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 invention relates to novel ligands of the estrogen receptors ? and ? of general formula II, which are useful as an active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumors and inflammatory diseases. The invention also relates to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.

Abstract: The invention relates to application systems for buccal application, comprising 17?-estradiol in a dosage of 50 to 400 ?g, preferably 200 to 400 ?g, particularly preferably 300 ?g, together with one or more pharmaceutically acceptable additives or media for implementing the treatment or minimization of hot flashes in women having estrogen deficiencies.

Abstract: The invention relates to novel ligands of the estrogen receptors ? and ? of general formula II, which are useful as an active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumors and inflammatory diseases. The invention also relates to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.

Abstract: The invention refers to 8?-substituted estra-1,3,5(10)-triene derivatives of general formula I their use as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action in the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.

Abstract: The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16?- and 16?-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.

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: 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 formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

Abstract: This invention relates to a process for the production of 4-(17&agr;-alkoxymethyl-17&bgr;-substituted-3-oxoestra-4,9-dien-11&bgr;-yl)benzaldehyde-(1E)-oxime derivatives of general formula (I) 1

Abstract: The pharmaceutical preparations for treating side effects, such as hot flashes, prostate enlargement and gynecomastia, during and/or after treatment with analogs or antagonists of gonadotropin-releasing hormone (GnRHa therapy) contain an effective amount of a chemically modified derivative of 17&agr;-estradiol, a chemically modified derivative of 17&bgr;-estradiol and/or a chemical modified derivative of estriol. Pharmaceutical preparations containing 14&agr;, 15&agr;-methylene-1,3,5(10),8-tetraene-3,17&agr;-diol are particularly preferred.

Abstract: The process for making crystals of a 11&bgr;-benzaldoxim-estra-4,9-diene derivative having a predetermined average particle size in a predetermined size range and a maximum particle size that does not exceed a predetermined maximum value, includes subjecting a supersaturated solution containing a special 11&bgr;-benzaldoxim-estra-4,9-diene derivative of formula (I) to a wet milling by a wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.

Abstract: New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, especially for administration in post-menopausal women and in men. The compounds of the invention can also inhibit aromatase and sulfatase.

Abstract: A method and kit for measurement of a steroid by means of a competitive immunoassay, preferably a competitive enzyme immunoassay. The method and kit involve the use of a steroid analogue conjugated to a label. The steroids that are amenable to detection by the method and kit of the present invention include estradiol and progesterone. The method comprises the steps of: a. incubating a mixture of a test sample suspected of containing a given steroid, a solid phase coupled to an antibody specific for that steroid, and a conjugate of an analogue of that steroid to form steroid/antibody complexes and conjugate/antibody complexes on said solid phase; b. separating said solid phase from said mixture; c. measuring the amount of label present in said mixture or in said solid phase; and d. determining the amount of steroid in said sample from the amount of label. The kit comprises a solid phase coupled to an antibody specific for a steroid and a conjugate of an analogue of that steroid.

Abstract: The invention relates to a method for the preparation of a mixture of sulfated estrogens containing delta(8,9)-dehydro estrone [delta(8,9)DHE] or derivatives thereof.

Abstract: 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.

Abstract: Disclosed are estrane derivatives having a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X attached to the 17-position of the steroid nucleus, wherein X and n are as defined by the specification. The compounds are useful as antitumor agents and in the treatment of cardiac and circulatory disorders.

Abstract: The invention relates to a method of isomerisation of equilin or a derivative thereof to delta(8,9)-dehydro estrone ?delta(8,9)DHE!, characterized in that equilin or a derivative thereof is treated with a lithium salt of ethylenediamine or with lithium amide in dimethylsulfoxide.

Abstract: The disclosed invention is drawn to the organometallic oestrogen complex of formula (I): ##STR1## in which A is a C.sub.1-7 alkylene radical or C.sub.2-7 alkenylene or alkynylene radical; M.sub.x is one or more identical or different transition metals; L'.sub.y is one or more identical or different ligands complexing the metal(s) of M.sub.x ; and L is a ligand for covalently coupling M.sub.x to A; and R is H or a C.sub.1-7 alkyl or alkoxy group which may be optionally substituted, particularly with one or more halogens. These complexes are useful for the treatment of hormone-dependent cancers. Also, when the metals of the complex M.sub.x are radioactive isotopes suitable for imaging, the complexes are useful as imaging agents.

Abstract: This invention relates to a process for the preparation of 10-(2-propynyl)-estr-4-ene-3,17-dione, whereby this compound is synthesized utilizing ketals prepared from the addition of 2,2-dimethyl-1,3-propanediol to the starting compound, 19-norandrost-5(10)-ene-3,17-dione (NAD). A new process for the addition of the propynyl group to steroid epoxides by means of higher order cuprates is also described herein.

Abstract: The unsaturated 17.alpha.-cyanomethyl-17.beta.-hydroxy steroids of the formula I, ##STR1## in which R.sub.1 =Me, Eth; R.sub.2 =H, Me; R.sub.3 =H, OH, an acetoxy or alkoxy group; R.sub.4 =H, R.sub.5 =OH, an acetoxy, alkoxy group of R.sub.4 and R.sub.5 together represent a keto- or ketal group and double bonds are contained in the basic structure of the steroid, particularly between the 15 and 16 position in the steroid ring, from unsaturated 17-ketosteroids of the general formula II as described herein with the aforementioned meanings of R.sub.1 to R.sub.5 by reacting the unsaturated 17-ketosteroids with LiCH.sub.2 CN and subsequently hydrolyzing.The compounds of formula I are pharmacologically interesting steroid compounds or also intermediate products for the synthesis of highly-effective steroid products which can be used in human and veterinary medicine for the treatment of endocrine disorders and for reproductive control based on their specific hormonal/anti-hormonal actions.

Abstract: The present invention provides a method for producing (+)-estrone derivatives, characterized in that it comprises starting from a certain cyclopentadiene derivative, reacting the derivative with a certain diene compound by an asymmetric Diels-Alder reaction, and via intermediates obtaining a (+)-estron derivative represented by the following formula: ##STR1## wherein R is alkyl of 1-20 carbon atoms. According to the present invention, (+)-estron derivatives can be obtained by limited steps from the starting materials of dicyclopentadiene derivatives.

Abstract: A process for the production of 3-hydroxy-1,3,5(10)-estratrien-17-one by pyrolysis of 1,4-androstadiene-3,17-dione in the presence of 1,2,3,4-tetrahydronaphthalene as hydrogen donor is described, by 1,2,3,4-tetrahydronaphthalene, preheated to a temperature of 450.degree.-850.degree. C., in a mixing zone being mixed with a solution, heated to a temperature of up to 300.degree. C., of 1,4-androstadiene-3,17-dione, in 1,2,3,4-tetrahydronaphthalene, the mixture being heated in a pyrolysis zone at a retention time of 0.001 to 60 seconds to temperatures of 450.degree.-700.degree. C. and the product leaving the pyrolysis zone being cooled off, which is characterized in that the pyrolysis is performed under a pressure of 3.5.times.10.sup.6 to 3.times.10.sup.8 Pa.

Abstract: Deacylating agent represented by the formula (I): ##STR1## wherein R represents an insoluble polymer substituent, and R' and R" each represents an alkyl group, and a deacylation method using the above deacylating agent.

Abstract: The present invention relates to an estrogen complex which consists of an estrogen or an estrogen derivative complexed with an organometallic compound containing at least one free carbonyl ligand, the said estrogen complex containing at least one free hydroxyl radical and no free phenolic hydroxyl radical in the .alpha.-position to the site where the organometallic compound is attached.The complexes according to the invention are useful for the determination of hormone receptors.