| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 181 | 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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| 182 | 7-(Substituted)-9- (substituted glycyl)-amido)-6-demethyl-6-deoxytetracyclines | EP93107717.6 | 1993-05-12 | EP0582788A1 | 1994-02-16 | Sum, Phaik-Eng; Lee, Ving J.; Testa, Raymond T. |
The invention provides compounds of the formula:
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| 183 | Novel 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines | EP92114281.6 | 1992-08-21 | EP0536515A1 | 1993-04-14 | 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. |
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| 184 | 6-deoxy-6-hydroperoxy dehydrotetracyclines and process utilizing the same | US19959062 | 1962-06-04 | US3146265A | 1964-08-25 | SCOTT ALASTAIR I; BEDFORD COLIN T |
| 185 | 6-deoxy-6-demethyl-6-methylene-5-oxytetracyclines | US7644160 | 1960-12-19 | US2984686A | 1961-05-16 | BLACKWOOD ROBERT K; RENNHARD HANS H; BEEREBOOM JOHN J; STEPHENS JR CHARLES R |
| 186 | 9-(SUBSTITUTED AMINO)-ALPHA-6-DEOXY-5-OXY TETRACYCLINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS ANTIBIOTICS | PCT/IB1995000026 | 1995-01-12 | WO1995022529A1 | 1995-08-24 | PFIZER INC. |
| This invention relates to compounds of formula (I) wherein R<1> is hydrogen or -CH2NR<5>R<6>; R<2> is hydrogen or R<4>(CH2)nCO-; n is an integer from 0 to 4; R<3> is R<8>(CH2)mCO- or R<8>(CH2)mSO2-; m is an integer from 0 to 4; R<4>, R<5>, R<6> and R<8> are defined as in the specification and the pharmaceutically acceptable salts of such compounds. Compounds of formula (I) exhibit antibiotic activity against a wide range of gram-positive and gram-negative organisms, including organisms that are resistant to tetracycline antibiotics. | ||||||
| 187 | 7-Substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines | US11145508 | 2005-06-03 | USRE40183E1 | 2008-03-25 | Joseph J. Hlavka; Phaik-Eng Sum; Yakov Gluzman; Ving J. Lee; Adma A. Ross |
| The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics. | ||||||
| 188 | 2,3-oxidosqualene-lanosterol cyclase inhibitors | US09939872 | 2001-08-27 | US20020068753A1 | 2002-06-06 | Jean Ackermann; Johannes Aebi; Alexander Chucholowski; Henrietta Dehmlow; Olivier Morand; Sabine Wallbaum; Thomas Weller |
| The present invention relates to piperidine derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes. | ||||||
| 189 | 2,3-oxidosqualene-lanosterol cyclase inhibitors | US09925188 | 2001-08-09 | US20020045777A1 | 2002-04-18 | Jean Ackermann; Johannes Aebi; Denise Blum; Alexander Chucholowski; Henrietta Dehmlow; Hans-Peter Maerki; Olivier Morand; Rene Trussardi; Elisabeth von der Mark; Sabine Wallbaum; Thomas Weller |
| The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes. | ||||||
| 190 | 9-amino-7-(substituted)-6-demethyl-6-deoxytetracyclines | US219568 | 1994-03-29 | US5401863A | 1995-03-28 | Joseph J. Hlavka; Phaik-Eng Sum; Yakov Gluzman; Ving J. Lee |
| Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines 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. | ||||||
| 191 | Method for the production of 9-amino-6-demethyl-6-deoxytetracycline | US928587 | 1992-08-13 | US5248797A | 1993-09-28 | Phaik-Eng Sum |
| 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. | ||||||
| 192 | Process for the production of alpha-6-deoxytetracyclines and hydrogenation catalyst useful therein | US477571 | 1990-02-09 | US4990636A | 1991-02-05 | Jagmohan Khanna; Kiran Bala; Inder P. S. Grover |
| A coordination compound useful as a hydrogenation catalyst, having the formula: ##STR1## wherein Ph is phenyl; R is hydrogen or C.sub.1 -C.sub.4 alkyl; and X is chloro, bromo or iodo. This compound is particularly useful as a homogeneous hydrogenation catalyst in the production of alpha-6-deoxytetracyclines, particularly the antibiotic doxycycline. The desired alpha-6-deoxy product is produced in high yields and stereospecificities, the process requiring the use of minimal quantities of rhodium metal in the hydrogenation catalyst per mole of the 6-methylenetetracycline hydrogenated. | ||||||
| 193 | Process for the production of alpha-6-deoxytetracyclines and hydrogenation catalyst useful therein | US263721 | 1988-10-28 | US4902447A | 1990-02-20 | Jagmohan Khanna; Kiran Bala; Inder P. S. Grover |
| A coordination compound useful as a hydrogenation catalyst, having the formula: ##STR1## wherein Ph is phenyl; R is hydrogen or C.sub.1 -C.sub.4 alkyl; and X is chloro, bromo or iodo. This compound is particularly useful as a homogeneous hydrogenation catalyst in the production of alpha-6-deoxytetracyclines, particularly the antibiotic doxycycline. The desired alpha-6-deoxy product is produced in high yields and stereospecificities, the process requiring the use of minimal quantities of rhodium metal in the hydrogenation catalyst per mole of the 6-methylenetetracycline hydrogenated. | ||||||
| 194 | Process for producing 7-amino-6-demethyl-6-deoxytetracycline | US201872 | 1988-06-03 | US4849136A | 1989-07-18 | Yutaka Saito; Masaji Kasai |
| 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. ##STR1## (wherein Ar denotes a substituted aryl group, and X stands for the residue of a mineral acid from which hydrogen atom has been eliminated). | ||||||
| 195 | Hydrolysis of 2-decarboxamido-2-cyano-6-deoxy-tetracycline derivatives | US13411961 | 1961-08-28 | US3069467A | 1962-12-18 | BEEREBOOM JOHN J; KENNETH BUTLER |
| 196 | 2,3-oxidosqualene-lanosterol cyclase inhibitors | US09939872 | 2001-08-27 | US06964974B2 | 2005-11-15 | Jean Ackermann; Johannes Aebi; Alexander Chucholowski; Henrietta Dehmlow; Olivier Morand; Sabine Wallbaum; Thomas Weller |
| The present invention relates to piperidine derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes. | ||||||
| 197 | 2,3-oxidosqualene-lanosterol cyclase inhibitors | US09925188 | 2001-08-09 | US06858651B2 | 2005-02-22 | Jean Ackermann; Johannes Aebi; Denise Blum; Alexander Chucholowski; Henrietta Dehmlow; Hans-Peter Maerki; Olivier Morand; Rene Trussardi; Elisabeth von der Mark; Sabine Wallbaum; Thomas Weller |
| The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes. | ||||||
| 198 | Method of using tetracycline compounds for inhibition of endogenous nitric oxide production | US697815 | 1996-08-30 | US5789395A | 1998-08-04 | Ashok R. Amin; Steven B. Abramson; Lorne M. Golub; Nungavaram S. Ramamurthy; Thomas F. McNamara; Robert A. Greenwald; Howard Trachtman |
| A method is disclosed for inhibiting endogenous production of nitric oxide (NO) in an in vivo, in vitro, or ex vivo mammalian system. The method employs a tetracycline compound to inhibit 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 mammalian 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. | ||||||
| 199 | 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines | US286096 | 1994-08-04 | US5494903A | 1996-02-27 | Joseph J. Hlavka; Phaik-Eng Sum; Yakov Gluzman; Ving J. Lee; Adma A. Ross |
| The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula ##STR1## wherein R, X, R.sup.5 and R.sup.6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics. | ||||||
| 200 | Process for producing 7-dimethylamino-6-demethyl-6-deoxytetracycline | US222886 | 1988-07-22 | US4918208A | 1990-04-17 | Ryoichi Hasegawa; Hiroaki Ohno; Kazuaki Sano; Yoshinori Saito |
| A process for producing 7-dimethylamino-6-demethyl-6-deoxytetracycline (minocycline) which comprises treating the reaction liquid containing minocycline and formaldehyde with hydroxylamine or urea, the reaction liquid being obtained after reductive methylation of 7-amino-6-demethyl-6-deoxytetracycline by using aldehyde, then subjecting the reaction liquid to an adsorption treatment with a nonionic adsorption resin (adsorbent), and subsequently eluting the intended product adsorbed to the adsorbent. | ||||||
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