| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 161 | Biological transformation of alpha-6-deoxytetracyclines to tetracyclines | US3433709D | 1965-12-07 | US3433709A | 1969-03-18 | MCCORMICK JERRY ROBERT DANIEL; SJOLANDER NEWELL OSCAR |
| 162 | 4-desdimethylamino-6-deoxy-tetracycline derivatives | US84192959 | 1959-09-24 | US3047626A | 1962-07-31 | STEPHENS JR CHARLES R; CONOVER LLOYD H |
| 163 | 신규한9-(치환글리실)아미도-6-데메틸-6-데옥시테트라사이클린및그의중간체,및그들의생산방법 | KR1019930015646 | 1993-08-12 | KR1019940003908A | 1994-03-14 | 파이크-엥숨; 빙제이리이; 레이먼드티이테스타 |
| 본 발명은 하기 일반식의 화합물을 제공한다, : 상기식에서 R,R 1 및 W는 명세서에서 정의된다. 이들 화합물은 항생제로서 유용하다. | ||||||
| 164 | 신규한9-아미노-7-(치환아미노)-6-데메틸-6-데옥시테트라사이클린 및 그의 생성 방법 | KR1019920018123 | 1992-10-02 | KR1019930007895A | 1993-05-20 | 조오지프제이라브카; 파이크-엥섬; 야코브글루즈만; 빙제이리이 |
| 테트라사이클린에 저항하는 유기체를 포함하는 넓은 스펙트럼의 유기체에 대해 활성을 가지는 신규한 9-아미노-7-(치환 아미노)-6-데메틸-6-데옥시테트라사이클린 이 공개된다. 본 발명의 신규한 화합물을 제조하는 중간체 및 방법이 또한 공개된다. | ||||||
| 165 | 신규한7-치환-9-치환아미노-6-데메틸-6-데옥시테트라사이클린화합물및그의제조방법 | KR1019920018122 | 1992-10-02 | KR1019930007894A | 1993-05-20 | 조오지프제이라브카; 파이크-엥섬; 야코브글루즈만; 빙제이리이; 에드머에이로스 |
| 테트라사이클린에 저항하는 유기체를 포함하는 넓은 스펙트럼의 유기체에 대해 활성을 가지는 신규한 7-치환-9-(치환 아미노)-6-데메틸-6-데옥시 테트라사이클린 화합물이 공개된다. 본 발명의 신규한 화합물을 제조하기 위한 중간체 및 방법이 또한 공개된다. | ||||||
| 166 | α-6-데옥씨-5-하이드록씨 테트라 싸이클린과 소듐 테트라메타포스 페이트의 수용성 복합체의 제조방법 | KR1019810004468 | 1981-11-19 | KR1019860000450B1 | 1986-04-26 | 이반빌락스 |
| A water-soluble complexes of α-6-deoxy-5-hydroxytetracycline (I) and Na tetrametaphosphate was prepd. from I. Thus, fleshly prepd. 4.33g of (HPO3)n (n=4) was treated with 1 ml of H2O and 20g of I H2O and later with 0.574g of NaOH in MeOH. After adding iso-PrOH, the growing cryst. compd. was filtered, washed, dried to give 21g of I and Na (HPO3)n (n=4) complexes. The major advantage of using this complexes is its decreased interference in the action in human serum of natural bactericides. The bioavailability of this complexes (4.32 μ g/ml/3h) was higher than that of I capsules. | ||||||
| 167 | Method for inhibiting expression of inducible nitric oxide synthase with tetracycline | US61286 | 1998-04-16 | US5919775A | 1999-07-06 | Ashok R. Amin; Steven B. Abramson; Lorne M. Golub; Nungavaram S. Ramamurthy; Thomas F. McNamara; Robert A. Greenwald; Howard Trachtman |
| The invention is a method of inhibiting the production of nitric oxide (NO) in an in vivo, in vitro, or ex vivo biological system. The method employs a tetracycline compound to inhibit the production of NO and/or to inhibit the expression or activity of an inducible isoform of nitric oxide synthase (iNOS). Preferably, the tetracycline compound has inhibitory activity for metalloproteinases. Also it is preferred that the tetracycline compound is provided to the biological system in an amount which has little or no antibacterial activity in the system. Accordingly, preferred tetracycline compounds are tetracycline compounds which have be modified to reduce or eliminate their antimicrobial activity. The method can be used to treat medical conditions in mammals characterized by NO production mediated by iNOS, including, for example, inflammatory conditions. | ||||||
| 168 | Substituted 7-and/or 9-amino-6-deoxytetracyclines | US59815866 | 1966-12-01 | US3341585A | 1967-09-12 | PANAYOTA BITHA; JOHN HLAVKA JOSEPH; MARTELL JR MICHAEL JOSEPH |
| 169 | 13-substituted-6-deoxytetracyclines and process utilizing the same | US17823762 | 1962-03-08 | US3165531A | 1965-01-12 | BLACKWOOD ROBERT K; RENNHARD HANS H; BEEREBOOM JOHN J; STEPHENS JR CHARLES R |
| 170 | Process for the 12a-hydroxylation of 12a-deoxytetracyclines | US6558760 | 1960-10-28 | US3043877A | 1962-07-10 | HOLMLUND CHESTER E; ANDRES WILLIAM W |
| 171 | 7-Methoxy-6-thiatetracyclines and their preparation | US600377 | 1975-07-30 | US3988468A | 1976-10-26 | Werner Rogalski; Richard Kirchlechner; Juergen Seubert; Rudolf Gottschlich; Walter Hameister; Rolf Bergmann; Helmut Wahlig |
| 7-Methoxy-6-thiatetracyclines of the formula ##SPC1##Wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are H or alkyl of 1 to 4 carbon atoms, and the physiologically acceptable acid addition salts thereof. | ||||||
| 172 | 6-demethyl-6-deoxytetracycline, anti-tumor antibiotic | US41159564 | 1964-11-16 | US3326761A | 1967-06-20 | KENT ROBERT E |
| 173 | SUBSTITUTED TETRACYCLIC OXAZEPINE AND THIAZEPINE DERIVATIVES WITH 5-HT2 RECEPTOR AFFINITY | EP95937007.0 | 1995-10-25 | EP0789702A1 | 1997-08-20 | FERNANDEZ-GADEA, Francisco Javier; SIPIDO, Victor, Karel; ANDRES-GIL, José Ignacio; MEERT, Theo, Frans |
| This invention concerns the compounds of Formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. In said formula, R?1 and R2¿ each independently are hydrogen; C¿1-6? alkyl; C1-6 alkylcarbonyl; trihalomethylcarbonyl; C1-6 alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6 alkylcarbonyloxy, C1-6 alkyloxycarbonyl or aryl; or R?1 and R2¿ taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R?3 to R10¿ each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluormethoxy, carboxyl, nitro, amino, mono-or di(C¿1-6?alkyl)amino, C1-6 alkylcarbonylamino, aminosulfonyl, mono-or di(C1-6alkyl)- aminosulfonyl, C1-6 alkyl, C1-6 alkyloxy, C1-6alkylcarbonyl, C1-6 alkyloxycarbonyl; R?11¿ is hydrogen, C¿1-6?alkyl, or trifluoromethyl; R?12¿ is hydrogen, C¿1-6? alkyl, cyano, or trifluorotmethyl; n is zero to 6; and X is O, S, S(=O) or S(=O)2. The compounds of formula (I)may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders. | ||||||
| 174 | 9-amino-7-substituted-6-demethyl-6-deoxytetracyclines | EP92114054.7 | 1992-08-18 | EP0535346B1 | 1995-11-02 | Hlavka, Joseph J.; Sum, Phaik-Eng; Gluzman, Yakov; Lee, Ving J. |
| 175 | Process for producing 7-amino-6-demethyl-6-deoxytetracycline | EP88109054.2 | 1988-06-07 | EP0294762A1 | 1988-12-14 | Saito, Yutaka; Kasai, Masaji |
This invention provides a new process for producing 7-amino-6-demethyl-6-deoxytetracycline (Compound 3) which is an intermediate for the synthesis of minocycline. Compound 3 can be obtained by reduction of Compound 1 using a dithionite as reducing agent. This invention also provides a method to produce Compound 3 from Compound 2 in one pot.
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| 176 | Method for the production of 9-amino-6-demethyl-6-deoxytetracycline | EP93107720.0 | 1993-05-12 | EP0582791B1 | 1997-04-23 | Sum, Phaik-Eng |
| 177 | Method for the production of 9-amino-6-demethyl-6-deoxytetracycline | EP93107720.0 | 1993-05-12 | EP0582791A1 | 1994-02-16 | Sum, Phaik-Eng |
The invention relates to a novel method for producing [4S-(4alpha, 12aalpha)]-9-amino-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide, hereinafter called 9-amino-6-demethyl-6-deoxytetracycline, which compound is a valuable intermediate for synthesis of tetracyclines. |
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| 178 | 新穎7–(取代)–8–(取代)–9–[(經取代胺乙醯基)醯胺基]–6–去甲基–6–去氧四環素 | TW081108726 | 1992-11-03 | TW270923B | 1996-02-21 | 非恩.桑; 約瑟夫.J.霍瓦卡; 敏.J.李; 羅蒙.T.提斯塔 |
| 本發明提供下式化合物 □ (Ⅰ)其中R、R3、R4及W定義於專利說明書中。此等化合物可充作抗生素。 | ||||||
| 179 | Novel 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines | EP92114281.6 | 1992-08-21 | EP0536515B1 | 2001-12-19 | Hlavka, Joseph J.; Sum, Phaik-Eng; Gluzman, Yakov; Lee, Ving J.; Ross, Adma A. |
| Novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention. | ||||||
| 180 | 9-(substituted glycyl) amido - 6-demethyl-6-deoxytetracyclines as antibiotic agents | EP93110689.2 | 1993-07-05 | EP0582829A1 | 1994-02-16 | Sum, Phaik-Eng; Lee, Ving J.; Testa, Raymond T. |
The invention provides compounds of the formula:
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