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首页 / 专利库 / 氧四环素 / 专利数据
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 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.
182 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.
183 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines US455923 1995-05-31 US5530117A 1996-06-25 Joseph J. Hlavka; Phaik-Eng Sum; Yakov Gluzman; Ving J. Lee; Adma A. Ross
The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.
184 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.
185 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.
186 Process for the preparation of 6-demethyl-6-deoxy-6-methylene-5-oxytetracyclin and the 11A-chloro-derivative thereof US646574 1984-08-31 US4659515A 1987-04-21 Gyorgy Lugosi; Maria Hima nee Toth; Maria Bakonyi; Sandor Szoke
The invention relates to a new and improved process for the preparation of 6-demethyl-6-deoxy-6-methylene-5-oxytetracycline and the 11a-chloro derivative thereof by dehydrating 11a-chloro-5-oxytetracycline-6,12-hemiketal, which comprises treating 11a-chloro-5-oxytetracycline-6,12-hemiketal or an acid salt thereof with a dehydrating mixture formed by the reaction of chloro sulfonic acid and formic acid and isolating the 11a-chloro-6-demethyl-6-deoxy-6-methylene-5-oxytetracycline and salt thus obtained and optionally dehalogenating the same by reaction with a reducing agent.The advantage of the process of the present invention is that it is simple, economical and suitable for industrial scale manufacture and provides a pure product of high quality by excellent yields.
187 7- 디메틸 아미노-6-데메틸-6- 데옥시 테트라사이클린 염산염의 회수 방법 KR1019730000321 1973-02-24 KR1019760000303B1 1976-06-26 마아틴토부크스
188 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.
189 7-Dimethylamino-6-Demethyl-6-Deoxytetracycline Skin Treatment Kit US11459778 2006-07-25 US20070166274A1 2007-07-19 Leonard L. MAZUR; Joseph J. Krivulka
A method to ameliorate the skin-irritating effects of topical tretinoin treatment by providing the tretinoin-using patient with a skin-care kit which includes (1) topical tretinoin; and (2) a skin cleanser formulated to minimize tretinoin-induced skin irritation, and (3) a skin moisturizer formulated to reduce tretinoin-induced skin irritation; and (4) packaging to present the aforementioned components together as a unified system.
190 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.
191 7-(substituted-9-(substituted amino)-6-demethyl-6-deoxytetracyclines US352407 1994-12-08 US5495018A 1996-02-27 Phaik-Eng Sum; Ving J. Lee; Joseph J. Hlavka; Raymond T. Testa
The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.
192 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.
193 4-(n-mono-substituted) hydrazones of 4-dedimethylamino-4-oxo-tetracycline US44030565 1965-03-16 US3345370A 1967-10-03 CARLYLE ESSE ROBERT; GEORGE SIEGER
194 9- (substituted amino) -alpha-6-deoxy-5-oxy tetracycline derivatives, their preparation and their use as antibiotics US682640 1996-07-22 US5834450A 1998-11-10 Wei-guo Su
This invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in the specification and the pharmaceutically acceptable salts of such compounds. Compounds of the formula I exhibit antibiotic activity against a wide range of gram-positive and gram-negative organisms, including organisms that are resistant to tetracycline antibiotics.
195 Method for the production of 9-amino-6-demethyl-6-deoxytetracycline EP93107720.0 1993-05-12 EP0582791B1 1997-04-23 Sum, Phaik-Eng
196 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.

197 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. (wherein Ar denotes a substituted aryl group, and X stands for the residue of a mineral acid from which hydrogen atom has been eliminated).

198 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.

199 Novel 2-carboxamido-n-imidomethyl-6-demethyl-6-deoxytetracyclines US43571365 1965-02-26 US3275652A 1966-09-27 MARTELL JR MICHAEL JOSEPH; STEPHEN TOMCUFCIK ANDREW
200 6-deoxy-6-demethyl-6-halomethylene tetracyclines and their 11a-chloro and fluoro derivatives US41083964 1964-10-09 US3250809A 1966-05-10 BLACKWOOD ROBERT K; RENNHARD HANS H; BEEREBOOM JOHN J; STEPHENS JR CHARLES R