ES482774A1 - Un procedimiento para preparar una nueva composicion anti- bacteriana potenciada. - Google Patents
Un procedimiento para preparar una nueva composicion anti- bacteriana potenciada.Info
- Publication number
- ES482774A1 ES482774A1 ES482774A ES482774A ES482774A1 ES 482774 A1 ES482774 A1 ES 482774A1 ES 482774 A ES482774 A ES 482774A ES 482774 A ES482774 A ES 482774A ES 482774 A1 ES482774 A1 ES 482774A1
- Authority
- ES
- Spain
- Prior art keywords
- thienamycin
- type compound
- antibacterial composition
- inhibitor
- dipeptidase inhibitor
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 229940090955 Dipeptidase inhibitor Drugs 0.000 title 1
- 230000000844 anti-bacterial effect Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 abstract 2
- 102000004860 Dipeptidases Human genes 0.000 abstract 1
- 108090001081 Dipeptidases Proteins 0.000 abstract 1
- WKDDRNSBRWANNC-ATRFCDNQSA-N Thienamycin Chemical compound C1C(SCCN)=C(C(O)=O)N2C(=O)[C@H]([C@H](O)C)[C@H]21 WKDDRNSBRWANNC-ATRFCDNQSA-N 0.000 abstract 1
- WKDDRNSBRWANNC-UHFFFAOYSA-N Thienamycin Natural products C1C(SCCN)=C(C(O)=O)N2C(=O)C(C(O)C)C21 WKDDRNSBRWANNC-UHFFFAOYSA-N 0.000 abstract 1
- 229940124350 antibacterial drug Drugs 0.000 abstract 1
- -1 beta -lactam compound Chemical class 0.000 abstract 1
- 239000000890 drug combination Substances 0.000 abstract 1
- 150000003952 β-lactams Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
- C07D477/10—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
- C07D477/12—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
- C07D477/16—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6 with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 3
- C07D477/20—Sulfur atoms
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
- C07F9/3808—Acyclic saturated acids which can have further substituents on alkyl
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
1. Un procedimiento para preparar una nueva composición antibacteriana potenciada que comprende una combinación de un compuesto del tipo de tienamicina y un inhibidor de la dipeptidasa (E.C.3.4.13.11), caracterizándose dicho procedimiento porque consiste en las siguientes etapas: a) al combinar un compuesto del tipo de la tienamicina de fórmula- 01: **(Fórmula-01)** donde X puede ser CH2 o S; R2 puede ser hidrógeno, -S-CH2-CH2- NHR3, donde R3 es hidrógeno, acetilo, formidoilo o acetimidoilo, -S(O)-CH=CHNHCOCH3 y -S-CH=CHNHCOCH3 y R6 es CHCH3 - R7, donde R7 es hidrógeno, hidroxio o sulfoniloxi o bien R6 es H, con un inhibidor de la dipeptidasa de la siguiente fórmula-02: **(Fórmula-02)** donde R2 y R3 son radicales hidrocarburo de 3 a 10 y 1 a 15 átomos de carbono respectivamente; en cualquiera de estas cadenas hidrocarbonadas R2 o R3, de 1 a 6 átomos de hidrógeno pueden haber sido sustituidos por halógenos o un grupo metileno no terminal puede haber sustituido por oxígeno o azufre, incluidas las formas oxidadas de este último, además, un hidrógeno terminal de R3 también puede haber sido sustituido por un grupo hidroxilo o tiol que puede estar acilado o carbamoilado; o el hidrógeno puede haber sido sustituido por un grupo amino, que puede estar derivatizado como en un grupo acilamino, ureido, amidino, guanidino, alquil-amino o amino sustituido, incluídos los agrupamientos de nitrógeno cuaternario; o alternativamente, puede estar sustituido por grupos ácido como ácido carboxílico, fosfónico o sulfónico o ésteres o amidas de los mismos, así como ciano; o combinaciones de los mismos, tal como un agrupamiento aminoácido terminal y R1 es hidrógeno o (alquil inferior C1- 6)aminoalquilo o dialquilaminoalquilo o un catión farmacéuticamente aceptable, estando comprendida la relación del compuesto del tipo de tienamicina a inhibidor de dipeptidasa entre 1:3 y 30:1 aproximadamente, b) mezclar la combinación resultante de la etapa anterior con un vehículo farmacéutico, opcionalmente adaptado para inyección.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92721378A | 1978-07-24 | 1978-07-24 | |
| US5023279A | 1979-06-22 | 1979-06-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES482774A1 true ES482774A1 (es) | 1980-09-01 |
Family
ID=26728043
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES482774A Expired ES482774A1 (es) | 1978-07-24 | 1979-07-23 | Un procedimiento para preparar una nueva composicion anti- bacteriana potenciada. |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP0007614B1 (es) |
| AR (1) | AR244550A1 (es) |
| AU (1) | AU529315B2 (es) |
| CA (1) | CA1136549A (es) |
| CZ (1) | CZ280583B6 (es) |
| DD (1) | DD145059A5 (es) |
| DE (1) | DE2964609D1 (es) |
| EG (1) | EG14367A (es) |
| ES (1) | ES482774A1 (es) |
| FI (1) | FI792282A (es) |
| GR (1) | GR69997B (es) |
| HK (1) | HK23286A (es) |
| HU (1) | HU182973B (es) |
| IE (1) | IE51691B1 (es) |
| IL (1) | IL57798A (es) |
| NZ (1) | NZ190993A (es) |
| PH (1) | PH16620A (es) |
| PT (1) | PT69955B (es) |
| SK (1) | SK278357B6 (es) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4880793A (en) * | 1978-07-24 | 1989-11-14 | Merck & Co., Inc. | Combination of thienamycin-type antibiotics with dipeptidase inhibitors |
| US5071843A (en) * | 1978-07-24 | 1991-12-10 | Merck & Co., Inc. | Combination of 2-substituted carbapenems with dipeptidase inhibitors |
| GR70784B (es) * | 1979-11-02 | 1983-03-23 | Merck & Co Inc | |
| PT73640B (en) * | 1980-09-17 | 1983-10-19 | Merck & Co Inc | Process for preparing chemical compounds selectively inhibit the metabolism of dipeptidase |
| DE3173503D1 (en) * | 1980-09-17 | 1986-02-27 | Merck & Co Inc | Antibacterial composition of thienamycin type compound and a dipeptidase inhibitor |
| DE48301T1 (de) * | 1980-09-24 | 1983-01-20 | Merck & Co., Inc., 07065 Rahway, N.J. | 2-(cyclopropancarboxamido)-2-alkensaeuren, deren ester und salze und daraus bestehende bakterienhemmende zusammensetzungen mit einer verbindung des typs thienamycin. |
| NZ201471A (en) * | 1981-08-10 | 1985-09-13 | Merck & Co Inc | Antibacterial compositions containing penems and dipeptidase inhibitors |
| JPS6025952A (ja) * | 1983-07-20 | 1985-02-08 | Sumitomo Chem Co Ltd | 光学活性２，２−ジメチルシクロプロパン−１−カルボン酸誘導体の製造法 |
| DE3574674D1 (de) * | 1984-04-30 | 1990-01-18 | Merck & Co Inc | Mischung von 2-substituierten carbapenemen mit dipeptidase-inhibitoren. |
| CA1273012A (en) * | 1984-07-02 | 1990-08-21 | Burton G. Christensen | 1-methylcarbapenems having an externally alkylated mono- of bicyclic 2-quarternary heteroarylalkylthio substituent |
| IE851586L (en) * | 1984-07-02 | 1986-01-02 | Interchem Internat S A | I methylcarbapenems having a 2-quaternary¹heteroarylalkylthio substituent |
| CA1273011A (en) * | 1984-07-02 | 1990-08-21 | Susan M. Schmitt | Carbapenems having an externally alkylated mono- or bicyclic 2-quaternary heteroarylalkylthio substituent |
| DK165665C (da) * | 1984-10-15 | 1993-06-14 | Sankyo Co | Laegemiddel indeholdende et penem- eller carbapenemantibiotikum og et aminosyrederviat |
| US4680292A (en) * | 1984-12-13 | 1987-07-14 | Merck & Co., Inc. | Carbapenems and 1-methylcarbapenems having a 2-heteroaryliumaliphatic substituent |
| US4739113A (en) * | 1986-05-30 | 1988-04-19 | Merck & Co., Inc. | Bis(cyclopropanecarboxamido)alkadienedioic acids as renal dipeptidase inhibitors |
| EP0464900A3 (en) | 1990-06-26 | 1992-07-22 | Merck & Co. Inc. | 2-biphenyl-carbapenems |
| CA2052730A1 (en) | 1990-10-11 | 1992-04-12 | Frank P. Dininno | 2-(substituted-dibenzofuranyl and dibenzothienyl) carbapenem antibacterial agents |
| EP1161947B1 (en) * | 1991-02-01 | 2005-06-08 | Daiichi Suntory Pharma Co., Ltd. | Oral antibacterial compositions and method for the improvement of gastrointestinal absorption of penem or carbapenem antibiotics |
| US6297231B1 (en) | 1996-10-28 | 2001-10-02 | Merck & Co., Inc. | Stabilized carbapenem antibiotic compositions and method of making |
| US6255300B1 (en) | 1997-09-09 | 2001-07-03 | Merck & Co., Inc. | Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment |
| US6277843B1 (en) | 1997-09-17 | 2001-08-21 | Merck & Co., Inc. | Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment |
| US6271222B1 (en) | 1998-05-28 | 2001-08-07 | Merck & Co., Inc. | Penem antibacterial compounds, compositions and methods of treatment |
| US6288054B1 (en) | 1998-06-02 | 2001-09-11 | Merck & Co., Inc. | Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment |
| US6310055B2 (en) | 1998-06-02 | 2001-10-30 | Merck & Co., Inc. | Halophenoxy substituted carbapenem antibacterial compounds |
| US6284753B2 (en) | 1998-06-02 | 2001-09-04 | Merck & Co., Inc. | Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment |
| CA2335497A1 (en) | 1998-06-25 | 1999-12-29 | Merck & Co., Inc. | Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment |
| JP2002518497A (ja) | 1998-06-25 | 2002-06-25 | メルク エンド カムパニー インコーポレーテッド | （複素環）メチル置換カルバペネムカルバペネム抗細菌物質 |
| US6346526B1 (en) | 1998-06-25 | 2002-02-12 | Merck & Co., Inc. | Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment |
| EP1089730A4 (en) | 1998-06-25 | 2001-10-24 | Merck & Co Inc | CARBAPENEM-BASED ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SAME, AND THERAPEUTIC METHODS |
| JP2002518496A (ja) | 1998-06-25 | 2002-06-25 | メルク エンド カムパニー インコーポレーテッド | （複素環）メチル置換カルバペネムカルバペネム抗細菌物質 |
| US6316488B1 (en) | 1999-06-17 | 2001-11-13 | Merck & Co., Inc. | Antibiotic compound |
| US6221859B1 (en) | 1999-08-27 | 2001-04-24 | Merck & Co., Inc. | Carbapenem antibacterial compositions and methods of the treatment |
| WO2012104793A1 (en) * | 2011-02-02 | 2012-08-09 | Indian Council Of Medical Research | An antibacterial and antiviral compound |
| EP2723737A1 (en) | 2011-06-27 | 2014-04-30 | Kyorin Pharmaceutical Co., Ltd. | Bridged bicyclic compounds for the treatment of bacterial infections |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2272684A1 (en) * | 1975-01-07 | 1975-12-26 | Ito Shojiro | Antibiotic-unsaturated acid compsns. - having a synergistic effect against gram positive and negative bacteria |
-
1979
- 1979-07-04 AR AR79277427A patent/AR244550A1/es active
- 1979-07-12 NZ NZ190993A patent/NZ190993A/xx unknown
- 1979-07-12 PH PH22771A patent/PH16620A/en unknown
- 1979-07-13 IL IL57798A patent/IL57798A/xx unknown
- 1979-07-16 AU AU48932/79A patent/AU529315B2/en not_active Expired
- 1979-07-20 GR GR59656A patent/GR69997B/el unknown
- 1979-07-20 FI FI792282A patent/FI792282A/fi not_active Application Discontinuation
- 1979-07-20 CA CA000332316A patent/CA1136549A/en not_active Expired
- 1979-07-20 HU HU79ME2286A patent/HU182973B/hu unknown
- 1979-07-20 PT PT69955A patent/PT69955B/pt unknown
- 1979-07-23 SK SK5137-79A patent/SK278357B6/sk unknown
- 1979-07-23 ES ES482774A patent/ES482774A1/es not_active Expired
- 1979-07-23 CZ CS795137A patent/CZ280583B6/cs unknown
- 1979-07-24 EP EP79102615A patent/EP0007614B1/en not_active Expired
- 1979-07-24 DE DE7979102615T patent/DE2964609D1/de not_active Expired
- 1979-07-24 DD DD79214580A patent/DD145059A5/de unknown
- 1979-07-24 EG EG443/79A patent/EG14367A/xx active
- 1979-08-08 IE IE1388/79A patent/IE51691B1/en not_active IP Right Cessation
-
1986
- 1986-04-03 HK HK232/86A patent/HK23286A/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| EG14367A (en) | 1984-09-30 |
| EP0007614B1 (en) | 1983-01-26 |
| NZ190993A (en) | 1981-10-19 |
| AU4893279A (en) | 1980-01-31 |
| PT69955B (pt) | 1981-06-11 |
| DD145059A5 (de) | 1980-11-19 |
| IE51691B1 (en) | 1987-02-18 |
| EP0007614A1 (en) | 1980-02-06 |
| AU529315B2 (en) | 1983-06-02 |
| SK513779A3 (en) | 1997-01-08 |
| FI792282A (fi) | 1980-01-25 |
| CA1136549A (en) | 1982-11-30 |
| GR69997B (es) | 1982-07-23 |
| CZ280583B6 (cs) | 1996-02-14 |
| IL57798A0 (en) | 1979-11-30 |
| IL57798A (en) | 1986-11-30 |
| DE2964609D1 (en) | 1983-03-03 |
| PH16620A (en) | 1983-11-28 |
| PT69955A (en) | 1979-08-01 |
| CZ513779A3 (en) | 1995-10-18 |
| AR244550A1 (es) | 1993-11-30 |
| IE791388L (en) | 1980-01-24 |
| HK23286A (en) | 1986-04-11 |
| SK278357B6 (en) | 1997-01-08 |
| HU182973B (en) | 1984-03-28 |
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