BR0316569A - 9a-n-(n'-carbamoil-gama-aminopropila), 9a-n-(n'-tiocarbamoil-gama-aminopropila), 9a-n-[n'-(beta-cianoetil)-n'-carbamoil-gama-aminoprop ila] e 9a-n-[n'-(beta-cianoetil)-n'-tiocarbamoil-gama-aminop ropila] n"-substituìdas derivadas de 9-desoxo-9-diidro-9a-aza-9a-homoeritromicina a e 5-o-desosaminil-9-desoxo-9-diidro-9a-aza-9a-homoerit ronolida a - Google Patents
9a-n-(n'-carbamoil-gama-aminopropila), 9a-n-(n'-tiocarbamoil-gama-aminopropila), 9a-n-[n'-(beta-cianoetil)-n'-carbamoil-gama-aminoprop ila] e 9a-n-[n'-(beta-cianoetil)-n'-tiocarbamoil-gama-aminop ropila] n"-substituìdas derivadas de 9-desoxo-9-diidro-9a-aza-9a-homoeritromicina a e 5-o-desosaminil-9-desoxo-9-diidro-9a-aza-9a-homoerit ronolida aInfo
- Publication number
- BR0316569A BR0316569A BR0316569-8A BR0316569A BR0316569A BR 0316569 A BR0316569 A BR 0316569A BR 0316569 A BR0316569 A BR 0316569A BR 0316569 A BR0316569 A BR 0316569A
- Authority
- BR
- Brazil
- Prior art keywords
- aminopropyl
- gamma
- aza
- cyanoethyl
- dihydro
- Prior art date
Links
- -1 beta-cyanoethyl Chemical group 0.000 title abstract 5
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 abstract 1
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 abstract 1
- 125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 abstract 1
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 abstract 1
- 125000005809 3,4,5-trimethoxyphenyl group Chemical group [H]C1=C(OC([H])([H])[H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 abstract 1
- 125000006201 3-phenylpropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- ZUSWDTWYONAOPH-UHFFFAOYSA-N [2-(trifluoromethyl)phenyl]hydrazine;hydrochloride Chemical group [Cl-].[NH3+]NC1=CC=CC=C1C(F)(F)F ZUSWDTWYONAOPH-UHFFFAOYSA-N 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 239000003120 macrolide antibiotic agent Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 150000007522 mineralic acids Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000007524 organic acids Chemical class 0.000 abstract 1
- 235000005985 organic acids Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 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
-
- 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
-
- 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
-
- 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
- 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
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
"9a-N-(N<39>-CARBAMOIL-GAMA-AMINOPROPILA), 9a-N-(N<39>-TIOCARBAMOIL-GAMA-AMINOPROPILA), 9a-N-¢N<39>-(BETA-CIANOETIL)-N<39>-CARBAMOIL-GAMA-AMI NOPROPILA! E 9a-N-¢N<39>-(BETACIANOETIL)-N<39>-TIOCARBAMOIL-GAMA-A MINOPROPILA! N<39><39>-SUBSTITUìDAS DERIVADAS DE 9-DESOXO-9-DIIDRO-9a-AZA-9a-HOMOERITROMICINA A E 5-O-DESOSAMINIL-9-DESOXO-9-DIIDRO-9a-AZA-9a-HOMOERIT RONOLIDA A". A presente invenção refere-se a 9a-N-(N<39>-carbamoil-<sym>-aminopropila), 9a-N-(N<39>-tiocarbamoil-<sym>-aminopropila), 9a-N-¢N<39>-(<225>-cianoetil)-N<39>-carbamoil-<sym>-aminopropil a! e 9a-N-¢N<39>-(<225>-cianoetil)-N<39>-tiocarbamoil-<sym>-aminopro pila! N<39><39>-substituídas derivadas de 9-desoxo-9-diidro-9a-aza-9a-homoeritromicina A e 5-O-desosaminil-9-desoxo-9-diidro-9a-aza-9a-homoeritronolida A, novo antibiótico de macrolida semi-sintético da série azalida, da fórmula geral 1, onde R representa H ou porção cladinosila, R¬ 1¬ representa H ou (porção <225>cianoetila, R¬ 2¬ representa grupo isopropila, 1-naftila, 2-naftila, benzila, 2-(trifluormetil)fenila, 3-fenilpropila, <225>-feniletila, etoxicarbonilmetila, 1-(1-naftil)etila, 3,4,5-trimetoxifenila e 2,4-diclorofenila, e X representa O e S, e seus sais de adição farmaceuticamente aceitáveis com ácidos inorgânicos ou orgânicos, ao processo para preparação das composições farmacêuticas bem como ao uso de suas composições no tratamento de infecções bacterianas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HR20020991A HRP20020991A2 (en) | 2002-12-12 | 2002-12-12 | N"-Substituted 9a-N-(N'-carbamoyl-Gamma-aminopropyl), 9a-N-(N'? -thiocarbamoyl-Gamma-aminopropyl), 9a-N-(N'-((Beta-cyanoethyl)-N'-carbamoyl-Gamma? -aminopropyl) and 9a-N-(N'-(Beta-cyanoethyl)-N'-thiocarbamoyl-Gamma? -aminopropyl) derivatives of 9-de |
| PCT/HR2003/000062 WO2004052904A2 (en) | 2002-12-12 | 2003-12-10 | Novel semisynthetic macrolide antibiotics of the azalide series |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0316569A true BR0316569A (pt) | 2005-10-04 |
Family
ID=32500425
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0316569-8A BR0316569A (pt) | 2002-12-12 | 2003-12-10 | 9a-n-(n'-carbamoil-gama-aminopropila), 9a-n-(n'-tiocarbamoil-gama-aminopropila), 9a-n-[n'-(beta-cianoetil)-n'-carbamoil-gama-aminoprop ila] e 9a-n-[n'-(beta-cianoetil)-n'-tiocarbamoil-gama-aminop ropila] n"-substituìdas derivadas de 9-desoxo-9-diidro-9a-aza-9a-homoeritromicina a e 5-o-desosaminil-9-desoxo-9-diidro-9a-aza-9a-homoerit ronolida a |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US7342000B2 (pt) |
| EP (1) | EP1585753B1 (pt) |
| JP (1) | JP2006510660A (pt) |
| KR (1) | KR20050085555A (pt) |
| CN (1) | CN100335489C (pt) |
| AR (1) | AR042351A1 (pt) |
| AT (1) | ATE327999T1 (pt) |
| AU (1) | AU2003285599A1 (pt) |
| BR (1) | BR0316569A (pt) |
| CA (1) | CA2509599A1 (pt) |
| CL (1) | CL2003002585A1 (pt) |
| CO (1) | CO5640139A2 (pt) |
| CY (1) | CY1106321T1 (pt) |
| DE (1) | DE60305741T2 (pt) |
| DK (1) | DK1585753T3 (pt) |
| ES (1) | ES2266883T3 (pt) |
| HR (1) | HRP20020991A2 (pt) |
| IS (1) | IS2309B (pt) |
| MX (1) | MXPA05006220A (pt) |
| PL (1) | PL377322A1 (pt) |
| PT (1) | PT1585753E (pt) |
| RS (1) | RS80204A (pt) |
| RU (1) | RU2328503C2 (pt) |
| WO (1) | WO2004052904A2 (pt) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20020885B1 (en) | 2002-11-11 | 2007-05-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | SUBSTITUTED 9a-N-{N'-[4-(SULFONYL)PHENYLCARBAMOYL]}DERIVATIVES 9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERITHROMYCIN A AND 5-O-DESOZAMINYL-9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERITHRONOLIDE A |
| DE602006016231D1 (de) * | 2005-01-14 | 2010-09-30 | Glaxosmithkline Zagreb | 9a-carbamoyl-y-aminopropyl- und 9a-thiocarbamoyl-y-aminopropyl-azalide mit antimalaria-aktivität |
| WO2006085228A2 (en) * | 2005-01-14 | 2006-08-17 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | 9a-carbamoyl-y-aminopropyl and 9a-thiocarbamoyl-y-aminopropyl-azalides with antimalarial activity |
| WO2007125414A2 (en) * | 2006-05-03 | 2007-11-08 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | 9a-substituted azalides for the tratment of malaria |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI7910768A8 (en) | 1979-04-02 | 1996-06-30 | Pliva Pharm & Chem Works | Process for pripering 11-aza-4-0-cladinosyl-6-0-desosaminyl-15-ethyl- 7,13,14-trihydroxy-3,5,7,9,12,14-hexamethyl- oxacyclopentadecane-2-one and their derivatives |
| FR2473525A1 (fr) | 1980-01-11 | 1981-07-17 | Roussel Uclaf | Nouvelles oximes derivees de l'erythromycine, leur procede de preparation et leur application comme medicaments |
| BE892397A (nl) | 1982-03-08 | 1982-07-01 | Marchand Paul | Wereldwijde draadloze telefonie voor 10 miljard abonnees |
| US4474768A (en) | 1982-07-19 | 1984-10-02 | Pfizer Inc. | N-Methyl 11-aza-10-deoxo-10-dihydro-erytromycin A, intermediates therefor |
| PH19293A (en) * | 1982-11-15 | 1986-03-04 | Pfizer | Epimeric azahomoerythromycin,pharmaceutical composition containing the same and method of use thereof |
| US4492688A (en) | 1983-11-25 | 1985-01-08 | Pfizer Inc. | Antibacterial cyclic ethers of 9-deoxo-9a-aza-9a-homoerythromycin A and intermediates therefor |
| US4464527A (en) * | 1983-06-30 | 1984-08-07 | Pfizer Inc. | Antibacterial 9-deoxo-9a-alkyl-9a-aza-9a-homoerythromycin A derivatives and intermediates therefore |
| MX13723A (es) | 1987-11-10 | 1993-05-01 | Pfizer | Procedimiento para preparar derivados de 9-desoxo-9a-alil- y propargil-9a-aza-9a-homoeritromicina a |
| HRP931480B1 (en) * | 1993-12-08 | 1997-08-31 | Sour Pliva | 9a-N-(N'-CARBAMONYL) and 9a-N-(N'-THIOCARBAMONYL) DERIVATES OF 9-DEOXO-9a-HOMOERYTHROMYCIN A |
| WO1997035590A1 (en) * | 1996-03-25 | 1997-10-02 | Platt Chris E | 10-aza-9-deoxo-11-deoxy-erythromycin a and derivatives combined with sulfisoxazole |
| HRP970714B1 (en) * | 1997-12-31 | 2003-08-31 | Pliva Pharm & Chem Works | Beta,beta-disubstituted derivatives of 9-deoxo-9a-n-ethenyl-9a-aza-9a-homoerythromycin a |
| HRP990130B1 (en) * | 1999-05-03 | 2004-06-30 | Pliva D D | HALOGEN DERIVATIVES 9a-N-(N'-ARYLCARBAMOYL)- AND 9a-N-(N'-ARYLTHIOCARBAMOYL)-9-DEOXO-9a-AZA-9a OF HOMOERYTHROMYCIN A |
| ES2275621T3 (es) * | 2000-12-21 | 2007-06-16 | Glaxo Group Limited | Antibioticos macrolidos. |
| HRP20010146B1 (en) | 2001-02-28 | 2005-10-31 | Pliva D.D. | 9a-N-(N'-(PHENYLSULFONYL)CARBAMOYL) DERIVATIVES OF 9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERYTHROMYCIN A AND OF 5-O-DESOSAMINYL-9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERYTHRONOLIDE A |
| HRP20020886A2 (en) | 2002-11-11 | 2005-06-30 | PLIVA-ISTRAŽIVAČKI INSTITUT d.o.o. | SUBSTITUTED 9a-N-[N'-(BENZENSULFONYL)CARBAMOYL-γ-AMINOPROPYL) AND 9a-N(N' -(?-CYANOETHIL)-N' -(b |
| HRP20020885B1 (en) | 2002-11-11 | 2007-05-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | SUBSTITUTED 9a-N-{N'-[4-(SULFONYL)PHENYLCARBAMOYL]}DERIVATIVES 9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERITHROMYCIN A AND 5-O-DESOZAMINYL-9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERITHRONOLIDE A |
-
2002
- 2002-12-12 HR HR20020991A patent/HRP20020991A2/hr not_active Application Discontinuation
-
2003
- 2003-12-10 DE DE60305741T patent/DE60305741T2/de not_active Expired - Fee Related
- 2003-12-10 RS YU80204A patent/RS80204A/sr unknown
- 2003-12-10 ES ES03778598T patent/ES2266883T3/es not_active Expired - Lifetime
- 2003-12-10 US US10/538,376 patent/US7342000B2/en not_active Expired - Fee Related
- 2003-12-10 AR ARP030104537A patent/AR042351A1/es not_active Application Discontinuation
- 2003-12-10 RU RU2005121892/04A patent/RU2328503C2/ru not_active IP Right Cessation
- 2003-12-10 DK DK03778598T patent/DK1585753T3/da active
- 2003-12-10 MX MXPA05006220A patent/MXPA05006220A/es active IP Right Grant
- 2003-12-10 CN CNB2003801057628A patent/CN100335489C/zh not_active Expired - Fee Related
- 2003-12-10 PT PT03778598T patent/PT1585753E/pt unknown
- 2003-12-10 AU AU2003285599A patent/AU2003285599A1/en not_active Abandoned
- 2003-12-10 PL PL377322A patent/PL377322A1/pl unknown
- 2003-12-10 JP JP2004558858A patent/JP2006510660A/ja active Pending
- 2003-12-10 AT AT03778598T patent/ATE327999T1/de not_active IP Right Cessation
- 2003-12-10 CA CA002509599A patent/CA2509599A1/en not_active Abandoned
- 2003-12-10 BR BR0316569-8A patent/BR0316569A/pt not_active IP Right Cessation
- 2003-12-10 EP EP03778598A patent/EP1585753B1/en not_active Expired - Lifetime
- 2003-12-10 WO PCT/HR2003/000062 patent/WO2004052904A2/en not_active Ceased
- 2003-12-10 KR KR1020057010623A patent/KR20050085555A/ko not_active Withdrawn
- 2003-12-11 CL CL200302585A patent/CL2003002585A1/es unknown
-
2005
- 2005-05-31 IS IS7875A patent/IS2309B/is unknown
- 2005-07-08 CO CO05067476A patent/CO5640139A2/es not_active Application Discontinuation
-
2006
- 2006-08-25 CY CY20061101203T patent/CY1106321T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AR042351A1 (es) | 2005-06-15 |
| CO5640139A2 (es) | 2006-05-31 |
| HRP20020991A2 (en) | 2005-02-28 |
| HK1086273A1 (en) | 2006-09-15 |
| WO2004052904A2 (en) | 2004-06-24 |
| IS7875A (is) | 2005-05-31 |
| RU2328503C2 (ru) | 2008-07-10 |
| CN1726222A (zh) | 2006-01-25 |
| CN100335489C (zh) | 2007-09-05 |
| DE60305741D1 (de) | 2006-07-06 |
| ATE327999T1 (de) | 2006-06-15 |
| JP2006510660A (ja) | 2006-03-30 |
| RS80204A (sr) | 2006-12-15 |
| PT1585753E (pt) | 2006-08-31 |
| ES2266883T3 (es) | 2007-03-01 |
| RU2005121892A (ru) | 2006-01-20 |
| WO2004052904A3 (en) | 2004-09-02 |
| EP1585753B1 (en) | 2006-05-31 |
| MXPA05006220A (es) | 2005-11-17 |
| CY1106321T1 (el) | 2011-10-12 |
| DE60305741T2 (de) | 2007-06-14 |
| CL2003002585A1 (es) | 2005-01-28 |
| PL377322A1 (pl) | 2006-01-23 |
| IS2309B (is) | 2007-10-15 |
| US7342000B2 (en) | 2008-03-11 |
| EP1585753A2 (en) | 2005-10-19 |
| AU2003285599A8 (en) | 2004-06-30 |
| DK1585753T3 (da) | 2006-10-02 |
| CA2509599A1 (en) | 2004-06-24 |
| KR20050085555A (ko) | 2005-08-29 |
| AU2003285599A1 (en) | 2004-06-30 |
| US20060252709A1 (en) | 2006-11-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE 6A., 7A. E 8A. ANUIDADE(S), |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2129 DE 25/10/2011. |