Chalcogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/25)
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Patent number: 8101605Abstract: 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: GrantFiled: December 3, 2010Date of Patent: January 24, 2012Assignee: Aquinox Pharmaceuticals Inc.Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
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Publication number: 20110319440Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.Type: ApplicationFiled: September 2, 2011Publication date: December 29, 2011Applicant: GRUENENTHAL GmbHInventors: 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
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Publication number: 20110178065Abstract: 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: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Applicant: BIOMARIN PHARMACEUTICAL INC.Inventors: Daniel Chu, Bing Wang, Tao Ye
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Publication number: 20110136802Abstract: 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: ApplicationFiled: December 3, 2010Publication date: June 9, 2011Applicant: Aquinox Pharmaceuticals Inc.Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
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Publication number: 20110086821Abstract: 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: ApplicationFiled: October 4, 2010Publication date: April 14, 2011Applicant: Trustees of Tufts CollegeInventors: Stuart B. Levy, Mark L. Nelson
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Publication number: 20100247797Abstract: 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: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: FUJIFILM CORPORATIONInventor: Tsutomu UMEBAYASHI
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Publication number: 20100204186Abstract: Aromatized A-ring derivatives of tetracycline compounds are described.Type: ApplicationFiled: April 22, 2010Publication date: August 12, 2010Applicant: Paratek Pharmaceuticals, Inc.Inventor: Mark L. Nelson
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Patent number: 7595309Abstract: 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: GrantFiled: May 24, 2004Date of Patent: September 29, 2009Assignees: 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
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Patent number: 7329654Abstract: 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: GrantFiled: December 2, 2002Date of Patent: February 12, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Ramesh M. Kanojia, Nareshkumar F. Jain, Raymond Ng, Zhihua Sui, Jiayi Xu
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Patent number: 7326696Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.Type: GrantFiled: December 15, 2003Date of Patent: February 5, 2008Assignee: 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
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Patent number: 6858732Abstract: 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: GrantFiled: March 1, 2002Date of Patent: February 22, 2005Assignee: Vision-Ease Lens, Inc.Inventors: Xuzhi Qin, J. Thomas Ippoliti
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Patent number: 6818635Abstract: 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: GrantFiled: June 29, 2001Date of Patent: November 16, 2004Assignees: Paratek Pharmaceuticals, Inc., Trustees of Tufts CollegeInventors: Mark L. Nelson, Roger Frechette, Peter Viski, Beena Bhatia, David Messersmith
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Publication number: 20020193354Abstract: 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: ApplicationFiled: June 29, 2001Publication date: December 19, 2002Inventors: 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
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Publication number: 20020103177Abstract: An androgenic steroid compound of the formula: 1Type: ApplicationFiled: January 22, 2002Publication date: August 1, 2002Inventors: C. Edgar Cook, John A. Kepler, Yue-Wei Lee, Mansukh C. Wani
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Patent number: 6398987Abstract: 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: GrantFiled: November 3, 2000Date of Patent: June 4, 2002Assignee: Corning S.A.Inventors: Olivier Breyne, You-Ping Chan, Patrick Jean
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Patent number: 6384045Abstract: 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: GrantFiled: June 24, 1999Date of Patent: May 7, 2002Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 5998464Abstract: 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: GrantFiled: April 23, 1998Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Gool F. Patel, Gary H. Rasmusson, Richard L. Tolman
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Patent number: 5958970Abstract: 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: GrantFiled: July 29, 1997Date of Patent: September 28, 1999Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 5955493Abstract: 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: GrantFiled: April 30, 1998Date of Patent: September 21, 1999Assignee: Biochem Pharma, Inc.Inventor: Simon Lemaire
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Patent number: 5645768Abstract: 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: GrantFiled: December 28, 1995Date of Patent: July 8, 1997Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Herbert Zinner
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Patent number: 5310909Abstract: 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: GrantFiled: November 21, 1990Date of Patent: May 10, 1994Assignee: Ciba-Geigy CorporationInventors: Evelyn Fischer, Walter Fischer, Jurgen Finter, Kurt Meier, Martin Roth
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Patent number: 5276053Abstract: 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: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5225554Abstract: 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: GrantFiled: July 18, 1990Date of Patent: July 6, 1993Assignee: SRI InternationalInventors: Mitchell A. Avery, Clive Jennings-White
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Patent number: 5180736Abstract: 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: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5177218Abstract: 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: GrantFiled: December 30, 1991Date of Patent: January 5, 1993Assignee: Ciba-Geigy CorporationInventors: Walter Fischer, Jurgen Finter, Heinz Spahni
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Patent number: 5104985Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 28, 1991Date of Patent: April 14, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 5071853Abstract: 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: GrantFiled: February 27, 1990Date of Patent: December 10, 1991Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
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Patent number: 5047554Abstract: 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: GrantFiled: January 31, 1990Date of Patent: September 10, 1991Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 4853410Abstract: 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: GrantFiled: October 9, 1987Date of Patent: August 1, 1989Assignee: Pfizer Inc.Inventor: Christopher A. Lipinski
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Patent number: 4585876Abstract: 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: GrantFiled: November 14, 1983Date of Patent: April 29, 1986Assignee: Ciba-Geigy CorporationInventors: Walter Fischer, Jurgen Finter, Hans Zweifel
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Patent number: 4565779Abstract: 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: GrantFiled: December 23, 1983Date of Patent: January 21, 1986Assignee: Sony CorporationInventors: Seiichi Arakawa, Hirofumi Kondo, Junetsu Seto
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Patent number: 4312868Abstract: Isothiochromans are described. The compounds possess hypotensive and antipsychotic properties; methods and compositions using them are described.Type: GrantFiled: May 15, 1979Date of Patent: January 26, 1982Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4229582Abstract: 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: GrantFiled: October 13, 1978Date of Patent: October 21, 1980Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventor: Richard Kirchlechner