Abstract: The present invention discloses compositions and methods for selectively delivering apoptosis inducing agents to the tumor prior to conventional therapeutic treatment protocol. Specifically, the present invention relates to an ensemble (or ‘AAAPT bioconjugate’) comprising an apoptogen (A) and a tumor targeting group (T), wherein the apoptogen is either connected directly to the targeting group or optionally attached through an intervening linker (L). The apoptogen may be a small or large molecule that activates apoptosis pathway and causes cell death. The targeting vector may be a small or large molecule that delivers the apoptogen selectively to the tumors. The linker may comprise simple alkylene chain or may contain functional groups that are capable of being cleaved by enzymatic process.

Abstract: Provided is a metal complex which is excellent in quantum yield and full width at half maximum of a light emission spectrum. The metal complex is represented by the following formula (1): wherein M represents an iridium atom or the like, n1 represents 1 to 3, n2 represents 0 to 2, X1 to X8 represent a carbon atom or the like, R1 to R8 represent a hydrogen atom or the like, one of Xa and Xb is a single bond, and the other is a group represented by —CR11R12—CR13R14—, R11 to R14 represent an alkyl group or the like, ring A represents a heteroaromatic ring, and A1-G1-A2 represents an anionic bidentate ligand.

Abstract: The present invention relates to compounds derived from steroids of the general formula (I) wherein L represents a linker and R# represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).

Abstract: The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.

Abstract: The present application discloses 17? hydroxy steroid dehydrogenase (17? HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17? HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17? HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17? HSD1 and 17? HSD3 that have a spiro-morpholine substituent at C20.

Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.

Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.

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 methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception.

Abstract: Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds.

Abstract: The subject matter of the instant invention is pertinent to the field of treatment of hormone-dependent conditions. New compounds and methods for treating these conditions are disclosed. Embodiments of the instant invention disclose methods for treating endometriosis, dysmenorrhea, breast cancer, uterine fibroids and endometrial hyperproliferation.

Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of the formula I with a progesterone antagonising effect and processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and also their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular of uterus fibroids (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeding, meningiomas, hormone-dependent breast cancers and troubles associated with the menopause or for monitoring fertility and emergency contraception.

Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-benzylidene derivatives of the formula I, in which Y and X are each as defined in the claims and the description, to a process for preparation thereof and to the use thereof as medicaments.

Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-aryl derivatives of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.

Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-ethynylphenyl derivatives of the formula I, in which R1 and X are each as defined in the claims and the description, and to a process for preparation thereof and to the use thereof as medicaments.

Abstract: The invention relates to 17?-alkyl-17?-oxy-oestratrienes of the formula (I), to processes for their preparation, to the use of the 17?-alkyl-17?-oxy-oestratrienes for preparing pharmaceuticals and to pharmaceutical preparations comprising these compounds.

Abstract: Steroid compounds possessing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: 3,15-substituted estrone compounds which act as inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17?-estradiol concentration, as well as the general use of selective 17?-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.

Abstract: The present invention provides quinaldine-based semisquaraines, symmetrical and unsymmetrical squaraine dyes represented by the general formulae 1, 2 and 3 and/or pharmaceutically acceptable derivatives thereof as sensitizers for photodynamic therapeutical and industrial applications. These symmetrical and unsymmetrical squaraine dyes posses absorption which extends well into the photodynamic window (650-800 nm) and hence are useful for the treatment of deep seated tumors. The absorption of these dyes can be tuned by changing the substituents on the quinaldine moiety thereby enabling the development of a library of dyes which have absorption ranging from 650 to 800 nm. They also exhibited fluorescence emission in the long wavelength region making them useful as near infrared fluorescence sensors for the detection of tumors. These dyes are non-toxic in the dark and exhibit good photocytotoxicity.

Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: This application is directed to the use of steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.

Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.

Abstract: The subject invention provides a compound according to Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.

Abstract: Compositions and methods for treating a cancer in mammals by administering selective estrogen receptor modulators particularly compounds represented by: or any other of the structures contained herein, or of a stereoisomer, enantiomer, rotomer, tautomer or pharmaceutically acceptable salt form thereof.

Abstract: The invention relates to the use of a deoxynojirimycin derivative, or pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of insulin resistance, hyperpigmentation and/or inflammatory processes in the skin, a fungal disease, overweight and obesity, or a microbacterial infection.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: There are provided according to the invention compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and——represents a single or a double bond; and salts and solvates thereof. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.

Abstract: Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: An amphoteric compound based on a sterol skeleton, the 3-position of the sterol ring system being substituted by one or more amphoteric groups having an isoelectric point of between about 4 and 9, together with liposomes containing such compounds and their uses.

Abstract: A sterol derivative with a pKa value of between 3.5 and 8, according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent linking groups, is suggested, as well as liposomes comprising such sterol derivatives.

Abstract: Disclosed is a sterol derivative having a pKa value of 3.5-8 according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent bonding groups. The invention also relates to liposomes containing said sterol derivatives.

Abstract: The present invention relates to useful diterpenes and pharmaceutical compositions containing them of the formula: for use in the treatment of cardiovascular and inflammatory diseases and for cancers susceptible to an NF-?B inhibitor and an endothelin receptor inhibitor. The present invention also relates to compounds and methods useful to inhibit cell proliferation and for the induction of apoptosis.

Abstract: wherein X may be —CH2—O—CH2— or —CH2—, wherein n may be 1, 2, 3, 4 or 5 when X is —CH2—O—CH2—, wherein n may be 2, 3, 4, 5, 6, 7, 8, 9 or 10 when X is —CH2—, wherein o may be 1, 2 or 3, wherein Y may be O or 17?-OH, where the dotted line represents the presence or absence of a second chemical bond, wherein R1 may be selected from the group consisting of H, straight alkyl groups of 1 to 5 carbon atoms, and branched alkyl groups of 3 to 5 carbon atoms, wherein R2 may be selected for the group consisting of H, straight alkyl groups of 1 to 4 carbon atoms, branched alkyl groups of 3 or 4 carbon atoms, F, Cl, Br, I, —CF3, —NO2, —OR1, where R1 is as defined hereinabove, —COR1, where R1 is as defined hereinabove, and —CH2OH. These compounds possess anticancer activity against hormono-dependent breast, uterus as well as ovarian cancers.

Abstract: The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I): {wherein R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group or, etc.; R3 represents a hydrogen atom etc.; R4 represents a hydrogen atom etc.; R5 represents a hydrogen atom etc.; R6 represents a cyano group, an amino group, COR53 (wherein R53 represents a substituted lower alkyl group etc.), a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, etc}, or pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to steroid compounds of general formula X, which may advantageously be employed to stimulate meiosis in human oocytes, the steroid being specifically characterized by amino nitrogen bonded to C17 of the steroid skeleton via a spacer A.

Abstract: The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ?O and ?N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.

Abstract: There are provided compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents a 4-7 membered non-aromatic ring containing 1-3 heteroatoms selected from O, N and S optionally substituted with one or more methyl, ethyl or halogen groups; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and (a) represents a single or a double bond; and salts and solvates thereof; processes for preparing them and their use in therapy.

Abstract: The subject of the invention is a method for preparing compounds of general formula (I): 1

Abstract: The invention relates to a process for preparing compounds of formula (I): 1

Abstract: The present invention concerns the use of methods and/or compositions related to the synthesis and use of fatty asparagine, cysteine and/or serine derivatives. In particular, the invention concerns methods and compositions for the production of liposomes including fatty asparagine, cysteine and/or serine derivatives.

Abstract: Disclosed are compounds having the formula: 1

Abstract: A process for the preparation of compounds of formula (I) 1

Abstract: This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I in which R11 is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the description. The compounds have antiestrogenic properties or tissue-selective estrogenic properties and are suitable for the production of pharmaceutical agents.

Abstract: A compound of the formula 1

Abstract: The invention concerns biotin derivatives of general formula (I), wherein: R1 represents a specific compound; X1 represents a carbonaceous chain, preferably of 1 to 10 carbon atoms, substituted or not, optionally comprising one or several carbonyl or oxycarbonyl groups, and/or a —NH— group, in particular a chain of formula —HN(CH2)n—O—CO wherein n is an integer between 1 and 5 and optionally comprising one or several ether, amide and/or amino functions; Y represents a hydrocarbon chain of 1 to 5 carbon atoms, substituted or not; R2 represents a hydrogen atom, or a protecting group, in particular R2 represents an alkyl group of 1 to 5 carbon atoms. The invention is useful as vectors, in particular for implementing methods for detecting interactions between biological compounds, and in pharmaceutical compositions.

Abstract: The present invention provides novel C24-sulfone analogs of 1&agr;,25-dihydroxy vitamin D3, compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1&agr;,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.

Abstract: Disclosed is a sterol derivative having a pKa value of 3.5-8 according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent bonding groups. The invention also relates to liposomes containing said sterol derivatives.

Abstract: The invention relates to a sterol skeleton based compound wherein one or several amphoteric groups with an isoelectric point of between 4 and 9 are substituted on the 3rd position of the ring system, in addition to liposomes containing said compounds.