The Other Cyclo In The Bicyclo Ring System Is A Pyrrole Ring (including Hydrogenated) (e.g., Pyrrolo[3,2-d]pyrimidine, Etc.) Patents (Class 514/265.1)
-
Patent number: 10561659Abstract: Disclosed is a method of treating in a subject hair loss disorders that are beneficially treated by administering a JAK1 and/or JAK2 inhibitor. The method comprises administering to the subject an amount in the range of about 4 mg to about 50 mg of Compound (I), or a pharmaceutically acceptable salt thereof. This invention also provides compositions comprising Compound (I) and the use of such compositions in the described methods.Type: GrantFiled: May 4, 2017Date of Patent: February 18, 2020Assignee: Concert Pharmaceuticals, Inc.Inventors: Amanda T. Wagner, James V. Cassella, Philip B. Graham, Virginia Braman, Vinita Uttamsingh, Jana Von Hehn, Colleen E. Hamilton
-
Patent number: 10561660Abstract: The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.Type: GrantFiled: June 19, 2017Date of Patent: February 18, 2020Inventors: Simona Bindi, Davide Carenzi, Ilaria Motto, Maurizio Pulici
-
Patent number: 10555949Abstract: The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.Type: GrantFiled: April 17, 2018Date of Patent: February 11, 2020Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.Inventors: Zhaozhong Ding, Hao Wu, Fei Sun, Lifang Wu, Ling Yang
-
Patent number: 10533011Abstract: Provided are methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.Type: GrantFiled: June 30, 2016Date of Patent: January 14, 2020Assignee: ACEA THERAPEUTICS, INC.Inventors: Long Mao, Jia Liu, Yile Chen, Yuning Hua, Kongen Dai, Yimei Bao, Bojie Weng, Xiaopeng Mo, Jian Wu, Xiao Xu, Wanhong Xu, Xiaobo Wang
-
Patent number: 10512649Abstract: Disclosed are 9-deazaaadenine derivatives of the general formula (I) and pharmaceutically acceptable salts thereof, wherein A is OH or NH2, and B is H or NH2. Methods for treating, preventing and/or suppressing a Zika virus infection with the compounds disclosed are also provided. Pharmaceutical compositions comprising the disclosed compounds are also provided. Such pharmaceutical compositions may optionally contain one or more additional active agents.Type: GrantFiled: March 6, 2017Date of Patent: December 24, 2019Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pravin L. Kotian, Shanta Bantia
-
Patent number: 10493073Abstract: The present invention relates to pyrimidine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.Type: GrantFiled: July 10, 2018Date of Patent: December 3, 2019Assignee: Merck Patent GmbHInventors: Hui Qiu, Richard D. Caldwell, Lesley Liu-Bujalski
-
Patent number: 10494374Abstract: The present invention relates to methods of using compounds of Formula I, wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.Type: GrantFiled: April 5, 2019Date of Patent: December 3, 2019Assignee: CYSTIC FIBROSIS FOUNDATIONInventors: Joseph Walter Strohbach, David Christopher Limburg, John Paul Mathias, Atli Thorarensen, Rajiah Aldrin Denny, Christoph Wolfgang Zapf, Daniel Elbaum, Lori Krim Gavrin, Ivan Viktorovich Efremov
-
Patent number: 10463667Abstract: The present invention provides active metabolites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: April 25, 2017Date of Patent: November 5, 2019Assignees: INCYTE INCORPORATION, INCYTE HOLDINGS CORPORATIONInventors: James D. Rodgers, Argyrios G. Arvanitis, Jack Guoen Shi, Stacey Shepard
-
Patent number: 10457640Abstract: Provided herein are synthetic methods for the preparation of EZH2 inhibitors.Type: GrantFiled: October 18, 2017Date of Patent: October 29, 2019Assignee: Constellation Pharmaceuticals, Inc.Inventors: Rishi G. Vaswani, Michael Charles Hewitt
-
Patent number: 10449196Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.Type: GrantFiled: September 18, 2017Date of Patent: October 22, 2019Assignee: ACEA Therapeutics, Inc.Inventors: Xiao Xu, Xiaobo Wang, Long Mao, Li Zhao, Biao Xi
-
Patent number: 10442811Abstract: The present invention relates to crystalline form A of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)-benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), a method for preparing the crystalline form A, and the use thereof.Type: GrantFiled: February 4, 2017Date of Patent: October 15, 2019Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.Inventors: Zhaozhong Ding, Fei Sun, Yinghu Hu, Yilong Zhou, Zheng Wang, Rui Zhao, Ling Yang
-
Patent number: 10407430Abstract: Provided are Janus kinase 1 selective inhibitors of Formula 1 or Formula 2: wherein R1, R2, and X are as described herein. Pharmaceutical uses thereof, for example, for the treatment of a disease associated with a Janus kinase, are also provided.Type: GrantFiled: August 19, 2016Date of Patent: September 10, 2019Assignees: YANG JI CHEMICAL CO., LTD., HAN WHA PHARMA CO., LTD.Inventors: Chieyeon Chough, Sunmin Lee, Misuk Joung, Hyun Uk Jeong, Hong-sik Moon
-
Patent number: 10398685Abstract: The present disclosure describes methods of treating pancreatic cancer and limiting over-expression of oncogenes, activating tumor suppressor genes or regulating signaling proteins in patients comprising administering compounds and pharmaceutical combinations as described herein.Type: GrantFiled: February 4, 2019Date of Patent: September 3, 2019Assignee: ChemoCentryx, Inc.Inventors: Petrus Bekker, Shichang Miao, Israel Charo, Tom Schall
-
Patent number: 10385056Abstract: The invention relates to a 4-substituted pyrrolo[2,3-d]pyrimidine compound and the use thereof in preparing medications for treating JAK-targeted diseases such as rheumatoid, immune system diseases, and tumor. The 4-substituted pyrrolo[2,3-d]pyrimidine compound of the invention is as shown in chemical formula I. The activity experimental results of the invention show that the new compound has obvious effect and activity in inhibition of Janus kinases, JAK-STAT, cell proliferation of human lymphocytoma, and rheumatoid arthritis.Type: GrantFiled: March 24, 2015Date of Patent: August 20, 2019Assignee: JIANGSU CAREFREE PHARMACEUTICAL CO., LTDInventors: Yinlin Qin, Mei Su, Shousheng Yan, Xianzhi Wu, Tao Chen, Jianhua Jiang
-
Patent number: 10385064Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.Type: GrantFiled: July 25, 2017Date of Patent: August 20, 2019Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
-
Patent number: 10377773Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, X1, X2, X3, n, and m are described herein.Type: GrantFiled: February 27, 2018Date of Patent: August 13, 2019Assignee: FORMA Therapeutics, Inc.Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell
-
Patent number: 10336750Abstract: The present disclosure provides compositions and methods for treating ocular disorders in mammals especially in and not limited to humans and mice. The present disclosure further provides methods of treating cancer and appetite suppression using the compositions which are novel small molecule inhibitors of CaMKK2. In addition, these derived compositions can regulate non-ocular disorders, such as cancer and appetite suppression by modulating and inhibiting CaMKK2 and the regulation of the macrophage mediated diseases.Type: GrantFiled: December 20, 2017Date of Patent: July 2, 2019Assignee: Duke UniversityInventors: Scott W. Cousins, David M. Gooden, Priyatham S. Mettu
-
Patent number: 10336763Abstract: The present invention relates to crystal forms B, C and D of Ribociclib succinate salt and derivatives thereof, and their preparation method and composition. The crystal forms B, C and D of Ribociclib succinate salts are obtained by adding 7-cyclopentyl-N,N-dimethyl-2-(5-(piperain-1-yl)pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide solution into succinic acid solution for reaction, stirring the solution under high temperature, filtering the solution after cooling off.Type: GrantFiled: August 3, 2018Date of Patent: July 2, 2019Assignee: CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO. LTD.Inventors: Satyanarayana Kamani, Tzu-Chiang Lu, Hsin-Yun Chang, Chin-Cheng Mai
-
Patent number: 10301315Abstract: The present invention relates to compounds of Formula I, wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.Type: GrantFiled: November 17, 2017Date of Patent: May 28, 2019Assignee: CYSTIC FIBROSIS FOUNDATION THERAPEUTICS, INC.Inventors: Joseph Walter Strohbach, David Christopher Limburg, John Paul Mathias, Atli Thorarensen, Rajiah Aldrin Denny, Christoph Wolfgang Zapf, Daniel Elbaum, Lori Krim Gavrin, Ivan Viktorovich Efremov
-
Patent number: 10251888Abstract: The present disclosure describes methods of treating pancreatic cancer and limiting over-expression of oncogenes, activating tumor suppressor genes or regulating signaling proteins in patients comprising administering compounds and pharmaceutical combinations as described herein.Type: GrantFiled: June 13, 2017Date of Patent: April 9, 2019Assignee: ChemoCentryx, Inc.Inventors: Petrus Bekker, Shichang Miao, Israel Charo, Tom Schall
-
Patent number: 10196390Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.Type: GrantFiled: March 13, 2017Date of Patent: February 5, 2019Assignee: Nimbus Lakshmi, Inc.Inventors: Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren
-
Patent number: 10189850Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: GrantFiled: March 12, 2018Date of Patent: January 29, 2019Assignee: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
-
Patent number: 10189849Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: GrantFiled: March 12, 2018Date of Patent: January 29, 2019Assignee: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
-
Patent number: 10189851Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: GrantFiled: March 12, 2018Date of Patent: January 29, 2019Assignee: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
-
Patent number: 10174056Abstract: A compound having the structure of below Formula(I), or pharmaceutically acceptable salts thereof, are useful as Janus kinase inhibitors, wherein R1 and L1 are as herein described.Type: GrantFiled: May 26, 2016Date of Patent: January 8, 2019Assignee: WUXI FORTUNE PHARMACEUTICAL CO., LTDInventors: Hao Wu, Weiwei Mao, Yiqiang Huang, Lili Fan, Shuhui Chen
-
Patent number: 10150770Abstract: A crystal form I of a Janus Kinase (JAK) inhibitor (3aR,5s,6aS)—N-(3-methoxyl-1,2,4-thiadiazole-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate of formula (I) is provided. Also provided is a method of preparing the crystal form I of the JAK inhibitor of formula (I). The preparation method includes crystallizing any crystal form or amorphous compound solid of formula (I) in a single organic solvent to obtain the form I crystal. The crystal form I has excellent crystal stability and chemical stability. Additionally, the crystal solvent used to produce the crystal form I has low toxicity and a relatively low content of residual solvent, making the compound better suited for clinical treatment.Type: GrantFiled: September 9, 2015Date of Patent: December 11, 2018Assignee: Jiangsu Hengrui Medicine Co., Ltd.Inventors: Piaoyang Sun, Guaili Wu, Xiaohui Gao, Yongjiang Chen, Lingjia Shen
-
Patent number: 10118928Abstract: Methods of treating infections due to Helicobacter pylori (H. pylori), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering inhibitors of H.Type: GrantFiled: February 6, 2015Date of Patent: November 6, 2018Assignees: Albert Einstein College of Medicine, Inc., Victoria Link LimitedInventors: Vern L. Schramm, Keith Clinch, Shivali Ashwin Gulab
-
Patent number: 10072012Abstract: The present invention provides process for preparing crystalline Pemetrexed dipotassium (I) Form-SP9 characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2?° peaks selected from the XRPD peak set of 5.0, 12.5, 17.2, 20.8, 22.4, 25.7, 26.9 and 27.9±0.2 2?°. The invention also provides process for preparing its pharmaceutical composition thereof, which may be useful for anti-cancer treatment.Type: GrantFiled: November 11, 2014Date of Patent: September 11, 2018Assignee: Shilpa Mecicare LimitedInventors: Bhagat Raj Pipal, Venkata Reddy Gayam, Akshay Kant Chaturvedi
-
Patent number: 10023577Abstract: A crystal form of JAK kinase inhibitor bisulfate and a preparation method thereof are provided. In particular, a type II crystal of (3aR,5s,6aS)—N-(3-methoxyl-1,2,4-thiadiazole-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate and a preparation method thereof are described. The preparation method includes steps of crystallizing any solid crystal form or amorphous compound of formula (I) in a single organic solvent or a mixed organic solvent to obtain a type II crystal form of the compound of formula (I). The type II crystal form of the compound of formula (I) obtained by the described methods has good crystal stability and chemical stability. In addition, the solvent used for crystallization has low toxicity and residue, which is better suited for use in clinical treatment.Type: GrantFiled: October 9, 2015Date of Patent: July 17, 2018Assignee: JIANGSU HENGRUI CO., LTD.Inventors: Piaoyang Sun, Guaili Wu, Quanliang Zhang, Yongjiang Chen, Lingjia Shen
-
Patent number: 10016430Abstract: There are disclosed certain 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one compounds of formula (I), and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions.Type: GrantFiled: March 9, 2017Date of Patent: July 10, 2018Assignee: AstraZeneca ABInventors: Tord Bertil Inghardt, Petra Johannesson, Ulrik Jurva, Erik Michaelsson, Eva-Lotte Lindstedt-Alstermark, Nicholas Tomkinson, Jeffrey Paul Stonehouse, Li-Ming Gan
-
Patent number: 9975907Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: GrantFiled: July 27, 2016Date of Patent: May 22, 2018Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Yun-Long Li, Brian W. Metcalf, Andrew P. Combs
-
Patent number: 9968608Abstract: A pharmaceutical composition of Pemetrexed represented by formula (I), which is a liquid ready to use solution formulation or a lyophilized pharmaceutical composition for parenteral administration comprising a pharmaceutically acceptable organic amine, an inert gas and optionally containing at least one or more pharmaceutically acceptable excipients. Also provided are processes for preparation of the ready to use solution formulation or lyophilized pharmaceutical composition of the present invention.Type: GrantFiled: July 1, 2016Date of Patent: May 15, 2018Assignee: Fresenius Kabi Oncology LimitedInventors: Dhiraj Khattar, Rajesh Khanna, Mukti Yadav, Krishanu Burman
-
Patent number: 9962388Abstract: The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.Type: GrantFiled: August 14, 2015Date of Patent: May 8, 2018Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.Inventors: Zhaozhong Ding, Hao Wu, Fei Sun, Lifang Wu, Ling Yang
-
Patent number: 9957276Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: GrantFiled: November 10, 2016Date of Patent: May 1, 2018Assignee: GI Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
-
Patent number: 9937183Abstract: Methods and compounds for treating, preventing, reducing the risk of and/or delaying the onset of a microbial infection in a subject are disclosed herein, wherein the microbial infection is caused by one or more microorganisms (e.g., one or more bacteria) which can be used as a biological weapon, such as Bacillus anthracis, Franciscella tularensis, Yersinia pestis, Burkholderia mallei, and Burkholderia pseudomallei. Also disclosed are pharmaceutical compositions or kits for treating, preventing, reducing the risk of and/or delaying the onset of a microbial infection.Type: GrantFiled: September 9, 2014Date of Patent: April 10, 2018Assignee: Melinta Therapeutics, Inc.Inventors: Zoltan F. Kanyo, Ashoke Bhattacharjee
-
Patent number: 9879005Abstract: The present disclosure provides compositions and methods for treating ocular disorders in mammals especially in and not limited to humans and mice. The present disclosure further provides methods of treating cancer and appetite suppression using the compositions which are novel small molecule inhibitors of CaMKK2. In addition, these derived compositions can regulate non-ocular disorders, such as cancer and appetite suppression by modulating and inhibiting CaMKK2 and the regulation of the macrophage mediated diseases.Type: GrantFiled: February 5, 2016Date of Patent: January 30, 2018Assignee: Duke UniversityInventors: Scott W. Cousins, David M. Gooden, Priyatham S. Mettu
-
Patent number: 9867826Abstract: The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: GrantFiled: August 24, 2016Date of Patent: January 16, 2018Assignee: Merck Patent GmbHInventors: Ruoxi Lan, Xiaoling Chen, Yufang Xiao, Bayard R. Huck, Andreas Goutopoulos
-
Patent number: 9855246Abstract: The present invention relates to stable, preservative- and antioxidant-free liquid formulations of phenylephrine and ketorolac for injection.Type: GrantFiled: September 28, 2016Date of Patent: January 2, 2018Assignee: Omeros CorporationInventors: Gregory A. Demopulos, Hui-rong Shen, Clark E. Tedford
-
Patent number: 9856261Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: August 5, 2016Date of Patent: January 2, 2018Assignee: Auspex Pharmaceuticals, Inc.Inventors: Tadimeti Rao, Chengzhi Zhang
-
Patent number: 9833448Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 14, 2016Date of Patent: December 5, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
-
Patent number: 9815841Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).Type: GrantFiled: January 28, 2015Date of Patent: November 14, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Xiao Ding, Qian Liu, Kai Long, Yingxia Sang, Luigi Piero Stasi, Zehong Wan, Qiongfeng Xu, Colin Michael Edge
-
Patent number: 9795606Abstract: Compounds of Formula I: wherein: one of X and X? is N and the other of X and X? is C, are described, along with compositions containing the same and methods of use thereof in the treatment of cancer.Type: GrantFiled: February 3, 2016Date of Patent: October 24, 2017Assignee: The University of North Carolina at Chapel HillInventors: Xiaodong Wang, Jing Liu, Weihe Zhang, Stephen Frye, Dmitri Kireev
-
Patent number: 9789113Abstract: The present application provides pharmaceutical compositions derived from pemetrexed dipotassium Nonahydrate and its process thereof. The present application also provides a method of treating cancer by administering intravenously the reconstituted lyophilized compositions into a patient in need thereof.Type: GrantFiled: June 23, 2015Date of Patent: October 17, 2017Assignee: SHILPA MEDICARE LIMITEDInventors: Pradeep Shivakumar, Akshay Kant Chaturvedi
-
Patent number: 9682066Abstract: The present disclosure relates to the field of cancer treatment, and more specifically to the field of treatment of primary malignant brain tumors. Provided herein are methods of treating primary brain tumors, including gliomas, by administering to a patient in need thereof a therapeutically effective amount of the aromatase inhibitor letrozole.Type: GrantFiled: December 4, 2013Date of Patent: June 20, 2017Assignee: University of CincinnatiInventors: Pankaj Desai, Nimita Dave
-
Patent number: 9668959Abstract: The present invention relates to compositions and methods for modulating melanin production, secretion and/or accumulation in human skin cells. In particular, the present invention relates to the use of A3 adenosine receptor antagonists in compositions and methods for the treatment and amelioration of hyper-pigmentation conditions and for the lightening of skin, and to the use of A3 adenosine receptor agonists in compositions and methods for the treatment and amelioration of hypo-pigmentation conditions and for the tanning of skin.Type: GrantFiled: November 13, 2015Date of Patent: June 6, 2017Assignee: ORADIN PHARMACEUTICAL LTD.Inventors: Lea Levana Madi, Rafi Korenstein
-
Patent number: 9642855Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.Type: GrantFiled: August 31, 2015Date of Patent: May 9, 2017Assignee: Pfizer Inc.Inventors: Paul Galatsis, Matthew Merrill Hayward, Bethany Lyn Kormos, Travis T. Wager, Lei Zhang, Antonia Friederike Stepan, Jaclyn Louise Henderson, Ravi G. Kurumbail, Patrick Robert Verhoest
-
Patent number: 9630970Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.Type: GrantFiled: April 13, 2016Date of Patent: April 25, 2017Assignee: Nimbus Lakshmi, Inc.Inventors: Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren
-
Patent number: 9624178Abstract: The present invention provides substituted cyclopenta and cyclopentyl pyrimidine bicyclic compounds of Formula III, and 5,6-saturated and unsaturated and pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: GrantFiled: April 3, 2014Date of Patent: April 18, 2017Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
-
Patent number: 9616063Abstract: There are disclosed certain 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one compounds of formula (I), and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions.Type: GrantFiled: November 25, 2015Date of Patent: April 11, 2017Assignee: AstraZeneca ABInventors: Tord Bertil Inghardt, Petra Johannesson, Ulrik Jurva, Eva-Lotte Lindstedt-Alstermark, Nicholas Tomkinson, Jeffrey Paul Stonehouse
-
Patent number: 9585895Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.Type: GrantFiled: November 19, 2015Date of Patent: March 7, 2017Assignee: Omeros CorporationInventors: Gregory A. Demopulos, Pamela Pierce Palmer, Jeffrey M. Herz