141 |
9-substituted minocycline compound |
JP2002509074 |
2001-06-29 |
JP2004502752A |
2004-01-29 |
イスメイル モハメド; コザ ダレル; シャーハン パウル; ステープルトン カレン; ドゥモーネイ ジミー; ネルソン マーク エル.; バーマ アチュル; バウザー トッド; バティア ビーナ; ビスキー ピーター; フレシェット ロジャー; ホーキンス パウル; マッキンタイアー ラウラ; リュー グイ; レニー グレン; ワーコル タッド |
本発明は、少なくとも一部において、新規の9−置換ミノサイクリン化合物に関する。 これらのミノサイクリン化合物は、細菌感染症および新生物形成性疾患のような多くのテトラサイクリン化合物−反応状態を治療するため、更には例えば、テトラサイクリン排出の阻害および遺伝子発現の変調のような、一般的ミノサイクリンおよびテトラサイクリン化合物の公知の他の適用のために使用することができる。 |
142 |
Amino acid derivative anticonvulsant |
JP50065093 |
1992-06-04 |
JP3330374B2 |
2002-09-30 |
エル コーン,ハロルド; ワトスン,ダレル |
|
143 |
Amino acid derivative anticonvulsant |
JP2001371994 |
2001-12-05 |
JP2002241355A |
2002-08-28 |
KOHN HAROLD L; WATSON DARRELL |
PROBLEM TO BE SOLVED: To obtain a new compound capable of acting on a central nerve, especially having an antispasmodic action. SOLUTION: The compounds are represented by formula (I) [R is an aryl, an aryl lower alkyl group or the like; R1 is hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl, an aryl lower alkyl, an aryl or the like; R2 and R3 are hydrogen, a lower alkenyl, a lower alkynyl or the like; n is 1-4; A and Q are independently O or S], their N-oxides or pharmaceutically acceptable salts and anticonvulsants comprising them. |
144 |
Novel acyl - and dipeptide-like compound, and a manufacturing method thereof, a pharmaceutical composition comprising the same |
JP2000557223 |
1999-06-23 |
JP2002519338A |
2002-07-02 |
ジャック ボーエ; オリヴィエ リチャード マルタン |
(57)【要約】 【課題】 一般式Iの新規化合物と、有効成分として酸の形または有機または無機塩基との塩の形の化合物を含む医薬組成物と、医薬品として利用。 【解決手段】 一般式(I)を有するN-アシル−ジペプチド様化合物: 【化1】 (置換基A、B、X、Y、R
1 、R
2およびn、m、p、qは請求項に定義の意味を有する) |
145 |
Compound having growth hormone releasing characteristic |
JP24793598 |
1998-08-13 |
JPH11209336A |
1999-08-03 |
HANSEN THOMAS KRUSE; PESCHKE BERND; LAU JESPER; LUNDT BEHREND FRIEDRICH; ANKERSEN MICHAEL; WATSON BRETT; MADSEN KJELD |
PROBLEM TO BE SOLVED: To obtain the subject new compound sowing more raised bioavailability than that of an already-known compound, useful for treating bodily disorders caused by deficiency of growth hormone. SOLUTION: This compound is shown by formula I [R<1> is H or a 1-6C alkyl; R<2> is a 1-6C alkyl; (a) and (b) are each 1 or 2; G and J are each a group of formula II or formula III (R<27> to R<31> are each H, a halogen or the like); D is a group of formula IV (R<7> to R<10> are each H, a 1-6C alkyl which may be substituted with amino or the like; (n) and (m) are each 0-3; (o) and (p) are each 0 or 1; M is O, S or the like); E is a group of the formula, CONR<12> R<13> (R<12> is H or a 1-6C alkyl which may be substituted with a halogen or the like; R<13> is a 1-6C alkyl which may be substituted with hydroxy or the like)] such as (4-(1-aminocyclobutyl)but-2-enoic acid ((1R)-1-(((1R)-1-(1-methylcarbamoyl-2- phenylethyl)methylcarbamoyl)-2-(2-naphthyl)ethyl)methylamide. The compound of formula I is obtained, for example, by starting from ethyl chloroformate and 3-tert-butoxycarbonylamino-3-methylbutanoic acid. |
146 |
Water-soluble, non-ionic x-ray contrast agents and methods for their preparation |
JP50670592 |
1992-03-19 |
JPH0768197B2 |
1995-07-26 |
ケーレル、ゲルノト; ブルンス、ヴィルフリート |
|
147 |
New Haidorokisamu acid |
JP21253986 |
1986-09-09 |
JPH0764800B2 |
1995-07-12 |
ロジヤー マツケイ ウイリアム; フイリツプ デイケンズ ジヨナサン; ニーン ジヨフレイ; ケイス ドナルド デビツド |
|
148 |
New arylglycinamide derivative and its production |
JP19688293 |
1993-07-14 |
JPH0692921A |
1994-04-05 |
MIYAJI HIROYUKI; SEGAWA MITSURU; TAGAMI EMIKO; OKUBO HIDEO |
PURPOSE:To provide a new arylglycinamide derivative useful as an agent for the treatment of urinary disturbance such as incontinence of urine and pollakiuria. CONSTITUTION:The compound of formula I [Ar is (substituted) phenyl or (substituted) naphthyl; R1 and R4 are H or 1-3C alkyl; R2 is 1-6C alkyl, 3-6C cycloalkyl, (substituted) 1-4C alkyl, norbornyl, adamantyl or (substituted) phenyl; R3 is H, 1-6C alkyl or together with R2 form an alkylene; R5 is 1-6C alkyl or 5-6C cycloalkyl; R6 is H, 1-6C alkyl or together with R5 form an alkylene; (m) is 2 or 31 and its salt, e.g. N-cyclohexyl-alpha-[[2-(t-butylamino) ethyl]amino]phenylacetic acid amide. The compound can be produced by reacting a compound of formula II (X is eliminable group) with a compound of formula III. |
149 |
JPH0468304B2 - |
JP11555485 |
1985-05-30 |
JPH0468304B2 |
1992-11-02 |
HERUBERUTO KURENKU |
|
150 |
JPH04500377A - |
JP50614189 |
1989-05-30 |
JPH04500377A |
1992-01-23 |
|
|
151 |
Amino acid derivative |
JP4869389 |
1989-03-02 |
JPH023646A |
1990-01-09 |
KUIRIKO BURANKA; BERUNAA NAITOHARUTO; HENRI RAMUTSU; HAINTSU SHIYUTAADORAA; BORUFUGANGU BOSUTORU |
NEW MATERIAL: Compounds of formula I [R
1 is H, methyl; R
2 is ethyl, propyl, pyrazol-3-yl, etc.; R
3 is isobutyl, benzyl, etc.; R
4 and R
5 are each H, (substituted) alkanoyl, etc.; R
6 is formula II, formula III (D is CH, N; R
7 is alkyl, aryl, etc.; R
8 is H or R
7; R
9 is H or alkyl R
10 and R
11 are each R
7, cycloalkyl, etc.); A is formula IV, -Y-Z (R
12 is phenyl, naphthyl, etc.; R
13 is H, alkoxycarbonyl alkyl, etc.; Y is N, phenyl alanine, etc.; Z is acyl)].
EXAMPLE: (S)-α-[(S),-α-[(t-Butylsulfonyl)methyl]hydrocinnamamide], -N-[(1S,2R,3 S)-1-(cyclohexylmethyl)-2,3-dihydroxy-4-methyopentyl)] imidazole-4-propionamide.
USE: Renin inhibitor, useful for the suppression and prophylaxis of hypertension and cardiac insufficiency.
PROCESS: For example, a compound of formula V is reacted with a compound of formula VI to obtain a compound of formula I.
COPYRIGHT: (C)1990,JPO |
152 |
Alpha-aminoacyl beta-aminoacyl aminodiol as antihypertensive agent |
JP24729088 |
1988-09-30 |
JPH01113353A |
1989-05-02 |
GUNNAA JIEEMUSU HANSON; JIYON SUTANISURAUSU BARAN |
NEW MATERIAL: A compd. expressed by formula I [wherein R
9 is H, alkyl or formula II (Y is CH
2, O, S, etc.; T is H, lower alkyl, etc.; m and n are each 1 to 4), etc.; R
1 is H, lower alkyl, etc.; R
2 is lower alkyl, benzyl, etc.; R
3 is lower alkyl, aryl, etc.; R
4 to R
6 and R
8 are H or lower alkyl; R
7 is cycloalkyl, phenyl, etc.].
EXAMPLE: Boc-L-phenylalaninyl-D,L-α-methyl-β-alanineamide of (2S,3R,4S)-2- amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane.
USE: Antihypertensive agent, especially useful as a renin inhibitor.
PREPARATION: An allyl acetate expressed by formula III is used as the starting material and is subjected top ozonization, alkylation, reduction, coupling, etc., to obtain the compd. of formula I.
COPYRIGHT: (C)1989,JPO |
153 |
Simultaneous production of aniline and oxamide |
JP13179088 |
1988-05-31 |
JPS643155A |
1989-01-06 |
EITO DORENTO |
PURPOSE: To simultaneously obtd. aniline and oxamide by allowing an arom. nitro compd. to react with CO and an amine in the presence of a specified catalyst system by changing an amount of the amine.
CONSTITUTION: An arom. nitro compd. of formula I [where X is halogen, alkyl, alkoxy, aryloxy, etc., and (n) is 0-5] is allowed to react with CO and an excess (mol) of an amine of the formula NHR
2 (R is alkyl) over the nitro compd. preferably at 70-150°C to obtain the objective aniline of formula II and the objective oxamide of formula III. At this time, the reaction is carried out in the presence of a catalyst system consisting of metal Pd or its compd., a bidentate ligand of the formula, R
1R
2-M-A-M-R
3R
4 (where M is P, As or Sb, A is a divalent org. bridge-like group, etc., and each of R
1-R
4 is substd. hydrocarbon), e.g. 1,3-di(diphenylphosphino)propane and an acid or its transition metallic salt, e.g. acetic acid or copper acetate.
COPYRIGHT: (C)1989,JPO |
154 |
Novel amino-propanol derivative, manufacture, cardiac and circulatory disease remedy, intermediate and manufacture |
JP3768988 |
1988-02-22 |
JPS63233962A |
1988-09-29 |
HERUBERUTO SHIMON; HERUMUUTO MIHIERU; BUORUFUGANGU BARUCHIYU |
|
155 |
2-aminoacetamide derivative |
JP2295788 |
1988-02-04 |
JPS63216853A |
1988-09-09 |
RONARUDO SHII GURIFUISU; JIEIMUZU JIEI NEIPIA |
|
156 |
Novel optically active derivative of (r)-5-pentylamino-5-oxopentanoic acid antagonistic against cholecystokinin and manufacture |
JP2641788 |
1988-02-04 |
JPS63201156A |
1988-08-19 |
FURANCHIESUKO MAKOBETSUKU; ROORANDO KISUTE; WARUTAA PERISU; RUIIJI ROBATEI |
|
157 |
JPS6224429B2 - |
JP10403982 |
1982-06-18 |
JPS6224429B2 |
1987-05-28 |
AKUSERU KUREEMAN; YURUGENSU MARUTENSU; HORUSUTO UAIGERU |
|
158 |
Novel hydroxamic acid |
JP21253986 |
1986-09-09 |
JPS62103052A |
1987-05-13 |
JIYONASAN FUIRITSUPU DEIKENZU; DEBITSUDO KEISU DONARUDO; JIYOFUREI NIIN; UIRIAMU ROJIYAA MATSUKEI |
|
159 |
JPS616061B2 - |
JP10403882 |
1982-06-18 |
JPS616061B2 |
1986-02-24 |
AKUSERU KUREEMAN; YURUGENSU MARUTENSU; HORUSUTO UAIGERU |
|
160 |
Manufacture of d,l-carnitineamide-chloride |
JP11555485 |
1985-05-30 |
JPS611649A |
1986-01-07 |
HERUBERUTO KURENKU |
|