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| Number | Title | Issue Date |
| 8183401 | Exemestane and its intermediates and methods of making the same A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exe... | 05/22/2012 |
| 8022234 | Compounds and compositions The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compos... | 09/20/2011 |
| 7667056 | Process and new intermediates for the preparation of steroids with a progestogen activity The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (I). Said process is characterized by the regioselec... | 02/23/2010 |
| 7323454 | Etonogestrel esters The subject invention provides new progestogen esters and uses thereof. ... | 01/29/2008 |
| 6855836 | 17-Methylene steroids, process for their production and pharmaceutical compositions that contain these compounds The invention relates to 17-methylene steroids, process for their production and pharmaceutical compositions that contain these compounds. The compounds according to the invention have a hybrid-type profile of action in the sense that they act as inhibitors o... | 02/15/2005 |
| 6737417 | Compounds with hydroxycarbonyl-halogenoalkyl side chain The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general f... | 05/18/2004 |
| 6596885 | 19-Nor steroids having a thiocarbonated chain in position 11beta, their preparation process and the intermediates of this process, their use as medicaments and compositions Novel compounds having a formula selected from the group consisting of ##STR1## wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds having a remarkable anti-estrogenic and anti-prolife... | 07/22/2003 |
| 6579864 | 3-methylene steroid derivatives The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R1 is H or together with R3 forms a ଲ-epoxide or R1 is absent if there is a 5-10 or 4-5 double bond; R2 is (C... | 06/17/2003 |
| 6503896 | Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecul... | 01/07/2003 |
| 6468981 | Compositions and methods for targeting pharmaceutically active materials to cells containing androgen receptors A water soluble delivery system for nucleic acids to cells having androgen receptors, preferably prostate cells, is provided comprising a steroid moiety capable of binding to said receptors, said steroid moiety being covalently linked to a polycationic ma... | 10/22/2002 |
| 6177417 | Cholanic acid ring based 4-(trifluoroacetyl)phenyl derivatives, process for preparation and use thereof The present invention relates to a cholanic acid ring based 4-(trifluoroacetyl)phenyl derivatives of the following formula 1, process for preparation and use thereof. The cholanic acid ring based 4-(trifluoroacetyl)phenyl derivatives of the present invent... | 01/23/2001 |
| 5952319 | Androgenic steroid compounds and a method of making and using the same An androgenic steroid compound of the formula: ##STR1## wherein: X, Y, Z, R1, R2, R3, R5 and R6 are as defined herein.... | 09/14/1999 |
| 5521169 | Ascosteroside and analogs thereof useful in antifungal compositions for methods of treating infections and inhibition of fungal growth Ascosteroside, obtainable by cultivation of a strain of Ascotricha amphitricha A.T.C.C. No. 74237, analogs thereof and salts and prodrugs of these compounds. The compounds have antifungal activity for use in a method for treating and preventing a fungal i... | 05/28/1996 |
| 5443758 | Non-linear optical material containing steroidal ketone compound A steroidal ketone compound having a substituted or unsubstituted aromatic group or heterocyclic aromatic group is useful as a non-linear optical material in a non-linear optical device.... | 08/22/1995 |
| 5364847 | Inhibitors of sex steroid biosynthesis and methods for their production and use Certain steroidal and non-steroidal compounds have been found to inhibit androgen and estrogen formation. Such inhibition may aid in the reduction of the activity of these hormones and may be useful in the treatment of diseases where, for example, inhibit... | 11/15/1994 |
| 5252565 | Haloethyl-substituted steroid enzyme inhibitors The present invention is directed to a group of compounds which are haloethyl substituted steroidal enzyme inhibitors. These compounds are useful as aromatase, 19-hydroxylase, and aldosterone biosynthesis inhibitors and they are prepared from the correspo... | 10/12/1993 |
| 5236913 | 11-methylene-oestr-15-enes, processes for their preparation, and pharmaceutical compositions The present invention is concerned with novel 11-methylene-oestr-15-enes of the formula: ##STR1## wherein R1 =H or acyl with 1-18 C-atoms, preferably H, R2 =ethinyl, vinyl, chloroethinyl, allyl or propinyl; ethinyl being preferr... | 08/17/1993 |
| 5162312 | 11ଲ-substituted 16, 17-methylene-estra-4,9-dien-3-ones 11ଲ-substituted-16, 17-methylene-estra-4,9-dien-3-ones of formula I ##STR1## wherein R1 is a methyl or ethyl group; R2 is H; a C1-6 -alkyl, -alkoxymethyl, -alkanoyl or -alkoxcarbonyl group ; 2-meth... | 11/10/1992 |
| 5086047 | Novel steroids 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, option... | 02/04/1992 |
| 5034548 | Steroid derivatives useful as hypocholesterolemics Lanosterols substituted in the 14 and/or 15 position(s) which are active in inhibiting lanosta-8,24-dien-3ଲ-ol 14-methyl-demethylase activity, suppressing 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) activity, decreasing cholesterol... | 07/23/1991 |
| 4990635 | Synthesis of 6-methylene derivatives of androsta-1,4-diene-3,17-dione The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula (I) ##STR1## wherein each of R1 and R3, independently, is hydrogen or C1 -C6 alkyl; R2 | 02/05/1991 |
| 4945064 | Estrane and androstane derivatives, process for producing them and preparations containing these compounds Estrane and androstane derivatives of formula I ##STR1## wherein X is bromine, iodine, triphenyltin or trialkyltin of 1 to 6 carbon atoms per alkyl radical, Y represents two hydrogen atoms or methylene, Z represents two hydrogen atoms, oxo or alkylenediox... | 07/31/1990 |
| 4925834 | 3-methylene-4-androsten-17-ones, process for their production and pharmaceutical preparations containing them A 3-methylene-4-androsten-17-one of formula I ##STR1## wherein Ra represents a hydrogen atom or a saturated or unsaturated straight-chain or branched-chain, optionally substituted alkyl radical with 1-6 carbon atoms, in which Ra... | 05/15/1990 |
| 4921638 | 17ଲ-cyano-9,17-dihydroxyandrost-4-en-3-one The invention is the compound 17ଲ-cyano-9, 17-dihydroxyandrost-4-en-3-one (I) which is particularly useful as an intermediate in the production of the 17-halo silyl ethers (II).... | 05/01/1990 |
| 4920114 | 19-fluoro- or cyano-21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors 19-Fluoro- and cyano- substituted 21-hydroxyprogesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pat... | 04/24/1990 |
| 4876045 | Process for the preparation of methylene derivatives of androsta-1,4-diene-3,17-dione The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula ##STR1## wherein each of R1 and R3, independently, is hydrogen or C1 -C6 alkyl; R2 | 10/24/1989 |
| 4873233 | 17-Substituted androsta-1,4-dien-3-one derivatives The invention relates to new 17-hydroxy androsta-1,4-diene-3-one derivatives of the following formula ##STR1## wherein each of R and R3, independently, is hydrogen or C1 -C6 alkyl; R1 is hydrogen, halogen o... | 10/10/1989 |
| 4870069 | 11ଲ-alkynyl-estrenes and -estradienes, their production and pharmaceutical preparations containing them 11ଲ-substituted steroids of the formula ##STR1## wherein A and B together represent a second bond between the 6-position and 7-position carbon atoms, or, respectively, are each H; X is O, two H atoms or hydroximino; Z is the residue of a pentagonal ... | 09/26/1989 |
| 4865767 | Novel radioactive steroids Novel radioactive steroids labelled with tritium of the formula ##STR1## wherein 3 H is tritium and R and R1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic ca... | 09/12/1989 |
| 4861763 | 17 -(substituted-methyl)-17ଲ-hydroxy/esterified hydroxy steroids and their progestational use Steroids of the formula: ##STR1## which are characterized by a 17-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17ଲ-hydroxy/esterified hydroxy substitutent. The steroids of this invention ... | 08/29/1989 |
| 4824830 | 6- or 7-methylenandrosta-1,4-diene-3,17-dione derivatives and process for their preparation The invention relates to new 6- or 7-methylenandrosta-1,4-diene-3,17-diones of the following formula ##STR1## wherein R is hydrogen or fluorine; R1 is hydrogen or C1 -C6 alkyl; R2 is hydrogen or halogen; on... | 04/25/1989 |
| 4822528 | 4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and process for their preparation The invention relates to 4-substituted 6-alkylidenandrostene-3,17-dione derivatives of the following formula ##STR1## wherein each of R1, R2 and R3 is, independently, hydrogen or C1 -C6 alkyl; R | 04/18/1989 |
| 4808578 | 6-Alkylidene 10 ଲ-alkynylestrene derivatives and pharmaceutical methods for their use The invention relates to 6-substituted 10ଲ-alkynylestrene derivatives wherein the 6 substituent is amino, azido, halogen or an alkylidene group and to corresponding 6,7-dihalo analogs. The invention provides also a process for the preparation of the abov... | 02/28/1989 |
| 4808616 | 6-substituted androsta-1,4-diene-3,17-diones The invention relates to 6-alkylidenandrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R2, independently, is hydrogen or C1 -C6 alkyl and R1 is hy... | 02/28/1989 |
| 4794119 | Aqueous crystalline suspension of steroid glycoesters An aqueous crystalline suspension of a 17-tertiary steroid glycoester contains a compound of Formula I ##STR1## wherein X is two hydrogen atoms or an oxygen atom, Y is two hydrogen atoms or a methylene group, R1 is hydrogen or methyl, Z is hydr... | 12/27/1988 |
| 4777165 | 6, 16ଲ-dimethyl corticoids and their anti-inflammatory use 6,16ଲ-Dimethyl corticoids of general Formula I ##STR1## wherein the bond -------- is a single bond or a double bond, and X is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom, Z is a hydrogen atom or, jointly with X,... | 10/11/1988 |
| 4753932 | Novel 10-substituted steroids 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 carbocyc... | 06/28/1988 |
| 4670427 | 1,2-methylene-6-methylene- and 6-methylpregnenes, their preparation and pharmaceutical use 1,2-methylene-6-methylene- and 6-methylpregnenes of Formula I ##STR1## wherein A is ##STR2## and R is a hydrogen atom, an acyl group, or an alkoxymethyl group are strong antiandrogens, and suitable for the topical treatment ... | 06/02/1987 |
| 4664850 | Novel radioactive steroids Novel radioactive steriods labelled with tritium of the formula ##STR1## wherein 3 H is tritium and R and R1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic ca... | 05/12/1987 |
| 4648995 | Chemical synthesis A compound of the formula, ##STR1## wherein R may be H or acyl; X may be H, acyl, or lower alkyl; Z may be H, hydroxy, or acyloxy; Y may be lower alkyl, aryl, alkyl substituted aryl or vinyl; and the non-toxic pharmaceutically acceptable salts thereo... | 03/10/1987 |
