
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Patent number: 9023843Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and/or reducing the risk of microbial infections in humans and animals.Type: GrantFiled: October 15, 2010Date of Patent: May 5, 2015Assignee: Melinta Therapeutics, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Shili Chen, Marco DeVivo, Rongliang Lou, Brian T. Wimberly
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Publication number: 20150087639Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.Type: ApplicationFiled: July 18, 2013Publication date: March 26, 2015Applicant: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
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Publication number: 20150072975Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.Type: ApplicationFiled: November 18, 2014Publication date: March 12, 2015Inventors: Berangere Gaucher, JR., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin XU
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Patent number: 8969339Abstract: The present disclosure is directed to methods of identifying a compound that binds to or interacts with a protein receptor involved in bone formation. Specifically, the disclosure is directed to methods of identifying a compound that regulates a Wnt pathway in a cell by binding to or interacting with cavities in proteins such as LRP5, LRP 6 and/or frizzled receptor and interfering with receptor binding to other proteins in a Wnt pathway. The present disclosure is further directed to methods and compositions that comprise an identified compound for treating or preventing a disease in a mammal in which Wnt pathway suppression plays a role.Type: GrantFiled: November 14, 2012Date of Patent: March 3, 2015Assignee: Enzo Biochem, Inc.Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
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Publication number: 20150031652Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: August 1, 2014Publication date: January 29, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 8933222Abstract: The present invention provides methods of synthesizing oxadiazoanthracene derivatives of the formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, R, R1, R2, R3, R4 and R5 are as herein described, and methods of synthesizing precursors to these oxadiazoanthracene derivatives.Type: GrantFiled: March 5, 2014Date of Patent: January 13, 2015Assignee: TransTech Pharma, LLCInventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Thomas Scott Yokum, Kalpathy Santhosh, Mustafa Guzel, Christopher Behme, Stephen Thomas Davis
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Publication number: 20150011540Abstract: The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: ApplicationFiled: July 7, 2014Publication date: January 8, 2015Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Thomas P. Maduskuie, JR.
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Patent number: 8927541Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.Type: GrantFiled: December 17, 2010Date of Patent: January 6, 2015Assignee: Basilea Pharmaceutica AGInventors: Bérangère Gaucher, Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin Xu
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Publication number: 20140349992Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: Sunovion Pharmaceuticals Inc.Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Publication number: 20140343032Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: May 16, 2014Publication date: November 20, 2014Applicant: HOFFMANN-LA ROCHE INC.Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Buyu Kou, Gangqin Li, Xianfeng Lin, Haixia Liu, Hong Shen, Houguang Shi, Guolong Wu, Zhisen Zhang, Mingwei Zhou, Wei Zhu
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Publication number: 20140330007Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 8877945Abstract: The present invention provides redox drug derivatives. In particular, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, (3R,4R,5S)-4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid ethyl ester, (3S)-3-(aminomethyl)-5-methylhexanoic acid, (3S)-1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-?-?-diphenyl-3-pyrrolidineacetamide, (1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4-(diaminomethylideneamino)-2-hydroxy-cyclopentane-1-carboxylic acid and (2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid redox derivatives.Type: GrantFiled: May 17, 2010Date of Patent: November 4, 2014Assignee: Redx Pharma LimitedInventors: Derek Lindsay, Peter Jackson
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Publication number: 20140309219Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m are defined in the specification. 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 inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3K?.Type: ApplicationFiled: June 24, 2014Publication date: October 16, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Edcon Chang, Tony Gibson, Bohan Jin, Nicholas Scorah, Qing Dong
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Patent number: 8846908Abstract: The present disclosure relates to 2,4-pyrimidinediamines substituted with tricyclic carbamates and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, such as JAK2 or JAK3, is therapeutically useful.Type: GrantFiled: September 23, 2009Date of Patent: September 30, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Somasekhar Bhamidipati, Vadim Markovtsov
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Publication number: 20140288062Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
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Publication number: 20140275030Abstract: The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, James D. Rodgers
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Publication number: 20140275055Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan
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Publication number: 20140275056Abstract: The present invention is directed to a compound of Formula (I): The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael A. Letavic, Dale A. Rudolph