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JP2004509971A |
The invention relates to 17alpha fluoroalkyl steroids of the general formula (I). STEROID (I), wherein R3 represents a group of the formula CnFmHo, wherein n=1, 2, 3, 4, 5 or 6, m>1 and m+o=2n+1. The invention further relates to methods ...
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JP3510651B2 |
PURPOSE: To provide a new compd. useful as a treating agent of cardiovascular diseases such as heart failure and hypertension, acting on cardiovascular system. CONSTITUTION: A deriv. of formula I {the dotted line shows α- or β- configu...
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JP2004506599A |
This invention relates to methods for treating asthma or allergy in a mammal by administering a 3-aminosteroid compound to a mammal in need thereof. The 3-aminosteroid compound being capable of down regulating the IL-9 pathway and allevi...
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JP2004505990A |
According to one aspect of the invention, there is provided a compound of formula (I) and solvates thereof. There are also provided compositions containing the compound, processes for preparing it, and its use in therapy.
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JPWO2001081364A1 |
Formula (I) [In the formula, R1 and R2 are the same or different, and represent hydrogen or lower alkyl, etc., R3 represents hydrogen, etc., R4 represents hydrogen, etc., R5 represents hydrogen, etc., R6 represents cyano, etc. Estra-1,3,...
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JP3479682B2 |
To provide a new borazine compound having a steroid skeleton, and to provide a method for efficiently producing the borazine compound. This borazine compound is represented by general formula (I) {R1 is an alkyl or aralkyl group; R2 is a...
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JP3476157B2 |
PURPOSE: To provide the subject new compound having an activity to inhibit absorption of bile acid in the small intestine and useful as a lipid level lowering agent to lower the level of cholesterol and the like by reacting bile acid wit...
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JP2003533480A |
The present invention describes a method for programming a specific course and rate of metabolism for a parent drug compound that leads to an inactive or very weakly active and nontoxic metabolite when the modified drug compound is admin...
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JP2003531916A |
A compound of the formula: and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein R groups are as defined by the present specification. The compounds may be formulated int...
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JP2003530329A |
Many compounds have poor bioavailability or variable bioavailability because of poor absorption of the compound in the small intestine. Conjugation of the compound with bile acid to form a prodrug will increase the bioavailibility of the...
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JP3445271B2 |
Compounds of formula (I), wherein R17 and R'17 are such that: either R17 and R'17 together form ketone, hydrazono, oxime or methylene, or R17 is hydroxyl, hydroxymethyl or acyloxy and R'17 is hydrogen, alkyl or optionally substitued alke...
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JP3441730B2 |
Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to either of the foregoing, are utilized for the treatment and/or prevention of vaginal atrophy, hypogonadism, dim...
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JP2003238413A |
To provide a steroid sulfatase inhibitor containing a thiophosphate derivative or its pharmacologically permissible salt as an active component.The steroid sulfatase inhibitor contains a thiophosphate derivative of formula (I) (R1 and R2...
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JP2003522728A |
Certain novel sterol derivatives can be used for regulating the meiosis in oocytes and in male germ cells.
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JP3429341B2 |
PURPOSE: To obtain a novel steroid useful as a versatile intermediate for active type vitamin Ds which improve bone mass. CONSTITUTION: A steroid of formula I [R1 is CH2OH, (CH2)3OH or the like; R2 is a protecting group; R3 is an alkoxy ...
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JP2003192693A |
To provide a new steroid derivative having surface activity.The steroid derivative is expressed by general formula (1) (R1 and R2 are each independently a (substituted) cyclopentanoperhydrophenanthrene skeleton; and R3 is a bivalent carb...
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JP3424978B2 |
PURPOSE: To obtain a new compound usuful as a drug effective as hypolipidemic medicine with a small amount which suppress the bile acid absorption concentration-dependently and antagonistically, and has high affinity for the peculiar bil...
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JP2003176297A |
To provide a pharmaceutical composition which is effective on the treatments of estrogen-dependent tumors.This pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent and a compound which contains a ring sys...
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JP3418428B2 |
PURPOSE: To provide the novel steroid compounds whose steroid skeleton is bound at carbon atom 17 to a spiromethylene ring having progestational activity and antiprogenstational activities, and useful as contraceptive medicines. CONSTITU...
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JP2003159052A |
To provide an affinity column chromatography for isolation, selection of an enzyme included in a material, in an inexpensive and simple operation.The affinity column chromatography uses an immobilized carrier obtained by immobilizing a b...
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JP3391151B2 |
PURPOSE: To obtain the subject new derivative which is a specific cholesterol derivative having an N-carbonylimidazolyl oxyalkylene chain, can be bonded to a functional substance at its end through a covalent bond and is useful as a comp...
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JP3377856B2 |
A compound represented by the following formula: X-Y-Z, wherein Y is represented by any of the formulae (III) to (V), X represents a monovalent group of a tetracycline compound, and Z represents a monovalent group of a stereoid compound ...
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JP3378245B2 |
Angiostatic steroids for use in controlling neovascularization and ocular hypertension are disclosed. Pharmaceutical compositions of the angiostatic steroids and methods for their use in treating neovascularization and ocular hypertensio...
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JP2003503419A |
This invention describes a 11beta-long-chain-substituted estratriene of general formula (I), in which R<11 >is a long-chain radical that has a nitrogen atom and optionally a sulfur atom, which in addition can be functionalized in the ter...
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JP2003502437A |
Novel phytosterol and/or phytostanol derivatives, including salts thereof, are represented by general formulae (I or II) wherein R is a phytosterol or phytostanol moiety; R2 is oxygen or hydrogen (H2) and R3 is an aromatic or heterocycli...
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JP2002543218A |
This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein: R1 is H or methyl; R2 is 5alpha- or 5beta-H; R3 is an optionally substituted N-attached heteroaryl grou...
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JP3357427B2 |
17-(3-Furyl) and (4-pyridazinyl)-5 beta ,14 beta -androstane derivatives of formula (I) wherein the symbol @ , the symbol ---, Y, R, R<1>, R<2> and R<3> have the meaning indicated in the specification. Processes of making the said compou...
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JP3344764B2 |
Monoquaternary 2,16-bispiperidinylandrostane neuromuscular blocking derivatives having the formula: wherein R1 is ethyl; R2 is methyl or allyl; and X<-> is a pharmaceutically acceptable anion; or pharmaceutically acceptable salts thereof.
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JP2002536456A |
The present invention relates to pharmaceutically active unsaturated cholestane derivatives, to pharmaceutical compositions comprising them as active substances and to the use of these novel compounds for the preparation of medicaments. ...
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JP2002533471A |
The invention relates to new 7 alpha , 17 alpha , 17 beta -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-ter...
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JP3325026B2 |
PCT No. PCT/US94/07220 Sec. 371 Date Oct. 31, 1995 Sec. 102(e) Date Oct. 31, 1995 PCT Filed Jun. 27, 1994 PCT Pub. No. WO95/00147 PCT Pub. Date Jan. 5, 1995Compounds of formula (I), wherein: R1 is selected from the group consisting of hy...
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JP2002255993A |
To obtain a pharmacological composition effective for treating an estrogen-dependent tumor.This pharmacological composition comprises a pharmacologically acceptable carrier or diluent and a compound which contains a ring system and a sul...
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JP2002523422A |
The present invention relates to novel compounds comprising a steroid hormone linked to a DNA-interacting molecule that target nucleic acids to the cell nucleus. Further, the invention relates to a method for introducing nucleic acids in...
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JP3308094B2 |
PURPOSE: To stereoselectively obtain the composition useful as intermediate product for production of medicaments from an easily available starting compound in high yield and with a secure method by using specific hydroxy cholanic acid e...
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JP2002521487A |
The present invention relates to nitrate salts of compounds having therapeutic activity in bony disorders, such compounds being characterized in that they contain at least a reactive group capable of being salified with nitric acid.
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JP2002518516A5 |
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JP3292318B2 |
PURPOSE: To obtain the captioned polymers which exert favorable influences on enterohepatic circulation, reduce cholesterol concentration in blood, exhibit superior remedial effects and are useful for the prevention of arteriosclerosis b...
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JP2002515883A |
Fatty acid derivatives of disulfide-containing compounds (for example, disulfide-containing peptides or proteins) comprising fatty acid-conjugated products with a disulfide linkage are employed for delivery of the compounds to mammalian ...
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JP2002505292A |
A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromicin and novobiocin.
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JP2002505336A |
Novel sterol derivatives of formula (I), in which: R1 represents a hydroxyl group or protected hydroxyl group, R2 represents a hydrogen atom and a double bond is present at c, or R1 and R2 together represent an oxo group and a double bon...
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JP3256236B2 |
Nucleosides and linked nucleosides functionalized to include alkylthiol chemical functionality at ribofuranosyl positions, nucleosidic base positions, or on internucleoside linkages. In certain embodiments, the compounds of the invention...
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JP2002500616A |
6 alpha -Hydroxy-21-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]-1-pip
erazinyl]-16 alpha -methylpregna-1,4,9(11)-triene-3,20-dione, 6 beta -hydroxy-21-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]-1-pip
erazinyl]-16 alpha -methylpregna-1,4,9...
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JP2001527088A |
This invention describes the new 11beta-halogen-7alpha-substituted estratrienes of general formula Iin whichR<11 >is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the descr...
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JP2001525855A |
Novel and anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependant disorders. Preferred compounds have 1,3,5-estratiene nucleus, and are substituted at the C-17 or C-11 posi...
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JP3237882B2 |
PURPOSE: To prepare a bile acid derivative having high affinity for the specified bile acid transport system of the small intestine, inhibiting bile acid absorption in a concentration-dependent and competitive manner and effective for th...
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JP3226919B2 |
The present invention concerns steroidic 5 alpha -reductase inhibitors having the following formula (I) wherein Y is oxygen or sulphur; R is a group: a) -OR4, wherein R4 is hydrogen or a C1-C6 alkyl group; b) wherein each of R5 and R6, i...
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JP2001520235A |
The invention provides estrogens and antiestrogens of formula (I) having structure (I) wherein R is (II), (III), (IV), or (V); R<1> and R<2> are each, independently, alkyl of 1-6 carbon atoms, or are alkyl groups which are taken together...
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JP3224538B2 |
Marker components are provided which are compatible with aqueous solutions, exhibit favorable fluorescence properties and exhibit decreased non-specific binding to macromolecules in solution. These marker components are useful in applica...
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JP3219408B2 |
The present invention provides a pharmaceutical composition comprising a compound admixed with a pharmaceutically acceptable diluent or carrier; wherein the compound has the the formula wherein each of R1 and R2 is independently selected...
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JP2001517296A |
Fluorescent dyes which are free of aggregation and serum binding are provided. These dyes are suitable for applications such as fluorescence immunoassays, in vivo imaging and in vivo tumor therapy. Fluorescence immunoassays methods are p...
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