Chalcogen Bonded Directly At 2- And 4-positions Patents (Class 544/285)
-
Patent number: 9834520Abstract: The present invention provides a heterocyclic compound having an ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I): wherein Ar is a the partial structure (1) to the partial structure (5), Q is a bivalent group selected from the group consisting of (Ia)-(If), and B is a ring optionally having substituent(s), or a salt thereof.Type: GrantFiled: March 13, 2014Date of Patent: December 5, 2017Assignee: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Junya Shirai, Yoshiyuki Fukase, Ayumu Sato, Mitsunori Kouno, Yoshihide Tomata, Atsuko Ochida, Kazuko Yonemori, Tsuneo Oda, Tomoya Yukawa
-
Publication number: 20150141400Abstract: The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 24, 2013Publication date: May 21, 2015Inventors: Takeshi Murata, Hatsuo Kawada, Satoshi Niizuma, Sousuke Hara, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Toshiyuki Mio
-
Publication number: 20150119411Abstract: Described herein are compounds, pharmaceutical compositions and methods for treating a respiratory syncytial virus infection in a subject, or for inhibiting replication of respiratory syncytial virus.Type: ApplicationFiled: June 5, 2013Publication date: April 30, 2015Inventors: Jennifer E. Golden, Jeffrey Aube, Denise S. Simpson, Daniel P. Flaherty, Daljit S. Matharu, William E. Severson, Lynn Rasmussen
-
Publication number: 20150110723Abstract: The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.Type: ApplicationFiled: May 28, 2013Publication date: April 23, 2015Applicant: EMORY UNIVERSITYInventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
-
Publication number: 20150004698Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.Type: ApplicationFiled: August 29, 2014Publication date: January 1, 2015Applicants: YALE UNIVERSITY, UNIVERSITY OF SOUTH FLORIDAInventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
-
Publication number: 20140378475Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: June 25, 2014Publication date: December 25, 2014Inventors: Douglas G. Batt, Myra Beaudoin Bertrand, George Delucca, Michael A. Galella, Soo Sung Ko, Charles M. Langevine, Qingjie Liu, Qing Shi, Anurag S. Srivastava, Joseph A. Tino, Scott Hunter Watterson
-
Publication number: 20140350033Abstract: ANT-ligands having a substituted nitrogeneous heterocycle A wherein A is a substituted pyrimidinone of formula I wherein R1 is —(CH2)n-CO—OH; —(CH2)n-CO—OR; —(CH2)n-CO—NHR; —(CH2)n-CO—N(R, R?); —(CH2)n-OH; —(CH2)n-OR; —(CH2)n-OAr; —(CH2)n-C(R,R?)—(CH2)n-OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.Type: ApplicationFiled: June 5, 2014Publication date: November 27, 2014Applicants: MITOLOGICS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE VERSAILLES-SAINT QUENTIN-EN-YVELINES (UVSQ)Inventors: Annie BORGNE-SANCHEZ, Etienne JACOTOT, Catherine BRENNER
-
Patent number: 8865704Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: GrantFiled: October 6, 2010Date of Patent: October 21, 2014Assignee: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
-
Publication number: 20140275711Abstract: Disclosed are novel 1-(arylmethyl)-5,6,7,8-tetrahydroquinazoline-2,4-diones and analogs thereof, represented by the Formula I, wherein Ar, A, B, R3-R6 are defined herein. Compounds having Formula I are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity, such as cancer.Type: ApplicationFiled: November 1, 2012Publication date: September 18, 2014Inventors: Suixiong Cai, Ye Edward Tian, Lizhen Wu, Lijun Liu, Xiaozhu Wang, Yangzhen Jiang, Guoxiang Wang, Xiuyan Zhang, Qingbing Xu, Zheng Meng
-
Publication number: 20140256753Abstract: Provided is a process for treating or preventing a viral infection in a subject, wherein the viral infection is from a flavivirus selected from the group consisting of Hepatitis C Virus (genotypes 1-7) and Japanese Encephalitis Virus.Type: ApplicationFiled: August 10, 2012Publication date: September 11, 2014Applicants: Sanford-Burnham Medical Research Institute, Southern Research InstituteInventors: Marintha L. Heil, Nicholas D.P. Cosford, Robert Ardecky, Jiwen Zou
-
Publication number: 20140221405Abstract: Novel compounds of formulae (I) to (VII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylfulfonamide derivatives which are effective platelet ADF receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 31, 2013Publication date: August 7, 2014Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-MaGuire
-
Publication number: 20140206705Abstract: Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I).Type: ApplicationFiled: March 12, 2014Publication date: July 24, 2014Applicant: AJINOMOTO CO., INC.Inventors: Noriyasu KATAOKA, Riho KODAMA, Akinori TATARA
-
Publication number: 20140187550Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: ApplicationFiled: December 16, 2013Publication date: July 3, 2014Applicant: Novartis AGInventor: Roger John Taylor
-
Publication number: 20140100239Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, L1, L2, X, Y and Z have defined meanings.Type: ApplicationFiled: December 6, 2013Publication date: April 10, 2014Applicant: Janssen Pharmaceutica NVInventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
-
Publication number: 20140031358Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.Type: ApplicationFiled: March 12, 2012Publication date: January 30, 2014Applicant: Eternity Bioscience Inc.Inventors: Dong Liu, Minsheng Zhang, Kan He, Lianshan Zhang
-
Publication number: 20140023642Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.Type: ApplicationFiled: March 31, 2012Publication date: January 23, 2014Applicant: Impact Therapeutics, Inc.Inventors: Sui Xiong Cai, Ye Edward Tian, Haijun Dong, Qingbing Xu, Lizhen Wu, Lijun Liu, Yangzhen Jiang, Qingli Bao, Guoxiang Wang, Feng Yin, Chengyun Gu, Xiuhua Hu, Xiaozhu Wang, Sishun Kang, Shengzhi Chen
-
Patent number: 8633209Abstract: Provided herein are hydrobromide salts of a pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating a proliferative disease.Type: GrantFiled: August 31, 2011Date of Patent: January 21, 2014Assignee: Ambit Biosciences CorporationInventors: Timothy David Gross, Patrick B. O'Donnell
-
Patent number: 8633211Abstract: A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: GrantFiled: March 4, 2008Date of Patent: January 21, 2014Assignee: Novartis AGInventor: Roger John Taylor
-
Publication number: 20140018376Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of Rasmussen's encephalitis and/or certain forms of epilepsy.Type: ApplicationFiled: October 20, 2010Publication date: January 16, 2014Inventors: Hans Allgeier, Yves Auberson, Thomas Blaettler, David Carcache, Philipp Floersheim, Wolfgang Froestl, Christel Guibourdenche, Hans o Kalkman, Joerg Kallen, Manuel Koller, Kurt Lingenhohl, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud, Christine Strohmaier
-
Patent number: 8623884Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, L1, L2, X, Y and Z have defined meanings.Type: GrantFiled: November 17, 2011Date of Patent: January 7, 2014Assignee: Janssen Pharmaceutica, NVInventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
-
Patent number: 8614229Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: August 27, 2008Date of Patent: December 24, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
-
Publication number: 20130302378Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.Type: ApplicationFiled: July 8, 2013Publication date: November 14, 2013Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
-
Publication number: 20130296332Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
-
Patent number: 8575185Abstract: The present invention provides quinazolinedione derivatives of Formulae Ia and Ib, which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, depression and dementia.Type: GrantFiled: February 26, 2010Date of Patent: November 5, 2013Assignee: Reviva Pharmaceuticals, Inc.Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Sureshbabu Dadiboyena, Kouacou Adiey
-
Publication number: 20130252979Abstract: The present invention relates to a novel crystalline anhydrous form of [(5-chlorothiophene-2-ylsulfonylcarbamoyl)-(4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)phenyl)amide, potassium salt, and its use in the treatment or prevention of a condition or a disorder with platelet ADP receptor inhibition, in particular, P2Y12 inhibition, in animals, particularly humans. It also relates processes for making such a novel crystalline form. The present invention also relates to a solid, oral for mulation of this novel crystalline form, its preparation and use thereof.Type: ApplicationFiled: December 5, 2011Publication date: September 26, 2013Inventors: Ulrich Meier, Nicole Bieri, Dieter Becker, Julien Taillemite, Marie-Pierre Filliot, Tanja Meister
-
Patent number: 8524721Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 10, 2011Date of Patent: September 3, 2013Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
-
Patent number: 8513268Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: GrantFiled: July 28, 2011Date of Patent: August 20, 2013Assignee: Novartis AGInventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
-
Patent number: 8450333Abstract: The present invention provides compounds capable of regulating apoptosis, e.g., via regulating mitochondrial fission or fusion. The present invention also provides methods of screening for compounds capable of regulating apoptosis and methods of treating conditions association with apoptosis.Type: GrantFiled: February 8, 2008Date of Patent: May 28, 2013Assignee: The Regents of The University of CaliforniaInventors: Jodi Nunnari, Ann Cassidy-Stone, Mark Kurth
-
Publication number: 20130123285Abstract: The present invention provides an assay for screening any agent that modulates the ability of A3G to bind with RNA. The invention provides an agent identified by high throughput screening methods and methods of treatment using the identified agent as a means of inhibiting HIV infection and reducing the emergence of viral drug-resistance.Type: ApplicationFiled: May 13, 2011Publication date: May 16, 2013Applicant: UNIVERSITY OF ROCHESTERInventors: Harold C. Smith, Kimberly Prohaska, William M. McDougall
-
Publication number: 20130096145Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of spasticity.Type: ApplicationFiled: June 24, 2011Publication date: April 18, 2013Applicant: Novartis AGInventor: Hans O. Kalkman
-
Publication number: 20130090346Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment or prevention of photosensitive epilepsy.Type: ApplicationFiled: September 5, 2012Publication date: April 11, 2013Inventors: Donald Johns, Georges Imbert, Klaus Kucher
-
Publication number: 20130066072Abstract: Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I).Type: ApplicationFiled: October 1, 2012Publication date: March 14, 2013Applicant: AJINOMOTO CO., INC.Inventor: AJINOMOTO CO., INC.
-
Publication number: 20130053381Abstract: The invention relates to a 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative being (A) a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; or (B) a compound selected from a certain group of 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivatives disclosed in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them. In a first aspect, the invention provides prodrugs of AMPA receptor antagonists which potentially useful in the treatment of a wide range of disorders, particularly epilepsy.Type: ApplicationFiled: May 18, 2011Publication date: February 28, 2013Inventors: Yves Auberson, David Carcache, Andreas Lerchner, Joachim Nozulak
-
Patent number: 8309561Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: December 21, 2007Date of Patent: November 13, 2012Assignee: Ajinomoto Co., Inc.Inventors: Kazuyuki Sagi, Tatsuya Okuzumi, Tatsuhiro Yamada, Shunsuke Kageyama, Yoichiro Shima, Tadakiyo Nakagawa, Munetaka Tokumasu, Masayuki Sugiki, Hajime Ito, Itsuya Tanabe, Tamotsu Suzuki, Akira Nakayama, Kazuyuki Ubukata, Kenji Shinkai, Yasuhiro Tanaka, Misato Noguchi, Ayatoshi Andou, Yoriko Yamamoto, Noriyasu Kataoka, Koichi Fujita
-
Patent number: 8299085Abstract: The present invention relates to 1H-Quinazoline-2,4-dione derivatives of formula(I) wherein the substituents are defined as in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them.Type: GrantFiled: July 26, 2005Date of Patent: October 30, 2012Assignee: Novartis AGInventors: Hans Allgeier, Wolfgang Froestl, Manuel Koller, Henri Mattes, Joachim Nozulak, Silvio Ofner, David Orain, Vittorio Rasetti, Johanne Renaud, Nicolas Soldermann, Philipp Floersheim
-
Patent number: 8268844Abstract: Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride: are useful as ?4 integrin inhibitors.Type: GrantFiled: September 20, 2010Date of Patent: September 18, 2012Assignee: Ajinomoto Co., Inc.Inventors: Koichi Fujita, Shinichiro Takahashi, Tatsuya Okuzumi, Tatsuhiro Yamada, Kotaro Okado, Noriyasu Kataoka, Haruko Hirashima, Hideyuki Yamaguchi
-
Patent number: 8242126Abstract: The invention relates to quinazolinedione derivatives of the general formula (I): wherein A, R1, R2, R3, R4, m, n, p, p?, and r are as defined herein, processes for the preparation thereof and their therapeutic applications.Type: GrantFiled: April 5, 2010Date of Patent: August 14, 2012Assignee: SanofiInventors: Annie Clauss, Christophe Glaess, Gilbert Marciniak, Nicolas Muzet, Jean-Francois Nave, André Seyer, Bertrand Vivet
-
Publication number: 20120196851Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: October 6, 2010Publication date: August 2, 2012Applicant: SIENA BIOTECH S.P.A.Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
-
Patent number: 8222405Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: November 22, 2010Date of Patent: July 17, 2012Assignee: Ajinomoto Co., Inc.Inventors: Shingo Makino, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
-
Publication number: 20120149688Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 10, 2011Publication date: June 14, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
-
Publication number: 20120129876Abstract: The present invention provides novel sulfonylurea salts of a salt of formula (I) and polymorph forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a salt of formula (I) or a pharmaceutically acceptable form thereof.Type: ApplicationFiled: June 22, 2011Publication date: May 24, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Emma Sharp, Louisa Jane Quegan, Anjali Pandey, Juan Wang, Matthew Nieder, Wolin Huang
-
Publication number: 20120122903Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of neuronal ceroid lipofuscinosis.Type: ApplicationFiled: July 23, 2010Publication date: May 17, 2012Inventors: Hans O Kalkman, Henri Mattes
-
Publication number: 20120115846Abstract: The subject matter of the invention is quinazolinedione derivatives of formula (I), methods for obtaining same and therapeutic uses thereof, such as cancer, diabetes, muscle diseases, bone diseases, cardiovascular diseases, central nervous system diseases, peripheral nervous system diseases, inter alia.Type: ApplicationFiled: October 7, 2011Publication date: May 10, 2012Applicant: SANOFIInventors: Annie CLAUSS, Christophe GLAESS, Gilbert MARCINIAK, Jean-Francois NAVE, Bertrand VIVET
-
Publication number: 20120094997Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, Ra, R2a, R2b, R1, and X have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Dylan B. England, Kenneth M. Gigstad, Alexandra E. Gould, Liting Ma, He Xu
-
Publication number: 20120065216Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, L1, L2, X, Y and Z have defined meanings.Type: ApplicationFiled: November 17, 2011Publication date: March 15, 2012Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
-
Publication number: 20120058987Abstract: The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof, as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to CNS) and/or associated with the peripheral nervous system (abbreviated to PNS).Type: ApplicationFiled: March 25, 2010Publication date: March 8, 2012Applicant: SANOFIInventors: Gilbert Marciniak, Jean-Francois Nave, Fabrice Viviani
-
Publication number: 20120020881Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: December 4, 2009Publication date: January 26, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
-
Publication number: 20120009172Abstract: The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: alone or in combination with a second agent which can be aspirin or a thrombolytic agent.Type: ApplicationFiled: September 16, 2011Publication date: January 12, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Daniel D. Gretler, Pamela B. Conley, Patrick Andre, Athiwat Hutchaleelaha, David R. Phillips, Anjali Pandey, Robert M. Scarborough, Carroll Anna Crew Scarborough, Wolin Huang
-
Publication number: 20110313154Abstract: A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3? which is a group corresponding to R3 is protected.Type: ApplicationFiled: August 26, 2011Publication date: December 22, 2011Applicant: AJINOMOTO CO., INC.Inventors: Noriyasu KATAOKA, Kotaro OKADO, Tatsuhiro YAMADA, Koichi FUJITA, Tamotsu SUZUKI, Tatsuya OKUZUMI, Masayuki SUGIKI, Akinori TATARA
-
Patent number: 8080557Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, L1, L2, X, Y and Z have defined meanings.Type: GrantFiled: June 28, 2005Date of Patent: December 20, 2011Assignee: Janssen Pharmaceutica, NVInventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacbous Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters