CO5700818A2 - Derivados de oxazol de tetraciclina - Google Patents
Derivados de oxazol de tetraciclinaInfo
- Publication number
- CO5700818A2 CO5700818A2 CO06055450A CO06055450A CO5700818A2 CO 5700818 A2 CO5700818 A2 CO 5700818A2 CO 06055450 A CO06055450 A CO 06055450A CO 06055450 A CO06055450 A CO 06055450A CO 5700818 A2 CO5700818 A2 CO 5700818A2
- Authority
- CO
- Colombia
- Prior art keywords
- optionally substituted
- carbon atoms
- substituted carbon
- alkyl
- atoms
- Prior art date
Links
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 13
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 239000011593 sulfur Substances 0.000 abstract 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 2
- 229920002554 vinyl polymer Polymers 0.000 abstract 2
- -1 -CH2NR1R2 Chemical group 0.000 abstract 1
- 125000003435 aroyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 229930195734 saturated hydrocarbon Natural products 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/62—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems having two or more ring systems containing condensed 1,3-oxazole rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
- C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/65—Tetracyclines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
- C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
- C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
- C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
De acuerdo con la presente invención, se suministran compuestos representados por la Fórmula (I); En donde: X se selecciona del grupo hidrógeno, amino, NR11R12, alquilo de 1 a 12 átomos de carbono opcionalmente sustituido, arilo de 6, 10 o 14 átomos de carbono opcionalmente sustituido, vinilo opcionalmente sustituido, alquinilo de 2 a 12 átomos de carbono opcionalmente sustituido y halógeno;A" es una porción seleccionada del grupo: R11 y R12 son cada uno independientemente H o alquilo de 1 a 12 átomos de carbono o R11 y R12 cuando se toman opcionalmente juntos con el átomo de nitrógeno al cual cada uno está unido forman un anillo de hidrocarburo saturado de 3 a 7 miembros; Y se selecciona de hidrógeno, alquilo de 1 a 12 átomos de carbono opcionalmente sustituido, arilo de 6, 10 o 14 átomos de carbono opcionalmente sustituido, alquenilo de 2 a 12 átomos de carbono opcionalmente sustituido, vinilo, alquinilo de 2 a 12 átomos de carbono opcionalmente sustituido y halógeno;R se selecciona de alquilo de 1 a 12 átomos de carbono opcionalmente sustituido, alquenilo de 2 a 12 átomos de carbono opcionalmente sustituido, alquinilo de 2 a 12 átomos de carbono opcionalmente sustituido, -CH2NR1R2, arilo de 6, 10 o 14 átomos de carbono opcionalmente sustituido, aralquilo de 7 a 16 átomos de carbono opcionalmente sustituido, aroilo de 7 a 13 átomos de carbono opcionalmente sustituido, SR3, heteroarilo de 5 o 6 átomos por anillo opcionalmente sustituido, que contiene 1 a 4 heteroátomos que pueden ser iguales o diferentes, independientemente seleccionados de nitrógeno, oxígeno y azufre, y heteroarilcarbonilo de 5 o 6 átomos por anillo opcionalmente sustituido que contiene 1 a 4 heteroátomos que pueden ser iguales o diferentes, independientemente seleccionados de nitrógeno, oxígeno y azufre; ...
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US52792803P | 2003-12-08 | 2003-12-08 | |
| US58482304P | 2004-07-01 | 2004-07-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5700818A2 true CO5700818A2 (es) | 2006-11-30 |
Family
ID=34681543
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO06055450A CO5700818A2 (es) | 2003-12-08 | 2006-06-08 | Derivados de oxazol de tetraciclina |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US7176225B2 (es) |
| EP (2) | EP1692117B1 (es) |
| JP (1) | JP4848287B2 (es) |
| KR (1) | KR101164262B1 (es) |
| CN (1) | CN100545151C (es) |
| AR (1) | AR047274A1 (es) |
| AT (2) | ATE444290T1 (es) |
| AU (1) | AU2004297243B2 (es) |
| BR (1) | BRPI0417421A (es) |
| CA (1) | CA2546895A1 (es) |
| CO (1) | CO5700818A2 (es) |
| CR (1) | CR8437A (es) |
| DE (1) | DE602004023417D1 (es) |
| EC (1) | ECSP066605A (es) |
| ES (2) | ES2372635T3 (es) |
| IL (2) | IL176162A (es) |
| MY (1) | MY146098A (es) |
| NO (1) | NO20062629L (es) |
| PA (1) | PA8619601A1 (es) |
| PE (1) | PE20050995A1 (es) |
| RU (1) | RU2415844C2 (es) |
| SG (1) | SG148216A1 (es) |
| TW (1) | TW200528437A (es) |
| UA (2) | UA83266C2 (es) |
| WO (1) | WO2005056538A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101171408B1 (ko) | 2004-05-21 | 2012-08-08 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 테트라사이클린 및 이의 유사체의 합성 |
| US7858601B2 (en) | 2004-10-25 | 2010-12-28 | Paratek Pharmaceuticals, Inc. | 4-substituted tetracyclines and methods of use thereof |
| AR057032A1 (es) * | 2005-05-27 | 2007-11-14 | Wyeth Corp | Tigeciclina y metodos de preparacion |
| AR057324A1 (es) * | 2005-05-27 | 2007-11-28 | Wyeth Corp | Tigeciclina y metodos para preparar 9-aminominociclina |
| AR057033A1 (es) * | 2005-05-27 | 2007-11-14 | Wyeth Corp | Tigeciclina y metodos para preparar 9-nitrominociclina |
| AU2006272698B2 (en) * | 2005-07-21 | 2012-11-01 | Paratek Pharmaceuticals, Inc. | 10-substituted tetracyclines and methods of use thereof |
| US8486921B2 (en) | 2006-04-07 | 2013-07-16 | President And Fellows Of Harvard College | Synthesis of tetracyclines and analogues thereof |
| US8440646B1 (en) | 2006-10-11 | 2013-05-14 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for treatment of Bacillus anthracis infections |
| WO2008127361A2 (en) | 2006-10-11 | 2008-10-23 | President And Fellows Of Harvard College | Synthesis of enone intermediate |
| US8121767B2 (en) * | 2007-11-02 | 2012-02-21 | GM Global Technology Operations LLC | Predicted and immediate output torque control architecture for a hybrid powertrain system |
| EP2220033B1 (en) * | 2007-11-14 | 2014-12-17 | Sandoz AG | Crystalline forms of tigecycline hydrochloride |
| JP2011527708A (ja) | 2008-07-11 | 2011-11-04 | ニュメディックス | 減少した抗菌活性および神経保護作用の利点を有するテトラサイクリン誘導体 |
| US8513224B2 (en) | 2008-12-18 | 2013-08-20 | Sandoz Ag | Crystalline form C of tigecycline dihydrochloride and methods for its preparation |
| US9073829B2 (en) | 2009-04-30 | 2015-07-07 | President And Fellows Of Harvard College | Synthesis of tetracyclines and intermediates thereto |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US26253A (en) * | 1859-11-29 | Vegetable-cutter | ||
| US2482055A (en) | 1948-02-11 | 1949-09-13 | American Cyanamid Co | Aureomycin and preparation of same |
| US3007965A (en) | 1959-02-13 | 1961-11-07 | American Cyanamid Co | New tetracyclines produced by streptomyces aureofaciens |
| US3043875A (en) | 1959-10-22 | 1962-07-10 | Pfizer & Co C | Halogenated tetracycline derivatives and processes for their preparation |
| FR1430859A (es) | 1960-05-23 | 1966-05-25 | ||
| US3338963A (en) | 1960-10-28 | 1967-08-29 | American Cyanamid Co | Tetracycline compounds |
| US3148212A (en) | 1961-12-22 | 1964-09-08 | American Cyanamid Co | Reductive alkylation process |
| US3360557A (en) | 1963-05-10 | 1967-12-26 | American Cyanamid Co | 9-hydroxytetracyclines and a process of preparing same |
| USRE26253E (en) | 1963-05-17 | 1967-08-15 | And z-alkylamino-g-deoxytetracycline | |
| US3341585A (en) | 1966-05-06 | 1967-09-12 | American Cyanamid Co | Substituted 7-and/or 9-amino-6-deoxytetracyclines |
| US3360561A (en) | 1967-06-19 | 1967-12-26 | American Cyanamid Co | Nitration of tetracyclines |
| US3518306A (en) | 1968-02-19 | 1970-06-30 | American Cyanamid Co | 7- and/or 9-(n-nitrosoalkylamino)-6-demethyl-6-deoxytetracyclines |
| US4806529A (en) | 1982-11-18 | 1989-02-21 | Trustees Of Tufts College, Tufts University | Tetracycline activity enhancement |
| US5494903A (en) | 1991-10-04 | 1996-02-27 | American Cyanamid Company | 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines |
| DE122006000058I1 (de) * | 1991-10-04 | 2007-01-18 | Wyeth Corp | 7-Substituierte-9-substituierte Amino-6-Demethyl-6-Deoxy-Tetracycline |
| US5328902A (en) * | 1992-08-13 | 1994-07-12 | American Cyanamid Co. | 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines |
| CO5190716A1 (es) * | 1999-08-10 | 2002-08-29 | Smithkline Beecham Corp | 4,4-diaril-ciclohexanos 1,4-sustituidos |
| WO2003005971A2 (en) * | 2001-07-13 | 2003-01-23 | Paratek Pharmaceuticals, Inc. | Tetracycline compounds having target therapeutic activities |
-
2004
- 2004-07-12 UA UAA200606344A patent/UA83266C2/ru unknown
- 2004-10-30 UA UAA200606646A patent/UA83268C2/ru unknown
- 2004-12-01 TW TW093137032A patent/TW200528437A/zh unknown
- 2004-12-07 JP JP2006542866A patent/JP4848287B2/ja not_active Expired - Fee Related
- 2004-12-07 ES ES09010915T patent/ES2372635T3/es not_active Expired - Lifetime
- 2004-12-07 RU RU2006118367/04A patent/RU2415844C2/ru not_active IP Right Cessation
- 2004-12-07 CA CA002546895A patent/CA2546895A1/en not_active Abandoned
- 2004-12-07 PE PE2004001203A patent/PE20050995A1/es not_active Application Discontinuation
- 2004-12-07 AR ARP040104570A patent/AR047274A1/es unknown
- 2004-12-07 EP EP04813199A patent/EP1692117B1/en not_active Expired - Lifetime
- 2004-12-07 AT AT04813199T patent/ATE444290T1/de not_active IP Right Cessation
- 2004-12-07 AU AU2004297243A patent/AU2004297243B2/en not_active Ceased
- 2004-12-07 MY MYPI20045049A patent/MY146098A/en unknown
- 2004-12-07 BR BRPI0417421-6A patent/BRPI0417421A/pt not_active IP Right Cessation
- 2004-12-07 DE DE602004023417T patent/DE602004023417D1/de not_active Expired - Lifetime
- 2004-12-07 AT AT09010915T patent/ATE525365T1/de not_active IP Right Cessation
- 2004-12-07 SG SG200809014-4A patent/SG148216A1/en unknown
- 2004-12-07 WO PCT/US2004/040850 patent/WO2005056538A1/en active Application Filing
- 2004-12-07 ES ES04813199T patent/ES2331574T3/es not_active Expired - Lifetime
- 2004-12-07 KR KR1020067013606A patent/KR101164262B1/ko not_active IP Right Cessation
- 2004-12-07 EP EP09010915A patent/EP2157085B1/en not_active Expired - Lifetime
- 2004-12-07 CN CNB2004800364939A patent/CN100545151C/zh not_active Expired - Fee Related
- 2004-12-07 PA PA20048619601A patent/PA8619601A1/es unknown
- 2004-12-08 US US11/007,621 patent/US7176225B2/en not_active Expired - Fee Related
-
2006
- 2006-06-05 EC EC2006006605A patent/ECSP066605A/es unknown
- 2006-06-06 CR CR8437A patent/CR8437A/es not_active Application Discontinuation
- 2006-06-06 IL IL176162A patent/IL176162A/en not_active IP Right Cessation
- 2006-06-08 NO NO20062629A patent/NO20062629L/no not_active Application Discontinuation
- 2006-06-08 CO CO06055450A patent/CO5700818A2/es unknown
- 2006-12-13 US US11/638,138 patent/US7365087B2/en not_active Expired - Fee Related
-
2008
- 2008-03-24 US US12/053,856 patent/US20080177080A1/en not_active Abandoned
-
2010
- 2010-05-27 IL IL206050A patent/IL206050A/en not_active IP Right Cessation
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