Abstract: Disclosed are compounds of the formula: wherein R1, R2, R3 and R4 are independently hydrogen, C1-C6 alkyl, halo, a sulfate, a glucuronide, —OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, —N(CH2)n; a phosphate group, and a phosphinate group; R9 is hydrogen, halogen or alkyl; R11 is selected from the group consisting of H, C1-C6 alkyl, halogen, a sulfate, a glucoronide, —SO2NH2, —COOH, —CN, —CH2CN—, —NHCN—, —CHO, ?CHOCH3, —COO salt, —OSO2alkyl, —NH2, and —NHCO(CH2)n; R12 is selected from the group consisting of H, a C1-C6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, a glucoronide, —NH2, —SO2NH2, —COOH, —CN, —CH2CN, —NHCN, —CHO, —COOsalt, —OSO2alkyl, —SH, —SCH3, —CH[(CH2)nCH3]COOCH3, —(CH2)mCOOCH3, —(CH2)m—O—CH3, —(CH2)m—O—(CH2)nCH3, (CH2)m—S—CH3, —(CH2)m—S—(CH2)nCH3, —(CH2)m—NH—(CH2)nCH3, —C2-C8 alkenyl-O—(CH2)nCH3, —C2-C8 alkenyl-S—(CH2)

Abstract: The invention relates to a solid pharmaceutical composition comprising solid amorphous fulvestrant, said composition being formulated in combination with a solubilizing composition. The invention also relates to a method for preparing said composition and a kit including the composition.

Abstract: The invention relates to a solid pharmaceutical composition comprising solid amorphous fulvestrant, said composition being formulated in combination with a solubilizing composition. The invention also relates to a method for preparing said composition and a kit including the composition.

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 relates to a process for production of a steroid compound having a partial structure represented by Formula (2) by oxidizing a steroid compound having a partial structure represented by Formula (1), without the need of any special apparatus, in a safe and economical manner, with less adverse affect on environment, in a simple and high efficient manner. Specifically, the invention relates to a process for producing a steroid compound having a partial structure of ring A and ring B of the steroid skeleton represented by Formula (2): wherein R represents a hydrogen atom or C1-6 alkyl group, comprising the step of reacting a steroid compound having a partial structure of ring A and ring B of the steroid skeleton represented by Formula (1): wherein R is the same as above; with a catalytic amount of copper halide in the presence of oxygen.

Abstract: Processes useful in the preparation of pharmaceutical compounds such as fulvestrant and processes for the preparation of fulvestrant.

Abstract: Disclosed are compounds of the formula: wherein R1, R2, R3 and R4 are independently hydrogen, C1-C6 alkyl, halo, a sulfate, a glucuronide, —OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, —N(CH2)n; a phosphate group, and a phosphinate group; R9 is hydrogen, halogen or alkyl; R11 is selected from the group consisting of H, C1-C6 alkyl, halogen, a sulfate, a glucoronide, —SO2NH2, —COOH, —CN, —CH2CN—, —NHCN—, —CHO, ?CHOCH3, —COO salt, —OSO2alkyl, —NH2, and —NHCO(CH2)n; R12 is selected from the group consisting of H, a C1-C6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, a glucoronide, —NH2, —SO2NH2, —COOH, —CN, —CH2CN, —NHCN, —CHO, —COOsalt, —OSO2alkyl, —SH, —SCH3, —CH[(CH2)nCH2]COOCH2, —(CH2)mCOOCH3, —(CH2)m—O—CH3, —(CH2)m—O—(CH2)nCH3, (CH2)m—S—CH3, —(CH2)m—S—(CH2)nCH3, —(CH2)m—NH—(CH2)nCH3, —C2-C8 alkenyl-O—(CH2)nCH3, —C2-C8 alkenyl-S—(CH2)

Abstract: A compound of formula (1) wherein R1 represents hydrogen or an acetyl group and R2 represents a methyl, acetyl, or benzyl group, is useful as an intermediate in making fulvestrant. The compound (1) can be isolated as a crystalline material and can be provided in a ratio of 7-alpha epimer to 7-beta epimer in the range of 95:5 to 100:0.

Abstract: A compound having the structure: wherein R1 and Z are as described above, X is selected from the group consisting of: C1-C6 alkyl, a substituted alkyl, a halogen, a halogenated alkyl, a glucuronide, —NH2, —SO2NH2, —COOH, —CN, —CH2CN, —NHCN, —CHO, —COOsalt, —OSO2alkyl, —SH, —SCH3—CH(CH2)nCOOCH3, —(CH2)n—O—CH3, —CH2OH, —(CH2)n—O—NH2, —NH(CH2)nCH3, NH(CH2)nOCH3, —NH(CH2)nCHOH—COOH, —N(CH3)2, —(CH2)n(NH)CH2OH, —NHCOOH, —(CH2)nNHCOOH, —NO2, —SCN, —SO2alkyl, —B(OH)2, —(CH2)nN(CH3)—SO2—NH3, —(CH2)nNH—SO2—NH2, —NHC(?S)CH3, and —NHNH2; R3 is selected from the group consisting of: H, a C1-C6 alkyl, a substituted alkyl, a halogen, and a halogenated alkyl; R4 and Y are independently selected from a group consisting of: O, —OH, —H, a —C1-C6 alkyl, a substituted alkyl, a halogen, a halogenated alkyl, a sulfate, a glucuronide, a bulky group, a phenyl or a substituted phenyl group, a cyclo- or heterocyclo group, piperidine, piperazine, morpholine, pyrimidine, —NH2, —N(CH2)nCH3; a phosphate group, a phosphinate group, whe

Abstract: The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R1, R2, R3, R6, R7, R8, R9, R11, R11?, R14, R15, R15?, R16, R17 and R17? have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention.

Abstract: A 11.beta.-aryl-19-norprogesterone steroid of the formula: ##STR1## wherein (i) R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, OH, OC(O)CH.sub.3, or OC(O)R.sup.5, wherein R.sup.5 is C.sub.2-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl or aryl, R.sub.2 is H, R.sup.3 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, R.sup.4 is H, CH.sub.3, F or Cl, R.sup.6 is H, (CH.sub.3).sub.2 N, CH.sub.3 O, CH.sub.3 CO, CH.sub.3 S, CH.sub.3 SO, CH.sub.3 SO.sub.2, and X is O or NOCH.sub.3 ; or(ii) R.sup.1 and R.sup.2 taken together are a carbon-carbon bond and R.sup.3, R.sup.4, R.sup.6 and X are as defined above; or(iii) R.sup.1 and R.sup.3 taken together are --CH.sub.2 -- or --N.dbd.N--CH.sub.2 --, R.sup.2 is H and R.sup.4, R.sup.6 and X are as defined above; or(iv) R.sup.2 and R.sup.3 taken together are .dbd.CH.sub.2 and R.sup.1, R.sup.4, R.sup.6 and X are as defined above.