Sulfur Bonded Directly To The Cyclopentanohydrophenanthrene Ring System Patents (Class 552/523)
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Publication number: 20110098260Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.Type: ApplicationFiled: December 1, 2010Publication date: April 28, 2011Applicant: Harbor BioSciences, Inc.Inventor: James M. Frincke
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Publication number: 20090325918Abstract: Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effect mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and it the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in men.Type: ApplicationFiled: June 16, 2008Publication date: December 31, 2009Inventors: John C. Somberg, Vassant V. Ranade
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Patent number: 7629334Abstract: The use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as components for the combined use together with an estrogen for the manufacture of a medicament for HRT as well as in respective HRT-methods and methods of treating hormone deficiency and hormone irregularity symptoms. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. J867, J912, J956 and J1042 are the mesoprogestins preferred herein.Type: GrantFiled: August 31, 2000Date of Patent: December 8, 2009Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Kristof Chwalisz, Walter Elger, Gerd Schubert
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Patent number: 7342004Abstract: There is provided use of a compound of Formula XI: wherein R3 is a sulphamate group and at least of R1 or R2 is a thioether group as disclosed by the present specification, capable of inhibiting steroid sulphatase.Type: GrantFiled: February 14, 2003Date of Patent: March 11, 2008Assignee: Sterix Ltd.Inventors: Barry Victor Lloyd Potter, Michael John Reed, Graham Keith Packham, Matthew Paul Leese
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Patent number: 6673783Abstract: Novel 17,20-methanofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.Type: GrantFiled: March 7, 2002Date of Patent: January 6, 2004Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Tore Duvold
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Publication number: 20030203855Abstract: There is provided a compound comprising a steroidal ring system and a group R1 selected from any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula —L—R3, wherein L is an optional linker group and R3 is an aromatic hydrocarbyl group.Type: ApplicationFiled: February 14, 2003Publication date: October 30, 2003Inventors: Barry Victor Lloyd Potter, Michael John Reed, Bertrand Leblond, Matthew Paul Leese
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Publication number: 20030176405Abstract: This invention describes the new 8&bgr;-substituted estratrienes of general formula I in which R2, R3, R6, R6′, R7, R7′, R9, R11, R11′, R12, R14, R15, R15′, R16, R16′, R17 and R17′ have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.Type: ApplicationFiled: April 1, 2003Publication date: September 18, 2003Inventors: Olaf Peters, Alexander Hillisch, Ina Thieme, Walter Elger, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier, Vladimir Patchev
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Publication number: 20030134829Abstract: A compound is described. The compound has the formula (Ia) as presented in the FIG. 1; wherein: X is a ring having at least 4 atoms in the ring; K is hydrocarbyl group; Rh1 is an optional halo group; Rh2 is an optional halo group; at least one of Rh1 and Rh2 is present; Rs is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group. The compound is capable of inhibiting steroid sulphatase (STS) activity.Type: ApplicationFiled: June 7, 2002Publication date: July 17, 2003Inventors: Michael John Reed, Barry Victor Lloyd Potter, Hatem Hejaz, Atul Purohit
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Patent number: 6593319Abstract: Novel 17,20-dihydrofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.Type: GrantFiled: August 14, 2001Date of Patent: July 15, 2003Assignee: Leo Pharmaceutical Products, Ltd. A/SInventors: Tore Duvold, Welf von Daehne
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Publication number: 20030064971Abstract: Novel 17,20-methanofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.Type: ApplicationFiled: March 7, 2002Publication date: April 3, 2003Inventor: Tore Duvold
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Patent number: 6534490Abstract: Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.Type: GrantFiled: December 21, 2000Date of Patent: March 18, 2003Assignee: Jenapharm GmbH & Co. KG.Inventors: Sven Ring, Sigfrid Schwarz, Walter Elger, Birgitt Schneider, Günter Kaufmann, Lothar Sobek
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Publication number: 20020193357Abstract: A compound of formula (I): 1Type: ApplicationFiled: May 2, 2002Publication date: December 19, 2002Inventors: Ching Song, Shutsung Liao
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Patent number: 6388109Abstract: Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are distinguished by hormonal (gestagenic and/or androgenic) activity.Type: GrantFiled: December 20, 2000Date of Patent: May 14, 2002Assignee: Jenapharm GmbH & Co. KGInventors: Sigfrid Schwarz, Gerd Schubert, Sven Ring, Walter Elger, Birgitt Schneider, Günter Kaufmann, Lothar Sobek
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Patent number: 6355630Abstract: This invention provides estrogens and antiestrogens of formula I having the structure wherein X, Y, Z, and R are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 13, 1998Date of Patent: March 12, 2002Assignee: American Home Products CorporationInventors: Chris P. Miller, Ivo Jirkovsky, Bach Dinh Tran
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Patent number: 6326503Abstract: A compound having the formula (4): wherein X is oxygen or sulfur, R9 and R10 are each a hydrogen or a protecting group, and R11 is an aliphatic hydrocarbon, a —COR12 group where R12 is alkyl, aryl or alkoxy, or a group of formula wherein R5 and R6 are each hydrogen or hydroxyl, m is 1 to 4, and n is 0-2.Type: GrantFiled: August 18, 2000Date of Patent: December 4, 2001Assignee: Chugai Seiyaku Kabushiki KaishaInventor: Akira Kawase
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Patent number: 6143737Abstract: The present invention is directed to compounds of formula I ##STR1## wherein the substituents are as defined in the specification. Also disclosed are compositions and method of use of the compounds.Type: GrantFiled: June 21, 1996Date of Patent: November 7, 2000Assignee: Georgetown UniversityInventors: Robert Clarke, Abdel H. Talebian, Alem Ghiorghis, Fabio Leonessa, Charles Hammer
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Patent number: 5892069Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.Type: GrantFiled: April 25, 1997Date of Patent: April 6, 1999Assignee: The Children's Medical Center CorporationInventors: Robert John D'Amato, Moses Judah Folkman
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Patent number: 5646316Abstract: The present invention relates to a bile acid derivative, which comprises a bile acid derivatized at the carboxyl group with a hydroxamic acid or hydroxamate ester. The carboxyl group in the bile acid compound can also be derivatized with an amino acid or oligopeptide, whose C-terminus is derivatized with a hydroxamic acid or a hydroxamate ester. The present invention also relates to a method of use of a bile acid or a bile acid derivative to inhibit a metalloproteinase enzyme, comprising contacting a metalloproteinase with an effective amount of a bile acid or bile acid derivative. In another embodiment, the present invention further relates to a method of use of a bile acid or bile acid derivative to therapeutically treat a disease, which is ameliorated by inhibiting a metalloproteinase enzyme. In this method, a therapeutically effective amount of a bile acid, a bile acid derivative or physiologically acceptable salts thereof, is administered to a human or other mammal.Type: GrantFiled: April 25, 1995Date of Patent: July 8, 1997Assignee: OsteoArthritis Sciences, Inc.Inventors: Alan R. Jacobson, Douglas G. Gabler, Jozef Oleksyszyn
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Patent number: 5321019Abstract: Compounds of formula I: ##STR1## in which the various R groups have the meanings defined in the disclosure are useful as medicaments for the treatment of hepatobiliary diseases.Type: GrantFiled: January 11, 1993Date of Patent: June 14, 1994Assignee: Giuliani S.p.A.Inventors: Giangermano Giuliani, Giuliano Frigerio, Roberto Pellicciari
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Patent number: 5093507Abstract: 10.beta.,11.beta.-bridged steroids of Formula I ##STR1## wherein R.sup.1 is H or methyl;R.sup.2 is H, a cyanide residue, a heteroaryl residue, a straight-chain or branched aliphatic, e.g., alkyl group of up to 20 carbon atoms, optionally exhibiting double or triple bonds and, if desired, being substituted by one or several oxo groups, a C.sub.4-7 cycloalkyl or C.sub.4-7 cycloalkenyl group, an OR.sup.3 --, SR.sup.3 --, --OSO.sub.2 --R.sup.11 -- group wherein R.sup.11 means a perfluroinated C.sub.1 -C.sub.4 -alkyl group or an NR.sup.3 R.sup.4 -group wherein R.sup.3 means an H atom or C.sub.1 -C.sub.8 -alkyl residue, R.sup.4 means R.sup.3, a cyanide or a C.sub.1 -C.sub.10 -acyl residue, or R.sup.3 and R.sup.4 jointly with the inclusion of N means of 5- or 6-membered heterocyclic ring wherein the ring can additionally contain a further hetero atom N, O, or S, or a 4-cyano-, 4-methoxy- or 4-dimethylamino-substituted phenyl group,A and B either mean jointly a further bond between C4 and C5, or A is an .alpha.Type: GrantFiled: June 16, 1989Date of Patent: March 3, 1992Assignee: Schering AktiengesellschaftInventors: Cornelius Scheidges, Eckhard Ottow, Gunter Neef, Sybille Beier, Walter Elger
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Patent number: 5086047Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl, alkylthio and haloalkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, optionally substituted arylthio of 6 to 10 carbon atoms, aryl of 6 to 12 carbon atoms, acyl of an organic carboxylic acid of 1 to 12 carbon atoms, --CN, cycloalkyl of 3 to 6 carbon atoms and --(CH.sub.2).sub.m --Re, m is an integer from 1 to 3, Re is --OH or --SH or --Salk, Alk is alkyl of 1 to 6 carbon atoms, X is selected from the group consisting of oxygen, N--O--R.sub.1, ##STR2## or =X is H.sub.2 or ##STR3## R.sub.A and R.sub.B are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 6 carbon atoms, R.sub.1 is hydrogen or alkyl of 1 to 6 carbon, R' is hydrogen or acyl, the wavy lines indicate --or -position, Y is selected from the group consisting of oxygen, NOR, ##STR4## or =Y is ##STR5## H.sub.Type: GrantFiled: December 24, 1990Date of Patent: February 4, 1992Assignee: Roussel Uclaf, Department des BrevetsInventors: Jean-Francois Gourvest, Dominique Lesuisse
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Patent number: 5034548Abstract: Lanosterols substituted in the 14 and/or 15 position(s) which are active in inhibiting lanosta-8,24-dien-3.beta.-ol 14.alpha.-methyl-demethylase activity, suppressing 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) activity, decreasing cholesterol synthesis and reducing serum cholesterol levels are disclosed.Type: GrantFiled: October 16, 1990Date of Patent: July 23, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: James L. Gaylor, Paul R. Johnson, Soo S. Ko, Ronald L. Magolda, Simon H. Stam, James M. Trzaskos
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Patent number: 4988684Abstract: A compound of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 6 carbon atoms unsubstituted or substituted with at least one member of the group consisting of alkoxy and alkylthio of 1 to 4 carbon atoms, --NO.sub.2, --CN and halogen, X and Y together are .dbd.O or Y is hydrogen and X is --OH, etherified --OH or esterified --OH, the dotted lines in the 1(2), 6(7) and 9(11) positions indicate a possible double bond with the proviso that R.sub.1 is alkyl of 1 to 6 carbon atoms when X and Y are .dbd.O and there is a double bond in at least one of the 1(2), 6(7) and 9(11) positions having aromatase inhibiting activity.Type: GrantFiled: December 21, 1989Date of Patent: January 29, 1991Assignee: Roussel UclafInventors: Jean-Francois Gourvest, Dominique Lesuisse, Daniel Philibert, Jean P. Vevert
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Patent number: 4987128Abstract: Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R.sub.Type: GrantFiled: February 24, 1987Date of Patent: January 22, 1991Assignee: Roussel UclafInventors: Lucien Nedelec, Francois Nique, Anne-Marie Moura
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Patent number: 4913852Abstract: Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of .DELTA.-4-pregnene-3,20-dione or with derivatives of .DELTA.-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields.Type: GrantFiled: February 24, 1988Date of Patent: April 3, 1990Inventors: Catherine Milioni, Constantin Efthyimiopoulos, Bernard Koch, Louis Jung, Jean Jung