Chalcogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/25)
  • Patent number: 8101605
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: January 24, 2012
    Assignee: Aquinox Pharmaceuticals Inc.
    Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
  • Publication number: 20110319440
    Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.
    Type: Application
    Filed: September 2, 2011
    Publication date: December 29, 2011
    Applicant: GRUENENTHAL GmbH
    Inventors: Claudia HINZE, Otto Aulenbacher, Bernd Sundermann, Stefan Oberboersch, Elmar Friderichs, Werner Englberger, Babette-Yvonne Koegel, Klaus Linz, Hans Schick, Helmut Sonnenschein, Birgitta Henkel, Valerie Sarah Rose, Michael Jonathan Lipkin
  • Publication number: 20110178065
    Abstract: Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
    Type: Application
    Filed: January 13, 2011
    Publication date: July 21, 2011
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Publication number: 20110136802
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
    Type: Application
    Filed: December 3, 2010
    Publication date: June 9, 2011
    Applicant: Aquinox Pharmaceuticals Inc.
    Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
  • Publication number: 20110086821
    Abstract: Methods and compositions for treating Cryptosporidium parvum related disorders in a mammal are discussed. Several novel tetracycline compounds useful for treating Cryptosporidium parvum related disorders are also included.
    Type: Application
    Filed: October 4, 2010
    Publication date: April 14, 2011
    Applicant: Trustees of Tufts College
    Inventors: Stuart B. Levy, Mark L. Nelson
  • Publication number: 20100247797
    Abstract: A photocurable composition is provided that includes a compound represented by Formula (I) below, in Formula (I), X denotes O, S, or NRa, n1 denotes 0 or 1, and R1 to R14 and Ra independently denote a hydrogen atom, a halogen atom, or a monovalent substituent, at least one of R1 to R14 and Ra not being a hydrogen atom.) There is also provided an inkjet recording method that includes (a1) a step of discharging the photocurable composition onto a recording medium and (b1) a step of curing the photocurable composition by irradiating the discharged photocurable composition with light.
    Type: Application
    Filed: March 26, 2010
    Publication date: September 30, 2010
    Applicant: FUJIFILM CORPORATION
    Inventor: Tsutomu UMEBAYASHI
  • Publication number: 20100204186
    Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.
    Type: Application
    Filed: April 22, 2010
    Publication date: August 12, 2010
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventor: Mark L. Nelson
  • Patent number: 7595309
    Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Grant
    Filed: May 24, 2004
    Date of Patent: September 29, 2009
    Assignees: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Beena Bhatia, David Messersmith, Mohamed Y. Ismail, Todd Bowser, Laura McIntyre, Darrell J. Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul K. Verma, Tadeusz Warchol, Upul Bandarage
  • Patent number: 7329654
    Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: February 12, 2008
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ramesh M. Kanojia, Nareshkumar F. Jain, Raymond Ng, Zhihua Sui, Jiayi Xu
  • Patent number: 7326696
    Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.
    Type: Grant
    Filed: December 15, 2003
    Date of Patent: February 5, 2008
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Kwasi Ohemeng, Roger Frechette, Paul Abato, Victor Amoo, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Laura Honeyman, Mohamed Y. Ismail, Oak Kim, Rachid Mechiche, N. Laxma Reddy, Atul K. Verma, Peter Viski, Tadeusz Warchol, Ivan Yanachkov
  • Patent number: 6858732
    Abstract: Benzodioxino-naphtho[1,2-b]pyran compounds having particularly advantageous photochromic properties, such as, high sensitivity/coloration, two distinct absorption bands in the 430-500 nm range and 520-620 nm range of the visible spectrum may be generally described as a naphthopyran having a central nucleus of the formula: wherein F is a 1,4-benzodioxine ring with its 2,3 positions fused to the i, j, or k faces; and R1 and R2 are the atoms or groups providing photochromic properties to the naphthopyran.
    Type: Grant
    Filed: March 1, 2002
    Date of Patent: February 22, 2005
    Assignee: Vision-Ease Lens, Inc.
    Inventors: Xuzhi Qin, J. Thomas Ippoliti
  • Patent number: 6818635
    Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: November 16, 2004
    Assignees: Paratek Pharmaceuticals, Inc., Trustees of Tufts College
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Beena Bhatia, David Messersmith
  • Publication number: 20020193354
    Abstract: The present invention pertains to novel 7,9-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: June 29, 2001
    Publication date: December 19, 2002
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Laura McIntyre, Beena Bhatia, Paul Hawkins, Laxma Reddy, Karen Stapleton, Tad Warchol, Paul Sheahan
  • Publication number: 20020103177
    Abstract: An androgenic steroid compound of the formula: 1
    Type: Application
    Filed: January 22, 2002
    Publication date: August 1, 2002
    Inventors: C. Edgar Cook, John A. Kepler, Yue-Wei Lee, Mansukh C. Wani
  • Patent number: 6398987
    Abstract: The present invention relates to novel compounds of the naphthopyran type which have a perfluoroalkyl group (X) in position 5. These compounds are of formula (I) given below: These compounds (I) possess interesting photochromic properties. The invention also relates to their preparation, their applications as photochromes as well as the compositions and matrices containing them.
    Type: Grant
    Filed: November 3, 2000
    Date of Patent: June 4, 2002
    Assignee: Corning S.A.
    Inventors: Olivier Breyne, You-Ping Chan, Patrick Jean
  • Patent number: 6384045
    Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: May 7, 2002
    Assignee: Kansas State University Research Foundation
    Inventors: Duy H. Hua, Jean-Pierre Perchellet
  • Patent number: 5998464
    Abstract: The compounds of the present invention are those of structural formula (I) ##STR1## wherein X is oxygen or sulfur. Pharmaceutical compositions and methods of use of the compounds in the treatment of hyperandrogenic conditions are disclosed. In addition, the combination of the compounds with other active agents such as finasteride, minoxidil and retinoic acid or a derivative thereof is disclosed.
    Type: Grant
    Filed: April 23, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Gool F. Patel, Gary H. Rasmusson, Richard L. Tolman
  • Patent number: 5958970
    Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.
    Type: Grant
    Filed: July 29, 1997
    Date of Patent: September 28, 1999
    Assignee: Kansas State University Research Foundation
    Inventors: Duy H. Hua, Jean-Pierre Perchellet
  • Patent number: 5955493
    Abstract: The present invention relates to morphinan derivatives that are neuroprotective against excitatory amino acid (EAA) cytotoxicity. In particular, morphinan derivatives of the invention act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor and are useful as protective agents against peripheral and central nervous system NMDA-receptor mediated toxicity and convulsions.
    Type: Grant
    Filed: April 30, 1998
    Date of Patent: September 21, 1999
    Assignee: Biochem Pharma, Inc.
    Inventor: Simon Lemaire
  • Patent number: 5645768
    Abstract: A photochromic compound, in particular, for tinting optical elements made of a plastic material has reduced mobility in plastic material. The photochromic compound is a photochromic 2H-pyran and is distinguished by the aromatic residues being chemically rigidly attached in the 2-position to a spiropyran.
    Type: Grant
    Filed: December 28, 1995
    Date of Patent: July 8, 1997
    Assignee: Optische Werke G. Rodenstock
    Inventors: Manfred Melzig, Herbert Zinner
  • Patent number: 5310909
    Abstract: Compounds of the formula I ##STR1## in which X is O, S, SO, SO.sub.2 or NR.sub.13, R.sub.13 is, for example, methyl, and R.sub.1 to R.sub.12, independently of one another, are, for example, H, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 Alkoxy, halogen or --CN. The compounds are photosensitive and photochromic and are suitable as photosensitizers and simultaneously as color indicators, and as photoswitchable color filters.
    Type: Grant
    Filed: November 21, 1990
    Date of Patent: May 10, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Evelyn Fischer, Walter Fischer, Jurgen Finter, Kurt Meier, Martin Roth
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5225554
    Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring material. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.
    Type: Grant
    Filed: July 18, 1990
    Date of Patent: July 6, 1993
    Assignee: SRI International
    Inventors: Mitchell A. Avery, Clive Jennings-White
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5177218
    Abstract: Compounds of formula I or III or mixtures thereof ##STR1## wherein R is unsubstituted C.sub.6 -C.sub.14 aryl or C.sub.6 -C.sub.14 aryl which is substituted by C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, phenyl, benzyl, --CN, --CF.sub.3, halogen or --COOR.sub.3, x is 1 or 2, and R.sub.1 is H, linear or branched C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl or C.sub.2 -C.sub.12 alkynyl, C.sub.7 -C.sub.16 aralkyl, C.sub.8 -C.sub.16 alkaralkyl, --CH.sub.2 COOR.sub.3 or C.sub.1 -C.sub.12 acyl, wherein R.sub.3 is H, C.sub.1 -C.sub.18 alkyl, cyclohexyl, cyclopentyl, phenyl, C.sub.1 -C.sub.12 alkylphenyl, benzyl or C.sub.1 -C.sub.12 alkylbenzyl, are reversible photochromic systems which can be used for contrast formation, light absorption or for the reversible optical storage of information.
    Type: Grant
    Filed: December 30, 1991
    Date of Patent: January 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Jurgen Finter, Heinz Spahni
  • Patent number: 5104985
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: April 14, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 5047554
    Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
    Type: Grant
    Filed: January 31, 1990
    Date of Patent: September 10, 1991
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
  • Patent number: 4853410
    Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: August 1, 1989
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Patent number: 4585876
    Abstract: Novel xanthones and thioxanthones of the formula I ##STR1## in which A, X, Y, Z, E and E' are as defined in patent claim 1, are described. A is preferably --S-- and E and E' are preferably bonded in the ortho-position relative to one another. The compounds (I) are suitable, for example, as sensitizers for photocrosslinkable polymers or photocurable compositions, or for use in mixtures with polymers with H donor groups for image formation, in particular electrically conductive coatings and patterns, by means of electroless deposition of metals.
    Type: Grant
    Filed: November 14, 1983
    Date of Patent: April 29, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Jurgen Finter, Hans Zweifel
  • Patent number: 4565779
    Abstract: Novel photochromic compounds are disclosed, which compounds are represented by the general formula ##STR1## in which R.sub.1 represents an alkyl group having 1 to 20 carbon atoms, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently represent an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a halogen atom, a nitro group, a cyano group or a dimethylamino group, and R.sub.6, R.sub.7 and R.sub.8 independently represent a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, or a halogen atom, and correspondingly 97 to 50 wt % of a film-forming polymer. Photosensitive compositions and materials comprising the compounds are also described.
    Type: Grant
    Filed: December 23, 1983
    Date of Patent: January 21, 1986
    Assignee: Sony Corporation
    Inventors: Seiichi Arakawa, Hirofumi Kondo, Junetsu Seto
  • Patent number: 4312868
    Abstract: Isothiochromans are described. The compounds possess hypotensive and antipsychotic properties; methods and compositions using them are described.
    Type: Grant
    Filed: May 15, 1979
    Date of Patent: January 26, 1982
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4229582
    Abstract: A process for the preparation of racemic 6-thiatetracycline derivatives comprises treating a mixture of epimers of corresponding 1,4,4a,5,5a,6,11,12a-octahydro-3,12-dihydroxy-1,11-dioxo-6-thianaphthacene -2-carboxamides with a saturated heterocyclic secondary amine having a total of 4 to 12 carbon atoms for a sufficient length of time at temperatures of about 15.degree.-120.degree. C.
    Type: Grant
    Filed: October 13, 1978
    Date of Patent: October 21, 1980
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventor: Richard Kirchlechner