CO4940506A1 - DERIVATIVES OF 9-OXYME ERYTHROMYCIN - Google Patents
DERIVATIVES OF 9-OXYME ERYTHROMYCINInfo
- Publication number
- CO4940506A1 CO4940506A1 CO98033538A CO98033538A CO4940506A1 CO 4940506 A1 CO4940506 A1 CO 4940506A1 CO 98033538 A CO98033538 A CO 98033538A CO 98033538 A CO98033538 A CO 98033538A CO 4940506 A1 CO4940506 A1 CO 4940506A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- integer
- optionally substituted
- formula xvi
- ring
- Prior art date
Links
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 title 2
- 229960003276 erythromycin Drugs 0.000 title 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 7
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001589 carboacyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Molecular Biology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Genetics & Genomics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
Un compuesto de la fórmula 1 o una sal farmacéuticamenteaceptable del mismo, en la que X es -CR7 R8 -o-NR7 -; o X es junto con R2 forma N=CR4 R5 ; o X y R2 juntos forman un anillo heterocíclico de fórmula XVI:En la que dicho anillo de fórmula XVI, r y p son cada uno de ellos independientemente un número entero de 1 a 3, q es O ó 1 y X1 es -CH2 -, O, -C(O)-, -C(S)-, -CH=CH-, CH(OH)CH(OH)-, o -NH-; y donde las partes (CH2 )r y (CH2 )p de dicho anillo de fórmula XVI están opcionalmente sustituidas con 1 a 4 sustituyentes y el átomo de nitrógeno cuando X1 es -NH- está opcionalmente sustituido con 1 sustituyente, estando dichos sustituyentes opcionales independientemente seleccionados entre el grupo constituido por -C(O) o (alquilo C1 -C10 ), alcoxi C1 -C10 , alcanoílo C1 -C10 , halógeno, nitro, ciano, heterociclilo de 5-10 elementos, alquilo C1 -C10 , -NR7 R8 , arilo C6 -C10 , -S(O)n (alquilo C1 -C10 ) donde n es un número entero de 0 a 2, y -SO2 NR7 R8 ; R1 es H o alquilo C1 -C10 , donde 1 a 3 carbonos de dicho alquilo están opcionalmente remplazados por un hetero+atomo seleccionado entre O, S y N, estando dicho alquilo opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente entre el grupo constituido por -C(O) O (alquilo C1 -C10 ), alcoxi C1 -C10 , alcanoílo C1 -C10 , halógeno, nitro, ciano, heterociclilo de 5-10 elementos, alquilo C1 -C10 , -NR7 R8 , arilo C1 -C10 , -S(O)n (alquilo C1 -C10 ) donde n es un número entero de 0 a 2 , y -SO2 NR7 R8 ; R2 es (y) H; R4 , -C(=)R4 , -C(O)OR4 , o -(CR7 R8 )m R3 cuando X es -NR7 -, o (II) H, R4 , o -CR7 R8 -, donde para ambos (i) y (ii) m es un número entero de 0 a 6 y tanto R7 como R8 pueden variar en cada caso en que m sea mayor que 1;...A compound of formula 1 or a pharmaceutically acceptable salt thereof, wherein X is -CR7 R8 -o-NR7 -; or X is together with R2 form N = CR4 R5; or X and R2 together form a heterocyclic ring of formula XVI: Wherein said ring of formula XVI, r and p are each independently an integer from 1 to 3, q is O or 1 and X1 is -CH2 -, O , -C (O) -, -C (S) -, -CH = CH-, CH (OH) CH (OH) -, or -NH-; and where the (CH2) r and (CH2) p parts of said ring of formula XVI are optionally substituted with 1 to 4 substituents and the nitrogen atom when X1 is -NH- is optionally substituted with 1 substituent, said optional substituents being independently selected between the group consisting of -C (O) or (C1-C10 alkyl), C1-C10 alkoxy, C1-C10 alkanoyl, halogen, nitro, cyano, 5-10-membered heterocyclyl, C1-C10 alkyl, -NR7 R8, C6 -C10 aryl, -S (O) n (C1-C10 alkyl) where n is an integer from 0 to 2, and -SO2 NR7 R8; R1 is H or C1-C10 alkyl, where 1 to 3 carbons of said alkyl are optionally replaced by a hetero + atom selected from O, S and N, said alkyl being optionally substituted with 1 to 3 substituents independently selected from the group consisting of -C (O) O (C1-C10 alkyl), C1-C10 alkoxy, C1-C10 alkanoyl, halogen, nitro, cyano, 5-10 membered heterocyclyl, C1-C10 alkyl, -NR7 R8, C1-C10 aryl, -S (O) n (C1-C10 alkyl) where n is an integer from 0 to 2, and -SO2 NR7 R8; R2 is (y) H; R4, -C (=) R4, -C (O) OR4, or - (CR7 R8) m R3 when X is -NR7 -, or (II) H, R4, or -CR7 R8 -, where for both (i ) and (ii) m is an integer from 0 to 6 and both R7 and R8 may vary in each case where m is greater than 1; ...
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4934997P | 1997-06-11 | 1997-06-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO4940506A1 true CO4940506A1 (en) | 2000-07-24 |
Family
ID=21959341
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO98033538A CO4940506A1 (en) | 1997-06-11 | 1998-06-11 | DERIVATIVES OF 9-OXYME ERYTHROMYCIN |
Country Status (31)
| Country | Link |
|---|---|
| EP (1) | EP0988308A1 (en) |
| JP (1) | JP2000513026A (en) |
| KR (1) | KR20010013660A (en) |
| CN (1) | CN1259135A (en) |
| AP (1) | AP9801253A0 (en) |
| AR (1) | AR012244A1 (en) |
| AU (1) | AU7226798A (en) |
| BG (1) | BG103947A (en) |
| BR (1) | BR9810021A (en) |
| CA (1) | CA2293335A1 (en) |
| CO (1) | CO4940506A1 (en) |
| CZ (1) | CZ9904388A3 (en) |
| EA (1) | EA199901016A1 (en) |
| GT (1) | GT199800074A (en) |
| HN (1) | HN1998000073A (en) |
| HR (1) | HRP980316A2 (en) |
| HU (1) | HUP0002252A3 (en) |
| ID (1) | ID24529A (en) |
| IL (1) | IL132767A0 (en) |
| IS (1) | IS5251A (en) |
| MA (1) | MA26505A1 (en) |
| NO (1) | NO996108L (en) |
| OA (1) | OA11225A (en) |
| PA (1) | PA8451801A1 (en) |
| PE (1) | PE79899A1 (en) |
| PL (1) | PL337606A1 (en) |
| TN (1) | TNSN98083A1 (en) |
| TR (1) | TR199902995T2 (en) |
| TW (1) | TW448174B (en) |
| WO (1) | WO1998056800A1 (en) |
| ZA (1) | ZA985018B (en) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HN1998000159A (en) * | 1997-10-29 | 1999-02-09 | Monsanto Co | DERIVATIVES OF 9- AMINO - 3 CETO ERITROMICINA |
| AU5299499A (en) * | 1998-09-22 | 2000-04-10 | Pfizer Products Inc. | Carbamate and carbazate ketolide antibiotics |
| FR2786188B1 (en) * | 1998-11-24 | 2002-10-31 | Hoechst Marion Roussel Inc | NOVEL ERYTHROMYCIN DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS MEDICAMENTS |
| US6258785B1 (en) | 1998-12-02 | 2001-07-10 | Pfizer Inc. | Crystalline 9-E-(O-methyl)oxime of 11, 12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribohexopyranosyloxy)-6-O-methyl-12,11-(iminocarbonyl-(2-(3-(4-(3-pyridinyl)1H-imadazol-1-yl)propyl)hydrazono))-3-oxoerythromycin |
| EP1298138B1 (en) * | 1998-12-10 | 2006-11-02 | Pfizer Products Inc. | Carbamate and Carbazate Ketolide Antibiotics |
| US6284732B1 (en) * | 1998-12-18 | 2001-09-04 | Bio-Rad Laboratories, Inc. | Peptides and peptide analogues designed from HFE protein and their uses in the treatment of iron overload diseases |
| WO2000063225A2 (en) * | 1999-04-16 | 2000-10-26 | Kosan Biosciences, Inc. | Macrolide antiinfective agents |
| SK15162001A3 (en) | 1999-05-24 | 2003-02-04 | Pfizer Products Inc. | 13-Methyl-erythromycin derivatives |
| PT1181300E (en) * | 1999-06-07 | 2004-02-27 | Abbott Lab | DERIVATIVES 6-O-CARBAMATE OF CETOLID |
| ID27331A (en) * | 1999-09-29 | 2001-03-29 | Pfizer Prod Inc | MAKING ANTIBIOTIC-ANTIBIOTIC KETOLIDA CARBAMATE |
| EP1114826A3 (en) * | 1999-12-29 | 2001-10-31 | Pfizer Products Inc. | Novel antibacterial and prokinetic macrolides |
| EP1439186A3 (en) * | 1999-12-29 | 2004-11-03 | Pfizer Products Inc. | Intermediates for novel antibacterial and prokinetic macrolides |
| US6946446B2 (en) | 2000-02-24 | 2005-09-20 | Abbott Laboratories | Anti-infective agents useful against multidrug-resistant strains of bacteria |
| US6403776B1 (en) | 2000-07-05 | 2002-06-11 | Pfizer Inc. | Synthesis of carbamate ketolide antibiotics |
| WO2003090761A1 (en) * | 2002-04-25 | 2003-11-06 | Abbott Laboratories | 9-oxime macrolide antibacterials |
| US7091196B2 (en) | 2002-09-26 | 2006-08-15 | Rib-X Pharmaceuticals, Inc. | Bifunctional heterocyclic compounds and methods of making and using same |
| WO2004080391A2 (en) * | 2003-03-10 | 2004-09-23 | Optimer Pharmaceuticals, Inc. | Novel antibacterial agents |
| JP5383037B2 (en) | 2004-02-27 | 2014-01-08 | リブ−エックス ファーマシューティカルズ，インコーポレイテッド | Macrocyclic compounds and methods of making and using them |
| US9453042B2 (en) | 2007-10-25 | 2016-09-27 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
| WO2010048600A1 (en) | 2008-10-24 | 2010-04-29 | Cempra Pharmaceuticals, Inc. | Methods for treating resistant diseases using triazole containing macrolides |
| US9937194B1 (en) | 2009-06-12 | 2018-04-10 | Cempra Pharmaceuticals, Inc. | Compounds and methods for treating inflammatory diseases |
| CN108310000A (en) | 2009-09-10 | 2018-07-24 | 森普拉制药公司 | Treat malaria, the method for tuberculosis and MAC diseases |
| CN102146085B (en) * | 2010-02-09 | 2014-03-26 | 北京理工大学 | 9-oxime-ether ketolide derivative, and preparation method and medical composite thereof |
| KR20180101643A (en) | 2010-03-22 | 2018-09-12 | 셈프라 파마슈티컬스, 인크. | Crystalline forms of a macrolide, and uses therefor |
| CA2799937A1 (en) | 2010-05-20 | 2011-11-24 | Cempra Pharmaceuticals, Inc. | Processes for preparing macrolides and ketolides and intermediates therefor |
| US9815863B2 (en) | 2010-09-10 | 2017-11-14 | Cempra Pharmaceuticals, Inc. | Hydrogen bond forming fluoro ketolides for treating diseases |
| CA2868262A1 (en) | 2012-03-27 | 2013-10-03 | Cempra Pharmaceuticals, Inc. | Parenteral formulations for administering macrolide antibiotics |
| AU2014239959A1 (en) | 2013-03-14 | 2015-10-01 | Cempra Pharmaceuticals, Inc. | Methods for treating respiratory diseases and formulations therefor |
| AU2014233240B2 (en) | 2013-03-15 | 2018-08-09 | Cempra Pharmaceuticals, Inc. | Convergent processes for preparing macrolide antibacterial agents |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL99995A (en) * | 1990-11-21 | 1997-11-20 | Roussel Uclaf | Erythromycin derivatives, their preparation and pharmaceutical compositions containing them |
| US5527780A (en) * | 1992-11-05 | 1996-06-18 | Roussel Uclaf | Erythromycin derivatives |
| FR2718450B1 (en) * | 1994-04-08 | 1997-01-10 | Roussel Uclaf | New erythromycin derivatives, their preparation process and their use as drugs. |
-
1998
- 1998-05-15 CN CN98805848A patent/CN1259135A/en active Pending
- 1998-05-15 ID IDW991570A patent/ID24529A/en unknown
- 1998-05-15 TR TR1999/02995T patent/TR199902995T2/en unknown
- 1998-05-15 CZ CZ19994388A patent/CZ9904388A3/en unknown
- 1998-05-15 HU HU0002252A patent/HUP0002252A3/en unknown
- 1998-05-15 WO PCT/IB1998/000741 patent/WO1998056800A1/en not_active Application Discontinuation
- 1998-05-15 CA CA002293335A patent/CA2293335A1/en not_active Abandoned
- 1998-05-15 EA EA199901016A patent/EA199901016A1/en unknown
- 1998-05-15 EP EP98919394A patent/EP0988308A1/en not_active Withdrawn
- 1998-05-15 BR BR9810021-1A patent/BR9810021A/en not_active IP Right Cessation
- 1998-05-15 AU AU72267/98A patent/AU7226798A/en not_active Abandoned
- 1998-05-15 JP JP11501928A patent/JP2000513026A/en active Pending
- 1998-05-15 PL PL98337606A patent/PL337606A1/en unknown
- 1998-05-15 KR KR1019997011672A patent/KR20010013660A/en not_active Ceased
- 1998-05-15 IL IL13276798A patent/IL132767A0/en unknown
- 1998-05-19 HN HN1998000073A patent/HN1998000073A/en unknown
- 1998-05-21 PA PA19988451801A patent/PA8451801A1/en unknown
- 1998-06-04 AP APAP/P/1998/001253A patent/AP9801253A0/en unknown
- 1998-06-05 GT GT199800074A patent/GT199800074A/en unknown
- 1998-06-08 TW TW087109086A patent/TW448174B/en active
- 1998-06-08 PE PE1998000470A patent/PE79899A1/en not_active Application Discontinuation
- 1998-06-09 AR ARP980102703A patent/AR012244A1/en unknown
- 1998-06-10 MA MA25105A patent/MA26505A1/en unknown
- 1998-06-10 TN TNTNSN98083A patent/TNSN98083A1/en unknown
- 1998-06-10 ZA ZA9805018A patent/ZA985018B/en unknown
- 1998-06-11 HR HR60/049,349A patent/HRP980316A2/en not_active Application Discontinuation
- 1998-06-11 CO CO98033538A patent/CO4940506A1/en unknown
-
1999
- 1999-11-16 IS IS5251A patent/IS5251A/en unknown
- 1999-12-03 BG BG103947A patent/BG103947A/en unknown
- 1999-12-03 OA OA9900269A patent/OA11225A/en unknown
- 1999-12-10 NO NO996108A patent/NO996108L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EA199901016A1 (en) | 2000-06-26 |
| CZ9904388A3 (en) | 2002-10-16 |
| EP0988308A1 (en) | 2000-03-29 |
| TW448174B (en) | 2001-08-01 |
| MA26505A1 (en) | 2004-12-20 |
| OA11225A (en) | 2003-07-17 |
| NO996108D0 (en) | 1999-12-10 |
| AU7226798A (en) | 1998-12-30 |
| ZA985018B (en) | 1999-12-10 |
| TR199902995T2 (en) | 2000-02-21 |
| PL337606A1 (en) | 2000-08-28 |
| ID24529A (en) | 2000-07-20 |
| BG103947A (en) | 2000-07-31 |
| IS5251A (en) | 1999-11-16 |
| HRP980316A2 (en) | 1999-04-30 |
| IL132767A0 (en) | 2001-03-19 |
| WO1998056800A1 (en) | 1998-12-17 |
| TNSN98083A1 (en) | 2005-03-15 |
| KR20010013660A (en) | 2001-02-26 |
| PA8451801A1 (en) | 2000-05-24 |
| JP2000513026A (en) | 2000-10-03 |
| GT199800074A (en) | 1999-11-27 |
| NO996108L (en) | 2000-02-10 |
| HUP0002252A2 (en) | 2000-12-28 |
| PE79899A1 (en) | 1999-08-25 |
| AP9801253A0 (en) | 1999-12-04 |
| HN1998000073A (en) | 1999-01-08 |
| CN1259135A (en) | 2000-07-05 |
| HUP0002252A3 (en) | 2002-01-28 |
| AR012244A1 (en) | 2000-09-27 |
| CA2293335A1 (en) | 1998-12-17 |
| BR9810021A (en) | 2000-09-19 |
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