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JP5095413B2 |
There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(1
9),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acet
amide, which process is characterized by irradiating a compound re...
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JP2012524778A |
Compounds of Structural Formula I or pharmaceutically acceptable salts thereof, are effective inhibitors of angiogenesis:
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JP2012515754A |
An agent selected from A/B-cis furostane, furostene, spirostane and spirostene steroidal sapogenins and ester, ether, ketone and glycosylated forms thereof is used to induce self-regulated homeostasis of neurotrophic factors (NFs), for e...
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JP4845320B2 |
Methods of using 7alpha,11beta-dimethyl-17beta-hydroxyestra-4,14-dien-3-one (III)
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JP4790263B2 |
The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, S represents a...
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JP4729752B2 |
To provide a method for selective deprotection of an acetal originated from aldehyde under a mild condition. The invention relates to the method for deprotection of acetal comprising conversion of acetal group originated from aldehyde gr...
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JP4719144B2 |
The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide ...
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JP2011507878A |
The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are...
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JP4629030B2 |
The invention relates to a process for preparing compounds of formula (I): in which R1, R2, R3, n and X are as defined in the description, and to the intermediate compounds for implementing this process.
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JP4589869B2 |
A process for producing a raw material for the formation of proton-exchanged zeolite analogues whose cations are wholly or partially exchanged by H<+> and which contain zeolite having tektosilicate structure, characterized by the step of...
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JP4545929B2 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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JP4545868B2 |
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JP4536373B2 |
This invention relates to nanoparticles comprising spironolactone. The nanoparticles have a mean diameter, measured by photon spectroscopy, in the range of from about 300 nm to about 900 nm.
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JP2010520178A |
The mineralcorticoid receptor antagonist comprises spironolactone, eplerenone and drospirenone. Glucocorticoid, progesterone receptor antagonist and estrogen receptor antagonist are also included. The estrogen is ethinylestradiol. ACTIVI...
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JP4476480B2 |
A compound selected from the group consisting of a compound of the formulawherein the substituents are defined as set forth in the specification which compounds are useful for the treatment of osteoporosis.
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JP4450435B2 |
The invention relates to a method of alleviating the symptoms of PMS and anxiety. The method comprises nasally administering a steroid which is a human vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor...
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JP2010031034A |
To provide a method of treatment, sapogenin, related compounds and their derivatives.There is disclosed a method of treatment of non-cognitive neurodegeneration, non-cognitive neuromuscular degeneration, motor-sensory neurodegeneration, ...
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JP4414231B2 |
The invention relates to a method of screening cellular polypeptides for pro-apoptotic or anti-apoptotic activity in a cell of a particular cell-type, said method comprising a. culturing cells of said particular cell-type under non apopt...
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JP4368945B2 |
The invention relates to compounds of the formula : wherein : R1, R2, R3, R4 and R6 each independently represent hydrogen or a (C1-C6)alkyl, R5 is hydrogen, a (C1-C6)alkyl or a group -COR7 where R7 is a (C1-C6)alkyl, n is zero or one, an...
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JP2009537470A |
The present invention relates to the use of drospirenone for manufacture of a medicament for prevention of development of high blood pressure (>140/90 mm Hg) in a patient who is predisposed to develop high blood pressure. The present inv...
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JP4331478B2 |
The invention relates to a process for the production of 4-(17alpha-methyl-substituted 3-oxoestra-4,9-dien-11beta-yl)benzaldehyde-(1E or 1Z)-oximes of general formula (I), in which R1 is a hydrogen atom, a C1-6-alkyl radical or a CnF2n+1...
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JP2009167188A |
To provide a new compound having a specific strong progesterone-like property and devoid of residual androgenic activity.The compound is expressed by formula (I), wherein R1, R2, R3, R4, R5 and R6 are each a hydrogen atom or a specific s...
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JP4263478B2 |
The invention relates to a method for the production of 4-(17alpha substituted 3-oxoestra-4,9-dien-11beta-yl)benzaldehyd-(1E or 1Z)-oximes of general formula (I), where R1-H, C1-6 alkyl or a CnF2n+1 group; R2-C1-4 alkyl, X=E- or Z-OH; an...
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JP4260886B2 |
A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, ...
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JP4215603B2 |
New aromatic diamine derivatives and the preparations thereof are disclosed. The inventive diamine derivatives can be added to conventional polymerization reactions of tetracarboxylic acids and diamines to form new polyamic acids. After ...
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JP4146897B2 |
Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I wherein: -A-A- represents the group -CHR4-CHR5- or CR4-CR5- R3, R4 and R5 are ...
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JP4145350B2 |
The invention relates to a 3 alpha -hydroxy, 17-(un)substituted derivatives of the androstane series and 3 alpha -hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at the recently identif...
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JPWO2006062129A1 |
The present invention has the formula (I).(5α, 7α) -3-spiro-2'-(1', 3'-dioxolan) -24-oxocholest-22-en-7-yl benzoate (unsaturated ketone (I)) The crude product containing the unsaturated ketone (I) obtained from the reaction step is dis...
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JP4097697B2 |
PCT No. PCT/EP96/04506 Sec. 371 Date Apr. 20, 1998 Sec. 102(e) Date Apr. 20, 1998 PCT Filed Oct. 17, 1996 PCT Pub. No. WO97/14696 PCT Pub. Date Apr. 24, 1997Compounds of the general formula Ia and Ib are described in which R1 and R2 are ...
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JP2008100996A |
To synthesize epoxymexrenone and an epoxymexrenone-based compound.Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone compounds of the formula I, wherein: -A-A- re...
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JP2008512439A |
A method for converting a steroid substrate having a 4,7-carbonyl bridge into a structure containing a 7α-alkoxycarbonyl substituent by reacting the substrate with an alkoxy group source, preferably in the presence of a base, is describ...
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JP4039683B2 |
A codrug composition of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug composition, and methods of use of the codrug for the treatment of various medical conditions. The codrug may ...
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JP4012293B2 |
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JP2007530557A |
Processes are described for epoxidation reactions. In particular, the process comprises the conversion of a steroid substrate having an olefinic unsaturation in the steroid nucleus to a structure comprising a 9,11-epoxy substituent by re...
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JP2007528388A |
The present invention relates to liquid pharmaceutical compositions comprising steroidal drugs, such as drospirenone, in molecularly dispersed form. The compositions are adapted for oral administration and preferably to be absorbed from ...
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JP3984315B2 |
The invention relates to a method of the preparation of a steroid derivative ketal according to the general formula I: wherein R1 is CH3 or C2H5; R2 is OH; R3 is H, CH3; C IDENTICAL CH, CH2Hal,, or CH2CN; or R2 and R3 together are O; R4 ...
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JP3983796B2 |
This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3 alpha -hydroxy,3 beta -substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereosele...
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JP3977462B2 |
The invention relates to a 11-(substituted phenyl)-estra-4,9-diene derivative of formula I wherein A is a residue of a 5- or 6-membered ring containing 2 heteroatoms which are not connected to each other and independently selected from O...
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JP3950489B2 |
PURPOSE: To obtain the subject compound used for betamethasone source material, etc., by dehydrating a 17α-hydroxy-17β-cyanoandrosta-diene-3-one to an novel intermediate, bringing a CN group to a methyl ketone and methylating after epo...
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JP2007016043A |
To provide an aldosterone receptor antagonist drug eplerenone having a new crystalline form which exhibits relatively high physical stability at normal temperatures of storage and use.A process for preparing Form L crystalline eplerenone...
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JP2006315997A |
To provide a substance useful for treatment, etc., of life-style related diseases and capable of effectively controlling serum lipid concentration and blood sugar.The present invention provides a cholesterol oxide which can be functional...
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JP3845482B2 |
To isomerize an equilin into a delta (8,9)-dehydroestrone easily convertible to a component of a composite estrogen composition for hormone exchange therapy, etc., by treating an equilin with ethylenediamine Li salt or Li amide. An equil...
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JP3844358B2 |
Novel acridinium esters that are useful, either alone or when incorporated into liposomes, as chemiluminescent agents in binding assays (e.g., immunoassays and gene probe assays) with improved sensitivity are disclosed. In addition, the ...
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JP2006524289A |
This invention relates to soluble derivatives of wortmannin that utilizes water-soluble polymers as carriers for a drug and includes compounds having the structures as described within the specification.
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JP2006522078A |
Dehydro-epiandrosterone (DHEA) derivatives (I) are new. Dehydro-epiandrosterone (DHEA) derivatives (A) are new. [Image] n : 1 or 2; R 1, R 2oxo or -O-W-O-; W : 2-8C linear, branched, cyclic, saturated or unsaturated alkyl (preferably CH ...
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JP2006519255A |
Methods for the preparation of the 19-norprogesterone of formula I and its intermediates, in crystalline and amorphous forms.
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JP3814284B2 |
This invention relates to processes for the preparation of 7-carboxy substituted steroid compounds of Formula I,
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JP2006151994A |
To provide a simple method for converting a pregnane-3,20-dione compound into a 3α-hydroxy-3β-substituted-pregnane.An unprotected dione is chemoselectively and stereoselelctively converted into a 3(R)-pregnane-3-spiro-2'-oxiran-20-one ...
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JP2006515869A |
The process comprises (a) forming 17±-acetoxy-11²-(4-N,N-dimethylaminophenyl)-19-norpregna-4
,9-diene-3,20-dione (VA-2914) isopropanol hemisolvate crystals by dissolving in isopropanol and subsequently crystallising; (b) separating the...
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JP3770904B2 |
PCT No. PCT/EP93/01606 Sec. 371 Date Apr. 18, 1995 Sec. 102(e) Date Apr. 18, 1995 PCT Filed Jun. 22, 1993 PCT Pub. No. WO94/04553 PCT Pub. Date Mar. 3, 1994.A process for the production of 1-methyl-3-keto- DELTA 1,4 steroids of general f...
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