IE40523B1 - Novel benzylpyrimidines - Google Patents
Novel benzylpyrimidinesInfo
- Publication number
- IE40523B1 IE40523B1 IE1870/74A IE187074A IE40523B1 IE 40523 B1 IE40523 B1 IE 40523B1 IE 1870/74 A IE1870/74 A IE 1870/74A IE 187074 A IE187074 A IE 187074A IE 40523 B1 IE40523 B1 IE 40523B1
- Authority
- IE
- Ireland
- Prior art keywords
- sulphanilamido
- sulphonamides
- nhr
- sept
- pyrimidine
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
- C07D207/327—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
- C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Pharmacology & Pharmacy (AREA)
- Communicable Diseases (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
1484481 Compositions containing benzylpyrimidines F HOFFMANN-LA ROCHE & CO AG 11 Sept 1974 [12 Sept 1973] 39617/74 Heading A5B [Also in Division C2] An antibacterial composition contains a benzylpyrimidine of the formula: wherein R<SP>1</SP> and R<SP>2</SP> are (C 1 -C 3 ) alkyl or alkoxy, or (C 2 or C 3 ) alkenyl or alkenyloxy; Z is NO 2 , NH 2 , pyrrolo, pyrrolidino, piperidino, NHR<SP>4</SP>, -N(R<SP>4</SP>) 2 , -NHR<SP>5</SP>, -NR<SP>4</SP>R<SP>5</SP>, -NR<SP>4</SP>COOR<SP>4</SP>, -NHCOOR<SP>4</SP>, -NHCONHR<SP>3</SP>, -NHCSNHR<SP>3</SP>, -N 3 , -N=N-N(R<SP>4</SP>) 2 or -N(NO)R<SP>4</SP>, R<SP>3</SP> is H, (C 1 -C 3 ) alkyl or (C 2 -C 3 ) alkenyl and R<SP>5</SP> is acyl, and salts thereof; in association with a compatible pharmaceutical carrier. Compounds of the above formula inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulphonamides with which they may be combined. Specified sulphonamides are sulphisoxazole, sulphadimethoxine, sulphamethoxazole, 4-sulphanilamido-5, 6-dimethoxy-pyrimidine, 2-sulphanilamido-4, 5- dimethyl-pyrimidine, sulphaquinoxaline, sulphadiazine sulphamonomethoxine and 2-sulphanilamido-4, 5-dimethylisoxazole. Other inhibitors for enzymes involved in the folic acid biosynthesis may also be incorporated in the compositions. They may be applied orally, rectally or parenterally.
[GB1484481A]
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IE1983/77A IE40525B1 (en) | 1973-09-12 | 1974-09-09 | Hydrocinnamic acid nitriles |
| IE1982/77A IE40524B1 (en) | 1973-09-12 | 1974-09-09 | -cyano-hydrocinnamaldehyde acetals |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH1305773A CH591456A5 (en) | 1973-09-12 | 1973-09-12 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IE40523L IE40523L (en) | 1975-03-12 |
| IE40523B1 true IE40523B1 (en) | 1979-06-20 |
Family
ID=4388903
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IE1870/74A IE40523B1 (en) | 1973-09-12 | 1974-09-09 | Novel benzylpyrimidines |
Country Status (28)
| Country | Link |
|---|---|
| JP (1) | JPS6042238B2 (en) |
| AR (2) | AR207764A1 (en) |
| AT (1) | AT338797B (en) |
| BE (1) | BE819773A (en) |
| BR (1) | BR7407614D0 (en) |
| CA (1) | CA1037476A (en) |
| CH (1) | CH591456A5 (en) |
| CU (1) | CU34115A (en) |
| DD (2) | DD122785A5 (en) |
| DE (1) | DE2443682C2 (en) |
| DK (1) | DK135683B (en) |
| ES (7) | ES429949A1 (en) |
| FI (1) | FI58638C (en) |
| FR (1) | FR2242984B1 (en) |
| GB (3) | GB1484481A (en) |
| HK (1) | HK181A (en) |
| HU (1) | HU170427B (en) |
| IE (1) | IE40523B1 (en) |
| IL (1) | IL45510A (en) |
| LU (1) | LU70878A1 (en) |
| NL (1) | NL155827B (en) |
| NO (1) | NO140858C (en) |
| PH (1) | PH10643A (en) |
| PL (2) | PL99159B1 (en) |
| SE (1) | SE419443B (en) |
| SU (3) | SU577987A3 (en) |
| YU (3) | YU217874A (en) |
| ZA (1) | ZA745317B (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4515948A (en) * | 1973-09-12 | 1985-05-07 | Hoffmann-La Roche Inc. | 2,4-Diamino-5-(4-amino and 4-dimethylamino-3,5-dimethoxy benzyl)pyrimidines |
| JPS5481278A (en) * | 1977-10-18 | 1979-06-28 | Wellcome Found | Manufacture of triiseccaminomethane |
| CH639273A5 (en) * | 1978-09-12 | 1983-11-15 | Hoffmann La Roche | DIURETIC MEANS. |
| DE3250132C2 (en) * | 1981-11-09 | 1997-01-16 | Mallinckrodt Veterinary Inc | 2,4-Di:amino-5-benzyl-pyrimidine derivs. prepn. |
| FR2516081B1 (en) * | 1981-11-09 | 1987-05-29 | Wellcome Found | SYNTHESIS OF BENZYLPYRIMIDINES AND INTERMEDIATES FOR THE SYNTHESIS |
| GB2180836A (en) * | 1985-09-27 | 1987-04-08 | William James Stephen Barker | Sunscreen |
| JPH0431685Y2 (en) * | 1987-06-01 | 1992-07-30 | ||
| US4900859A (en) * | 1987-12-03 | 1990-02-13 | Hoffman-La Roche Inc. | Process for 4-dimethylamino-3,5-dimethoxybenzaldehyde |
| CA1300166C (en) * | 1987-12-03 | 1992-05-05 | Alfredo Guerrato | Process for the preparation of a benzoic acid ester |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1103931B (en) * | 1957-02-21 | 1961-04-06 | Wellcome Found | Process for the preparation of 2,4-diamino-5-benzylpyrimidine derivatives |
| US3485840A (en) * | 1964-11-12 | 1969-12-23 | Hoffmann La Roche | 2,4-diamino - 5 - (2',4',5'-substituted benzyl) pyrimidines,intermediates and processes |
-
1973
- 1973-09-12 CH CH1305773A patent/CH591456A5/xx not_active IP Right Cessation
-
1974
- 1974-01-01 AR AR255569A patent/AR207764A1/en active
- 1974-08-06 YU YU02178/74A patent/YU217874A/en unknown
- 1974-08-19 ZA ZA00745317A patent/ZA745317B/en unknown
- 1974-08-21 IL IL45510A patent/IL45510A/en unknown
- 1974-08-21 CA CA207,509A patent/CA1037476A/en not_active Expired
- 1974-09-02 FI FI2561/74A patent/FI58638C/en active
- 1974-09-03 NL NL7411685.A patent/NL155827B/en not_active IP Right Cessation
- 1974-09-04 DK DK468374AA patent/DK135683B/en unknown
- 1974-09-06 PL PL1974195308A patent/PL99159B1/en unknown
- 1974-09-06 PL PL1974173909A patent/PL97757B1/en unknown
- 1974-09-09 SE SE7411382A patent/SE419443B/en unknown
- 1974-09-09 IE IE1870/74A patent/IE40523B1/en unknown
- 1974-09-09 PH PH16253A patent/PH10643A/en unknown
- 1974-09-10 DD DD190238A patent/DD122785A5/xx unknown
- 1974-09-10 JP JP49103536A patent/JPS6042238B2/en not_active Expired
- 1974-09-10 FR FR7430568A patent/FR2242984B1/fr not_active Expired
- 1974-09-10 DD DD181015A patent/DD116824A5/xx unknown
- 1974-09-10 LU LU70878A patent/LU70878A1/xx unknown
- 1974-09-11 ES ES429949A patent/ES429949A1/en not_active Expired
- 1974-09-11 NO NO743271A patent/NO140858C/en unknown
- 1974-09-11 GB GB39617/74A patent/GB1484481A/en not_active Expired
- 1974-09-11 SU SU7402058406A patent/SU577987A3/en active
- 1974-09-11 HU HUHO1718A patent/HU170427B/hu not_active IP Right Cessation
- 1974-09-11 AT AT735174A patent/AT338797B/en not_active IP Right Cessation
- 1974-09-11 BE BE148396A patent/BE819773A/en not_active IP Right Cessation
- 1974-09-11 GB GB47894/76A patent/GB1484483A/en not_active Expired
- 1974-09-11 CU CU34115A patent/CU34115A/en unknown
- 1974-09-11 GB GB47893/76A patent/GB1484482A/en not_active Expired
- 1974-09-12 BR BR7614/74A patent/BR7407614D0/en unknown
- 1974-09-12 DE DE2443682A patent/DE2443682C2/en not_active Expired
-
1975
- 1975-04-25 ES ES437007A patent/ES437007A1/en not_active Expired
- 1975-04-25 ES ES437013A patent/ES437013A1/en not_active Expired
- 1975-04-25 ES ES437012A patent/ES437012A1/en not_active Expired
- 1975-04-25 ES ES437011A patent/ES437011A1/en not_active Expired
- 1975-04-25 ES ES437009A patent/ES437009A1/en not_active Expired
- 1975-04-25 ES ES437008A patent/ES437008A1/en not_active Expired
- 1975-06-20 SU SU7502145932A patent/SU571189A3/en active
- 1975-06-20 SU SU752145937A patent/SU609465A3/en active
- 1975-06-30 AR AR259408A patent/AR211387Q/en unknown
-
1980
- 1980-11-27 YU YU3015/80A patent/YU37153B/en unknown
- 1980-11-27 YU YU3016/80A patent/YU37154B/en unknown
-
1981
- 1981-01-08 HK HK1/81A patent/HK181A/en unknown
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