81 |
JPS50157351A - |
JP5383475 |
1975-05-02 |
JPS50157351A |
1975-12-19 |
|
|
82 |
JPS5034022B1 - |
JP3577968 |
1968-05-28 |
JPS5034022B1 |
1975-11-05 |
|
|
83 |
JPS4926214A - |
JP6814472 |
1972-07-07 |
JPS4926214A |
1974-03-08 |
|
|
84 |
JPS49180B1 - |
JP2414864 |
1964-04-30 |
JPS49180B1 |
1974-01-05 |
|
|
85 |
JPS4831107B1 - |
JP6465370 |
1970-07-24 |
JPS4831107B1 |
1973-09-26 |
|
|
86 |
化合物の不斉合成および疾患処置における使用 |
JP2020512701 |
2018-08-22 |
JP2020531566A |
2020-11-05 |
ヤン, ジュン; シュー, ウェンピン |
本出願は、とりわけ、式(I)のジアステレオマー化合物(例えば、α−アノルドリン)またはその塩の不斉合成を開示する。また、式(I)のジアステレオマー化合物(例えば、α−アノルドリン)またはその塩を単独でまたは少なくとも1つのさらなる薬剤と組み合わせて使用する、エストロゲン欠乏の処置ならびにエストロゲン欠乏症状の予防または軽減のための方法および組成物が提供される。さらに、式(I)のジアステレオマー化合物(例えば、α−アノルドリン)またはその塩との併用療法の状況におけるさらなる薬剤の副作用を軽減するための方法および組成物が提供される。
|
87 |
2-methylene--1α, 25- dihydroxyvitamin -19,21- dinor vitamin D3 analogues and their use |
JP2009504492 |
2007-04-06 |
JP2010505739A |
2010-02-25 |
マーガレット クラゲット−デーム; ヘクター エフ. デルカ; ラファル バリッキ; ローリ エー. プラム |
式Iの化合物が提供され、式中、X
1 、X
2 、およびX
3はHまたはヒドロキシ保護基から独立に選択される。 そのような化合物は薬学的組成物の調製において用いられ、様々な生物学的状態の治療において有用である。
|
88 |
Detection of cholesterol ozonation products |
JP2006525517 |
2004-09-03 |
JP2007504250A |
2007-03-01 |
ポール ウェントワース,; リチャード エー. レーナー, |
本発明は、アテローム硬化性プラーク物質によって生成されるコレステロールオゾン化生成物の検出ならびにコレステロールの蓄積および酸化に関する血管状態の検出方法に関する。 本発明によれば、コレステロールオゾン分解生成物は、アテローム硬化性プラーク中に存在する。 さらに、患者から採取した組織および体液中のコレステロールのオゾン化生成物の検出および定量は、アテローム硬化性病変が患者に実際に存在するかどうかの正確な指標である。 したがって、本発明は、アテローム硬化性病変が患者中に存在するかどうかを簡潔かつ正確に検出する方法を提供する。 |
89 |
New apoptosis inducing agent and method for producing the same |
JP2001159964 |
2001-05-29 |
JP2002356428A |
2002-12-13 |
MIYAMOTO TOMOFUMI; HIGUCHI RYUICHI; KODAMA KOTA |
PROBLEM TO BE SOLVED: To provide a new apoptosis inducing agent comprising a compound which is safe to human bodies.
SOLUTION: This apoptosis inducing agent comprises orostanal represented by formula 1 or a synthetic analogue of orostanal represented by formula 2 {wherein R is hydroxy group, a lower alkoxy group which may have a substituent group (methoxy, ethoxy, propioxy, butyloxy or the like), a lower acyloxy group which may have a substituent group (acetoxy, ethoxycarbonyl or the like), an amino group, a lower alkylamino group (methylamino, ethylamino, isopropylamino or the like), a di-lower alkylamino group (dimethylamino, diethylamino or the like) or a 5 or 6-membered nitrogen-containing heterocyclic group (pyrrolidin-1-yl, piperidino, morpholino, 4-morpholylcarbonyl, piperazin-1-yl, 4-methylpiperazin-1-yl or 4-ethylpiperazin-1-yl)} or a pharmacologically permissible salt thereof.
COPYRIGHT: (C)2003,JPO |
90 |
New glycyrrhetinic acid derivative and sweetener |
JP18903996 |
1996-07-18 |
JPH1028548A |
1998-02-03 |
MACHINAMI TOMOYA; SUAMI TETSUO |
PROBLEM TO BE SOLVED: To obtain a new glycyrrhetinic acid derivative, having a structure with a sweetness quality and a string sweetness similar to that of sugar and useful for a low-caloric sweetener substitutive for the sugar. SOLUTION: This new glycyrrhetinic acid derivative is a 3β-O-glycyrrhetinic acid ester of L-aspartic acid represented by formula I or a 3β-O-glycyrrhetinic acid ester of L-aspartyl dipeptide represented by formula II (X is glyciner of L-phenylalanine) and a salt thereof and the bond between the L-Asp and the 3β-O of the glycyrrhetinic acid and the bond between the L-Asp and the Z are α- or β-bonds. The derivative can be obtained by a method for condensing glycyrrhetinic acid having the carboy group protected as a benzyl ester with aspartic acid having the amino group protected with t-butoxycarbonyl group and one of carboxyl groups protected with benzyl group, and the removing the protecting groups according to the catalyst reduction and hydrolysis with an acid, etc. |
91 |
Photoaging inhibitor and dermal agent for external use |
JP17264096 |
1996-07-02 |
JPH09143050A |
1997-06-03 |
MATSUMOTO KATSUO; TSURUOKA HIROKI; FUJIWARA NORIO; NISHIMORI YASUTOMO; YOKOYAMA YUKIKO |
PROBLEM TO BE SOLVED: To obtain a photoaging inhibitor consisting of a triterpenoid derivative, and a dermal agent for external use excellent in skin beautifying effects capable of preventing and improving wrinkles of the skin, etc. SOLUTION: This photoaging inhibitor is obtained by containing a triterpenoid derivative and it salt obtained by substituting H of carboxyl group at the position 28 in ursolic acid, oleanolic acid and betulinic acid [e.g.; a group of formula I (R1 is an aromatic ring; R2 is H or an aromatic ring)] and/or H of OH group binding with C at the position 1 [e.g.; a group of the formula I and formula II (R3 is an aromatic ring; n is 0-2] with a functional group, and at least one of the above functional groups has an aromatic ring. Further, by containing 0.0001-10wt.% triterpenoid derivative or its salts, a preparation of skin cosmetic material such as a cream, a milky lotion and an oil, can be prepared. This photoaging inhibitor can manifest a sufficient photoaging inhibiting effect by a small blending amount in blending into the composition. The skin cosmetic material can be used safely without any ill effect. |
92 |
Novel 3-keto-delta4,9-19-norsteroid derivative |
JP4602390 |
1990-02-28 |
JPH02275895A |
1990-11-09 |
DANIERU FUIRIBEERU; JIYAN JIYORUJIYU TOUUCHI; JIERUMAN KOSUTORUUSU; ROJIE DORAE |
NEW MATERIAL: A compd. represented by formula I [wherein R
1' is a (substd.) thienyl, furyl, a cycloalkyl or a (substd.) phenyl, R
2 is methyl or ethyl, R
3' is H, a (substd.) alkyl, an alkenyl or a (protected) acetyl, R
4' is H, OH or a (substd.) 1-12C alkyl, R
3" is H or methyl at an α- or β-position and K is a ketone blocked in a form of ketal, thioketal, oxime and methyloxime].
EXAMPLE: 17β-Hydroxy-17α-(1-propynyl)-11β-(2'-thienyl)estra-4,9-dien-3-one.
USE: This new material is useful for hypertension, atherosclerosis, osteoporosis, diabetes, obesity, immune depression and agrypnia.
PROCESS: A dehydrating agent capable of liberating a protected functional group is allowed to act on a compd. represented by formula II.
COPYRIGHT: (C)1990,JPO |
93 |
Phosphinic acid substituted steroid as steroid 5alpha-reductase inhibitor |
JP33467289 |
1989-12-22 |
JPH02215796A |
1990-08-28 |
DENISU ARAN HORUTO; MAAKU ARAN REBII; BURAIAN UORUTAA METOKARUFU |
NEW MATERIAL: The compound (salt) of the formula I [R is H, a 1-4C alkyl; Z is the formula (CH
2)
n (n is 0-2); X is H, CL, F, Br, I, CF
3, C
1-6 alkyl; Y is H, CF
3, F, Cl, CH
3; R
1 is α-H or absent; R
2 is H, CH
3 or absent; R
3 is α-H, α-OH, α-acetoxy, etc.].
EXAMPLE: 17β-(N,N-diisopropylcarboxyamide)-androst-3,5-diene-3-phosphinic acid.
USE: Therapautic agent for acne vulgaris, seborrhea, hypertrichosis, prostatic hypertrophy or alopecia.
PROCESS: The compound of formula I is obtained, e.g. by using 4-ene-3-one compound of formula II (R' is identical to R
3) as the starting material, dissolving it in an organic solvent such as dimethylformamide, and treating it with hypophosphorous acid under an inert atmosphere.
COPYRIGHT: (C)1990,JPO |
94 |
Phosphonic acid substituted steroids as steroid 5alpha-reductase inhibitor |
JP33467189 |
1989-12-22 |
JPH02215795A |
1990-08-28 |
DENISU ARAN HORUTO; MAAKU ARAN REBII; BURAIAN UORUTAA METOKARUFU |
NEW MATERIAL: The compound of the formula I (ring A contains two or less double bonds; no adjacent double bonds exist in rings A-C; no double bond exists between 16C and 17C atoms in ring D when R has two substituents or a divalent substituent; Z is (CH
2)
n (n is 0-2); X is H, Cl, etc.; Y is H, CF
3, etc., but when no double bond exists between 5C and 6C atoms, Y is H; R
1 is α-H, but R
1 is absent when double bonds exist between 4C and 5C, 5C and 6C or 5C and 10C atoms; R
2 is H, CH
3, but R
2 is absent when the carbon atom to which it is bonded forms a double bond; R is α-H, cyano, keto, etc).
EXAMPLE: 17β-(N-t-butylcarboxyamide)-androst-3,5-diene-3-phosphonic acid.
USE: Steroid 5α-reductase inhibitor.
PROCESS: The compound is synthesized through compounds of formulae III and IV by using the compound of formula II (R
10 is R or a group convertible to R) as starting materials.
COPYRIGHT: (C)1990,JPO |
95 |
JPS6157320B2 - |
JP4378876 |
1976-04-19 |
JPS6157320B2 |
1986-12-06 |
ANDORU FUYURUSUTO; YURUKU GUTSUBIRAA; BERUNAA MAIAA; GERUHARUTO ZAUAA |
|
96 |
3-keto-delta 4,9,19-norsteroid novel derivatives, manufacture, use as drug, composition and novel intermediate |
JP3190983 |
1983-03-01 |
JPS58201800A |
1983-11-24 |
DANIERU FUIRIBEERU; JIYAN JIYORUJIYU TOUUCHI; JIERUMAN KOSUTORUUSU; ROJIE DORAE |
|
97 |
JPS5844360B2 - |
JP3473373 |
1973-03-28 |
JPS5844360B2 |
1983-10-03 |
ANDORU FURUSUTO; REO ARIGU; MARUSERU MYUURAA |
|
98 |
Manufacture of d-homosteroid of pregnanes |
JP17110982 |
1982-10-01 |
JPS5877899A |
1983-05-11 |
ANDORU FURUSUTO; REO ARIGU; MARUSERU MIYUURAA |
|
99 |
JPS5511680B1 - |
JP3011371 |
1971-05-06 |
JPS5511680B1 |
1980-03-26 |
|
|
100 |
Novel steroid |
JP3592378 |
1978-03-28 |
JPS53119862A |
1978-10-19 |
AASAA FURIIDORITSUHI MARUKUSU; KORUNERISU BUOSU |
|