Bicyclo Ring Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.04)
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Patent number: 12077536Abstract: Disclosed herein is a compound of Formula (I) for inhibiting Bcl-2 and treating disease associated with undesirable bcl-2 activity (Bcl-2 related diseases), a method of using the compounds disclosed herein for treating dysregulated apoptotic diseases including cancers and treating autoimmune disease, and a pharmaceutical composition comprising the same.Type: GrantFiled: May 23, 2022Date of Patent: September 3, 2024Assignee: BeiGene, Ltd.Inventors: Yunhang Guo, Hai Xue, Zhiwei Wang, Hanzi Sun
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Patent number: 11932618Abstract: Disclosed are novel compounds of Chemical Formula 1, optical isomers of the compounds, and pharmaceutically acceptable salts of the compounds or the optical isomers. The compounds, isomers, and salts exhibit excellent activity as GLP-1 receptor agonists. In particular, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used as therapeutic agents for metabolic diseases. Moreover, they exhibit excellent pharmacological safety for cardiovascular systems.Type: GrantFiled: March 13, 2023Date of Patent: March 19, 2024Assignee: ILDONG PHARMACEUTICAL CO., LTD.Inventors: Hong Chul Yoon, Kyung Mi An, Myong Jae Lee, Jin Hee Lee, Jeong-geun Kim, A-rang Im, Woo Jin Jeon, Jin Ah Jeong, Jaeho Heo, Changhee Hong, Kyeojin Kim, Jung-Eun Park, Te-ik Sohn, Changmok Oh, Da Hae Hong, Sung Wook Kwon, Jung Ho Kim, Jae Eui Shin, Yeongran Yoo, Min Whan Chang, Eun Hye Jang, In-gyu Je, Ji Hye Choi, Gunhee Kim, Yearin Jun
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Patent number: 11884665Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.Type: GrantFiled: June 15, 2022Date of Patent: January 30, 2024Assignee: Incyte CorporationInventors: Taisheng Huang, Xiaozhao Wang
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Patent number: 11643403Abstract: Disclosed are novel compounds of Chemical Formula 1, optical isomers of the compounds, and pharmaceutically acceptable salts of the compounds or the optical isomers. The compounds, isomers, and salts exhibit excellent activity as GLP-1 receptor agonists. In particular, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used as therapeutic agents for metabolic diseases. Moreover, they exhibit excellent pharmacological safety for cardiovascular systems.Type: GrantFiled: November 13, 2020Date of Patent: May 9, 2023Assignee: ILDONG PHARMACEUTICAL CO., LTD.Inventors: Hong Chul Yoon, Kyung Mi An, Myong Jae Lee, Jin Hee Lee, Jeong-geun Kim, A-rang Im, Woo Jin Jeon, Jin Ah Jeong, Jaeho Heo, Changhee Hong, Kyeojin Kim, Jung-eun Park, Te-ik Sohn, Changmok Oh, Da Hae Hong, Sung Wook Kwon, Jung Ho Kim, Jae Eui Shin, Yeongran Yoo, Min Whan Chang, Eun Hye Jang, In-Gyu Je, Ji Hye Choi, Gunhee Kim, Yearin Jun
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Patent number: 11390624Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.Type: GrantFiled: January 28, 2020Date of Patent: July 19, 2022Assignee: Incyte CorporationInventors: Taisheng Huang, Xiaozhao Wang
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Patent number: 11198675Abstract: Disclosed herein, inter alia, are compositions and methods for inhibiting DNA2.Type: GrantFiled: January 13, 2020Date of Patent: December 14, 2021Assignees: City of Hope, California Institute of TechnologyInventors: Binghui Shen, Judith Campbell, Li Zheng, Hongzhi Li, David Horne, Jun Xie, Kenneth Karanja
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Patent number: 10981967Abstract: A long-acting conjugate of a triple agonist which has activities to all of glucagon, GLP-1, and GIP receptors and uses thereof.Type: GrantFiled: January 31, 2019Date of Patent: April 20, 2021Assignee: HANMI PHARM. CO., LTD.Inventors: Euh Lim Oh, Jong Suk Lee, Young Jin Park, Chang Ki Lim, Sung Youb Jung, Se Chang Kwon
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Patent number: 10945771Abstract: The present invention is directed to azabicyclo[4.1.0]heptane compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.Type: GrantFiled: June 4, 2018Date of Patent: March 16, 2021Assignee: Merck Sharp & Dohme Corp.Inventors: Dane James Clausen, James I. Fells, Joseph A. Kozlowski, Ping Liu, Robert D. Mazzola, Jr.
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Patent number: 10759798Abstract: Crystalline forms, preparation methods and pharmaceutical compositions of ABT-199 monohydrochloride and ABT-199 dihydrochloride are disclosed. Compared with known ABT-199, they have one or more improved properties. They can be used to prepare drugs for the treatment and/or prevention of one or more diseases associated with overexpression of an anti-apoptotic BCL-2 family protein.Type: GrantFiled: September 14, 2016Date of Patent: September 1, 2020Assignee: Hangzhou SoliPharma Co., Ltd.Inventors: Xiaohong Sheng, Xiaoxia Sheng, Jianfeng Zheng
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Patent number: 10513528Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare a compound of formula (I): or a salt thereof.Type: GrantFiled: February 23, 2017Date of Patent: December 24, 2019Assignee: Taxis Pharmaceuticals, Inc.Inventors: Ravi Ponnaiah, Sudhakar Sunkari, Anil Kumar Soni, Savi Rami Reddy Athunuri, Thrisulapani Korrakuti, Pullarao Seelam, Ajit K. Parhi
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Patent number: 10507201Abstract: The present invention relates to therapeutic uses of compounds of formula (I) or a pharmaceutically acceptable salt thereofType: GrantFiled: February 28, 2019Date of Patent: December 17, 2019Assignee: NOVARTIS AGInventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Diana Graus Porta, Carolina Haefliger, Bo Han, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Masato Murakami, Pierre Nimsgern, Michael Palmer, Dale Porter, Sebastien Ripoche, Can Wang, Youzhen Wang, Andreas Weiss, Jing Xiong, Xianglin Zhao
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Patent number: 10463653Abstract: The present invention relates to therapeutic uses of compounds of formula (1) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 13, 2018Date of Patent: November 5, 2019Assignee: NOVARTIS AGInventors: Lv Liao, Jing Xiong
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Patent number: 10100044Abstract: The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.Type: GrantFiled: October 20, 2014Date of Patent: October 16, 2018Assignees: Suzhou Vigonvita Life Sciences Co., Ltd., Topharman Shanghai Co., Ltd., Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Zheng Liu, Chunhui Wu, Yongjian Liu, Rongxia Zhang, Yang He, Guanghui Tian, Jingshan Shen
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Patent number: 9987272Abstract: A pyrazolopyridine compound according to Formula I, able to inhibit JAK is disclosed, as well as pharmaceutically acceptable salts, a solvate thereof, solvates of the pharmaceutically acceptable salts and biologically active metabolites thereof. The compound may be prepared as a pharmaceutical composition, and may be used for the treatment or prophylaxis of a variety of conditions in mammals including humans, and particularly, such conditions as may be associated with aberrant JAK activity, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6.Type: GrantFiled: January 25, 2016Date of Patent: June 5, 2018Assignee: GALAPAGOS NVInventors: Christel Jeanne Marie Menet, Alastair James Hodges, Huw David Vater
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Patent number: 9988381Abstract: This invention provides a class of five-member-heterocycle fused pyridine compounds as shown below in Formula (X), pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, a method of producing the same, pharmaceutical compositions containing the compound, and use of the compounds in preparing medicament for preventing and/or treating diseases and tumors associated with abnormal protein tyrosine kinase.Type: GrantFiled: June 18, 2014Date of Patent: June 5, 2018Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.Inventors: Jingkang Shen, Meiyu Geng, Jian Ding, Bing Xiong, Jing Al, Yuchi Ma, Xin Wang, Xia Peng, Yuelei Chen, Danqi Chen, Tao Meng, Lanping Ma, Yinchun Ji
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Patent number: 9802917Abstract: The present invention relates to particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide, to a process of making said particles, to pharmaceutical compositions comprising said particles and to method of treating cancers using said pharmaceutical compositions.Type: GrantFiled: March 18, 2016Date of Patent: October 31, 2017Assignee: Novartis AGInventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Bo Han, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Franck Mallet, Julie Martz, Can Wang, Jing Xiong, Xianglin Zhao
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Patent number: 9751875Abstract: The present invention discloses a class of quinine compounds and pharmaceutically acceptable salts, solvates, prodrugs or optical isomers thereof. Also disclosed in the present invention are that the above compounds have a selective antagonistic effect on the receptor subtypes of M1 and M3, but have no significant effect on M2 receptor subtype, and the above compounds are characterized by rapid action, long-lasting efficacy, and low toxic and side-effects when used to treat rhinitis, post-cold rhinitis, chronic trachitis, airway hyperresponsiveness, asthma, chronic obstructive pulmonary diseases, cough, urinary incontinence, frequent urination, unstable bladder syndrome, bladder spasms, bladder inflammation and gastrointestinal diseases such as irritable bowel syndrome, spastic colitis, as well as duodenal and gastric ulcers.Type: GrantFiled: July 11, 2014Date of Patent: September 5, 2017Assignee: Beijing Fswelcome Technology Development Co., Ltd.Inventors: Chunjing Wang, Junyi Wang, Zejun Gao
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Patent number: 9493455Abstract: The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.Type: GrantFiled: December 30, 2013Date of Patent: November 15, 2016Assignee: ORIBASE PHARMAInventors: Gwénaël Cheve, Bénédicte Dayde-Cazals, Bénédicte Fauvel, Cédric Bories, Abdelaziz Yasri
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Patent number: 9487513Abstract: The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.Type: GrantFiled: February 21, 2013Date of Patent: November 8, 2016Assignee: LABORATORIOS DE DR. ESTEVE S.A.Inventors: José Luis Diaz Fernández, Ma Rosa Cuberes Altisent
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Patent number: 9475783Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.Type: GrantFiled: March 21, 2013Date of Patent: October 25, 2016Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
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Patent number: 9447075Abstract: Pyridazine derivatives that activate the excitatory amino acid transporter 2 (EAAT2), and methods use thereof for treating or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.Type: GrantFiled: August 2, 2012Date of Patent: September 20, 2016Assignees: The Brigham and Women's Hospital, Inc., The Ohio State UniversityInventors: Gregory D. Cuny, Marcie Glicksman, Xeuchao Xing, Chien-Liang Glenn Lin
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Patent number: 9403821Abstract: A method for making the compound is set forth utilizing the starting materialType: GrantFiled: October 17, 2014Date of Patent: August 2, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H. Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
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Patent number: 9394322Abstract: A method for making the compound is set forth utilizing the starting materialType: GrantFiled: October 17, 2014Date of Patent: July 19, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
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Patent number: 9296740Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: February 22, 2013Date of Patent: March 29, 2016Assignee: ChemoCentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu, Mark M. Gleason, Yibin Zeng, Kevin Lloyd Greenman
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Patent number: 9045479Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.Type: GrantFiled: December 12, 2012Date of Patent: June 2, 2015Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ganesh Prabhu, Ashok Tehim, Vidyadhar Paradkar, Marahanakuli Prasanna Dattatreya, Nanjegowda Jagadeesh Mavinhalli
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Publication number: 20150148331Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.Type: ApplicationFiled: July 24, 2014Publication date: May 28, 2015Inventors: Esther Birtalan, Peter Hoelig, David J. Lindley, Yeshwant D. Sanzgiri, Ping Tong
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Publication number: 20150148342Abstract: The present invention relates to bicyclic 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: November 26, 2014Publication date: May 28, 2015Applicant: INCYTE CORPORATIONInventors: Eddy W. Yue, Andrew P. Combs, Brent Douty
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Publication number: 20150148330Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 16, 2015Publication date: May 28, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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Publication number: 20150141406Abstract: The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: May 31, 2013Publication date: May 21, 2015Inventors: Hiroshi Nara, Masaki Daini, Akira Kaieda, Taku Kamei, Toshihiro Imaeda, Fumiaki Kikuchi
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Publication number: 20150141403Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: December 1, 2014Publication date: May 21, 2015Inventors: Jose Maria CID-NUNEZ, Daniel OEHLRICH, Andres Avelino TRABANCO-SUAREZ, Gary John TRESADERN, Juan Antonio VEGA RAMIRO, Gregor James MACDONALD
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Publication number: 20150141435Abstract: Disclosed herein are compounds of Formula I wherein R1, R2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.Type: ApplicationFiled: January 7, 2015Publication date: May 21, 2015Inventors: Patrick ROUSSEL, Jutta HEIM, Peter SCHNEIDER, Christian BARTELS, Yaoquan LIU, Glen DALE, Daniel MILLIGAN
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Patent number: 9034876Abstract: This application describes and provides a method of treating diseases or disorders characterized by chronic systemic inflammation, such as rheumatoid arthritis, using a compound that inhibits JAK2 kinase.Type: GrantFiled: June 6, 2013Date of Patent: May 19, 2015Assignee: Cephalon, Inc.Inventors: Pawel T. Dobrzanski, Matthew M. Seavey
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Publication number: 20150133465Abstract: The invention provides compounds of formula (I): wherein R1-R3, n, and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.Type: ApplicationFiled: November 7, 2014Publication date: May 14, 2015Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Yongzheng Zhang, Malvika Kaul
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Publication number: 20150133432Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 10, 2014Publication date: May 14, 2015Inventors: Stephanie HACHTEL, Christian SCHOENAU, Matthias LOEHN, Oliver PLETTENBURG, Stefania PFEIFFER-MAREK, Alexander SCHIFFER, Holger GAUL, Aimo KANNT, Juergen DEDIO, Angela DUDDA
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Patent number: 9029373Abstract: Compounds of formula (I): wherein R2, W, A, Y, and R1 are as defined in the specification, and pharmaceutically acceptable salts thereof, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: GrantFiled: August 5, 2014Date of Patent: May 12, 2015Assignee: Chiesi Farmaceutici S.p.A.Inventors: Monique Bodil Van Niel, Nicholas Charles Ray, Andrew Peter Cridland, Christopher Hurley, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani
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Publication number: 20150126515Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.Type: ApplicationFiled: January 25, 2013Publication date: May 7, 2015Applicant: PTC Therapeutics, Inc.Inventors: Guangming Chen, Amal Dakka, Gary Mitchell Karp, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Marla L. Weetall, Ellen Welch, Xin Zhao
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Publication number: 20150126503Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as phaType: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Inventors: Matthias HOFFMANN, Georg DAHMANN, Dennis FIEGEN, Sandra HANDSCHUH, Jasna KLICIC, Guenter LINZ, Gerhard SCHAENZLE, Andreas SCHNAPP, Stephen Peter EAST, Michael Philip MAZANETZ, Robert John SCOTT, Edward Walker
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Patent number: 9023853Abstract: The present invention provides a method for treating lupus in a subject, comprising the step of administering to the subject COMPOUND A.Type: GrantFiled: June 6, 2013Date of Patent: May 5, 2015Assignee: Cephalon, Inc.Inventors: Pawel T. Dobrzanski, Matthew M. Seavey
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Patent number: 9023839Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: GrantFiled: April 22, 2014Date of Patent: May 5, 2015Assignee: IRM LLCInventors: Valentina Molteni, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
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Publication number: 20150119387Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.Type: ApplicationFiled: June 15, 2012Publication date: April 30, 2015Applicant: Curegenix Inc.Inventor: Songzhou An
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Publication number: 20150119385Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.Type: ApplicationFiled: October 24, 2014Publication date: April 30, 2015Applicant: Novartis AGInventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
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Patent number: 9018214Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: April 20, 2012Date of Patent: April 28, 2015Assignee: Astex Therapeutics LimitedInventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
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Publication number: 20150111872Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.Type: ApplicationFiled: December 17, 2014Publication date: April 23, 2015Applicant: GALAPAGOS NVInventors: Nicolas DESROY, Bertrand HECKMANN, Reginald Christophe Xavier BRYS, Agnès Marie JONCOUR, Christophe PEIXOTO, Xavier Marie BOCK
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Patent number: 9012456Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: February 22, 2013Date of Patent: April 21, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Bernd Nosse
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Publication number: 20150105380Abstract: The present invention provides methods for treating polycystic kidney disease by administering a compound or pharmaceutical composition thereof having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein.Type: ApplicationFiled: September 23, 2014Publication date: April 16, 2015Applicant: ANGION BIOMEDICA CORP.Inventors: Prakash NARAYAN, Brian HUANG, Prani PAKA, Latha PAKA, Itzhak D. GOLDBERG
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Publication number: 20150105402Abstract: A process of production of trazodone or trazodone hydrochloride that comprises: (a) preparing an organic phase comprising trazodone in at least one organic solvent; (b) preparing an aqueous phase comprising at least one basic compound; (c) mixing said aqueous phase with said organic phase; (d) heating at a temperature of at least 40° C. for at least 30 minutes; (e) recovering said trazodone; and, optionally, (f) treating said trazodone with hydrochloric acid to obtain trazodone hydrochloride. Trazodone or trazodone hydrochloride comprising less than 15 ppm of allylating substances, and a pharmaceutical composition comprising said trazodone hydrochloride.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.Inventors: Marcello MARCHETTI, Tommaso Iacoangeli, Giovanni Battista Ciottoli, Giuseppe Biondi
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Publication number: 20150105401Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.Type: ApplicationFiled: October 7, 2014Publication date: April 16, 2015Applicant: The University of RochesterInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin J. Loweth, Torsten Wiemann
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Publication number: 20150105377Abstract: The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.Type: ApplicationFiled: March 12, 2013Publication date: April 16, 2015Inventors: Joseph M. Gozgit, Victor M. Rivera, William C. Shakespeare, Xiaotian Zhu, David C. Dalgarno
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Publication number: 20150104384Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.Type: ApplicationFiled: March 1, 2013Publication date: April 16, 2015Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
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Patent number: 9006247Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: May 25, 2011Date of Patent: April 14, 2015Assignee: AbbVie Inc.Inventors: Zhi-Fu Tao, Xilu Wang, Andrew J. Souers, Nathaniel D. Catron, Gerard M. Sullivan