The Hetero Ring Is Ortho-fused To The A Ring Patents (Class 540/57)
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Publication number: 20120289471Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.Type: ApplicationFiled: April 18, 2012Publication date: November 15, 2012Applicant: SIGNATURE R&D HOLDINGS, LLCInventor: V. Ravi Chandran
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Publication number: 20120077789Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal.Type: ApplicationFiled: December 1, 2011Publication date: March 29, 2012Applicant: DMI ACQUISITION CORP.Inventor: David Bar-Or
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Publication number: 20120035147Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal.Type: ApplicationFiled: October 19, 2011Publication date: February 9, 2012Applicant: DMI ACQUISITION CORP.Inventor: David Bar-Or
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Publication number: 20110171307Abstract: The present invention relates to the treatment of diseases and conditions with an effective amount of a steroid having those formulas given in the specification, or a pharmacologically-acceptable salt or ester thereof. The disease or conditions treatable according to the invention include angiogenic diseases and conditions of the eye, angiogenic diseases and conditions of the brain, inflammatory diseases and conditions of the eye, inflammatory diseases and conditions of the brain and neurodegenerative diseases.Type: ApplicationFiled: March 25, 2011Publication date: July 14, 2011Inventor: DAVID BAR-OR
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Publication number: 20110171306Abstract: The present invention relates to the treatment of diseases and conditions with an effective amount of a steroid having those formulas given in the specification, or a pharmacologically-acceptable salt or ester thereof. The disease or conditions treatable according to the invention include angiogenic diseases and conditions of the eye, angiogenic diseases and conditions of the brain, inflammatory diseases and conditions of the eye, inflammatory diseases and conditions of the brain and neurodegenerative diseases.Type: ApplicationFiled: March 25, 2011Publication date: July 14, 2011Inventor: David Bar-Or
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Patent number: 7112580Abstract: A compound of the formula: and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein R groups are as defined by the present specification. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.Type: GrantFiled: July 21, 2003Date of Patent: September 26, 2006Assignee: Inflazyme Pharmaceuticals Ltd.Inventors: Jeffery R Raymond, Claudia E Kasserra, Yaping Shen
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Patent number: 7041839Abstract: The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorde. In an embodiment of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred embodiment, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.Type: GrantFiled: June 22, 2001Date of Patent: May 9, 2006Assignee: Northeastern UniversityInventors: Robert N. Hanson, Carolyn Friel, Choon Young Lee
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Patent number: 5232915Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.Type: GrantFiled: January 14, 1992Date of Patent: August 3, 1993Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
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Patent number: 5134135Abstract: 2'-Alkylsulfonylsteroido[2,3-d]oxazoles, for example 2'-methylsulfonyl-5.alpha.-pregn-2-en-20-yno[2,3-d]oxazol-17.beta.-ol, which are useful as antiandrogenic agents, and proceses for preparation, method of use and compositions thereof are disclosed.Type: GrantFiled: June 21, 1990Date of Patent: July 28, 1992Assignee: Sterling Drug Inc.Inventors: John P. Mallamo, Joseph R. Wetzel
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Patent number: 5053405Abstract: 2'-Alkylsulfonylsteroido[3,2-d]thiazoles, for example 2'-methylsulfonyl-5.alpha.-pregn-2-en-20-yno[3,2-d]thiazol-17.beta.-ol, which are useful as antiandrogenic agents, and processes for preparation, method of use and compositions thereof are disclosed.Type: GrantFiled: June 21, 1990Date of Patent: October 1, 1991Assignee: Sterling Drug Inc.Inventors: Garry M. Pilling, John P. Mallamo
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Patent number: 4755595Abstract: An improvement in the epoxidation of certain 4,5-unsaturated steroids with peracetic acid, which comprises carrying out the reaction in methanol solution.Type: GrantFiled: November 1, 1985Date of Patent: July 5, 1988Assignee: Sterling Drug Inc.Inventors: Karl O. Gelotte, Chester J. Opalka, Jr.
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Patent number: 4634696Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.Type: GrantFiled: July 30, 1985Date of Patent: January 6, 1987Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert
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Patent number: 4605517Abstract: The method of preparing a 2.alpha.-cyano-4.alpha.,5.alpha.-epoxy-3-oxo steroid or a steroid fused at the 2- and 3-positions with a heterocyclic ring of controlled particle size which comprises dissolving the steroid in an organic solvent, precipitating the steroid by mixing a non-solvent for the steroid with the resulting solution, and controlling the time of mixing and the degree of agitation during mixing.Type: GrantFiled: October 11, 1984Date of Patent: August 12, 1986Assignee: Sterling Drug Inc.Inventors: Derek C. Riley, David Johnston