Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 546/121)
-
Patent number: 11633492Abstract: The compound of formula (II) is an advantageous intermediate for improving the process of synthesizing the linker-drug vc-seco-DUBA, as well as for the overall process for preparing an antibody-drug conjugate comprising the vc-seco-DUBA linker-drug. The methods of making the compound of formula (II) can include recovery of the compound as a solid, such as via crystallization, in high yields and purity.Type: GrantFiled: November 22, 2018Date of Patent: April 25, 2023Assignee: Byondis B.V.Inventors: Vladimir Janousek, Martin Kas
-
Patent number: 11459338Abstract: The compounds of Formula I, Formula Ia, and Formula Ib are described herein along with their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These compounds inhibit PRMT5 and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, schizophrenia, Alzheimer's disease, Parkinson's disease and the like.Type: GrantFiled: November 23, 2018Date of Patent: October 4, 2022Assignee: JUBILANT EPISCRIBE LLCInventors: Saravanan Vadivelu, Sridharan Rajagopal, Raghunadha Reddy Burri, Shivani Garapaty, Dhanalakshmi Sivanandhan, Manish Kumar Thakur, Tamizharasan Natarajan, Indu N Swamy, Nagendra Nagaraju, Subramaniam Kanagaraj, Zainuddin Mohd, Sayantani Sarkar, Swapan Kumar Samanta, Hariprakash
-
Patent number: 11434244Abstract: The present invention features novel peripherally-restricted non-benzodiazipene analogs with reduced blood brain barrier permeability and methods of use thereof for reducing tactile dysfunction, social impairment, and anxiety in a subject diagnosed with Autism Spectrum Disorder, Rett syndrome, Phelan McDermid syndrome, or Fragile X syndrome, or for treating touch over-reactivity, pain, or mechanical allodynia.Type: GrantFiled: May 29, 2019Date of Patent: September 6, 2022Assignee: President and Fellows of Harvard CollegeInventors: David D. Ginty, Lauren L. Orefice, Jinbo Lee
-
Patent number: 11261188Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. For example, such compounds include those having the structure: or pharmaceutically acceptable salts thereof. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel, including Dravet syndrome or epilepsy, using such compounds are also provided herein.Type: GrantFiled: November 28, 2017Date of Patent: March 1, 2022Assignee: PRAXIS PRECISION MEDICINES, INC.Inventors: Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron
-
Patent number: 11208417Abstract: The present invention provides a simple process of preparing avibactam. Piperidine-5-one-2S-carboxylate II as the raw material is subjected to condensation reaction with O-protecting hydroxylamine hydrochloride; the resulting compound is subjected to reduction and chiral resolution to obtain 5R-substituted oxyaminopiperidine-2S-carboxylic acid V in a basic condition; then, the compound of formula V is subjected to urea cyclization, acyl chlorination, and amidation with phosgene, solid phosgene, or diphosgene in a “one-pot” process, and then subjected to deprotection, sulfation, and tetrabutylammonium salt formation reaction to obtain (2S,5R)-2-carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl]oxy}sulfonyl tetra-n-butyl ammonium salt VII, and finally, the compound of formula VII is subjected to ion exchange to obtain avibactam I.Type: GrantFiled: March 6, 2018Date of Patent: December 28, 2021Assignee: XINFA PHARMACEUTICAL CO., LTDInventors: Yuxin Qi, Baolin Wang, Xin Xu, Lizhu Ju, Xinfa Li
-
Patent number: 11174256Abstract: The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.Type: GrantFiled: October 29, 2019Date of Patent: November 16, 2021Assignee: Gilead Sciences, Inc.Inventors: Peter A. Blomgren, Taryn Campbell, Jayaraman Chandrasekhar, Christopher T. Clark, Julian A. Codelli, Kevin S. Currie, Jeffrey E. Kropf, Yasamin Moazami, Nicole Nava, Leena Patel, Stephane Perreault, Jason K. Perry, Kassandra F. Sedillo, Natalie Seeger, Kirk L. Stevens, Jennifer Anne Treiberg, Suet C. Yeung, Zhongdong Zhao
-
Patent number: 11142499Abstract: The present application relates to methods of preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylic acid or its derivatives in an environment-friendly way. The method uses L-glutamic acid as a starting material, which is first subjected to esterification reaction in the presence of an acidic reagent, and then reacted successively with 2-haloacetate and N-protecting agent, or with N-protecting agent and 2-haloacetate under a basic condition to obtain compound IV; then, the obtained compound IV is subjected to intramolecular condensation into a ring under the action of a strong base to obtain N-protecting group piperidine-5-one-2S-carboxylate (V).Type: GrantFiled: March 6, 2018Date of Patent: October 12, 2021Assignee: XINFA PHARMACEUTICAL CO., LTDInventors: Yuxin Qi, Xinfa Li, Xin Xu, Baolin Wang, Hu Qu, Shungen Xie
-
Patent number: 11053237Abstract: The application includes a description of novel intermediates, of new manufacturing steps resulting in a novel and improved process for producing the intermediates and the final compounds, i.e., 6-alkynyl-pyridine derivatives. The intermediates of the invention are useful to produce 6-alkynyl-pyridine derivatives, which compounds are useful for the treatment of cancer.Type: GrantFiled: May 17, 2017Date of Patent: July 6, 2021Assignee: Boehringer Ingelheim International GmbHInventors: Guanghua Lu, Guenther Huchler, Thomas Krueger, Michael Pangerl, Marco Santagostino, Jean-Nicolas Desrosiers
-
Patent number: 10913737Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to imidazopyridine compounds, synthesis thereof, and methods of using same. Disclosed herein are various imidazo[1,2-a]pyhdine compounds and methods of using the novel compounds to treat or prevent tuberculosis in a subject or to inhibit fungal growth on plant species. Other embodiments include methods of synthesizing imidazo[1,2-a]pyridine compounds, such as the disclosed imidazo[1,2-a]pyridine compounds.Type: GrantFiled: February 5, 2018Date of Patent: February 9, 2021Assignee: UNIVERSITY OF NOTRE DAME DU LACInventors: Marvin J. Miller, Garrett C. Moraski, Lowell D. Markley, George E. Davis
-
Patent number: 10913738Abstract: Compounds having formula (I) (IX), and enantiomers, and diastereomers, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).Type: GrantFiled: February 12, 2018Date of Patent: February 9, 2021Assignee: Bristol-Myers Squibb CompanyInventors: Junqing Guo, Amy C. Hart, John E. Macor, Michael E. Mertzman, William J. Pitts, Steven H. Spergel, Scott Hunter Watterson, Murugaiah Andappan Murugaiah Subbaiah, Jie Chen, Carolyn Diane Dzierba, Guanglin Luo, Jianliang Shi, Sing-Yuen Sit
-
Patent number: 10781193Abstract: The present disclosure provides a reaction of a chlorine-containing compound using a flow reactor which is less restricted by a solvent to be used. In the present disclosure, an organic compound is produced by supplying a reaction substrate having at least one functional group which can react with chlorine and is selected from the group consisting of hydroxy group, a thiol group, an amino group, a carboxyl group, a thiocarboxyl group, and an acid amide group, and a chlorine-containing compound to a flow reactor together with a trialkyl amine having 9 to 40 carbon atoms and an organic solvent, and allowing the reaction substrate and the chlorine-containing compound to react with each other.Type: GrantFiled: January 10, 2019Date of Patent: September 22, 2020Assignee: KANEKA CORPORATIONInventors: Hiroaki Yasukouchi, Masaru Mitsuda, Akira Nishiyama, Makoto Funabashi
-
Patent number: 10745400Abstract: Provided herein are substituted imidazo[1,2-a]pyridines useful as inhibitors of BMP signaling. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted imidazo[1,2-a]pyridines.Type: GrantFiled: March 14, 2019Date of Patent: August 18, 2020Assignees: Vanderbuilt University, La Jolla Pharmaceuticals CompanyInventors: Corey R. Hopkins, Matthew Ritter, Charles C. Hong, Anish Vadukoot, Darren W. Engers, Craig W. Lindsley
-
Patent number: 10662190Abstract: It relates to improved processes of preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylate and oxalate thereof. In the present invention, L-glutamic acid or L-glutamic acid sodium salt as the starting material is reacted with chloroactic acid under an alkaline condition via a substitution reaction to obtain compound III; then, compound III is reacted with alcohol in the presence of acid reagent via esterification reaction to obtain compound IV; under the action of strong base, compound IV is subjected to intramolecular condensation into ring, hydrolysis-decarboxylation, and esterification to obtain compound V; compound V is condensed with benzyloxy amine hydrochloride salt in the presence of alkaline to obtain compound VI; compound VI is subjected to reduction and chiral resolution to obtain 5R-[(benzyloxy) amino] piperidine-2S-carboxylate oxalate (IIb) which is then neutralized to obtain 5R-[(benzyloxy) amino] piperidine-2S-carboxylate (IIa).Type: GrantFiled: March 2, 2018Date of Patent: May 26, 2020Assignee: XINFA PHARMACEUTICAL CO., LTDInventors: Baolin Wang, Yuxin Qi, Yinlong Zhao, Yuqi Teng, Jun Chen, Lizhu Ju, Xinfa Li
-
Patent number: 10618876Abstract: Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.Type: GrantFiled: September 21, 2018Date of Patent: April 14, 2020Assignees: OP BIO FACTORY CO., LTD., SEED RESEARCH INSTITUTE CO., LTD.Inventors: Teruhiko Ishikawa, Morita Iwami
-
Patent number: 10501459Abstract: This application relates to substituted imidazopyridines, compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to substituted imidazopyridines of Formula I and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.Type: GrantFiled: October 20, 2016Date of Patent: December 10, 2019Assignee: Neomed InstituteInventors: Mehrnaz Pourashraf, Marc-Andre Beaulieu, Stephen Claridge, Malken Bayrakdarian, Shawn Johnstone, Jeffrey S. Albert, Andrew Griffin
-
Patent number: 10426135Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.Type: GrantFiled: February 6, 2019Date of Patent: October 1, 2019Assignee: Pfizer Inc.Inventors: Mark Edward Schnute, Andrew Christopher Flick, Peter Jones, Neelu Kaila, Scot Richard Mente, John David Trzupek, Michael L. Vazquez, Goran Mattias Wennerstal, Li Xing, Edouard Zamaratski, Liying Zhang, Rayomand Jal Unwalla
-
Patent number: 10399971Abstract: The invention discloses a class of compounds for treating or preventing hyperuricemia or gout, which is a compound shown in general formula (I) or a pharmaceutically acceptable salt. These compounds and their pharmaceutically acceptable salts in the invention are useful for the promotion of uric acid excretion to treat or prevent hyperuricemia or gout.Type: GrantFiled: September 8, 2016Date of Patent: September 3, 2019Assignee: JIANGSU ATOM BIOSCIENCE AND PHARMACEUTICAL CO., LTD.Inventors: Dongfang Shi, Changjin Fu, Xi Cheng, Jianghua Zhu, Jie Wen, Jie Gu
-
Patent number: 10307748Abstract: A highly pure optically active proton pump inhibitor compound can be produced safely and inexpensively in a high yield and enantioselectivity by a method of producing an optically active sulfoxide of Formula 2 or a salt thereof, comprising oxidizing a sulfide of Formula 1 or a salt thereof with hydrogen peroxide using an iron salt in the presence of a chiral ligand of Formula 3; wherein A is CH or N; R1 is hydrogen atom, an alkyl optionally substituted by halogen(s), or an alkoxy optionally substituted by halogen(s); one to three R2 may exist, and each of R2 is independently an alkyl, a dialkylamino, or an alkoxy optionally substituted by halogen(s) or alkoxy(s); each of R3 is independently hydrogen atom, a halogen, cyano or the like; R4 is a tertiary alkyl; and * and ** represent respectively R configuration or S configuration.Type: GrantFiled: December 25, 2015Date of Patent: June 4, 2019Assignee: THE UNIVERSITY OF TOKYOInventors: Eiichi Nakamura, Laurean Ilies, Yoji Oderaotoshi, Takuhiro Izumi, Shigenobu Nishiguchi
-
Patent number: 10053460Abstract: The present invention relates to processes for preparing compounds of Formula I. Such compounds include interme-diates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1 ]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 30, 2015Date of Patent: August 21, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Zhijian Liu, Nobuyoshi Yasuda, Lu Yang, Artis Klapars, Kevin R. Campos, Mikhail Reibarkh
-
Patent number: 9980948Abstract: Disclosed is a compound which is useful as an AMPK activator.Type: GrantFiled: August 26, 2015Date of Patent: May 29, 2018Assignee: SHIONOGI & CO., LTD.Inventors: Yuusuke Tamura, Yu Hinata, Eiichi Kojima, Hiroki Ozasa
-
Patent number: 9908876Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to imidazopyridine compounds, synthesis thereof, and methods of using same. Disclosed herein are various imidazo[1,2-a]pyhdine compounds and methods of using the novel compounds to treat or prevent tuberculosis in a subject or to inhibit fungal growth on plant species. Other embodiments include methods of synthesizing imidazo[1,2-a]pyridine compounds, such as the disclosed imidazo[1,2-a]pyridine compounds.Type: GrantFiled: February 29, 2016Date of Patent: March 6, 2018Assignee: UNIVERSITY OF NOTRE DAME DU LACInventors: Marvin J. Miller, Garrett C. Moraski, Lowell D. Markley, George E. Davis
-
Patent number: 9890159Abstract: The present invention relates to a process comprising converting a compound of formula (I) into a compound of formula (II) by reaction with an organolithium reagent, which compound can be further converted into duocarmycin analogs consisting of a DNA-alkylating and a DNA-binding part, and still further into corresponding antibody-drug conjugates.Type: GrantFiled: June 5, 2014Date of Patent: February 13, 2018Assignee: Synthon Biopharmaceuticals B.V.Inventors: Tijl Huijbregts, Ronald Christiaan Elgersma, Patrick Henry Beusker, Johannes Albertus Frederikus Joosten, Rudy Gerardus Elisabeth Coumans, Henri Johannes Spijker, Wiro Menge, Franciscus Marinus Hendrikus De Groot
-
Patent number: 9862716Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.Type: GrantFiled: March 23, 2015Date of Patent: January 9, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi-Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Keith P. Moore, Ping Liu, Harold B. Wood, Chun Sing Li, Qinghua Mao, Douglas C. Beshore
-
Patent number: 9861620Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.Type: GrantFiled: September 26, 2014Date of Patent: January 9, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Tao Yu, Yonglian Zhang, Sherman Tim Waddell, Andrew Stamford, John S. Wai, Paul J. Coleman, John M. Sanders, Ronald Ferguson, Thomas H. Graham, Hong Li
-
Patent number: 9834557Abstract: A process for preparation of (2S, 5R)-7-oxo-6-sulphooxy-2-[((3R)-piperidine-3-carbonyl)-hydrazino carbonyl]-1,6-diaza-bicyclo[3.2.1]octane is disclosed.Type: GrantFiled: March 29, 2017Date of Patent: December 5, 2017Assignee: WOCKHARDT LIMITEDInventors: Sanjeev Joshi, Karuna Suresh Wankhede, Sunil Bhaginath Jadhav, Shivaji Sampatrao Pawar, Vinod Kashinath Ahirrao, Satish Bhawsar, Prasad Keshav Deshpande, Ravindra Dattatraya Yeole, Mahesh Vithalbhai Patel
-
Patent number: 9790223Abstract: A process for preparation of a compound of Formula (I) is disclosed.Type: GrantFiled: March 12, 2015Date of Patent: October 17, 2017Assignee: WOCKHARDT LIMITEDInventors: Vijay Prakash Chavan, Karuna Suresh Wankhede, Vikas Vithalrao Deshmukh, Satish Bhavsar, Kiran Ramchandra Patil, Ravindra Dattatraya Yeole, Prasad Keshav Deshpande, Mahesh Vithalbhai Patel
-
Patent number: 9688677Abstract: A process for preparation of a compound of Formula (I) is disclosed.Type: GrantFiled: March 12, 2015Date of Patent: June 27, 2017Assignee: WOCKHARDT LIMITEDInventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Mohammad Usman Shaikh, Mahesh Vithalbhai Patel
-
Patent number: 9676777Abstract: An optically active (2S,5R)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid compound defined by the following formula (F): wherein R1 represents CO2R, CO2M, or CONH2, wherein R represents an allyl group or a benzyl group, and M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.Type: GrantFiled: January 27, 2016Date of Patent: June 13, 2017Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Takao Abe, Masayuki Okue, Yoshiaki Sakamaki
-
Patent number: 9670201Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.Type: GrantFiled: September 24, 2015Date of Patent: June 6, 2017Assignee: Pfizer Inc.Inventors: Mark Edward Schnute, Andrew Christopher Flick, Peter Jones, Neelu Kaila, Scot Richard Mente, John David Trzupek, Michael L. Vazquez, Göran Mattias Wennerstål, Li Xing, Edouard Zamaratski, Liying Zhang
-
Patent number: 9670204Abstract: 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: GrantFiled: December 22, 2015Date of Patent: June 6, 2017Assignee: GALAPAGOS NVInventors: Nicolas Desroy, Bertrand Heckmann, Reginald Christophe Xavier Brys, Agnès Marie Joncour, Christophe Peixoto, Xavier Marie Bock
-
Patent number: 9670207Abstract: 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: May 25, 2016Date of Patent: June 6, 2017Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
-
Patent number: 9663518Abstract: A process for preparation of a compound of Formula (I) is disclosed.Type: GrantFiled: February 2, 2015Date of Patent: May 30, 2017Assignee: WOCKHARDT LIMITEDInventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Bharat Dond, Mahesh Vithalbhai Patel
-
Patent number: 9580424Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.Type: GrantFiled: May 13, 2015Date of Patent: February 28, 2017Assignee: Forest Laboratories Holdings LimitedInventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
-
Patent number: 9556174Abstract: A process for preparation of (2S, 5R)-Sulfuric acid mono-{[(4-aminopiperidin-4-yl) carbonyl]-7-oxo-1,6-diaza-bicyclo[3.2.1]-oct-6-yl} ester is disclosed which comprises reacting a compound of Formula (II) with a compound of Formula (III) to obtain a compound of Formula (IV).Type: GrantFiled: October 12, 2013Date of Patent: January 31, 2017Assignee: WOCKHARDT LIMITEDInventors: Karuna Suresh Wankhede, Mahesh Manikrao Surwase, Satish Bhawsar, Prasad Keshav Deshpande, Ravindra Dattatraya Yeole, Mahesh Vithalbhai Patel
-
Patent number: 9550772Abstract: 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: January 24, 2017Assignee: ORIBASE PHARMAInventors: Gwénaël Cheve, Bénédicte Dayde-Cazals, Bénédicte Fauvel, Cédric Bories, Abdelaziz Yasri
-
Patent number: 9518040Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.Type: GrantFiled: August 24, 2015Date of Patent: December 13, 2016Assignee: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
-
Patent number: 9447093Abstract: The present invention discloses compositions of novel DYRK1A protein inhibitors based on a 3,5-diarylazaindole motif and their preparation and use as medications in the treatment of cognitive disorders associated with dysfunction of DYRK1A protein, with Down's syndrome and with Alzheimer's disease.Type: GrantFiled: December 18, 2013Date of Patent: September 20, 2016Assignees: Centre National De La Recherche Scientifique (CNRS), Universite de Reims Champagne-Ardenne, Universite Paris Diderot Paris 7Inventors: Robert Dobb, Kevin Cariou, Stephanie Gourdain, Jean Maurice Delabar, Nathalie Janel, Fernando Rodrigues Lima, Julien Dairou, Clement Denhez
-
Patent number: 9402833Abstract: 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: May 29, 2015Date of Patent: August 2, 2016Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
-
Patent number: 9403820Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3K activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3K activity, are described herein.Type: GrantFiled: November 12, 2012Date of Patent: August 2, 2016Assignees: Intellikine LLC, Sigma-Aldrich Company LimitedInventors: Pingda Ren, Michael Martin, Christopher Peter Worrall, Susanna del Rio Gancedo
-
Patent number: 9387204Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: GrantFiled: November 26, 2013Date of Patent: July 12, 2016Assignee: Bayer Intellectual Property GmbHInventors: Swen Hölder, Armin Zülch, Thomas Bär, Thomas Maier, Astrid Zimmermann, Thomas Beckers, Volker Gekeler, Hemant Joshi, Yogesh Munot, Umesh Bhise, Sunil Chavan, Sachin Shivatare, Sarvesh Patel, Vikas Gore
-
Patent number: 9340541Abstract: Disclosed is a method for preparing a compound of Formula 1 by coupling of intermediates of Formula 2 and Formula 3 in the presence of an aluminum reagent of Formula 4 wherein R1, R2a, R2b and R2c are defined in the disclosure.Type: GrantFiled: December 31, 2013Date of Patent: May 17, 2016Assignee: E I DU PONT DE NEMOURS AND COMPANYInventor: Ahmad El-Awa
-
Patent number: 9199959Abstract: The present invention provides a novel compound having an antiviral action, in particular, an HIV replication inhibiting action, as well as a pharmaceutical composition, in particular, an anti-HIV agent. wherein, a broken line means the presence or absence of a bond; R1 is substituted or unsubstituted alkyl etc., R2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R3 is a substituted or unsubstituted aromatic carbocyclic group; R4 is a hydrogen atom etc.; R5 is a substituted or unsubstituted aromatic carbocyclic group etc.; Y is a single bond etc.; R6 is substituted or unsubstituted alkyl; R7 is —Z—R71 etc.; Z is —NR72—CO— etc.; R71 is substituted or unsubstituted alkyl etc.; R72 is a hydrogen atom etc.Type: GrantFiled: October 25, 2012Date of Patent: December 1, 2015Assignee: SHIONOGI & CO., LTD.Inventors: Tsutomu Iwaki, Kenji Tomita
-
Patent number: 9199984Abstract: Compounds of formula (I): wherein R1, R2, R3, R5, R6, A1, A2, A3, A4 assume meanings as defined in formula (I) are inhibitors of neutrophil elastase.Type: GrantFiled: July 12, 2013Date of Patent: December 1, 2015Assignee: CHIESI FARMACEUTICI S.p.A.Inventors: Carmelida Capaldi, Robert Andrew Heald, Nicholas Charles Ray, Jonathan Mark Sutton
-
Patent number: 9173878Abstract: The present invention provides a pharmaceutical composition used in improving brain function including a compound of formula (I).Type: GrantFiled: January 24, 2013Date of Patent: November 3, 2015Assignee: Tohoku UniversityInventor: Kohji Fukunaga
-
Patent number: 9145433Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.Type: GrantFiled: October 4, 2013Date of Patent: September 29, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
-
Patent number: 9120796Abstract: Provided herein are intermediates useful in the synthesis of ?-lactamase inhibitors, and methods of making said intermediates and ?-lactamase inhibitors.Type: GrantFiled: October 2, 2014Date of Patent: September 1, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Evan A. Hecker, Amy Baldwin
-
Patent number: 9108966Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a ?-lactam antibiotic at a fixed concentration have an MIC of 8 ?g/mL or less against one or more isogenic ?-lactamase expressing bacterial strains.Type: GrantFiled: March 17, 2014Date of Patent: August 18, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
-
Patent number: 9085560Abstract: A method of inhibiting phosphatidyl inositol-3 kinase (PI3 kinase), comprising: contacting the PI3 kinase with an effective amount of a compound or pharmaceutically acceptable salt of the formula below, wherein the variables R1, R2, W1, W2, W3, W4, W5, are W6 are defined herein.Type: GrantFiled: August 17, 2010Date of Patent: July 21, 2015Assignee: INTELLIKINE, INC.Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
-
Patent number: 9045478Abstract: 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, 2015Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ashok Tehim, Vidyadhar Paradkar, Prasanna M. Dattatreya, Nanjegowda Jagadeesh Mavinahalli
-
Publication number: 20150148334Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: June 27, 2014Publication date: May 28, 2015Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu