The Hetero Ring Contains Plural Oxygens Patents (Class 540/61)
Two of the cyclos share at least three ring members or a ring carbon is shared by three of the cyclos (e.g., bridged, peri-fused, etc.) (Class 540/62)
The hetero ring is ortho-fused to the d ring (Class 540/63)
  • Process for preparation of glucocorticoid steroids
    Patent number: 10233210
    Abstract: The present invention discloses a process for the preparation of 16, 17-acetals of pregnane derivatives having formula I wherein each substituent is independently selected from; R1 is H or CH3; R2 is C1-C6 linear or branched alkyl, alkynyl group or cycloalkyl group; aryl or heteroaryl group; or R1 and R2 combine to form saturated, unsaturated C3-C6 cyclic or heterocyclic ring; R3 and R4 are same or different and each independently represents H or halogen; R5 is —OH or —OCOR wherein R represents H or C1-C6 linear, branched or cyclic alkyl group that may be substituted.
    Type: Grant
    Filed: January 29, 2016
    Date of Patent: March 19, 2019
    Assignee: Coral Drugs Pvt. Ltd.
    Inventors: Vinayak Tripathi, Rajesh Kumar, Rohit Bhuwania, Binay Kumar Bhuwania
  • Contraceptive agents
    Patent number: 9670247
    Abstract: The invention provides compounds of formula I, II, III, or IV: wherein R1 to R11, X, and Y have any of the values defined in the specification. The compounds inhibit Na, K-ATPase ?4 and are useful as contraceptive agents.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: June 6, 2017
    Assignees: The University of Kansas, Regents of The University of Minnesota
    Inventors: Gustavo Blanco, Gunda I. Georg, Shameem Sultana Syeda
  • 2? oxo-voruscharin and derivatives thereof
    Patent number: 7981875
    Abstract: Compounds and pharmaceutical compositions which include 2? oxo-voruscharin and derivatives are disclosed. The compounds and pharmaceutical compositions are useful in methods of treating cancer, particularly pancreatic cancer.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: July 19, 2011
    Assignees: Unibioscreen S.A., Universite Libre de Bruxelles
    Inventors: Eric Van Quaquebeke, Jean-Claude Braekman, Gentiane Simon, Pierre Guissou, Odile Germaine Nacoulma, Janique Dewelle, Francis Darro, Robert Kiss
  • Use of the combination of ciclesonide and antihistamines for the treatment of allergic rhinitis
    Patent number: 7879832
    Abstract: The present invention relates to a combination of ciclesonide with antihistamines.
    Type: Grant
    Filed: August 29, 2003
    Date of Patent: February 1, 2011
    Assignee: Nycomed GmbH
    Inventors: Degenhard Marx, Helgert Müller
  • PROCESSES FOR THE PREPARATION OF CICLESONIDE AND ITS CRYSTAL MODIFICATION
    Publication number: 20100222572
    Abstract: Improved processes for the synthesis of ciclesonide, chemically termed as [11?,16?(R)]-16,17-[(cyclohexylmethylene)bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)pregna-1,4-diene-3,20-dione and its crystal modification.
    Type: Application
    Filed: September 18, 2007
    Publication date: September 2, 2010
    Applicant: CIPLA LIMITED
    Inventors: Manjinder Singh Phull, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
  • METHOD OF MAKING AND USING 7alpha,11beta-DIMETHYL-17beta-HYDROXYESTR-4-EN-3-ONE 17-UNDECANOATE
    Publication number: 20090023695
    Abstract: Methods of using 7?,11?-dimethyl-17?-hydroxy-4-estren-3-one bucyclate (I) and 7?,11?-dimethyl-17?-hydroxyestr-4-en-3-one 17-undecanoate (II) for various hormonal therapies, dosage forms comprising 7?,11?-dimethyl-17?-hydroxy-4-estren-3-one bucyclate and 7?,11?-dimethyl-17?-hydroxyestr-4-en-3-one 17-undecanoate, and processes for their preparation.
    Type: Application
    Filed: August 1, 2008
    Publication date: January 22, 2009
    Applicants: and Human Services
    Inventors: Richard P. Blye, Hyun K. Kim
  • 2? oxo-voruscharin and derivatives thereof
    Patent number: 7320971
    Abstract: 2? oxo-voruscharin compound and derivatives thereof are disclosed as well as pharmaceutical compositions which include 2? oxo-voruscharin compound or derivatives thereof. The disclosed 2? oxo-voruscharin compound and its derivatives are useful for cancer treatment. Methods of treating cancer using the disclosed compounds are also disclosed.
    Type: Grant
    Filed: October 9, 2003
    Date of Patent: January 22, 2008
    Assignee: Unibioscreen S.A.
    Inventors: Eric Van Quaquebeke, Jean-Claude Braekman, Gentiane Simon, Pierre Guissou, Odile Germaine Nacoulma, Janique Dewelle, Francis Darro, Robert Kiss
  • 3-nitrogen-6, 7-dioxygen steroids and uses related thereto
    Patent number: 7112580
    Abstract: 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: Grant
    Filed: July 21, 2003
    Date of Patent: September 26, 2006
    Assignee: Inflazyme Pharmaceuticals Ltd.
    Inventors: Jeffery R Raymond, Claudia E Kasserra, Yaping Shen
  • 3-nitrogen-6,7-dioxygen steroids and uses related thereto
    Patent number: 6635629
    Abstract: A compound of the formula or pharmaceutically acceptable salts, solvates, and stereoisomers thereof, in isolation or in mixture, wherein the 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: Grant
    Filed: April 30, 2001
    Date of Patent: October 21, 2003
    Assignee: Inflazyme Pharmaceuticals Ltd.
    Inventors: Jeffery R. Raymond, Claudia E. Kasserra, Yaping Shen
  • Stereoselective transacetalization of steroidal C-22 acetonide
    Publication number: 20030088090
    Abstract: The present invention is a process for the preparation of rofleponide of formula (II) 1
    Type: Application
    Filed: September 19, 2002
    Publication date: May 8, 2003
    Inventors: Lisa M. Reeder, Corey L. Stanchina
  • HIV integrase inhibitors
    Patent number: 6271402
    Abstract: Compound of formula I: wherein the R groups are as defined by the specification. The compounds are useful in the inhibition of HIV integrase, the treatment of infection of HIV and treatment of AIDS.
    Type: Grant
    Filed: December 13, 1999
    Date of Patent: August 7, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Sheo Bux Singh, Deborah L. Zink, Daria Jean Hazuda, Peter J. Felock, Anne W. Dombrowski
  • 6,7-oxygenated steroids and uses related thereto
    Patent number: 6046185
    Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6.alpha. and 7.beta. oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6.alpha. and 7.beta. oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and .delta.-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: April 4, 2000
    Assignees: Inflazyme Pharmaceuticals Ltd., The University of British Columbia, The University of Alberta
    Inventors: David L. Burgoyne, Yaping Shen, John M. Langlands, Christine Rogers, Joseph H.-L. Chau, Edward Piers, Hassan Salari
  • Silyl Compounds and their use
    Patent number: 5728826
    Abstract: The invention describes a process for the epimer enrichment of compounds of formula (I) by silation, fractionated crystallization and acid hydrolysis.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: March 17, 1998
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Beate Gutterer
  • Process for preparation of 9.alpha. -chloro-11.beta. formyloxypregna-3.20-diones
    Patent number: 5670676
    Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethylformamide; at a temperature within the range of about -78.degree. to about 0.degree. C.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: September 23, 1997
    Assignee: Schering Corporation
    Inventors: Richard W. Draper, Eugene J. Vater
  • Process for preparation of 9.alpha.-chloro-11.beta.-formyloxypregna-3,20-diones
    Patent number: 5602248
    Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethyl formamide; at a temperature within the range of about -78.degree. to about 0.degree. C., under anhydrous conditions under an inert atmosphere.
    Type: Grant
    Filed: March 16, 1995
    Date of Patent: February 11, 1997
    Assignee: Schering Corporation
    Inventors: Richard W. Draper, Eugene J. Vater
  • Process for the manufacture of budesonide
    Patent number: 5556964
    Abstract: The present invention relates to a novel process for the manufacture of (22 R,S)-16.alpha., 17.alpha.-butylidenedioxy-11.beta., 21-dihydroxypregna-1,4-diene-3,20 dione (I) by reacting 11.beta., 16.alpha., 17.alpha. 21-tetrahydroxypregna-1,4-diene (II) with butanal, CH.sub.3-- CH.sub.2 --CH.sub.2 --CHO, in acetonitrile in presence of p-toluenesulphonic acid as a catalyst.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: September 17, 1996
    Assignee: Aktiebolaget Astra
    Inventors: Robert G. Hofstraat, Petrus H. Raijmakers, Pieter Vrijhof
  • Antihypercholesterolemic compounds and related pharmaceutical compositions and methods of use
    Patent number: 5510340
    Abstract: Novel antihypercholesterolemic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R is a C-17 side chain, R.sup.1 is --OH, .dbd.O, or the like, and X and Y are N, N.fwdarw.O, CH, C--OH, C--OCH.sub.3 or C--Z. Methods of using the compound of formula (I) or other novel oxysterol analogs to treat hypercholesterolemia are provided, as are pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: April 23, 1996
    Assignee: SRI International
    Inventors: Wesley K. M. Chong, Wan-Ru Chao, Dennis M. Yasuda, John G. Johansson, Mitchell A. Avery, Masato Tanabe
  • 16,17-acetalsubstituted pregnane 21-oic acid derivatives
    Patent number: 5215979
    Abstract: The invention refers to compounds having activity against inflammatory, allergic, and dermatological conditions. The compounds are characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula R.sub.1 is selected from a straight or branched hydrocarbon chain having 1-4 carbon atoms.The invention also refers to processes for the preparation of these compounds, pharmaceutical preparations containing one of the compounds and a method for the treatment of inflammatory, allergic, muscoskeletal and dermatological conditions.
    Type: Grant
    Filed: October 16, 1991
    Date of Patent: June 1, 1993
    Assignee: Aktiebolaget Draco
    Inventors: Paul H. Andersson, Per T. Andersson, Bengt I. Axelsson, Ralph L. Brattsand, Bror A. Thalen, Jan W. Trofast
  • 16,17-acetalsubstituted androstane-17.beta.-carboxylic acid esters prossessing high binding affinity to the glucocorticosteroid receptor
    Patent number: 4950659
    Abstract: The invention refers to compounds having anti-inflamatory activity characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula the 1,2-position is saturated or is a double bondX.sub.1 is selected from hydrogen, fluorine, chlorine and bromineX.sub.2 is selected from hydrogen, fluorine, chlorine and bromineR.sub.1 is selected from hydrogen or a straight or branched hydrocarbon chain having 1-4 carbon atomsR.sub.2 is selected from hydrogen or straight and branched hydrocarbon chains having 1-10 carbon atoms andR.sub.3 is selected from ##STR2## is O or S R.sub.4 is selected from hydrogen, straight or branched hydrocarbon chains having 1-10 carbon atoms or from phenylR.sub.5 is selected from hydrogen or methyl andR.sub.
    Type: Grant
    Filed: March 25, 1986
    Date of Patent: August 21, 1990
    Assignee: Aktiebolaget Draco
    Inventors: Paul H. Andersson, Per T. Andersson, Bengt I. Axelsson, Bror A. Thalen, Jan W. Trofast