At Least Five Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/254)
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Patent number: 11878016Abstract: Methods and products for treating a subject diagnosed with an autism spectrum disorder, an intellectual disability, an anxiety disorder, a mood disorder, a disorder of social interaction, irritability, aggression, self-injurious behavior, hyperactivity, inattention, or Fragile X syndrome or brain neuroinflammation by administering a tablet or liquid or a solid ODT or ODF or SMEDDS containing a ticagrelor or ticagrelor salt or combination with a second agent which may include a magnesium ion containing-compound, a zinc ion containing-compound, a lysine or lysine salt, an arginine or arginine salt, lecithin, or a combination thereof, wherein the ODT or ODF or SMEDDS releases >50% of the ticagrelor or a pharmaceutically acceptable salt thereof and >50% of the second agent within 15 minutes.Type: GrantFiled: October 3, 2022Date of Patent: January 23, 2024Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Nava Zisapel, Moshe Laudon
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Patent number: 11655235Abstract: The present technology provides pyrrolidine and piperidine compounds or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. In particular, said compounds may be usefully applied in the treatment and prevention of FAP-mediated diseases.Type: GrantFiled: November 5, 2020Date of Patent: May 23, 2023Assignee: YUHAN CORPORATIONInventors: Tae Han Dong, Yoo Hoi Park, Tae Kyun Kim, Jae Eun Joo, Eun Hye Jung, Jae Won Jeong, Hyun Seung Lee, Do Hoon Kim, Ji Eun Yang, Jun Chui Park, Sang Myoun Lim, Na Ry Ha, Da In Chung, Ji Yeong Gal
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Patent number: 11525136Abstract: The present embodiments provide methods, compounds, and compositions useful for inhibiting APOL1 expression, which may be useful for treating, preventing, or ameliorating a disease associated with APOL1.Type: GrantFiled: September 18, 2020Date of Patent: December 13, 2022Assignee: Ionis Pharmaceuticals, Inc.Inventor: Susan M. Freier
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Patent number: 11053251Abstract: Described herein are GPR35 modulators and methods of using these compounds in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.Type: GrantFiled: January 23, 2020Date of Patent: July 6, 2021Assignee: Prometheus Biosciences, Inc.Inventor: Robert Higuchi
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Patent number: 10844071Abstract: In certain embodiments compounds corresponding in structure to the formula: are provided that are effective to lower p-tau and/or to prevent or reduce elevation of p-tau, particularly in response to stress (e.g., elevated cortisol levels). The compounds are useful in the treatment or prophylaxis of pathologies characterized by abnormal amyloid plaque and or tangle formation and/or deposition.Type: GrantFiled: February 21, 2020Date of Patent: November 24, 2020Assignee: BUCK INSTITUTE FOR RESEARCH ON AGINGInventors: Varghese John, Dale E. Bredesen
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Patent number: 10457684Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: December 20, 2018Date of Patent: October 29, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal
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Patent number: 10457686Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: December 20, 2018Date of Patent: October 29, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal
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Patent number: 10457685Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 and n are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: December 20, 2018Date of Patent: October 29, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal, Adriaan Pieter Ijzerman
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Patent number: 10450321Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: December 20, 2018Date of Patent: October 22, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Uwe Grether, Wolfgang Guba, Julian Kretz, Rainer E. Martin, Matthias Valentin Westphal, Adriaan Pieter Ijzerman
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Patent number: 10011605Abstract: The present invention relates to a process for preparation of triazolo[4,5-d] pyrimidine cyclopentane compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention also provides novel compounds that can be used as intermediates in the process for preparing triazolo[4,5-d] pyrimidine cyclopentane compounds. The process and the intermediates are particularly useful for the preparation of ticagrelor and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 11, 2015Date of Patent: July 3, 2018Assignee: FLAMMA SPAInventors: Anna Rencurosi, Massimo Previtali, Federico Della Negra, Francesco Mormile, Renato Canevotti
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Patent number: 9988380Abstract: The invention relates to compounds for use as quorum sensing inhibitors, and in particular, to quorum sensing inhibitors of Pseudomonas aeruginosa.Type: GrantFiled: March 10, 2014Date of Patent: June 5, 2018Assignees: Nanyang Technological University, National University of SingaporeInventors: Michael Givskov, Liang Yang, Yang Yi Sean Tan
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Patent number: 9932317Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.Type: GrantFiled: March 19, 2013Date of Patent: April 3, 2018Assignees: Imperial Innovations Limited, Emory UniversityInventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Snyder, Thota Ganesh, Jin Liu, Aiming Sun
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Patent number: 9512128Abstract: The present invention relates to aryl sulphide and aryl sulphoxide derivatives, to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation. The aryl sulphide and aryl sulphoxide derivatives have the general structure (I) in which the respective radicals have the meanings given in the description.Type: GrantFiled: December 18, 2013Date of Patent: December 6, 2016Assignee: Bayer Cropscience AGInventors: Bernd Alig, Silvia Cerezo-Galvez, Reiner Fischer, Adeline Koehler, Julia Johanna Hahn, Angela Becker, Kerstin Ilg, Arnd Voerste, Ulrich Goergens, Daniela Portz
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Patent number: 9487518Abstract: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substitutedType: GrantFiled: March 2, 2012Date of Patent: November 8, 2016Assignee: Janssen Sciences Ireland UCInventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts
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Patent number: 9067943Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: November 19, 2012Date of Patent: June 30, 2015Assignee: HOFFMANN-LA ROCHE INC.Inventors: Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
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Patent number: 9056838Abstract: The present invention is related to new intermediates and processes for preparing Ticagrelor disclosed in this patent application.Type: GrantFiled: April 6, 2012Date of Patent: June 16, 2015Assignee: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Vinod Kumar Kansal, Dhirenkumar Mistry, Sanjay Vasoya, Ghanshyam Pandey, Amit Taneja, Pramod Kadappa Shindey, Jiri Stohandl, Jaroslav Frantisek
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Patent number: 8987279Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: GrantFiled: May 8, 2013Date of Patent: March 24, 2015Assignee: Vernalis (R&D) LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
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Patent number: 8980893Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.Type: GrantFiled: November 21, 2013Date of Patent: March 17, 2015Assignee: Merial, Inc.Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
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Publication number: 20150073146Abstract: Provided are processes for preparing Ticagrelor and its intermediates that are useful in the processes. Also provided are salts of Ticagrelor, their processes and solid dispersion of Ticagrelor having Ticagrelor in amorphous form.Type: ApplicationFiled: April 5, 2013Publication date: March 12, 2015Inventors: Vilas Hareshwar Dahanukar, Goverdhan Gilla, Sreenivasulu Kurella, Shweta Mahajan Kulkarni, Raghupathi Reddy Anumula, Sampath Aalla, Yakambram Bojja, Ravi Ram Chandra Sekhar Elati, Veerender Murki, Venkata Annapurna Sasikala Cheemalapati
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Patent number: 8937150Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: May 4, 2011Date of Patent: January 20, 2015Assignee: AbbVie Inc.Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Publication number: 20150005498Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives, suitable for the preparation of Ticagrelor (TCG).Type: ApplicationFiled: September 14, 2012Publication date: January 1, 2015Applicant: Lek Pharmaceuticals d.d.Inventors: Nened Maras, Borut Zupancic
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Publication number: 20140378431Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Guenter Hoelzemann, Kai Schiemann, Ansgar Wegener
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Publication number: 20140371449Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.Type: ApplicationFiled: December 20, 2012Publication date: December 18, 2014Applicant: Lek Pharmaceuticals d.d.Inventors: Nenad Maras, Ivana Gazic Smilovic, Damjan Sterk
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Patent number: 8883802Abstract: The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4-hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2-methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).Type: GrantFiled: December 3, 2010Date of Patent: November 11, 2014Assignee: Astrazeneca ABInventors: Stephen David Cosgrove, Matthew Jonathan Jones, Anna Polyakova-Akkus, Valeriya Nikolayevna Smolenskaya, Brenton Skylar Wolfe
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Publication number: 20140323727Abstract: Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.Type: ApplicationFiled: July 1, 2014Publication date: October 30, 2014Inventors: Anil Shahaji Khile, Jayesh Patel, Nikhil Trivedi, Nitin Sharadchandra Pradhan
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Patent number: 8871785Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: March 21, 2013Date of Patent: October 28, 2014Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Carina E. Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Haolun Jin, Ralph Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten A. Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie O'Shea, Sundaramoorthi Swaninathan, William J. Watkins, Jennifer R. Zhang
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Publication number: 20140296258Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: October 31, 2013Publication date: October 2, 2014Applicant: AstraZeneca UK LimitedInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
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Publication number: 20140288046Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: April 11, 2014Publication date: September 25, 2014Applicant: HOFFMANN-LA ROCHE INC.Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
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Publication number: 20140256747Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.Type: ApplicationFiled: October 26, 2012Publication date: September 11, 2014Applicant: LEK PHARMACEUTICALS D.D.Inventors: Borut Zupancic, Nenad Maras, Damjan Sterk
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Patent number: 8802850Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: July 27, 2010Date of Patent: August 12, 2014Assignee: Auspex Pharmaceuticals, Inc.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20140206867Abstract: Disclosed herein is an improved process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Particularly described is an improved, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, [3aR-(3a?,4?,6?,6a?]-2-[[6-amino-2,2-dimethyltetrahydro-4H-cyclopenta-1,3-dioxol-4-yl]oxy]-ethanol, alternatively named, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol.Type: ApplicationFiled: June 13, 2012Publication date: July 24, 2014Applicant: Actavis Group PTC EHFInventors: Anil Shahaji Khile, Vignesh Nair, Nikhil Trivedi, Nitin Sharadchandra Pradhan
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Patent number: 8785653Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: June 20, 2013Date of Patent: July 22, 2014Assignee: H. Lundbeck A/SInventors: Ask Puschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morton Langgard
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Publication number: 20140194418Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.Type: ApplicationFiled: January 20, 2012Publication date: July 10, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
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Patent number: 8759357Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: October 1, 2010Date of Patent: June 24, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Gerald W. Shipps, Jr., Clifford C. Cheng, Xioahua Huang, Abdelghani Achab, Peter Orth, Johannes H. Voigt
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Publication number: 20140154772Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: November 27, 2013Publication date: June 5, 2014Applicant: ICOS CORPORATIONInventors: Chanchal SADHU, Ken DICK, Jennifer TREIBERG, C. Gregory SOWELL, Edward A. KESICKI, Amy OLIVER
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Patent number: 8741906Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: November 6, 2012Date of Patent: June 3, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
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Patent number: 8741909Abstract: The present invention relates to compounds of formula (I) and to compositions comprising the same and to the use of the compounds and their compositions in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the compounds.Type: GrantFiled: October 19, 2010Date of Patent: June 3, 2014Assignee: Respivert Ltd.Inventors: John King-Underwood, Kazuhiro Ito, Peter John Murray, George Hardy, Frederick Arthur Brookfield, Christopher John Brown
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Publication number: 20140148472Abstract: Disclosed are compounds able to modulate the activity of the GPR17 receptor in a highly specific way, which are useful in the treatment and diagnosis of diseases or dysfunctions involving the activation of said receptor. In particular, the compounds according to the invention can be used for neuroprotective and/or reparatory purposes, in cerebral, cardiac and renal ischaemia, in cerebral trauma, in chronic neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), and in demyelinating diseases such as multiple sclerosis.Type: ApplicationFiled: November 2, 2011Publication date: May 29, 2014Applicant: CENTRO CARDIOLOGICO MONZINO SpAInventors: Mariapia Abbracchio, Ivano Eberini, Chiara Parravicini, Claudia Martini, Maria Letizia Trincavelli, Simona Daniele
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Publication number: 20140148433Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: August 31, 2011Publication date: May 29, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
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Publication number: 20140094604Abstract: The present invention is related to new intermediates and processes for preparing Ticagrelor disclosed in this patent application.Type: ApplicationFiled: April 6, 2012Publication date: April 3, 2014Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Vinod Kumar Kansal, Dhirenkumar Mistry, Sanjay Vasoya, Ghanshyam Pandey, Amlt Taneja, Pramond Kadappa, Jiri Stohandl, Jaroslay Frantisek
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Publication number: 20140073624Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: February 19, 2013Publication date: March 13, 2014Applicant: RIB-X PHARMACEUTICALS, INC.Inventor: Rib-X Pharmaceuticals, Inc.
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Publication number: 20140038988Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Franz VON NUSSBAUM, Dagmar KARTHAUS, SONJA ANLAUF, Martina DELBECK, Volkhart Min-Jian LI, Daniel MEIBOM, Klemens LUSTIG
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Patent number: 8609668Abstract: A pharmaceutical composition comprising an effective amount of a compound of formulas (I-III) and a pharmaceutically acceptable carrier. Methods for treating a hepatitis virus in a patient comprising administering an effective amount of the compound of formulas (I-III) are also presented.Type: GrantFiled: May 4, 2007Date of Patent: December 17, 2013Assignees: Philadelphia Health & Education Corporation, Institute For Hepatitis and Virus ResearchInventors: Andrea Cuconati, Timothy M. Block, Xiaodong Xu
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Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Patent number: 8598184Abstract: The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: February 28, 2009Date of Patent: December 3, 2013Assignee: Tiger PharmatechInventor: Junhu Zhang
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Publication number: 20130317220Abstract: Provided herein is a novel process for the preparation of triazolo[4,5-d]pyrimidine derivatives. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of highly pure ticagrelor or a pharmaceutically acceptable salt thereof. Provided further herein is a novel process for the preparation of substituted cyclopentanamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a ticagrelor intermediate, 2-[[(3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]-dioxol-4-yl]oxy]-1-ethanol.Type: ApplicationFiled: December 16, 2011Publication date: November 28, 2013Applicant: Actavis Group Ptc EhfInventors: Vignesh Nair, Nikhil Trivedi, Anil Shahaji Khile, Nitin Sharadchandra Pradhan
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Patent number: 8501795Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: December 15, 2010Date of Patent: August 6, 2013Assignee: H. Lundbeck A/SInventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
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Publication number: 20130150577Abstract: Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.Type: ApplicationFiled: April 19, 2011Publication date: June 13, 2013Applicant: ACTAVIS GROUP PTC EHFInventors: Anil Shahaji Khile, Jayesh Patel, Nikhil Trivedi, Nitin Sharadchandra Pradhan
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Publication number: 20130137676Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 19, 2012Publication date: May 30, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8450328Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.Type: GrantFiled: June 25, 2009Date of Patent: May 28, 2013Assignee: Vernalis (R&D) LimitedInventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd