| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 81 | Tropane analogs and methods for inhibition of monoamine transport | US09875523 | 2001-06-06 | US20020010207A1 | 2002-01-24 | Peter C. Meltzer; Bertha K. Madras; Paul Blundell; Zhengming Chen |
| New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter. | ||||||
| 82 | Compounds and methods for synthesis and therapy | US606624 | 1996-02-26 | US5952375A | 1999-09-14 | Norbert W. Bischofberger; Choung U. Kim; Willard Lew; Hongtao Liu; Matthew A. Williams |
| Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described. | ||||||
| 83 | Detection method of nucleic acid by use of fluorescent pyrylium stain in intercalation into nucleic acids | US170689 | 1993-12-21 | US5624798A | 1997-04-29 | Nobuko Yamamoto; Tadashi Okamoto; Yoshinori Tomida; Takeshi Miyazaki; Masahiro Kawaguchi |
| A stain for a nucleic acid characterized by containing, as an effective component, a pyrylium salt compound having Y as a negative portion and a pyrylium ring or a pyrylium-similar ring, wherein the ring is comprised of X selected from O, S, Se and Te as a hetero atom and has substituents R.sup.1, R.sup.2 and R.sup.3, wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom, sulfonate group, amino group, substituted or unsubstituted aryl group, etc., R.sup.3 is -A or -L-A, L is -L.sup.1 -, -L.sup.2 -L.sup.3 - or -L.sup.4 -L.sup.5 -L.sup.6 -, and each of L.sup.1 to L.sup.6 is independently --(CH.dbd.CH)--, a divalent group derived from the substituted or unsubstituted aryl group, etc., A is a substituted or unsubstituted aryl group, etc., and Y.sup.- is an anion. A method for detecting a nucleic acid which comprises the steps of reacting a sample with the stain, and then detecting, by an optical means, the double-strand nucleic acid stained with the stain in the case that the double-strand nucleic acid is contained in the sample. | ||||||
| 84 | Substituted aromatic sulfonamides as antiglaucoma agents | US177211 | 1988-04-04 | US4820848A | 1989-04-11 | Gerald S. Ponticello; Charles N. Habecker |
| Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure. | ||||||
| 85 | Circulation-active substituted 1,4-dihydropyridine-3-carboxylic acid piperazides | US002094 | 1987-01-12 | US4753936A | 1988-06-28 | Gerhard Franckowiak; Gunther Thomas; Matthias Schramm; Michael Kayser; Rainer Gross; Martin Bechem |
| 1,4-Dihydropyridine-3-carboxylic acid piperazides of the formula ##STR1## in which R.sup.1 is CN or alkyl, preferably methyl,R.sup.2 is H, CN, NO.sub.2 or preferably carboxyalkyl,R.sup.3 is aryl or heterocyclic, andR.sup.4 is alkyl, cycloalkyl, aryl or an acyl radical,and physiologically acceptable salts thereof, are circulation active. Novel intermediates are also provided. | ||||||
| 86 | Aminoether compounds | US644911 | 1984-08-27 | US4636568A | 1987-01-13 | Myron S. Simon; David P. Waller |
| There are disclosed certain aminoether compounds which are useful as intermediates in the preparation of photographic image dye providing materials. The aminoethers are represented either by the formula ##STR1## wherein R is hydrogen or an alcohol protecting group and R.sub.1 is hydrogen, alkyl or aralkyl such as benzyl or phenethyl; or the formula ##STR2## wherein R.sub.2 and R.sub.3 are alkyl having from 1 to 6 carbon atoms or R.sub.2 and R.sub.3 together represent the carbon atoms necessary to form, together with the oxygen atoms to which they are bonded and >CH, a five or six member saturated heterocyclic moiety which may include substituted rings and fused rings. | ||||||
| 87 | Method for inhibiting monoamine oxidase-A and treating depression by administering 3-N-methyl-thioxanthen-9-one carboxamide 10,10-dioxide | US704744 | 1985-02-25 | US4623656A | 1986-11-18 | Morton Harfenist; Charles T. Joyner |
| 3-N-methylcarbamoylthioxanthen-9-one 10,10-dioxide of formula (I) ##STR1## is an inhibitor of monoamine oxidase-A, and is therefore useful in the prophylaxis and treatment of certain mental disorders such as depression. | ||||||
| 88 | Substituted and bridged tetrahydropyridines useful as calcium entry blockers | US614885 | 1984-05-29 | US4579851A | 1986-04-01 | David A. Claremon |
| Substituted dihydropyridines and substituted and bridged tetrahydropyridines are disclosed which are useful as calcium entry blockers. | ||||||
| 89 | Spiro-polycyclicimidazolidinedione derivatives | US961335 | 1978-11-16 | US4181728A | 1980-01-01 | Reinhard Sarges; John L. Belletire |
| Novel spiro-polycyclicimidazolidinedione derivatives useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. The derivatives include 2',3'-dihydro-spiro[imidazolidine-4,4'-[4'H]-naphtho[1,2-b]pyran]-2,5-dione, 2',3'-dihydro-spiro-[imidazolidine-4, 4'-[4'H]-naphtho[1,2-b]thiopyran]-2,5-dione, 1',2',3',4'-tetrahydro-spiro[imidazolidine-4,1'-benz[a]anthracene]2,5-dione, 2',3'-dihydro-spiro[imidazolidine-4,1'phenalene]-2,5-dione, 1',2',3',4'-tetrahydro-spiro[imidazolidine-4,1'-phenanthrene]-2,5-dione, the 2,1 isomers of the 2',3'-dihydro-4'H-pyran and 2',3'-dihydro-4'H-thiopyran derivatives, the 2',3'-dihydro-4'H-anthracenopyran and 2',3'-dihydro-4'H-anthracenothiopyran derivatives, the spiro-4,4' isomer of the tetrahydrophenanthrene derivative, the [b] isomer of the benzanthracene derivative and the mono or disubstituted 2',3'-dihydro-4'H-naphthopyran, 2',3'-dihydro-4'H-naphthothiopyran and tetrahydrophenanthrene derivatives. | ||||||
| 90 | Hydantoin therapeutic agents | US799586 | 1977-05-23 | US4130714A | 1978-12-19 | Reinhard Sarges |
| Several novel dextrotatory spiro-hydantoin compounds have been obtained by resolving the corresponding dl-compounds which are initially synthesized by first condensing the appropriate carbonyl ring compound, such as the corresponding 4-chromanone or thiochroman-4-one, as the case may be, with potassium cyanide and ammonium carbonate. The resulting optically-active hydantoin derivatives, such as d-6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione and d-6'-fluoro-spiro-[imidazolidine-4,4'-thiochroman]-2,5-dione, are particularly useful in preventing or alleviating chronic diabetic complications. | ||||||
| 91 | Hindered phenol derivatives of 9-thiabicyclononanes and stabilized compositions | US581189 | 1975-05-27 | US4000112A | 1976-12-28 | John F. Stephen |
| The 9-thiabicyclononane derivatives have the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently tertiary alkyl of 4 to 8 carbon atoms or .alpha.,.alpha.-dimethylbenzyl, and n is 0 to 2.The 9-thiabicyclononanes are prepared by reacting an alkali salt of 2,6-di-tert-alkylphenols with 2,6-dichloro-9-thiabicylo[3.3.1]nonane in a dipolar aprotic solvent. The sulfoxide and sulfones are prepared from the sulfides by oxidation with peracids.The compounds are useful as stabilizers for organic materials, particularly turbine oils and polyolefins, subject to oxidative degradation. | ||||||
| 92 | 癌の治療のためのインドールアミン−2,3−ジオキシゲナーゼの阻害剤およびそれらの使用方法 | JP2017551628 | 2016-04-01 | JP2018519245A | 2018-07-19 | ジェイムズ・アーロン・バログ; エミリー・シャーロット・チャーニー; ジェイ・エイ・マークウォルダー; スティーブン・ピー・サイツ; ウェイファン・シャン; デイビッド・ケイ・ウィリアムズ; スシール・ジェタナンド・ナラ; ソーミャ・ロイ; スーダマニ・タンガベル; ラメシュ・クマール・シストラ; スリニバス・チェルク; スリニバサン・タンガティルパティ; ヨダギリ・カニャボイナ; ナガラクシュミ・プリチャルラ; オードリス・ホアン |
| インドールアミン−2,3−ジオキシゲナーゼ(IDO)の酵素活性を調節または阻害する式(I)の化合物、前記化合物を含む医薬組成物、および本発明の化合物を用いる増殖性疾患(例えば、癌)、ウイルス感染症および/または炎症障害の治療方法が開示される。 | ||||||
| 93 | Eprosartan method of manufacturing | JP52813798 | 1998-02-13 | JP4537499B2 | 2010-09-01 | フリサック，ジョゼフ・ロバート; ラボー，クリフォード・エス; リウ，リ |
| 94 | Sulfonamide - substituted compounds, processes for their preparation, pharmaceutical or their use and pharmaceutical preparations containing them as a diagnostic agent | JP34546997 | 1997-12-15 | JP4317601B2 | 2009-08-19 | ウーヴエ・ゲルラハ; クラウス・ヴアイトマン; ハンス・ヨーヘン・ラング; ヨーアヒム・ブレンデル |
| 95 | Novel selective inhibitor to virus or bacterial neuraminidase | JP2005207906 | 2005-07-15 | JP2006036770A | 2006-02-09 | BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A |
| <P>PROBLEM TO BE SOLVED: To selectively inhibit virus (particularly influenza virus), especially glycolytic enzymes like neuraminidase, above all, viral or bacterial neuraminidase. <P>SOLUTION: Novel compounds of Formula (III) or Formula (IV) are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or an N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of this invention are also described. <P>COPYRIGHT: (C)2006,JPO&NCIPI | ||||||
| 96 | Of (S) -6- methyl -4H- thieno [2,3-b] thiopyran-2-sulfonamide 7,7-dioxide and related compounds - 5,6-dihydro - (S) -4- (ethylamino) enantioselective synthesis | JP4730794 | 1994-03-17 | JP3273096B2 | 2002-04-08 | デイビツド・ジエイ・マスレ; トーマス・ジエイ・ブラツクロツク; ポール・ソハー |
| 97 | The novel selective inhibitors of viral or bacterial neuraminidase | JP52644296 | 1996-02-26 | JPH11501908A | 1999-02-16 | エイ． ウィリアムズ，マシュー; ユー． キム，チョウン; ダブリュー． ビスチョフバーガー，ノーベルト; リウ，ホンタオ; レウ，ウィリアード |
| (57)【要約】 新規化合物が記載されている。 この化合物は、一般に、酸基、塩基性基、置換アミノまたはＮ-アシル、および必要に応じてヒドロキシル化アルカン部分を有する基を含む。 本発明のインヒビターを含む薬学的組成物もまた記載されている。 ノイラミニダーゼを含むことが推測される試料中のノイラミニダーゼを阻害する方法もまた記載されている。 抗原性物質、ポリマー、本発明の化合物と標識との結合体、およびノイラミニダーゼ活性の検出のためのアッセイ法もまた記載されている。 | ||||||
| 98 | Cyclic amine derivative | JP2815386 | 1986-02-12 | JPH07100688B2 | 1995-11-01 | 文憲 佐藤; 準 宇野; 俊介 成戸; 邦彦 武山; 和 細木; 美貴雄 黒川 |
| 99 | Fused n-phenylsulfonyl-n'-pyrimidinyl-urea and intermediate for preparation of fused n-phenylsulfonyl-n'-triazinylurea | JP25384993 | 1993-09-16 | JPH06234761A | 1994-08-23 | YOOZEFU EERENFUROINTO; BUERUNAA FUERII; UIRII MAIYAA; BUERUNAA TEPUFURU |
| PURPOSE: To obtain a new compound useful as an intermediate of herbicides and growth regulators. CONSTITUTION: A compound of formula I [R 1 is H, a halogen, nitro, a 1-4C (halo)alkyl or the like; A is a bridge of 3 or 4 atoms which contains 1 or 2 O, S or N and together with a linking C, forms a non-aromatic 5- or 6-membered heterocyclic ring system in which two Os are separated by at least one O, and O and S are only linked to each other when S is SO or SO 2] such as N-(2,3-dihydro-2-methylbenzo[b]furan-7-yl sulfonyl)-N'-(4,6-dimethylpyrimidin-2-yl) urea, obtained by reacting a fused phenylsulfonamide of formula II with an N-pyridminyl carbamate or an N-triazinyl carbamate of formula III [R is a (substd.) phenyl or an alkyl] in the presence of a base. COPYRIGHT: (C)1994,JPO | ||||||
| 100 | Imidazolyl, triazolyl and tetrazolyl compound | JP13522385 | 1985-06-18 | JPH0662581B2 | 1994-08-17 | ケネス・ステイーブン・ハーシ; チヤールズ・デビツド・ジヨンズ; ハロルド・メロン・タイラー |
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