首页 / 专利分类库 / 有机化学 / 无环或碳环化合物 / 羧酸酰胺,酸部分的碳架进一步被氨基取代
序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
41 9-substituted minocycline compound JP2008157219 2008-06-16 JP2009029785A 2009-02-12 NELSON MARK L; FRECHETTE ROGER; VISKI PETER; ISMAIL MOHAMED; BOWSER TODD; DUMORNAY JIMMY; RENNIE GLEN; LIU GUI; KOZA DARRELL; SHEAHAN PAUL; STAPLETON KAREN; HAWKINS PAUL; BHATIA BEENA; VERMA ATUL; MCINTYRE LAURA; WARCHOL TAD
<P>PROBLEM TO BE SOLVED: To provide a new 9-substituted minocycline compound. <P>SOLUTION: This new 9-substituted minocycline compound is e.g. expressed by the formula. The naphthyl thiourea part can be made as various substituents such as phenyl urea, phenyl sulfonic acid amide, etc. These minocycline compounds can be used for treating many tetracycline compound-responding states such as bacterial infectious diseases and neoplasm-forming diseases, and further used for e.g. the application to other than the publicly known general uses of the minocycline and tetracycline compounds, such as the inhibition of tetracycline discharge and modification of gene expression. <P>COPYRIGHT: (C)2009,JPO&INPIT
42 Carboxamide-based opioid compound JP2007513340 2005-05-11 JP2007537278A 2007-12-20 カーソン,ジヨン・アール; フイリツプ,ピテイス・エム
本発明は、中枢神経系疾患を治療または調節する薬剤として薬学的に用いるに有用なカルボキサミド系オピオイド化合物そして中枢神経系疾患を治療または調節する方法に向けたものである。
43 Non-glycosylated for the treatment of inflammatory disorders / non-glycoside / non-peptide small molecule psgl-1 mimetics JP2007503297 2005-03-18 JP2007529462A 2007-10-25 アイート,エーワルト・ミルコ; クラニッヒ,レモ
式(Ia)

または(Ib)

式中、記号、指標および置換基は以下の意味を有し、R はH、CN、NO 、CF 、F、Cl、Br、I、CH であり、R はH、CN、NO 、CF 、F、Cl、Br、I、CH 、Et、N−Pr、i−Pr、n−Bu、t−Bu、フェニル、チエニル、フリル、チアゾリルであり、R またはR いずれかはHでなければならず、R はH、CN、NO 、CF 、F、Cl、Br、I、CH 、Et、n−Pr、i−Pr、n−Bu、t−Bu、フェニル、チエニル、フリル、チアゾリル、次いで、Xは例えば式(II)

または式(III)

(R はH、CH 、CH CH )であり、または式(IV)

または式(V)

(Yは式(VI)

または式(VII)

)である]の少なくとも1つの化合物、または式(Ia)または(Ib)の前記で規定された化合物の医薬上許容される塩、エステルまたはアミドまたはプロドラッグ、および医薬で有用な医薬上許容される担体を含む医薬組成物。 該化合物は、E−、T−またはL−セレクチン結合によって媒介されるイン−ビトロおよびイン−ビボ結合プロセスを調節するために適用される。
44 Compounds with growth hormone releasing properties JP52323097 1996-12-16 JP3701686B2 2005-10-05 アンケルセン,ミハエル; クルセ ハンセン,トマス; ペシュケ,ベルント; マズセン,キェールド; ラウ,イェスパー; フリードリッヒ ルント,ベーレント; ワトソン,ブレット
45 Propionic acid derivative JP2002532408 2001-09-24 JP2004510757A 2004-04-08 エルケ・ディートリヒ−ヴェンゲンロト; クラウス・ウルバーンス; クラウディア・ヒルト−ディートリヒ; クレメンス・ルスティヒ; ズザンネ・ニコリク; ヒルマー・ビショッフ; ベルトルト・ヒンツェン; ミヒャエル・ヴォルテリング; ヨーゼフ・ペルナーシュトルファー
この発明は、新規な強PPAR−α−活性化化合物、例えば環動脈心疾患治療用化合物およびその製造法に関する。
46 Neurological disorders and neuropsychiatric disorders a medicament for the treatment JP54303497 1997-05-29 JP2002515037A 2002-05-21 オグナヤノフ,ヴァッシル,イリヤ; ヅアン,ジン; ベル,スタンレー,チャールス; ボルデン,ローレンス
(57)【要約】 本発明は、下記式の化合物又はその薬理学的に許容されうる塩を含む神経及び神経精神障害治療用医薬を提供する。
47 Compound having growth hormone-releasing characteristics JP32892999 1999-11-19 JP2000143613A 2000-05-26 HANSEN THOMAS KRUSE; PESCHKE BERND; LAU JESPER; LUNDT BEHREND FRIEDRICH; ANKERSEN MICHAEL; WATSON BRETT; MADSEN KJELD
PROBLEM TO BE SOLVED: To obtain a compound having growth hormone-releasing characteristics, having a more excellent property than that of a conventional compound and having an analogous property to a peptide. SOLUTION: This compound is expressed by formula I wherein, R1 and R2 are each H or a (aryl-substituted) (1-6C) alkyl; (a) and (b) are each 1 or 2; G is H, O-(CH2)k-R27 (wherein, R27 is H, a halogen or the like; (k) is 0-2) or the like; J is expressed by formula II (wherein, R32-R36 are each H, a halogen or the like) or the like; E is CONR12R13 [wherein, R12 and R13 are each H, a (substituted) (1-6C) alkyl or the like]; D is expressed by formula III [wherein, R3-R6 are each H, a (substituted) (1-6C) alkyl or the like; (n) is 0-3] or the like} and is e.g. (2E)-5-amino-5-methylhexa-2-enoic acid N-methyl-N-((1R)-1-(N- methyl-N-((1R-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphth yl)ethyl) amide. The compound of formula I is synthesized e.g. through dropping ethyl chloroformate into a solution of both 3-t-butoxycarbonylamino-3-methylbutanoic acid and triethylamine as a starting step.
48 The novel amino acid derivatives with improved multi-drug resistance activity JP51630696 1995-11-13 JPH10509151A 1998-09-08 ロバート イー. ゼル,; マシュー ダブリュー. ハーディング,
(57)【要約】 本発明は、治療剤または予防剤に対する細胞の感受性を維持するか、高めるか、または回復できる化合物に関する。 本発明はまた、これらの化合物を含有する薬学的組成物に関する。 本発明の化合物および薬学的組成物は、多薬耐性の拡大を防止するためおよび多薬耐性癌の治療に使用するために、多薬耐性細胞の治療に、特によく適合する。
49 Nmr diagnostic agent JP7371891 1991-03-14 JP2556627B2 1996-11-20 HAINTSU GURIISU; DOE ROOZENBERUKU; HANSUUYOAHIMU UAINMAN
50 Pharmaceutical composition JP3133087 1987-02-13 JP2543690B2 1996-10-16 HARARUDO MASHURAA
51 JPH07507814A - JP52142994 1994-03-15 JPH07507814A 1995-08-31
52 Pharmaceutical composition JP7644186 1986-04-01 JPH0755923B2 1995-06-14 アンドリュー・マルコーム・クレイトン; ウイリアム・アンソニー・ジェフリー
53 In contrast cholecystokinin have the antagonistic activity (r) -5- pentylamino-5 new optically active derivative and its manufacturing method of oxo-pentanoic acid JP2641788 1988-02-04 JPH075534B2 1995-01-25 フランチェスコ・マコベック; ルイージ・ロバティ; ローランド・キステ; ワルター・ペリス
54 Amino acid derivative anticonvulsants JP3174286 1986-02-15 JPH06104649B2 1994-12-21 ダーレル・ワトソン; ハロルド・エル・コーン
The present invention relates to anticonvulsant compounds useful in the treatment of epilepsy and other central nervous system disorders. The compounds of this invention have the following general formula: wherein R and R1, independently, are lower alkyl, aryl lower alkyl or phenyl, unsubstituted or substituted with at least one substituent; R2 and R3, independently, are hydrogen, lower alkyl, aryl lower alkyl or phenyl, unsubstituted or substituted with at least one substituent; and n is 1 to 4. The present compounds can be employed for preparing compositions to be used as anticonvulsant pharmaceuticals.
55 JPH0432061B2 - JP13108583 1983-07-20 JPH0432061B2 1992-05-28
56 JPH0322869B2 - JP15096483 1983-08-20 JPH0322869B2 1991-03-27 KORUDEI ARETSUKUSHISU; GIRETSUTO KURAUDE; ROBA YOSEFU; NIIBESU HOORU; YANSENSU DO BAREBEKE FUIRITSUPE; RANBERIN JORUGESU
57 Acyl anilide, preparation thereof and phamaceutical or veterinary pharmaceutical composition having anti-androgenic activity JP23057489 1989-09-07 JPH02131462A 1990-05-21 HAWAADO TATSUKAA
NEW MATERIAL: A compound of formula I (wherein R 1 is F, Cl, Br or CF 3; R 2 is CN, NO 2, F, Cl or R 3 and R 4 are H; R 5 is OH; R 6 is a 1-4C alkyl or CF 3; A 1 and A 2 are methylene; X 1 is S; and R 7 is phenyl). EXAMPLE: 4-Cyano-3-trifluoromethyl-N-(2-hydroxy-2-methyl-3-phenylthiopropionyl) aniline. USE: A therapeutic agent for acne, hirsutism, seborrhea, etc. PREPARATION: An amine of formula II is reacted with an acid of formula III or its reactive derivative in an N,N-dimethylacetamide solution, for example, to give the compound of formula I, etc. COPYRIGHT: (C)1990,JPO
58 Substituted amines JP1339689 1989-01-23 JPH0291052A 1990-03-30 GOTO GIICHI; NAGAOKA AKINOBU
PURPOSE: To provide a cerebral function improver and choline esterase inhibitor containing substituted amines including novel compounds and effective as a remedy for senile dementia and Alzheimers disease. CONSTITUTION: The objective agent contains, as an active component, a com pound of formula I[R 1 and R 2 are H, (substituted) hydrocarbon group or together with bonding N form a condensed heterocyclic group; R 3 is H, (substituted) hydrocarbon group or (substituted) acyl; R 4 is H or together with group R 3 forms group of formula II, formula III or (CH 2) m+1 (m is 0-2); A is (CH 2) l (l is 0-2) or CH=CH; X is one or more substituents; n is 4-7] or its salt {e.g., 2-[4-(N-benzyl-N-methyl)aminobutyl]-5-nitro-1H-isoindole-1,3-(2H)-dione hydrochlo ride}. The compound of formula I wherein R 1 is H or (OH-substituted) lower alkyl and R 2 is (substituted) α-aralkyl is novel. COPYRIGHT: (C)1990,JPO&Japio
59 Preparation of n-acetylphenylalanine JP27108088 1988-10-28 JPH01149757A 1989-06-12 HAINTSU ERUPENBATSUHA; KURAUSU GEERUMAN; PEETAA HERUSUTAAMAN; EAHARUTO IEEGAASU
PURPOSE: To easily and advantageously obtain the subject compd. useful for production of phenylalanine by opening the ring of 2-methyl-4-benzylidene-1,-3- oxazolin-5-one with water by and under a specific solvent and reaction conditions, then catalytically hydogenating the same. CONSTITUTION: The 2-methyl-4-benzylidene-1,3-oxazoline-5-one is subjected to the ring opening by the water to form 2acetoaminocinnamic acid, which is then catalytically hydogenated to obtain the N-acetylphenylalanine. At this time, the two reaction stages are executed in a mixture consisting of an alphat. 310C ketone or ether miscible with water and water (5 to 50 wt.%) as a solvent and the hydrogenation of the 2-acetoaminocinnamic acid is executed in the presence of a Pd-carrier catalyst at 10 to 50°C and under a pressure of 1 to 15 bar. COPYRIGHT: (C)1989,JPO
60 Novel compound having collagenase inhibiting activity, its production and pharmacological composition containing said compound JP114288 1988-01-06 JPS63258449A 1988-10-25 TERANSU KAATORAITO; ROMEENU BUUBUUTOUU TERO; IBU RERIEBURU; MARII KUROODO FURUNIEERU ZARIY
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