序号 | 专利名 | 申请号 | 申请日 | 公开(公告)号 | 公开(公告)日 | 发明人 |
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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 1はH、CN、NO 2 、CF 3 、F、Cl、Br、I、CH 3であり、R 2はH、CN、NO 2 、CF 3 、F、Cl、Br、I、CH 3 、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 1またはR 2いずれかはHでなければならず、R 3はH、CN、NO 2 、CF 3 、F、Cl、Br、I、CH 3 、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 4はH、CH 3 、CH 2 CH 3 )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。 |
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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、新規な強力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: |
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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 |