HUP0004323A2 - 6,11-Áthidalt eritromicinszármazékok, azokat tartalmazó gyógyszerkészítmények, valamint eljárás ilyen származékok előállítására - Google Patents
6,11-Áthidalt eritromicinszármazékok, azokat tartalmazó gyógyszerkészítmények, valamint eljárás ilyen származékok előállításáraInfo
- Publication number
- HUP0004323A2 HUP0004323A2 HU0004323A HUP0004323A HUP0004323A2 HU P0004323 A2 HUP0004323 A2 HU P0004323A2 HU 0004323 A HU0004323 A HU 0004323A HU P0004323 A HUP0004323 A HU P0004323A HU P0004323 A2 HUP0004323 A2 HU P0004323A2
- Authority
- HU
- Hungary
- Prior art keywords
- derivatives
- group
- molecule
- general formula
- present
- Prior art date
Links
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical class 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 abstract 3
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000035143 Bacterial infection Diseases 0.000 abstract 2
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 2
- NAWXUBYGYWOOIX-SFHVURJKSA-N (2s)-2-[[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]amino]-4-methylidenepentanedioic acid Chemical compound C1=CC2=NC(N)=NC(N)=C2C=C1CCC1=CC=C(C(=O)N[C@@H](CC(=C)C(O)=O)C(O)=O)C=C1 NAWXUBYGYWOOIX-SFHVURJKSA-N 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 230000000844 anti-bacterial effect Effects 0.000 abstract 1
- 125000000732 arylene group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000003120 macrolide antibiotic agent Substances 0.000 abstract 1
- 229940041033 macrolides Drugs 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
Abstract
A találmány új, baktériumellenes hatású, szemiszintetikusmakrolidokra, közelebbről meghatározva 6,11-áthidalteritromicinszármazékokra, az azokat tartalmazógyógyszerkészítményekre, valamint ilyen származékok előállítására,illetve baktériumos fertőzések kezelésére vonatkozik. A találmányszerinti 6,11-áthidalt eritromicinszármazékok (I) vagy (II) általánosképletében - bizonyos megkötésekkel - m értéke 0, 1, 2, 3, 4, 5, 6 vagy 7; n értéke 0, 1, 2, 3 vagy 4; az Rp szubsztituensek jelentése - az egyes előfordulási helyeikenegymástól függetlenül - hidrogénatom vagy hidroxilcsoportot védőcsoport; A nincs jelen a molekulában vagy -O- vagy -N(R1)- képletű csoport; B nincs jelen a molekulában vagy -(CH2)q-, -C(O)-(CH2)q-, -C(O)-O-(CH2)q-, -C(O)-NR1-(CH2)q-, -N=CH-(CH2)q-, -CH(OH)-(CH2)q- vagy -CH(OH)-CH(OH)-(CH2)q-; D nincs jelen a molekulában vagy jelentése - többek között -alkeniléncsoport, ariléncsoport, alkenilén-arilén-csoport, arilén-arilén-csoport vagy alkenilén-heteroarilén-csoport; E nincs jelen a molekulában vagy -(CH2)r-CH=CH-, -(CH2)r-O-, -(CH2)r-NR1-CH2-CH(OH)-, -(CH2)r-C(O)-O-, -(CH2)r-N(R1)-, -(CH2)r-O-C(O)-, -(CH2)r-C(O)-N(R1)- vagy -(CH2)r-N(R1)-C(O)-. A találmány szerinti (I)vagy (II) 6,11-áthidalt eritromicinszármazékokat különbözőeljárásokkal, például úgy állítják elő, hogy (10) általános képletűvegyületeket H2N-(CH2)m-A-B-D-X1 általános képletű vegyületekkelreagáltatnak, majd a keletkezett (12) általános képletű vegyületeketciklizálják és adott esetben redukálják. A találmány szerintivegyületek baktériumellenes fertőzések kezelésére alkalmasgyógyszerkészítmények hatóanyagai. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US96040097A | 1997-10-29 | 1997-10-29 | |
| US15826998A | 1998-09-22 | 1998-09-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUP0004323A2 true HUP0004323A2 (hu) | 2001-02-28 |
Family
ID=26854886
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0004323A HUP0004323A2 (hu) | 1997-10-29 | 1998-10-29 | 6,11-Áthidalt eritromicinszármazékok, azokat tartalmazó gyógyszerkészítmények, valamint eljárás ilyen származékok előállítására |
Country Status (23)
| Country | Link |
|---|---|
| EP (1) | EP1027361B1 (hu) |
| JP (1) | JP2001521038A (hu) |
| KR (1) | KR20010031591A (hu) |
| CN (1) | CN1278266A (hu) |
| AR (1) | AR015986A1 (hu) |
| AT (1) | ATE239750T1 (hu) |
| AU (1) | AU1286799A (hu) |
| BG (1) | BG104425A (hu) |
| BR (1) | BR9813317A (hu) |
| CA (1) | CA2307828A1 (hu) |
| CO (1) | CO4990972A1 (hu) |
| DE (1) | DE69814441T2 (hu) |
| DK (1) | DK1027361T3 (hu) |
| ES (1) | ES2198766T3 (hu) |
| HU (1) | HUP0004323A2 (hu) |
| IL (1) | IL134996A0 (hu) |
| NO (1) | NO20002099L (hu) |
| PL (1) | PL340253A1 (hu) |
| PT (1) | PT1027361E (hu) |
| SK (1) | SK6342000A3 (hu) |
| TR (1) | TR200001140T2 (hu) |
| TW (1) | TW486485B (hu) |
| WO (1) | WO1999021864A1 (hu) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6437106B1 (en) | 1999-06-24 | 2002-08-20 | Abbott Laboratories | Process for preparing 6-o-substituted erythromycin derivatives |
| US6472372B1 (en) * | 2000-12-06 | 2002-10-29 | Ortho-Mcneil Pharmaceuticals, Inc. | 6-O-Carbamoyl ketolide antibacterials |
| JP2005503416A (ja) | 2001-09-17 | 2005-02-03 | オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド | ６−ｏ−カルバメート−１１，１２−ラクト−ケトライド抗菌剤 |
| BR0214748A (pt) | 2001-12-05 | 2004-11-23 | Ortho Mcneil Pharm Inc | Derivados 6-oacil-cetolidas de eritromicina, úteis como antibacterianos |
| US6841664B2 (en) * | 2002-07-25 | 2005-01-11 | Enanra Pharmaceuticals, Inc. | 6,11-4-carbon bridged ketolides |
| US6753318B1 (en) | 2002-07-25 | 2004-06-22 | Enanta Pharmaceuticals, Inc. | 6,11-4-carbon bridged erythromycin derivatives |
| CN1659178A (zh) | 2002-05-13 | 2005-08-24 | 英安塔制药有限公司 | 6、11二环红霉素衍生物 |
| US7273853B2 (en) | 2002-05-13 | 2007-09-25 | Enanta Pharmaceuticals, Inc. | 6-11 bicyclic ketolide derivatives |
| US7910558B2 (en) * | 2002-05-13 | 2011-03-22 | Enanta Pharmaceuticals, Inc. | Bridged macrocyclic compounds and processes for the preparation thereof |
| CA2483875C (en) * | 2002-05-13 | 2008-09-23 | Enanta Pharmaceuticals, Inc. | 6,11 bicyclic erythromycin derivatives |
| US6645941B1 (en) * | 2003-03-26 | 2003-11-11 | Enanta Pharmaceuticals, Inc. | 6,11-3C-bicyclic 9a-azalide derivatives |
| US7414030B2 (en) | 2004-01-07 | 2008-08-19 | Enanta Pharmaceuticals, Inc. | 6-11 Bicyclic erythromycin derivatives |
| WO2005070113A2 (en) | 2004-01-09 | 2005-08-04 | Enanta Pharmaceuticals, Inc. | 9n-substituted 6-11 bicyclic erythromycin derivatives |
| WO2005080408A1 (en) * | 2004-01-23 | 2005-09-01 | Enanta Pharmaceuticals, Inc. | Bridged macrocyclic compounds and processes for the preparation thereof |
| US7384921B2 (en) | 2004-02-20 | 2008-06-10 | Enanta Pharmaceuticals, Inc. | Polymorphic forms of 6-11 bicyclic ketolide derivatives |
| US7384922B2 (en) | 2005-05-04 | 2008-06-10 | Enanta Pharmaceuticals, Inc. | 6-11 bridged oxime erythromycin derivatives |
| US7589067B2 (en) | 2005-10-12 | 2009-09-15 | Enanta Pharmaceuticals, Inc. | 6, 11-bridged tricyclic macrolides |
| US8273720B2 (en) | 2007-09-17 | 2012-09-25 | Enanta Pharmaceuticals, Inc. | 6,11-bicyclolides: bridged biaryl macrolide derivatives |
| US11673910B2 (en) | 2017-04-28 | 2023-06-13 | Zikani Therapeutics, Inc. | Macrolides with modified desosamine sugars and uses thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT876388E (pt) * | 1995-11-08 | 2004-07-30 | Abbott Lab | Derivados de eritromicina triciclica |
-
1998
- 1998-10-27 CO CO98062727A patent/CO4990972A1/es unknown
- 1998-10-27 AR ARP980105375A patent/AR015986A1/es unknown
- 1998-10-29 TR TR2000/01140T patent/TR200001140T2/xx unknown
- 1998-10-29 DE DE69814441T patent/DE69814441T2/de not_active Expired - Fee Related
- 1998-10-29 CN CN98810785A patent/CN1278266A/zh active Pending
- 1998-10-29 ES ES98956314T patent/ES2198766T3/es not_active Expired - Lifetime
- 1998-10-29 JP JP2000517973A patent/JP2001521038A/ja not_active Withdrawn
- 1998-10-29 PT PT98956314T patent/PT1027361E/pt unknown
- 1998-10-29 HU HU0004323A patent/HUP0004323A2/hu unknown
- 1998-10-29 DK DK98956314T patent/DK1027361T3/da active
- 1998-10-29 AT AT98956314T patent/ATE239750T1/de not_active IP Right Cessation
- 1998-10-29 IL IL13499698A patent/IL134996A0/xx unknown
- 1998-10-29 PL PL98340253A patent/PL340253A1/xx unknown
- 1998-10-29 WO PCT/US1998/022941 patent/WO1999021864A1/en not_active Application Discontinuation
- 1998-10-29 CA CA002307828A patent/CA2307828A1/en not_active Abandoned
- 1998-10-29 SK SK634-2000A patent/SK6342000A3/sk unknown
- 1998-10-29 BR BR9813317-9A patent/BR9813317A/pt not_active IP Right Cessation
- 1998-10-29 AU AU12867/99A patent/AU1286799A/en not_active Abandoned
- 1998-10-29 EP EP98956314A patent/EP1027361B1/en not_active Expired - Lifetime
- 1998-10-29 KR KR1020007004641A patent/KR20010031591A/ko not_active Application Discontinuation
- 1998-11-30 TW TW087117981A patent/TW486485B/zh active
-
2000
- 2000-04-25 NO NO20002099A patent/NO20002099L/no not_active Application Discontinuation
- 2000-05-11 BG BG104425A patent/BG104425A/bg unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO20002099D0 (no) | 2000-04-25 |
| AU1286799A (en) | 1999-05-17 |
| TW486485B (en) | 2002-05-11 |
| PL340253A1 (en) | 2001-01-29 |
| SK6342000A3 (en) | 2000-09-12 |
| DE69814441T2 (de) | 2004-04-08 |
| DE69814441D1 (de) | 2003-06-12 |
| EP1027361B1 (en) | 2003-05-07 |
| JP2001521038A (ja) | 2001-11-06 |
| PT1027361E (pt) | 2003-09-30 |
| ATE239750T1 (de) | 2003-05-15 |
| TR200001140T2 (tr) | 2001-05-21 |
| WO1999021864A1 (en) | 1999-05-06 |
| BG104425A (bg) | 2001-01-31 |
| CN1278266A (zh) | 2000-12-27 |
| CO4990972A1 (es) | 2000-12-26 |
| AR015986A1 (es) | 2001-05-30 |
| ES2198766T3 (es) | 2004-02-01 |
| IL134996A0 (en) | 2001-05-20 |
| CA2307828A1 (en) | 1999-05-06 |
| BR9813317A (pt) | 2000-08-22 |
| EP1027361A1 (en) | 2000-08-16 |
| KR20010031591A (ko) | 2001-04-16 |
| DK1027361T3 (da) | 2003-08-25 |
| NO20002099L (no) | 2000-06-29 |
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