1,3- Or 3,1-benzothiazines Patents (Class 544/50)
  • Patent number: 10358442
    Abstract: 2-homopiperazine-1-yl-4H-1, 3-bensothiazine-4-one derivatives of formula (I) are provided. They are useful in the treatment of bacterial infections, in particular tuberculosis, buruli ulcer and leprosy. A process for the preparation of 2-(homo)piperazine 1, 3-benzothiazine-4-one hydrochlorides is also provided.
    Type: Grant
    Filed: November 13, 2018
    Date of Patent: July 23, 2019
    Assignee: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)
    Inventors: Cole Stewart, Vadim Albertovich Makarov
  • Patent number: 10160754
    Abstract: 2-homopiperazine-1-yl-4H-1,3-bensothiazine-4-one derivatives of formula (I) are provided. They are useful in the treatment of bacterial infections, in particular tuberculosis, buruli ulcer and leprosy. A process for the preparation of 2-(homo)piperazine 1,3-benzothiazine-4-one hydrochlorides is also provided.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: December 25, 2018
    Assignee: Ecole Polytechnique Federale De Lausanne (EPFL)
    Inventors: Cole Stewart, Vadim Albertovich Makarov
  • Publication number: 20140303152
    Abstract: Benzothiazinethione derivatives of formula (I), their preparative methods and uses are provided. Benzothiazinethione derivatives of the invention have significant effect of inhibiting Mycobacterium tuberculosis.
    Type: Application
    Filed: June 15, 2011
    Publication date: October 9, 2014
    Applicant: SICHUAN UNIVERSITY
    Inventors: Luoting Yu, Yuquan Wei
  • Patent number: 8796264
    Abstract: The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: August 5, 2014
    Assignee: Ecole Polytechnique Federale de Lausanne (EPFL)
    Inventors: Vadim Makarov, Stewart Cole
  • Publication number: 20130274251
    Abstract: The present invention provides compounds of formula (1) acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as anti-cancer agents for preventions and treatments of PK- and RK-related disorders, in particular cancer. (I) wherein A is H or CN; Z is S, SO or S02; X1, X2, X3, X4, X5, Y1 and Y2 are each independently selected from H, halogen, alkyl, haloalkyl and OR1; and Y3 and Y4 are each OR1, wherein each R1 is independently H, C1-C4 alkyl, acyl, —(CH2CH20)n wherein n is an integer of 1 to 20, or a functional group that gives rise to hydroxyl upon hydrolysis.
    Type: Application
    Filed: December 27, 2011
    Publication date: October 17, 2013
    Applicant: NOVOTYR THERAPEUTICS LTD.
    Inventors: Hadas Reuveni, Alexander Levitzki
  • Publication number: 20130245007
    Abstract: The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria. (I).
    Type: Application
    Filed: November 21, 2011
    Publication date: September 19, 2013
    Applicant: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)
    Inventors: Vadim Makarov, Stewart Cole
  • Patent number: 8420634
    Abstract: Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: and the use of the products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.
    Type: Grant
    Filed: September 22, 2008
    Date of Patent: April 16, 2013
    Assignee: Rottapharm S.p.A.
    Inventors: Maurizio Anzini, Antonio Giordani, Francesco Makovec, Andrea Cappelli, Salvatore Vomero, Gianfranco Caselli, Lucio Claudio Rovati
  • Publication number: 20120289493
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors 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 Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 8, 2012
    Publication date: November 15, 2012
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20120258961
    Abstract: The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-? proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, ring A, Y and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 11, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Shinji Suzuki, Yuuji Kooriyama
  • Publication number: 20120245154
    Abstract: The present invention relates to an agent for treating or preventing disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound of formula (I), wherein, R1, R2a, R2b R3, R4a, R4b, ring A, and dashed line are described in this specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 8, 2010
    Publication date: September 27, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Kousuke Anan, Yukio Tada, Akihiro Hori, Moriyasu Masui
  • Publication number: 20120245155
    Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-?proteins. A compound of the formula (I): wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6a, R6b, X, Y, Z, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 9, 2010
    Publication date: September 27, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Syuhei Yoshida, Issei Kato, Kouki Fuchino, Yuuji Kooriyama, Yoshiyasu Baba, Norihiko Tanimoto
  • Publication number: 20120184518
    Abstract: Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 19, 2012
    Applicant: PROBIODRUG AG
    Inventors: Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
  • Publication number: 20120094984
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Application
    Filed: December 21, 2011
    Publication date: April 19, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Publication number: 20110160193
    Abstract: The present invention relates to novel benzothiazinone derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance. The solution of the present invention is a compound of formula I wherein R1 to R6 are as defined in the specification.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 30, 2011
    Applicant: Leibniz Institute for Natural Product Research and Infection Biology E.V.
    Inventors: A. Vadim Makarov, Stewart T. Cole, Ute Möllmann
  • Publication number: 20110003795
    Abstract: The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: May 6, 2010
    Publication date: January 6, 2011
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM
  • Publication number: 20100317850
    Abstract: Disclosed is a compound represented by General formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptable salt, which has an inhibitory activity of the production of A? or a BACE1-inhibiting activity, and is therefore useful as a prophylactic or therapeutic agent for A?-induced neurodegenerative diseases typified by Alzheimer-type dementia. Wherein the ring A represents a C6-14 aryl group or the like; L represents —NReCO— [wherein Re represents a hydrogen atom or the like] or the like; the ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a single bond or the like; Z represents a C1-3 alkylene group or the like; R1 and R2 independently represent a hydrogen atom or the like; and R3, R4, R5 and R6 independently represent a hydrogen atom, a halogen atom or the like.
    Type: Application
    Filed: January 16, 2009
    Publication date: December 16, 2010
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Publication number: 20100286130
    Abstract: The present invention relates to compounds of Formula (I) or salts thereof wherein R?, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.
    Type: Application
    Filed: June 25, 2008
    Publication date: November 11, 2010
    Inventors: Ute Moellmann, Vadim Makarov, Cole T. Stewart
  • Publication number: 20100234363
    Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor.
    Type: Application
    Filed: September 17, 2008
    Publication date: September 16, 2010
    Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.
    Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
  • Patent number: 7790726
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Grant
    Filed: August 14, 2006
    Date of Patent: September 7, 2010
    Assignee: Chemocentryx, Inc.
    Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
  • Publication number: 20100222331
    Abstract: The present invention encompasses compounds of general Formula (1) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: June 9, 2008
    Publication date: September 2, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald Engelhardt, Bodo Betzemeier, Guido Boehmelt, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Daniel Kuhn, Jens Juergen Quant, Ulrich Reiser, Otmar Schaaf, Flavio Solca, Heinz Stadtmueller, Ulrike Tontsch-Grunt, Matthias Treu, Stephan Karl Zahn
  • Publication number: 20100197670
    Abstract: Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: and the use of the products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.
    Type: Application
    Filed: September 22, 2008
    Publication date: August 5, 2010
    Inventors: Maurizio Anzini, Antonio Giordani, Francesco Makovec, Andrea Cappelli, Salvatore Vomero, Gianfranco Caselli, Lucio Claudio Rovati
  • Patent number: 7767665
    Abstract: This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: August 3, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Kajino, Yutaka Nakayama, Akira Kawada, Haruhide Kimura, Taisuke Tawaraishi
  • Patent number: 7659267
    Abstract: As prophylactic and/or therapeutic agents for cardiovascular diseases, bone or joint diseases, infectious diseases, inflammatory diseases, kidney diseases, etc. having safe and excellent effects of cell death inhibition, MIF binding, etc., there are provided compounds represented by formula: [wherein, R1 represents a halogen atom, etc., R2 represents a group represented by formula: (wherein, R3 represents hydrogen atom, an optionally substituted alkoxy, etc., R4 represents hydrogen atom, bromine atom, cyano, etc., R5 represents hydrogen atom, hydroxy, etc., R6 represents hydrogen atom, etc., R7 represents hydrogen atom, etc.) etc., and n represents an integer of 0 to 4] or salts thereof.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: February 9, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Kajino, Yutaka Nakayama, Haruhide Kimura
  • Patent number: 7659265
    Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: February 9, 2010
    Assignee: Wyeth
    Inventor: Bogdan Kazimierz Wilk
  • Publication number: 20090258856
    Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: June 23, 2009
    Publication date: October 15, 2009
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
  • Patent number: 7595343
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: September 29, 2009
    Assignee: MethylGene, Inc.
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
  • Patent number: 7566707
    Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: July 28, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
  • Patent number: 7560456
    Abstract: The invention relates to 3-pyridylcarboxamide derivatives of formula (I): wherein the various symbols are as defined in the description, compositions thereof, methods for controlling pests by applying same, and processes for their preparation.
    Type: Grant
    Filed: May 6, 2003
    Date of Patent: July 14, 2009
    Assignee: Merial Limited
    Inventors: Koichi Araki, Tetsuya Murata, Koshi Gunjima, Norihiko Nakakura, Eiichi Shimojo, Dale Robert Mitchell, Henricus Maria Martinus Bastiaans, David Stephen Carver, Daniel Allen, Christian Arnold, Waltraud Hempel, Olga Malsam, Jutta Maria Waibel
  • Publication number: 20090143345
    Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
    Type: Application
    Filed: February 12, 2009
    Publication date: June 4, 2009
    Applicant: Wyeth
    Inventor: Bogdan Kazimierz Wilk
  • Publication number: 20090093457
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: December 10, 2008
    Publication date: April 9, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
  • Publication number: 20090082343
    Abstract: This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
    Type: Application
    Filed: April 8, 2008
    Publication date: March 26, 2009
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Kajino, Yutaka Nakayama, Akira Kawada, Haruhide Kimura, Taisuke Tawaraishi
  • Publication number: 20090029975
    Abstract: A compound represented by the formula (I) or a salt thereof: (I) wherein R1 independently represents a halogen atom, a hydroxy, a nitro, an alkyl, alkenyl or alkynyl which may be halogenated, an alkoxy which may have a substituent, an acyl or an amino which may have a substituent; R2 represents a hydrogen atom or a hydrocarbon group which may have a substituent; R3 represents an electron-attracting group; n is an integer of 0 to 2; and m is an integer of 1 to 6. The compound has a capability of binding to a macrophage migration inhibitory factor (MIF), and is therefore useful as a prophylactic/therapeutic agent for a disease induced by oxidative stress or the like.
    Type: Application
    Filed: June 8, 2006
    Publication date: January 29, 2009
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Toshihiro Imaeda
  • Patent number: 7482337
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: October 28, 2003
    Date of Patent: January 27, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
  • Patent number: 7470681
    Abstract: This invention features pyrimidine compounds of formula (I): R1 is each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: December 30, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostik, Yumiko Wada
  • Patent number: 7465725
    Abstract: This invention features pyrimidine compounds of formula (I): R1 is aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: December 16, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Mitsunori Ono, Lijun Sun, Teresa Przewloka, Shijie Zhang, Elena Kostik, Weiwen Ying, Yumiko Wada, Keizo Koya
  • Publication number: 20080221089
    Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
    Type: Application
    Filed: February 12, 2008
    Publication date: September 11, 2008
    Inventors: Ankush Argade, Arvinder Sran, David Carroll, Jeffrey Clough, Kin Tso, Somasekhar Bhamidipati, Sambaiah Thota, Rajinder Singh, Vanessa Taylor, Hui Li, Esteban Masuda
  • Patent number: 7399759
    Abstract: This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
    Type: Grant
    Filed: September 2, 2002
    Date of Patent: July 15, 2008
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Kajino, Akira Kawada, Yutaka Nakayama, Haruhide Kimura, Taisuke Tawaraishi
  • Patent number: 7354915
    Abstract: Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: April 8, 2008
    Assignee: Wyeth
    Inventors: Puwen Zhang, Jeffrey Kern
  • Patent number: 7312211
    Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.
    Type: Grant
    Filed: August 26, 2004
    Date of Patent: December 25, 2007
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
  • Publication number: 20070213526
    Abstract: Processes are provided for purifying a compound of the structure: wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.
    Type: Application
    Filed: March 5, 2007
    Publication date: September 13, 2007
    Applicant: Wyeth
    Inventors: Mahmut Levent, Panolil Raveendranath, Bogdan Wilk, Donald Carl Boop, Marinus Cornelis Hofman
  • Publication number: 20070191603
    Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: February 7, 2007
    Publication date: August 16, 2007
    Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
  • Patent number: 7148217
    Abstract: This invention pertains to methods for controlling invertebrate pests comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula (I) wherein B is O, S or NR1; J is a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5; and R1, R2, R4, R5 and n are as defined in the disclosure.
    Type: Grant
    Filed: October 15, 2002
    Date of Patent: December 12, 2006
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas Paul Selby
  • Patent number: 6995154
    Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: February 7, 2006
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
  • Patent number: 6982261
    Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1–5; p=1–4; q=1–4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 15, 2003
    Date of Patent: January 3, 2006
    Assignees: Wyeth, Ligand Pharmaceuticals, Inc.
    Inventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Publication number: 20040186092
    Abstract: The invention provides compounds of the formula: 1
    Type: Application
    Filed: March 10, 2004
    Publication date: September 23, 2004
    Applicant: Roche Palo Alto LLC
    Inventors: David Bruce Repke, Russell Stephen Stabler, Ralph New Harris
  • Publication number: 20040186021
    Abstract: The invention relates to novel substituted benzo-nitrogen heterocycles of the formula (I) 1
    Type: Application
    Filed: January 9, 2004
    Publication date: September 23, 2004
    Inventors: Otto Schallner, Dorothee Hoischen, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 6794383
    Abstract: The present invention is intended to provide excellent preventives and/or remedies for heart diseases. Specifically, the present invention provides heart muscle cell apoptosis inhibitors, preventives and/or remedies for heart diseases, comprising a compound represented by the following formula: wherein R represents an optionally substituted hydrocarbon group, an optionally substituted aromatic heterocyclic group, or an optionally substituted amino group; or a salt thereof.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: September 21, 2004
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Haruhide Kimura, Seiichi Tanida, Tatsuhiko Kaneko
  • Publication number: 20040176361
    Abstract: The fused heterocyclic compound of the present invention, which is represented by the formula (I): 1
    Type: Application
    Filed: February 24, 2004
    Publication date: September 9, 2004
    Inventors: Masakazu Fujio, Hiroyuki Satoh, Atsushi Numata, Shinichi Takanashi, Yasuhiro Egi, Ryou Tatsumi
  • Publication number: 20040152696
    Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel 2-substituted bicyclic benzoheterocyclic compounds of Formula I: 1
    Type: Application
    Filed: July 29, 2003
    Publication date: August 5, 2004
    Applicant: Euro-Celtique S.A.
    Inventors: Qun Sun, Donald J. Kyle, Samuel F. Victory
  • Publication number: 20040132724
    Abstract: Compounds of formula (I) are modulators of STAT6 signal pathway activity, and can be used in the treatment of atopic dermatitis, urticaria, allergic asthma, allergic rhinitis, a food allergy, allergic conjunctivitis, hayfever, bullous pemphigoid, industrial sensitization, chronic rejection of transplants or COPD.
    Type: Application
    Filed: September 29, 2003
    Publication date: July 8, 2004
    Inventors: Hakan Bladh, Thomas Hansson, Grigorios Nikitidis, Carita Norden, Lars Pettersson, Mikael Varga