Chalcogen In Chain Between The Hetero Ring And The Cyclopentanohydrophenanthrene Ring System Patents (Class 540/113)
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Publication number: 20010039268Abstract: A subject of the invention is the compounds of formula (I): 1Type: ApplicationFiled: December 8, 2000Publication date: November 8, 2001Applicant: Hoechst Marion RousselInventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
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Patent number: 6271403Abstract: This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I in which side chain SK is a radical of partial formula The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.Type: GrantFiled: April 14, 2000Date of Patent: August 7, 2001Assignee: Schering AktiengesellschaftInventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Künzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
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Patent number: 6258792Abstract: The present invention discloses compounds which are cationic cholesteryl derivatives having a nitrogen-containing ring structure as their polar head group. These compounds are useful for delivering biologically active substances to cells and for transfecting nucleic acids into cells.Type: GrantFiled: September 25, 2000Date of Patent: July 10, 2001Assignee: University of PittsburghInventors: Hermant M. Deshmukh, Leaf Huang
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Patent number: 6180618Abstract: Compounds of formula (I) in which the radicals are as defined in the specification and claims, and physiologically tolerated and physiologically functional derivatives thereof and processes for their preparation are described. The compounds are suitable, for example, as hypolipidemic agents.Type: GrantFiled: September 29, 1999Date of Patent: January 30, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Siegfried Stengelin, Alfons Enhsen, Heiner Glombik, Werner Kramer, Eugen Falk
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Patent number: 6080735Abstract: This invention is relating to new estra-1,3,5(10)-trien-sulfamates carrying at the 3-position an R--SO.sub.2 --O--group, with R being an R.sup.1 R.sup.2 N--group in which R.sup.1 and R.sup.2, independently of each other, represent a hydrogen atom, an alkyl residue with 1-5 C atoms or, together with the N atom, a polymethylene-imino residue with 4-6 C atoms or a morpholino residue.The compounds, according to this invention, are suitable for hormonal contraception and climacteric hormone replacement therapy (HRT) as well as for treatment of gynecological and andrological diseases. Hence, only low hepatic estrogenicity is exhibited by the compounds according to this invention.Also described are processes for preparation of the compounds according to this invention and for preparation of pharmaceutical compositions.Type: GrantFiled: February 2, 1998Date of Patent: June 27, 2000Assignee: Jenapharm GmbH & Co. KGInventors: Sigfrid Schwarz, Walter Elger, Hans-Joachim Siemann, deceased, by Margit Lucas, heir, by Frank Siemann, heir, Gudrun Reddersen, Birgitt Schneider
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Patent number: 6046186Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.Type: GrantFiled: December 24, 1997Date of Patent: April 4, 2000Assignee: SRI InternationalInventors: Masato Tanabe, Richard H. Peters, Wan-Ru Chao, Kazuhiko Shigeno
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Patent number: 5866560Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.Type: GrantFiled: August 20, 1997Date of Patent: February 2, 1999Assignee: Schering AGInventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
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Patent number: 5824670Abstract: 17-Deoxycorticoid-21-carboxylic esters of the formula I ##STR1## are described, in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl and R(2) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(4) is OH, with an activated carboxylic acid of the formula III,R(5)-CO--X-R(1) III.The compounds I possess very strong local and topical antiinflammatory activity and exhibit a very good ratio of local to systemic antiinflammatory effect, which ratio is often clearly superior to that of structurally related corticoid 21-esters which do not carry any aryl or hetaryl group in the 21-ester residue or to that of analogous 17-deoxycorticoids having an unesterified, that is a free, 21-hydroxyl group.Type: GrantFiled: September 18, 1995Date of Patent: October 20, 1998Assignee: Hoechst AktiengesellschaftInventors: Ulrich Stache, Hans-Georg Alpermann, Manfred Bohn
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Patent number: 5760214Abstract: A compound represented by the following formula (I):X--Y--Z (I)?where Y is represented by the following formula (III): ##STR1## X is a monovalent group of a tetracycline type compound, and Z is a monovalent group of a steroid type compound such as estrogen!. The compound can concentrate on the bone tissue and has a bone resorption inhibition/ossification promotion functions.Type: GrantFiled: March 1, 1995Date of Patent: June 2, 1998Assignees: Iskra Industry Co., Ltd., Institute of Pharmacology, West China Univ. of Medical SciencesInventors: Hu Zheng, Lingling Weng
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Patent number: 5760025Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.Type: GrantFiled: March 31, 1995Date of Patent: June 2, 1998Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Hitoshi Kurata, Koki Ishibashi, Hiroyoshi Horikoshi, Takakazu Hamada
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Patent number: 5707982Abstract: A 19-nor-steroid having a formula selected from the group consisting of ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2##Type: GrantFiled: May 28, 1993Date of Patent: January 13, 1998Assignee: ROUSSEL UCLAFInventors: Andre Claussner, Daniel Philibert, Lucien Nedelec, Patrick Van De Velde, Francois Nique, Jean-Georges Teutsch
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Patent number: 5705495Abstract: The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.Type: GrantFiled: October 18, 1996Date of Patent: January 6, 1998Assignee: Jenapharm GmbH & Co. KG.Inventors: Sigfrid Schwarz, Walter Elger, Gudrun Reddersen, Birgitt Schneider, Ina Thieme, Margit Richter
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Patent number: 5668126Abstract: Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the enterohepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.G is a bile acid radical in the form of the free natural or chemically modified acids, the esters and amides, the salt forms and forms derivatized on alcohol groups.Type: GrantFiled: June 7, 1995Date of Patent: September 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Werner Kramer, Gunther Wess
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Patent number: 5646272Abstract: Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the entercepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.G is a bile acid radical in the form of the free natural or chemically modified acids, the esters and amides, the salt forms and forms derivatized on alcohol groups.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Hoechst AktiengesellschaftInventors: Werner Kramer, Gunther Wess
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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: 5608093Abstract: Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I ##STR1## are described in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl; n and m are zero or 1; R(2) is alkyl or --(CH.sub.2).sub.2 --OCH.sub.3 ; R(3) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(5) is OH, with an activated carboxylic acid of the formula III,R(6)--CO--(O).sub.n --(X)--R(1) III.The compounds I have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects, which ratio is often markedly superior to that of analogous corticoid 17-alkyl carbonate 21-esters which do not carry any aryl or heteraryl group in the 21-ester radical.Type: GrantFiled: August 25, 1994Date of Patent: March 4, 1997Assignee: Hoechst AktiengesellschaftInventors: Ulrich Stache, Hans-Georg Alpermann, Walter D urckheimer, Manfred Bohn
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Patent number: 5599806Abstract: The invention describes hydrazino and hydroxyamino-14.beta.-hydroxyandrostane derivatives having general formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration and A, B, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have the meanings given in the description and their use in the treatment of cardiovascular disorders such as heart failure and hypertension.Type: GrantFiled: May 18, 1995Date of Patent: February 4, 1997Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
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Patent number: 5583127Abstract: Disclosed are 17-iminomethylalkenyl and 17-iminoalkyl-14.beta.-hydroxy-5.beta.-androstane derivatives of the formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration or a Z or E configuration; A represents (CH.sub.2).sub.m or --(CH.dbd.CH).sub.n --; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3; R.sup.2 represents hydrogen or hydroxy; R.sup.1 represents hydrogen, C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may be the same or different, represent hydrogen, C.sub.1 -C.sub.4 alkyl or R.sup.4 and R.sup.5 may form, when taken together with the nitrogen atom, a five- or six- membered heterocyclic ring optionally containing one or more heteroatoms selected from oxygen and nitrogen; R.sup.3 represents NHC(.dbd.X)NR.sup.6 R.sup.7 or OR.sup.8 wherein R.sup.6 and R.sup.7, which may be the same or different, represent hydrogen, methyl, or C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.Type: GrantFiled: December 23, 1994Date of Patent: December 10, 1996Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
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Patent number: 5556845Abstract: A compound of the formula ##STR1## wherein the substituents are as defined in the specification.Type: GrantFiled: May 19, 1995Date of Patent: September 17, 1996Assignee: Roussel UclafInventors: Fran.cedilla.ois Nique, Jean-Georges Teutsch, Patrick Van De Velde
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Patent number: 5462933Abstract: Bile acid derivatives, processes for their preparation and use as pharmaceuticals Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the enterohepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.Type: GrantFiled: March 10, 1994Date of Patent: October 31, 1995Assignee: Hoechst AktiengesellschaftInventors: Werner Kramer, Gunther Wess
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Patent number: 5424304Abstract: Cardioactive steroidal compounds of the formula I ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 have the meanings shown in the description, and pharmaceutical compositions containing them.Type: GrantFiled: January 15, 1993Date of Patent: June 13, 1995Inventors: Giorgio Bertolini, Cesare Casagrande, Gabriele Norcini, Francesco Santangelo
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Patent number: 5412091Abstract: A compound of the formula ##STR1## in which ##STR2## is either a 3-keto-.DELTA.4-system or a 3-keto -.DELTA.1,4-system or a 3-OR.sub.4 - .DELTA.5-system in which R.sub.4 is hydrogen or a protector group of hydroxy, R is methyl --CH.sub.2 OH or --CH.sub.2 OR', in which R' is a protector group of hydroxy, R.sub.1 and R'.sub.1 are individually selected from the group consisting of methyl, a branched alkyl not possessing hydrogen in the .beta. position of 5 to 8 carbon atoms, aryl of up to 10 carbon atoms, heteroaryl of up to 10 carbon atoms and at least one heteroatom chosen from nitrogen, sulfur and oxygen and benzyl, n and m, are individually numbers 0 or 1, R.sub.2 and R.sub.3 are hydrogen or R.sub.2 is fluorine and R.sub.3 is formyloxy or acetyloxy and the dotted lines in position 9(11) indicate the optional presence of a second bond which is useful for the preparation of compounds of formula A.Type: GrantFiled: July 1, 1993Date of Patent: May 2, 1995Assignee: Roussel UclafInventors: Jean Boivin, Christine Chauvet, Samir Zard
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Patent number: 5334713Abstract: The present invention relates to N-long chain acyl neutral amino acid esters of the general formula (I): ##STR1## wherein X represents an ester-forming residue of a sterol; COR represents a long chain acyl group having 8 to 22 carbon atoms; R.sub.1 and R.sub.2 are identical or different from each other, each represents a hydrogen atom or a straight chain or branched alkyl group having 1 to 4 carbon atoms, or R.sub.1 and R.sub.2 together form an alkylene group; and n represents 0, 1 or 2. The compounds are particularly useful in cosmetic or pharmaceutical preparations for external use.Type: GrantFiled: October 21, 1992Date of Patent: August 2, 1994Assignee: Ajinomoto Co., Inc.Inventors: Tatsuya Hattori, Naoko Mikami
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Patent number: 5248773Abstract: A compound of the formula ##STR1## in which ##STR2## is either a 3-keto-.DELTA.4-system or a 3-keto -.DELTA.1,4-system or a 3-OR.sub.4 -.DELTA.5-system in which R.sub.4 is hydrogen or a protector group of hydroxy, R is methyl, --CH.sub.2 OH or --CH.sub.2 OR', in which R' is a protector group of hydroxy, R.sub.1 and R'.sub.1 are individually selected from the group consisting of methyl, a branched alkyl not possessing hydrogen in the .beta. position of 5 to 8 carbon atoms, aryl of up to 10 carbon atoms, heteroaryl of up to 10 carbon atoms and at least one heteroatom chosen from nitrogen, sulfur and oxygen and benzyl, n and m, are individually numbers 0 or 1, R.sub.2 and R.sub.3 are hydrogen or R.sub.2 is fluorine and R.sub.3 is formyloxy or acetyloxy and the dotted lines in position 9(11) indicate the optional presence of a second bond which are useful for the preparation of compounds of formula A.Type: GrantFiled: June 25, 1992Date of Patent: September 28, 1993Assignee: Roussel-UCLAFInventors: Jean Boivin, Christine Chauvet, Samir Zard
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Patent number: 5218109Abstract: Steroid compounds of the following general formulas (I), (II) and (III) are provided: ##STR1## In the above formulas, R.sup.1 and R.sup.2 each is a hydrogen atom or a hydroxyl-protecting group, R is a group of the formula --CH.sub.2 --X (in which X is a substituent such as a hydroxyl group), a carboxyl group or a protected carboxyl group, A.sup.1 is an aryl group, a lower alkyl group or an aralkyl group, and Z.sup.1, Z.sup.2, Z.sup.3 and Z.sup.4 each is a hydrogen atom, a hydroxyl group or a protected hydroxyl group.The above steroid compounds are useful as intermediates for the synthesis of vitamin D.sub.3 derivatives having a hydroxyl group at the 1.alpha.-position.Type: GrantFiled: March 5, 1990Date of Patent: June 8, 1993Assignee: Kuraray Co., Ltd.Inventors: Jiro Tsuji, Takashi Takahashi, Masao Tsuji, Naoshi Nakagawa, Tetsuo Takigawa
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Patent number: 5212166Abstract: The present invention concerns steroidic 5.alpha.-reductase inhibitors having the following formula (I) ##STR1## wherein Y is oxygen or sulphur;R is a group;a) --OR.sub.4, wherein R.sub.4 is hydrogen or a C.sub.1 -C.sub.6 alkyl group;b) ##STR2## wherein each of R.sub.5 and R.sub.6, independently, is hydrogen or a C.sub.1 -C.sub.6 alkyl group;c) ##STR3## wherein R.sub.7 is hydrogen or a C.sub.1 -C.sub.6 alkyl group and W is a group:(i) ##STR4## wherein R.sub.8 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalky group, a C.sub.6 -C.sub.6 cycloalkylalkyl group, a phenyl group or a benzyl group; or(ii) ##STR5## wherein R.sub.9 is a C.sub.1 -C.sub.6 alkyl group or a C.sub.5 -C.sub.6 cycloalkyl group; or(iii) ##STR6## wherein R.sub.5 and R.sub.6 are as defined above; d) ##STR7## wherein each of R.sub.10 and R.sub.11 is, independently, hydrogen or a C.sub.1 -C.sub.Type: GrantFiled: May 21, 1992Date of Patent: May 18, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Achille Panzeri, Marcella Nesi, Enrico Di Salle
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Patent number: 5208227Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionophore (GBR) complex.Type: GrantFiled: February 13, 1991Date of Patent: May 4, 1993Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger, Roberta E. Brinton, Deborah J. Burke, Bruce S. McEwen
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Patent number: 5124321Abstract: 17-halomethylene estratrienes of Formula I ##STR1## wherein R.sub.1 is hydrogen, a methyl or acyl group, andR.sub.2 is a halogen atom, show low affinity to the estrogen receptor and bring about a cellular membrane and blood/lymphatic vessel permeability that is increased as compared with estradiol.Type: GrantFiled: December 7, 1988Date of Patent: June 23, 1992Assignee: Schering AktiengesellschaftInventors: Peter Jungblut, Rudolf Wiechert, Rolf Bohlmann
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Patent number: 5120723Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.Type: GrantFiled: May 10, 1990Date of Patent: June 9, 1992Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger
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Patent number: 5099019Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.Type: GrantFiled: August 8, 1988Date of Patent: March 24, 1992Assignee: Upjohn CompanyInventors: John M. McCall, Donald E. Ayer, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
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Patent number: 4948533Abstract: The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17.alpha.-hydroxy-11.alpha.-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs.Type: GrantFiled: February 16, 1989Date of Patent: August 14, 1990Assignee: The Upjohn CompanyInventors: John M. Braughler, Edward D. Hall, Wendell Wierenga, John M. McCall
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Patent number: 4783528Abstract: A new class of macrocylic polyethers having a crown ether attached to a steroid by various connector units have been prepared. These novel structures have applications as ionophores and they form unique, nonionic vesicles (niosomes).Type: GrantFiled: June 5, 1987Date of Patent: November 8, 1988Assignee: University of Miami (Department of Chemistry)Inventor: George W. Gokel
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Patent number: 4753932Abstract: A novel steroid of the formula ##STR1## wherein X is methylene and R is an optionally substituted carbocyclic aryl or heterocyclic aryl or optionally substituted vinyl or ethynyl or X is a simple bond or --S-- and R is optionally substituted carbocyclic aryl or heterocyclic aryl, R.sub.2 is methyl or ethyl, R.sub.3 is selected from the group consisting of optionally substituted alkyl of 1 to 8 carbon atoms and optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and acyl, ##STR2## is selected from the group consisting of ##STR3## R.sub.6 is selected from the group consisting of hydrogen and methyl, the wavy line indicates .alpha. or .beta.- and the dotted line in 1(2) indicates the optional presence of a second carbon-carbon bond and novel process and intermediates therefore having anti-glucocorticoid activity.Type: GrantFiled: January 14, 1986Date of Patent: June 28, 1988Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Germain Costerousse, Vesperto Torelli, Daniel Philibert
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Patent number: RE35053Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.Type: GrantFiled: October 9, 1992Date of Patent: October 10, 1995Assignee: The Upjohn CompanyInventors: John M. McCall, E. Jon Jacobsen
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Patent number: RE35517Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.Type: GrantFiled: November 23, 1992Date of Patent: May 20, 1997Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan