BR9810321A - Derivados de piridazina de tiadiazolila de inibição de angiogênese - Google Patents

Derivados de piridazina de tiadiazolila de inibição de angiogênese

Info

Publication number
BR9810321A
BR9810321A BR9810321-0A BR9810321A BR9810321A BR 9810321 A BR9810321 A BR 9810321A BR 9810321 A BR9810321 A BR 9810321A BR 9810321 A BR9810321 A BR 9810321A
Authority
BR
Brazil
Prior art keywords
alk
alkyl
hydrogen
het
formula
Prior art date
Application number
BR9810321-0A
Other languages
English (en)
Inventor
Raymond Antoine Stokbroekx
Marc Andre Ceusters
Marcel Jozef Maria Van Der Aa
Marcel Gerebernusmaria Luycky
Marc Willems
Robert W Tuman
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR9810321A publication Critical patent/BR9810321A/pt

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433Thidiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/83Thioacids; Thioesters; Thioamides; Thioimides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/081,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/14Heterocyclic 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
    • C07D295/155Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Lubricants (AREA)
  • Paper (AREA)
  • Investigating Or Analyzing Materials By The Use Of Fluid Adsorption Or Reactions (AREA)

Abstract

Patente de Invenção: <B>"DERIVADOS DE PIRIDAZINA DE TIADIAZOLILA DE INIBIçãO DE ANGIOGêNESE"<D>. Esta invenção concerne os compostos de fórmula (I), as formas de N-óxido, os sais de adição de ácido farmaceuticamente aceitáveis e as suas formas esterioquimicamente isoméricas, onde R^ 1^ é hidrogênio, C~ 1-6~ alquila, C~ 1-6~ alquilóxi, C~ 1-6~ alquiltio, amino, mono- ou di(C~ 1-6~alquil)amino, Ar^ 1^, Ar^ 1^-NH-, C~ 3-6~ cicloalquila, hidroximetila ou benziloximetila; R^ 2^ e R^ 3^ são hidrogênio, ou tomados juntos podem formar um radical bivalente de fórmula -CH=CH-CH=CH-; R^ 4^, R^ 5^ e R^ 6^ são cada qual independentemente selecionados de hidrogênio, halo, C~ 1-6~alquila, C~ 1-6~alquilóxi, trifluorometila, nitro, amino, ciano, azido, C~ 1-6~ alquilóxiC~ 1-6~ alquila, C~ 1-6~ alquiltio, C~ 1-6~ alquiloxicarbonila ou Het^ 1^; ou quando R^ 4^ e R^ 5^ são adjacentes entre si eles podem ser tomados juntos para formar um radical de fórmula -CH=CH-CH=CH-; A é um radical bivalente de fórmula NR^ 7^-Alk^ 1^ -X-, NR^ 7^-Alk^ 1^-X-Alk^ 2^-, O-Alk^ 1^-X-, O-Alk^ 1^-X-Alk^ 2^ ou S-Alk^ 1^-X-; onde X é uma ligação direta, -O-, -S-, C=O, -NR^ 8^- ou Het^ 2^; R^ 7^ é hidrogênio, C~ 1-6~ alquila, ou Ar^ 2^ metila; R^ 8^ é hidrogênio, C~ 1-6~alquila, ou Ar^ 2^ metila; Alk^ 1^ é C~ 1-6~alcanodiila; Alk^ 2^ é C~ 1-4~alcanodiila; Ar^ 1^ e Ar^ 2^ são fenila opcionalmente substituída; fenila; Het^ 1^ e Het^ 2^ são heterociclos opcionalmente substituídos; tendo atividade de inibição de angiogênese; suas preparações, composições contendo-as e seus usos como um medicamento.
BR9810321-0A 1997-06-24 1998-06-22 Derivados de piridazina de tiadiazolila de inibição de angiogênese BR9810321A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP97201930 1997-06-24
US5219497P 1997-07-10 1997-07-10
PCT/EP1998/004021 WO1998058929A1 (en) 1997-06-24 1998-06-22 Angiogenesis inhibiting thiadiazolyl pyridazine derivatives

Publications (1)

Publication Number Publication Date
BR9810321A true BR9810321A (pt) 2000-09-05

Family

ID=8228477

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9810321-0A BR9810321A (pt) 1997-06-24 1998-06-22 Derivados de piridazina de tiadiazolila de inibição de angiogênese

Country Status (24)

Country Link
EP (1) EP0991649B1 (pt)
JP (1) JP2002512630A (pt)
CN (1) CN1198822C (pt)
AT (1) ATE235489T1 (pt)
AU (1) AU732129B2 (pt)
BR (1) BR9810321A (pt)
CA (1) CA2294551A1 (pt)
CZ (1) CZ296000B6 (pt)
DE (1) DE69812623T2 (pt)
DK (1) DK0991649T3 (pt)
EE (1) EE03828B1 (pt)
ES (1) ES2195374T3 (pt)
HU (1) HU225154B1 (pt)
ID (1) ID23443A (pt)
IL (1) IL133652A (pt)
MY (1) MY120046A (pt)
NZ (1) NZ501649A (pt)
PL (1) PL191409B1 (pt)
PT (1) PT991649E (pt)
RU (1) RU2194049C2 (pt)
SK (1) SK283705B6 (pt)
TR (1) TR199902955T2 (pt)
WO (1) WO1998058929A1 (pt)
ZA (1) ZA985467B (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6689883B1 (en) 1999-09-28 2004-02-10 Bayer Pharmaceuticals Corporation Substituted pyridines and pyridazines with angiogenesis inhibiting activity
US7977333B2 (en) 2000-04-20 2011-07-12 Bayer Healthcare Llc Substituted pyridines and pyridazines with angiogenesis inhibiting activity
US6903101B1 (en) 2000-08-10 2005-06-07 Bayer Pharmaceuticals Corporation Substituted pyridazines and fused pyridazines with angiogenesis inhibiting activity
EP2148878A4 (en) * 2007-04-20 2011-08-10 Merck Canada Inc NEW HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME-A-DELTA-9-DESATURASE
US9102669B2 (en) 2011-12-06 2015-08-11 Janssen Pharmaceutica Nv Substituted piperidinyl-pyridazinyl derivatives useful as SCD 1 inhibitors
US9238658B2 (en) 2011-12-06 2016-01-19 Janssen Pharmaceutica Nv Substituted piperidinyl-carboxamide derivatives useful as SCD 1 inhibitors
GB201309508D0 (en) * 2013-05-28 2013-07-10 Redx Pharma Ltd Compounds
GB201311953D0 (en) * 2013-07-03 2013-08-14 Redx Pharma Ltd Compounds

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6339868A (ja) * 1986-08-04 1988-02-20 Otsuka Pharmaceut Factory Inc ジ低級アルキルフエノ−ル誘導体
NZ326354A (en) * 1996-01-15 1999-05-28 Janssen Pharmaceutica Nv 3-(substituted-1-piperazinyl)-6-(substituted-1,2,4-thiadiazol-5 -yl)-pyridazine derivatives and medicaments

Also Published As

Publication number Publication date
IL133652A (en) 2003-04-10
SK176999A3 (en) 2000-09-12
DE69812623T2 (de) 2004-02-19
AU8853798A (en) 1999-01-04
IL133652A0 (en) 2001-04-30
JP2002512630A (ja) 2002-04-23
TR199902955T2 (xx) 2000-06-21
EP0991649B1 (en) 2003-03-26
NZ501649A (en) 2001-10-26
EP0991649A1 (en) 2000-04-12
ZA985467B (en) 1999-12-23
CZ450899A3 (cs) 2000-08-16
MY120046A (en) 2005-08-30
CN1198822C (zh) 2005-04-27
RU2194049C2 (ru) 2002-12-10
PT991649E (pt) 2003-08-29
ATE235489T1 (de) 2003-04-15
DK0991649T3 (da) 2003-07-21
SK283705B6 (sk) 2003-12-02
CN1261364A (zh) 2000-07-26
AU732129B2 (en) 2001-04-12
DE69812623D1 (de) 2003-04-30
WO1998058929A1 (en) 1998-12-30
ID23443A (id) 2000-04-20
PL191409B1 (pl) 2006-05-31
HUP0004457A2 (hu) 2002-02-28
HU225154B1 (en) 2006-07-28
HUP0004457A3 (en) 2002-03-28
ES2195374T3 (es) 2003-12-01
EE9900591A (et) 2000-08-15
CZ296000B6 (cs) 2005-12-14
EE03828B1 (et) 2002-08-15
CA2294551A1 (en) 1998-12-30
PL337657A1 (en) 2000-08-28

Similar Documents

Publication Publication Date Title
NZ326354A (en) 3-(substituted-1-piperazinyl)-6-(substituted-1,2,4-thiadiazol-5 -yl)-pyridazine derivatives and medicaments
NO171980C (no) Analogifremgangsmaate for fremstilling av terapeutisk aktive pyridazinaminderivater
BR9810321A (pt) Derivados de piridazina de tiadiazolila de inibição de angiogênese
BR9811769A (pt) Tetraidro gama-carbolinas
AP9901578A0 (en) Sulfonylbenzene compounds as anti-inflammatory/analgesic agents.
BR9811678A (pt) Derivados de 6-azauracila de inibição de il-5
NZ332310A (en) Optionally condensed pyrimidine substituted hexahydro-pyrido[4,3-b]indole derivatives and medicaments
MY113446A (en) 1,3-dihydro-1-(phenylalkenyl)-2h-imidazol-2-one derivatives
ATE500231T1 (de) Hiv hemmende pyrimidin derivate
BR9810314A (pt) Derivados de 5-substituìdo-1,2,4-tiadiazolila que inibem de angiogênese
HK1032404A1 (en) 2,4,4-Trisubstituted-1,3-dioxolane antifungals.
IL90879A0 (en) 3-piperidinyl-indazole derivatives,their preparation and antihypertensive compositions containing them
BG105331A (en) BENZOTHIENO[3,4-c]PYRIDINES AS ALPHA2 ANTAGONISTS
ATE246680T1 (de) Spiroimidazolinderivate und ihre verwendung als alpha2-adrenorezeptor-antagonisten und monoamino- wiederaufnahme-blocker

Legal Events

Date Code Title Description
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements