Abstract: The invention relates to a method of preparation of a soluble formulation of water-insoluble pentacyclic and tetracyclic terpenoids, wherein the water-insoluble terpenoid having a free carboxylic, hydroxy or amino functional group is derivatized on this functional group with a substituent selected from the group comprising substituents of general formula Xa bound to the hydroxy group of the terpenoid, wherein Xa is —OC—R—COOH, substituents of general formula Xa bound to the amino group of the terpenoid, wherein Xa is —OC—R—COOH, quarternary ammonium substituents of general formula Xb bound to the carboxy group of the terpenoid, wherein Xb is —(CH2)nN+R3Y—, quarternary ammonium substituents of general formula Xc bound to the carboxy group of the terpenoid, wherein Xc je —(CH2)nR+Y—, substituents of general formula Xd bound to the carboxy group of the terpenoid, wherein Xd represents —R—COOH, glycosylic substituents Xe bound by alpha or beta glycosidic bond to the hydroxy group or to the carboxy group of the te

Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.

Abstract: The present invention discloses modified process for preparing aromatase inhibitor Exemestane involving suitable oxidizing agents in suitable solvents.

Abstract: The present invention relates to the use of a combination of a PDE5-inhibitor and testosterone for the preparation of a medicament for the treatment of Female Sexual Dysfunction.

Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of Formula I with progesterone antagonizing action and method of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of fibroids of the uterus (myomas, uterine leiomyoma), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause or for fertility control and emergency contraception.

Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.

Abstract: There is provided a compound of Formula I wherein X is a ring system; R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R2 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein when X is a steroidal structure and both of R1 and R2 are sulphamate groups, the steroidal ring system (X) represents an oestrogen; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth.

Abstract: The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I wherein R1 and R2 independently represent H, methyl, C1-C4 acyl, benzoyl R3 represents C1-C4 alkyl or a group of formula CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1, and m+o=2n+1, R4 and R5 in each case represent H or, together, a methylene group or an additional double bond, R6 represents H, R7 represents OH, OC1-C4-alkyl, OC1-C11-acyl or OSO2NR1R2, the dashed lines in the B and C rings of the steroid skeleton additionally representing up to two double bonds, for the production of a medical drug for the treatment of tumor diseases which can be affected positively by inhibiting the tubulin polymerization. The inventive compounds are distinguished by the 2-alkoxy substitution in conjunction with the 17-hydroxy substitution. They have a special effect with regard to inhibiting tubulin polymerization and can be used, for example, for the treatment of prostate cancers.

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.

Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

Abstract: The invention relates to processes for obtaining steroids with a spirolactone group in position 17, particularly to industrially obtaining 6?,7?; 15?,16?-dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, commonly known as Drospirenone, as well as to intermediates useful in said process.

Abstract: The subject of the invention is a method for preparing compounds of general formula (I): in which A, Z, R3 are as defined in the description, and the intermediate compounds for carrying out this method.

Abstract: The present invention relates to 11?-fluoro-3-acetoxyestra-3,5-dien-17-one as a suitable intermediate in the preparation of 11-fluoro-substituted steroids and to the process for preparation thereof. For this purpose, 11?-hydroxyestra-4-ene-3,17-dione is reacted with 1 to 3 equivalents of n-nonafluorobutanesulfonyl fluoride and 3 to 5 equivalents of diazabicycloundecene (DBU) at ?40 to ?20° C. in an organic aprotic solvent and, after an aqueous workup, reacted with 5 to 10 equivalents of acetic anhydride and 0.01 to 1 equivalent of a strong acid. The desired product precipitates spontaneously out of the reaction solution and is obtained in a very high purity by filtration. The process is notable for the very high yield, avoidance of a chromatographic purification of the product, a reduced proportion of wastes and significantly increased process throughput. The process according to the invention is therefore especially suitable for preparing 11?-fluoro-3-acetoxyestra-3,5-dien-17-one on a large industrial scale.

Abstract: The present invention discloses modified process for preparing aromatase inhibitor Exemestane involving suitable oxidizing agents in suitable solvents.

Abstract: A process for the preparation of Drospirenone (I) according to the scheme (A) wherein the substituent R is defined in the description. The process improves the product yield and purity by reducing the formation of undesired side-products and is particularly convenient for industrial-scale manufacturing.

Abstract: A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2.

Abstract: The present invention relates to new steroid modulators of progesterone receptor activity and/or glucocorticoid receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to an in-vitro method of identifying a tumor resulting from a proliferative breast disease as responsive to anti-estrogen treatment. Further, the invention relates to an in-vitro method of identifying a candidate patient with a proliferative breast disease as suitable for anti-estrogen treatment. In a further aspect, the invention provides an in-vitro method of identifying an individual with a non-cancerous proliferative breast disease who is at risk of developing breast cancer. The invention also provides kits for performing the above methods.

Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: The present invention concerns a method for the controlled precipitation of organic compounds giving crystals with a very small average size and a very narrow size distribution.

Abstract: The invention provides for compounds having formula (1) wherein; R1 is O, (H,H), (H,OH), or NOR, with R being hydrogen, (C1-6) alkyl or (C1-6) acyl; R2 is hydrogen, methyl, ethyl, or ethenyl; R3 is hydrogen, methyl, ethyl, ethenyl, fluoro, or chloro; R4 is methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, ethyl, (C1-3) alkenyl, or (C1-3) alkynyl; R7 is hydrogen or (C1-15) acyl; and at least one of R5 or R6 is hydrogen; or a pharmaceutically acceptable salt thereof, for use as medicine for a treatment to increase androgen levels, for androgen supplementation, for testosterone replacement and for benign prostate hypertrophy and in a method of male contraception, preferably as sole means to achieve both progestagenic sterilitant effect and androgen supplementation.

Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

Abstract: Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11?-substitution. Said substitution is a hydrocarbon group which may be linear or branched, provided that it comprises, as the longest chain on carbon atom no. 11 of the steroid skeleton, one single linear chain having a length of from 5 to 9 carbon atoms, wherein said chain may be saturated or unsaturated. The resulting compounds have a desirable mixed agonist/antagonist profile for estrogen receptor ? and estrogen receptor ?.

Abstract: New crystalline polymorph of exemestane characterized by a powder X-ray diffraction pattern having peaks at 10.7±0.1, 15.9±0.1, and 18.1±0.1 2-theta degree.

Abstract: 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 exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).

Abstract: Disclosed are compounds of the formula (I) wherein R is C1-C30 alkyl, which may be optionally further substituted with one or more C5-C8 cycloalkyl groups, or a C5-C12 cycloalkyl, which may be optionally substituted with one or more C1-C30 alkyl groups, R? is hydrogen or lower alkyl, R? is a C1-C30 alkyl or halo, and the bond between C14 and C15 can be a single bond or double bond. Also disclosed are pharmaceutical compositions comprising such compounds and methods of use thereof. These compounds can find use in treating a number of diseases or conditions such as hypogonadism, hypergonadism, osteoporosis, and anemia, in providing hormonal therapy and contraception, as an anabolic agent, and in suppressing the release of hormones such as the luteinizing hormone.

Abstract: There is provided a compound of Formula I wherein X is a ring system; R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R2 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein when X is a steroidal structure and both of R1 and R2 are sulphamate groups, the steroidal ring system (X) represents an oestrogen; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth.

Abstract: A novel process for making estra-4,9(10)-diene-3,17-dione steroids from readily available 19-nor-androst-4-ene-3-one steroids by a straightforward three-step process. Products of this process are important intermediates in the preparation of biologically active substances.

Abstract: The invention relates to new 7&agr;, 17&agr;, 17&bgr;-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term antiandrogen therapy of prostate carcinoma.

Abstract: Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &agr;,&bgr;-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the &agr;,&bgr;-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

Abstract: A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.

Abstract: This invention relates to processes for the preparation of 7-carboxy substituted steroid compounds of Formula I, 1

Abstract: The invention relates to a process for the production of 4-(17&agr;-methyl-substituted 3-oxoestra-4,9-dien-11&bgr;-yl)benzaldehyde-(1E or 1Z)-oximes of general formula (I), in which R1 is a hydrogen atom, a C1-6-alkyl radical or a CnF2n+1 radical, whereby n is 1, 2 or 3, R2 is a C1-4-alkyl radical, X is an OH group in E- or Z-position, and Y is an OC1-6-alkyl group, an SC1-6-alkyl group or an OCH2CnF2+1 group, whereby n is 1, 2 or 3, which provides the target compounds of formula (I) with a high yield and good selectivity.

Abstract: The invention relates to novel solid body forms of mesoprogestin 11&bgr;-[4E-(hydroxyiminomethyl)-phenyl]-17&agr;-methoxymethyl-17&bgr;-methoxy-estra-4,9-dien-3-one (oxime J 867), particularly a highly pure and stable amorphous or highly crystalline form (ansolvate/anhydrate) of compound J 867. The invention also relates to methods for producing said novel solid body forms and to the use thereof in pharmaceutical compositions. The novel solid body forms are characterized by exhibiting a high degree of stability. The solid body forms of oxime J 867 can, in particular, be used in the area of fertility control and in hormone replacement therapy.

Abstract: This invention relates to 11&bgr;-(para-substituted)phenyl-estra-1,3,5(10)-trienes with a straight-chin or branched-chain, optionally partially or completely halogenated alkyl radical or alkenyl radical in each case with up to 5 carbon atoms, an ethinyl radical or prop-1-inyl radical in 8&bgr;-position.

Abstract: A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.

Abstract: Novel compounds having a formula selected from the group consisting of 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-proliferative activity.

Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives.

Abstract: 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.

Abstract: A process is disclosed for synthesizing oxandrolone 1 involving the bromination of compound 2 to obtain compound 3, followed by the highly selective de-bromination of compound 3 to obtain compound 4, followed by the oxidation of compound 4 to obtain compound 6, and finally the reduction of compound 6 to obtain oxandrolone 1.

Abstract: A compound of formula (I): 1

Abstract: The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 16&agr;-carboxylic acid substituted steroids and their esters is presented which exhibit excellent biological activity for use in pharmaceutical compositions for the treatment of symptomology associated with menopause. The present invention is therefore directed to compounds according to the structure: Where R is H, a C1 to C5 alkyl, vinyl, CF3, CH2CH2F, CH2CHF2 or CH2CF3; and m is from 0-2, or a pharmaceutically acceptable salt thereof. Preferably, R is methyl, ethyl, propyl, iso-propyl, butyl, iso-butyl, pentyl, neo-pentyl, vinyl, CF3, CH2CH2F, CH2CHF2 or CH2CF3 and m is 0. More preferably, R is methyl, ethyl, CH2CH2F, CH2CHF2 or CH2CF3 and m is 0.

Abstract: This invention provides estrogenic agents having the formula 1

Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.

Abstract: The invention is drawn to (7a, 17b)-7-methyl-17-(1-oxoundecyl)oxy-estr-4-en-3-one, (MENT undecanoate), their pharmaceutical formulation and method of use is described. Unexpected results of the said compound compared with testosterone undecanoate is disclosed.

Abstract: Intermediates for the preparation of a vitamin D derivative have the following formulas: wherein R9 and R10 may be the same or different and each represents a hydrogen atom or a protecting group, and in Formula (5) the conjugated double bond may be protected by a protecting group.

Abstract: An androgenic steroid compound of the formula: 1

Abstract: 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.

Abstract: 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.

Abstract: Methods for treating sex steroid-dependent diseases by inhibiting sex steroid activity include administration of novel compounds which include an androgenic nucleus substituted at a ring carbon with at least one substituent specified herein. Such compounds may function by inhibiting sex steroid synthesis (both estrogen and androgen synthesis) and/or by antagonistically blocking androgen receptors.