GB871753A - New phthalazines and process for their manufacture - Google Patents
New phthalazines and process for their manufactureInfo
- Publication number
- GB871753A GB871753A GB14680/58A GB1468058A GB871753A GB 871753 A GB871753 A GB 871753A GB 14680/58 A GB14680/58 A GB 14680/58A GB 1468058 A GB1468058 A GB 1468058A GB 871753 A GB871753 A GB 871753A
- Authority
- GB
- United Kingdom
- Prior art keywords
- pyridyl
- methyl
- amino
- dihydrophthalazine
- phthalazine
- 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61J1/00—Containers specially adapted for medical or pharmaceutical purposes
- A61J1/05—Containers specially adapted for medical or pharmaceutical purposes for collecting, storing or administering blood, plasma or medical fluids ; Infusion or perfusion containers
- A61J1/06—Ampoules or carpules
- A61J1/067—Flexible ampoules, the contents of which are expelled by squeezing
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
- B65D—CONTAINERS FOR STORAGE OR TRANSPORT OF ARTICLES OR MATERIALS, e.g. BAGS, BARRELS, BOTTLES, BOXES, CANS, CARTONS, CRATES, DRUMS, JARS, TANKS, HOPPERS, FORWARDING CONTAINERS; ACCESSORIES, CLOSURES, OR FITTINGS THEREFOR; PACKAGING ELEMENTS; PACKAGES
- B65D75/00—Packages comprising articles or materials partially or wholly enclosed in strips, sheets, blanks, tubes, or webs of flexible sheet material, e.g. in folded wrappers
- B65D75/40—Packages formed by enclosing successive articles, or increments of material, in webs, e.g. folded or tubular webs, or by subdividing tubes filled with liquid, semi-liquid, or plastic materials
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Mechanical Engineering (AREA)
- Pharmacology & Pharmacy (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
The invention comprises 1-hydrazino-4-(pyridyl-methyl)-phthalazines and acid addition salts thereof, wherein the benzene nucleus may further contain as substituents lower alkyl, amino or lower alkanoylamino groups ("lower" indicating 1-6 carbon atoms in the group), and the preparation thereof by reacting an appropriate 1-chloro-4-(pyridyl-methyl)phthalazine with hydrazine, and optionally hydrolysing the alkanoylamino group to form the amino group. 1-Chloro-4-[pyridyl-(41)-methyl]-phthalazine is prepared by condensing phthalic anhydride with 4-methylpyridine to form g -pyrophthalone which is heated with hydrazine to give 1-oxo4-[pyridyl-(41)-methyl] - 1:2-dihydrophthalazine and the last named compound is treated with phosphorus oxychloride and ammonia. 1 - Chloro-4-[pyridyl-(21)-methyl]phthalazine is similarly prepared through a -pyrophthalone and 1-oxo-4-[pyridyl-(21)-methyl]-1:2dihydrophthalazine. 1-Chloro-4-[pyridyl-(41)-methyl] - 7 - acetylamino-1,2-dihydrophthalazine is prepared by reacting 5-nitro- -pyrophthalone (from 4-nitrophthalic anhydride and g -picoline) with hydrazine to form 1-oxo-4[pyridyl-(41)-methyl]-7-amino-1:2-dihydrophthalazine, reacting the phthalazone with acetic anhydride to form 1-oxo-4-[pyridyl-(41)-methyl] - 7 - acetylamino1,2-dihydrophthalazine and treating this with phosphorus oxychloride.ALSO:Pharmaceutical compositions comprise 1-hydrazino - 4 - (pyridyl - methyl) - phthalazines wherein the benzene nucleus is unsubstituted or substituted by amino, lower alkanoylamino or lower alkyl groups ("lower" indicating 1-6 carbon atoms in the said groups) and acid addition salts thereof, together with a pharmaceutical carrier suitable for enteral or parenteral administration. The compositions may be in the form of tablets, dragees, pearls, capsules or in liquid form; they may additionally contain auxiliary substances such as preserving, stabilizing, wetting or emulsifying agents, salts for regulating osmotic pressure or buffers, or other therapeutically valuable substances. Preferably they contain 0.5-45.0% of the active phthalazine. Specified salts are hydrohalides, sulphates, nitrates, phosphates, thiocyanates, acetates, propionates, oxalates, malonates, succinates, citrates, tartrates, malates, methane-, ethane-, hydroxyethane-, benzene- and toluene-sulphonates, and salts with amino-acids and therapeutically active acids.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CH871753X | 1957-05-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
GB871753A true GB871753A (en) | 1961-06-28 |
Family
ID=4544087
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
GB14680/58A Expired GB871753A (en) | 1957-05-07 | 1958-05-07 | New phthalazines and process for their manufacture |
Country Status (3)
Country | Link |
---|---|
BE (1) | BE567431A (en) |
DE (1) | DE1061788B (en) |
GB (1) | GB871753A (en) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6258812B1 (en) | 1997-02-13 | 2001-07-10 | Novartis Ag | Phthalazines with angiogenesis inhibiting activity |
WO2003014090A1 (en) * | 2001-08-07 | 2003-02-20 | Pharmacia Italia S.P.A. | Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them |
US6686347B2 (en) | 1999-03-30 | 2004-02-03 | Novartis Ag | Phthalazine derivatives for treating inflammatory diseases |
US7399761B2 (en) | 2001-05-04 | 2008-07-15 | Novartis Ag | Phthalazine derivatives with angiogenesis inhibiting activity |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE19963607B4 (en) * | 1999-12-23 | 2005-12-15 | Schering Ag | Process for the preparation of 4- (heteroaryl-methyl) halo-1 (2H) -phthalazinones |
EP2277595A3 (en) | 2004-06-24 | 2011-09-28 | Novartis Vaccines and Diagnostics, Inc. | Compounds for immunopotentiation |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE848818C (en) * | 1945-12-21 | 1952-09-08 | Ciba Geigy | Process for the preparation of new hydrazine compounds and their derivatives |
DE932128C (en) * | 1952-10-01 | 1955-08-25 | Cassella Farbwerke Mainkur Ag | Process for the preparation of dihydrazino compounds |
DE951992C (en) * | 1953-07-09 | 1956-11-08 | Cassella Farbwerke Mainkur Ag | Process for the preparation of new hydrazine derivatives |
-
0
- BE BE567431D patent/BE567431A/xx unknown
-
1958
- 1958-04-30 DE DEC16745A patent/DE1061788B/en active Pending
- 1958-05-07 GB GB14680/58A patent/GB871753A/en not_active Expired
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6258812B1 (en) | 1997-02-13 | 2001-07-10 | Novartis Ag | Phthalazines with angiogenesis inhibiting activity |
US6514974B2 (en) | 1997-02-13 | 2003-02-04 | Novartis Ag | Pyrido-, pyrimido-, pyridazo- and pyrazo- pyridazines having angiogenesis inhibiting activity |
US6686347B2 (en) | 1999-03-30 | 2004-02-03 | Novartis Ag | Phthalazine derivatives for treating inflammatory diseases |
US6911440B2 (en) | 1999-03-30 | 2005-06-28 | Novartis Ag | Phthalazine derivatives for treating inflammatory diseases |
US7329660B2 (en) | 1999-03-30 | 2008-02-12 | Novartis Ag | Phthalazine derivatives for treating inflammatory diseases |
US7399761B2 (en) | 2001-05-04 | 2008-07-15 | Novartis Ag | Phthalazine derivatives with angiogenesis inhibiting activity |
US8034814B2 (en) | 2001-05-04 | 2011-10-11 | Novartis Ag | Phthalazine derivatives with angiogenesis inhibiting activity |
WO2003014090A1 (en) * | 2001-08-07 | 2003-02-20 | Pharmacia Italia S.P.A. | Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them |
US7432263B2 (en) | 2001-08-07 | 2008-10-07 | Pfizer Italia, S.R.L. | Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them |
Also Published As
Publication number | Publication date |
---|---|
DE1061788B (en) | 1959-07-23 |
BE567431A (en) |
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