BR0112225A - Compound, pharmaceutical composition, use of a compound, and process for preparing a compound - Google Patents

Compound, pharmaceutical composition, use of a compound, and process for preparing a compound

Info

Publication number
BR0112225A
BR0112225A BR0112225-8A BR0112225A BR0112225A BR 0112225 A BR0112225 A BR 0112225A BR 0112225 A BR0112225 A BR 0112225A BR 0112225 A BR0112225 A BR 0112225A
Authority
BR
Brazil
Prior art keywords
compound
alkyl
amino
alkoxy
hydrogen
Prior art date
Application number
BR0112225-8A
Other languages
Portuguese (pt)
Inventor
Jean Claude Arnoud
Original Assignee
Angiogene Pharm Ltd
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 Angiogene Pharm Ltd filed Critical Angiogene Pharm Ltd
Publication of BR0112225A publication Critical patent/BR0112225A/en

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Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D295/08—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 singly bound oxygen or sulfur atoms
    • C07D295/084—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • 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 System
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/091—Esters of phosphoric acids with hydroxyalkyl compounds with further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/30—Ortho- or ortho- and peri-condensed systems containing three rings containing seven-membered rings
    • C07C2603/32—Dibenzocycloheptenes; Hydrogenated dibenzocycloheptenes

Abstract

"COMPOSTO, COMPOSIçãO FARMACêUTICA USO DE UM COMPOSTO, E, PROCESSO PARA PREPARAR UM COMPOSTO". A invenção refere-se a derivados de colquinol da fórmula (I): em que R^ 1^, R^ 2^ e R^ 3^ são cada qual independentemente hidróxi, fosforilóxi (-OPO~ 3~H~ 2~), alcóxi C~ 1-4~ ou um éster hidrolisável in vivo de hidróxi, com a condição de que pelo menos 2 de R^ 1^, R^ 2^ e R^ 3^ sejam alcóxi C~ 1-4~; A é <sym>CO-, -C(O)O-, -CON(R^ 8^)- (em que R^ 8^ é hidrogênio, alquila C~ 1-4~ alcóxi C~ 1-3 alquila C~ 1-3~, aminoalquila C~ 1-3~, ou hidroxialquila C~ 1-3~); a é um inteiro de 1 a 4 inclusive; R^ a^R^ B^ são independentemente selecionados a partir de hidrogênio, hidróxi e amino: B é <sym>O-, -CO-, N(R^ 9^)CO-, -CON(R^ 9^)-, -N(R^ 9^)C(O)O-, -N (R^ 9^)CON(R^ 10^)-, -N(R^9 ^~)SO~ 2~-, -SO~ 2~N(R^ 9^) ou uma ligação única direta (em que R^ 9^ e R^ 10^ são independentemente selecionados a partir de hidrogênio, alquila C~ 1-4~, alcóxi C~ 1-3~ alquila C~ 1-3~, aminoalquila C~ 1-3~ e hidroxialquila C~ 1-3~); b é O ou um inteiro de 1 a 4 inclusive, (contanto que quando O for bis, B seja uma ligação direta); D é carbóxi, sulfo, tetrazolila, imidazolila, fosforilóxi, hidrorxi, amino, N-(alquil C~ 1-4~)amino, N,N-di(alquil C~ 1-3~)amino ou da fórmula Y^ 1^(CH~ 2~)~ 0~ R^ 11^ ou <sym>NHCH (R^ 12^)COOH; [ em que Y^ 1^ é uma ligação única direta, -0-, C(O)-, -N(R^ 13^)- ou <sym>C(O)N(R^ 13^)- (em que R^ 13^ é hidrogênio, alquila C,-4, alcóxi C~ 1-3~, alquila C~ 2-3~, aminoalquila C~ 2-3~ ou hidroxialquila C~ 2-3~); e é O ou um inteiro de 1 a 4 inclusive."COMPOUND, PHARMACEUTICAL COMPOSITION USE OF A COMPOUND, AND PROCESS TO PREPARE A COMPOUND". The invention relates to cholquinol derivatives of formula (I): wherein R 1, R 2, R 2 and R 3 are each independently hydroxy, phosphoryloxy (-OPO-3-H-2), C 1-4 alkoxy or an in vivo hydrolysable hydroxy ester, provided that at least 2 of R 4, R 2 and R 3 are C 1-4 alkoxy; A is <sym> CO-, -C (O) O-, -CON (R 8 R 8) - (wherein R 8 R 8 is hydrogen, C 1-4 alkyl-C 1-3 alkoxyC 1-3C, C 1-3 aminoalkyl, or C 1-3 hydroxyalkyl); a is an integer from 1 to 4 inclusive; R 2a 2 R 4 B 4 are independently selected from hydrogen, hydroxy and amino: B is <sym> O-, -CO-, N (R 9 9) CO-, -CON (R 9 9) -, -N (R ^ 9 ^) C (O) O-, -N (R ^ 9 ^) CON (R ^ 10 ^) -, -N (R ^ 9 ^) SO-2 ~ -, - SO ~ 2 ~ N (R ^ 9 ^) or a single direct bond (wherein R ^ 9 ^ and R ^ 10 ^ are independently selected from hydrogen, C 1-4 alkyl, C 1-3 alkoxy C 1-3 alkyl, C 1-3 aminoalkyl and C 1-3 hydroxyalkyl); b is O or an integer from 1 to 4 inclusive, (provided that when O is bis, B is a direct bond); D is carboxy, sulfo, tetrazolyl, imidazolyl, phosphoryloxy, hydroxy, amino, N- (C 1-4 alkyl) amino, N, N-di (C 1-3 alkyl) amino or of formula Y 1 (CH ~ 2 ~) ~ O ~ R ^ 11 ^ or NHS (R ^ 12 ^) COOH; [wherein Y ^ 1 ^ is a direct single bond, -0-, C (O) -, -N (R ^ 13 ^) - or <sym> C (O) N (R ^ 13 ^) - (in wherein R 13 is hydrogen, C 1-4 alkyl, C 1-3 alkoxy, C 2-3 alkyl, C 2-3 amino amino or C 2-3 hydroxyalkyl); and is O or an integer from 1 to 4 inclusive.

BR0112225-8A 2000-07-07 2001-07-04 Compound, pharmaceutical composition, use of a compound, and process for preparing a compound BR0112225A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP00401977 2000-07-07
EP00401976 2000-07-07
PCT/GB2001/002964 WO2002008213A1 (en) 2000-07-07 2001-07-04 Colchinol derivatives as angiogenesis inhibitors

Publications (1)

Publication Number Publication Date
BR0112225A true BR0112225A (en) 2003-05-06

Family

ID=26073520

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0112225-8A BR0112225A (en) 2000-07-07 2001-07-04 Compound, pharmaceutical composition, use of a compound, and process for preparing a compound

Country Status (19)

Country Link
EP (1) EP1301498A1 (en)
JP (1) JP2004504391A (en)
KR (1) KR20030022264A (en)
CN (1) CN1255392C (en)
AU (2) AU6623201A (en)
BR (1) BR0112225A (en)
CA (1) CA2410562A1 (en)
CZ (1) CZ200331A3 (en)
EE (1) EE200300015A (en)
HU (1) HUP0301742A3 (en)
IL (1) IL153325A0 (en)
IS (1) IS6668A (en)
MX (1) MXPA02012903A (en)
NO (1) NO20030055D0 (en)
NZ (1) NZ522661A (en)
PL (1) PL359181A1 (en)
RU (1) RU2003103603A (en)
SK (1) SK52003A3 (en)
WO (1) WO2002008213A1 (en)

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