GB871753A - New phthalazines and process for their manufacture - Google Patents

New phthalazines and process for their manufacture

Info

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
Application number
GB14680/58A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
BASF Schweiz AG
Original Assignee
Ciba AG
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Ciba AG filed Critical Ciba AG
Publication of GB871753A publication Critical patent/GB871753A/en
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61JCONTAINERS 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
    • A61J1/00Containers specially adapted for medical or pharmaceutical purposes
    • A61J1/05Containers specially adapted for medical or pharmaceutical purposes for collecting, storing or administering blood, plasma or medical fluids ; Infusion or perfusion containers
    • A61J1/06Ampoules or carpules
    • A61J1/067Flexible ampoules, the contents of which are expelled by squeezing
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B65CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
    • B65DCONTAINERS 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
    • B65D75/00Packages comprising articles or materials partially or wholly enclosed in strips, sheets, blanks, tubes, or webs of flexible sheet material, e.g. in folded wrappers
    • B65D75/40Packages 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.
GB14680/58A 1957-05-07 1958-05-07 New phthalazines and process for their manufacture Expired GB871753A (en)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Cited By (9)

* Cited by examiner, † Cited by third party
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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