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JP2004524325A |
The present invention relates to steroid derivatives for use as medicaments. More specifically, the invention also relates to the use of a steroid derivative of 5-androstene-, 5-pregnenolone or corresponding saturated derivatives (andros...
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JP3549125B2 |
Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic esters 21-carbonic esters of the formula I with A equal to CHOH and CHClm CH2, C=0, 9(11) double bond; Y equal to H, F, Cl; Z equal to H, F, methyl, R(1) equal to aryl, heta...
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JP3546886B2 |
PCT No. PCT/US94/02397 Sec. 371 Date Aug. 18, 1994 Sec. 102(e) Date Aug. 18, 1994 PCT Filed Mar. 16, 1994 PCT Pub. No. WO94/20520 PCT Pub. Date Sep. 15, 1994Compounds having a broad range of antimicrobial activity generally have a struct...
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JP2004518611A |
Aldosterone blockers used for the treatment and prevention of inflammation are disclosed
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JP2004107353A |
To provide a new sustained release formulation containing a compound, 7α-[9-(4, 4, 5, 5, 5-pentafluoropentylsulphinyl)nonyl]oestra-1, 3, 5(10)-triene-3, 17β-diol, suitable for administration by injection.The pharmaceutical formulation ...
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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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JP2004504403A |
The present invention relates to a process for the preparation of a compound of formula (I) which comprises the following step: wherein step (a) comprises oxidation of a solution containing the compound of formula (II) wherein the soluti...
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JP3490470B2 |
PURPOSE: To obtain a new compd. showing increased metabolism stability, antioxidant property and radical scavenging activity in comparison with natural bile acid and useful as an anti-cholestasis agent, choleretic, a hepatocyte protectin...
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JP3484197B2 |
Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2'-, 3'-, 5'-, nucleobase and internucleotide linkage sites. The folate can be attached via the alpha...
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JP3466651B2 |
PURPOSE: To obtain a new steroid which contains a methylene lactone group on 17-th position, which shows various hormonal activities and antihormonal activities and which is useful as a therapeutic drug for prostatic hyperfrophy, virilis...
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JP3462515B2 |
PURPOSE: To obtain the subject new compounds that have notable affinity to progesterone receptors, have little affinity to mineral corticoids, and are useful as drugs contg. anti-progestin activity having improved selectivity. CONSTITUTI...
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JP2003532420A |
Compositions and methods are provided for producing adenine nucleotide translocator (ANT) polypeptides and fusion proteins, including the production and use of recombinant expression constructs having a regulated promoter. ANT ligands an...
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JP2003531148A |
An efficient method for the synthesis of aminosterol compounds such as squalamine and compound 1436 is described. A method of the invention provides for regioselective sulfonation of a fused ring system. The fused ring system base can be...
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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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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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JP2003520238A |
The invention concerns the use of at least a compound selected in the group consisting of dehydroepiandrosterone, its chemical precursors, its chemical derivatives, its biological precursors and metabolic derivatives, for preparing a com...
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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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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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JP2002543069A |
An improved process for the preparation of single enantiomers of formula (I), and novel intermediates and processes thereto.
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JP2002542255A |
This invention describes the new ent-steroids of general formula (I) in which R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<8>, R<9>, R<10>, R<11> and R<19> have the meanings that are indicated in the description, as pharmaceutical active ...
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JP2002539134A |
The invention relates to 22R-hydroxycholesta-8,14-diene derivatives having general formula (I) wherein R1 is OR, OS03H or =NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; R4 is ...
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JP2002322168A |
To provide pharmaceutical compounds which reduce undesirable effects occurred at the region where is apart from the target site.Pharmaceutical compounds represented by general formula (I) or their salts or solvates, which are effective i...
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JP2002536455A |
3,16-Dihydroxy-1,3,5(10)-estratriene derivatives (I) are new. 3,16-Dihydroxy-1,3,5(10)-estratriene derivatives of formula (I) are new: [Image] thick black line in ring = single or double bond; R 1>H, halo, OH, Me, CF 3, OMe or OEt; R 2>H...
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JP2002308776A |
To provide a medicinal composition useful in the therapy for human prostatic adenocarcinoma.The medical composition for treating human prostatic adenocarcinoma contains a 5-α-reductase inhibiting compound such as 17β-(N-t- butylcarboxy...
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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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JP3328938B2 |
The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active comp...
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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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JP3295426B2 |
Novel antihypercholesterolemic agents are provided. An exemplary group of compounds has the structural formula (I) (I) wherein R is a C-17 side chain, R1 is -OH, =O, or the like, and X and Y are CH, C-OH, C-OCH3 or C-Z. Methods of using ...
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JP2002510295A |
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...
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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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JP2002047187A |
To obtain a telomerase inhibitor and an antitumor medicine comprising a substance having telomerase inhibitory actions as an active ingredient.This telomerase inhibitor comprises a compound represented by the following general formula (I...
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JP2001527552A |
The invention provides a pharmaceutically acceptable salt of 5 alpha -pregnan-3 beta , 16 alpha -diol-20-one 3-sulfate ester, which is useful as a progestational agent.
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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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JP2001526233A |
Compositions of angiostatic agents for treating GLC1A glaucoma and methods for their use are disclosed.
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JP2001526654A |
This invention provides estrogenic agents having formula (I) wherein A and B are each, independently, (a), (b), (c), or (d), R is SO3<->X<+>; X<+> is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 carbon atoms...
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JP2001526673A |
The invention relates to 20-aralkyl-5alpha-pregnane derivative having general formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 is (H,OR), (H,OSO3H) or NOR; R is H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is ind...
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JP2001525805A |
This invention provides a pharmaceutically acceptable salt of 5 alpha -pregn-16-en-3 beta -ol-20-one 3-sulfate ester, which is useful as a progestational agent.
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JP2001525806A |
This invention provides 3 beta -hydroxy-5,7,9-estratriene-17-one and a pharmaceutically acceptable salt of its 3-sulfate ester, which is useful as an estrogen.
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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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JP3231909B2 |
PURPOSE: To provide a new process for efficiently preparing the subject compound useful as a hormone agent, etc., by treating 21-(R,S)-acetoxy steroid compound with a diastereoselective hydrolyzing agent, sulfonylating the treated compou...
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JP2001322995A |
To provide a steroid derivative that can be derived to a variety of estrane derivatives, for example, an estrane-3-O-sulfamate derivative that acts as an inhibitory substance against estrogen sulfatase that produces estrogens as a pathog...
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JP2001523268A |
This invention provides a compound having formula (I) wherein R and R<1> are each, independently, hydrogen or SO3<->X<+>; X<+> is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 carbon atoms, or dialkylammonium...
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JP2001523266A |
This invention provides a pharmaceutically acceptable salt of 3 beta -hydroxy-5(10)-estrene-17-one 3-sulfate ester and a pharmaceutically acceptable salt of 3 alpha -hydroxy-5(10)-estrene-17-one 3-sulfate ester, which are useful as estro...
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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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JP2001518896A |
This invention provides estra-5(10),7-dien-3 beta -ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3 beta -ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-di...
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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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JP3205389B2 |
PURPOSE: To provide the new steroids having specific aromatase-inhibitory properties. CONSTITUTION: The steroids are compounds represented by the formula I (wherein: R is a substituent such as 1-4C alkyl or alkenyl group; Y is O or a res...
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JP3202240B2 |
The present invention relates to a process for the preparation and manufacture of 3-amino-substituted glycosylated bile acid derivatives. Novel intermediates and related compounds are also disclosed.
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JP2001509792A |
Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula Iwherein-A-A- represents the group -CHR4-CHR5- or -CR4=CR5-;R3, R4 and R5 are in...
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