LV10951B - 4-quinolinyl derivatives with anti-helicobacter activity - Google Patents

4-quinolinyl derivatives with anti-helicobacter activity Download PDF

Info

Publication number
LV10951B
LV10951B LVP-95-143A LV950143A LV10951B LV 10951 B LV10951 B LV 10951B LV 950143 A LV950143 A LV 950143A LV 10951 B LV10951 B LV 10951B
Authority
LV
Latvia
Prior art keywords
formula
compounds
compound
vvas
acid
Prior art date
Application number
LVP-95-143A
Other languages
English (en)
Other versions
LV10951A (lv
Inventor
Marc Gaston Venet
Jerome Emiles Georges Guillemont
Daniel Franck Jean Vernier
Franck Christopher Odds
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 LV10951A publication Critical patent/LV10951A/lv
Publication of LV10951B publication Critical patent/LV10951B/en

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (4)

  1. LV 10951 PATENTA FORMULA 1. Savienojums ar formulu r'
    tā farmaceitiski saderīgs pievienotas skābes sāls, tā stereoķīmiska izomēra forma, tā kvaternizēta forma vai tā Ņ-oksids, kur -A- apzīmē divvērtīgu radikālu ar formulu -N=CH-CH=CH- (a), -CH=N-CH=CH- (b), -N=N-CH=CH- (c), -N=CH-N=CH- (d), -N=CH-CH=N- (e), -CH=N-N=CH- (f). -N=N-N=CH- (g). -N=N-CH=N- (h) vai -CH=CH-CH=CH- CO; R1, R1, R3, R4, R5, R6 un R7 katrs neatkarīgi apzīmē ūdeņradi, halogēnu, hidroksilgrupu, C,.4alkiloksigrupu, C,.4alkilgrupu, trifluor-metilgrupu, aminogrupu, mono- vai di-(C,.4alkil)aminogrupu vai nitrogrupu, nodrošinot, ka, ja viens aizvietotājs fenilgrupā ir nitrogrupa, tad otrs aizvietotājs minētajā fenilgrupā ir citāds, kā nitrogrupa. 1 Savienojums, saskaņā ar 1. punktu, kur
  2. 2 R' apzīmē ūdeņradi, C,.4alkilgrupu, hidroksilgrupu, C^alkil-oksigrupu, nitrogrupu, aminogrupu vai mono* vai di-(C,.4al-kil)aminogrupu; R2, R3 un R4 katrs neatkarīgi apzīmē ūdeņradi, halogēnu, trifluor-metilgrupu, hidroksilgrupu vai C,.4alkiloksigrupu; R5 apzīmē ūdeņradi, halogēnu, hidroksilgrupu vai C^alkil-oksigrupu; R6 un R1 katrs neatkarīgi apzīmē ūdeņradi, halogēnu, hidroksilgrupu, C,.4alkiloksigrupu vai trifluormetilgrupu.
  3. 3. Savienojums, saskaņā ar 2. punktu, kur R', R2, R3, R5 un R6 apzīmē ūdeņradi, un R4 un R1 katrs neatkarīgi apzīmē ūdeņradi vai halogēnu.
    4. Savienojums, saskaņā ar 3. punktu, kur -A- apzīmē divvērtīgu radikālu ar formulu -N=N-CH=CH- (c) vai -N=CH-N=CH- (d) un R4 ir 3-halogēns.
    5. Savienojums, saskaņā ar 4, punktu, kas ir izvēlēts no grupas, kas sastāv no 4-[(3-hlorfenil)(1H-1,2,4-triazol-1-il)metil]hinolīna, tā farmaceitiski saderīgiem pievienotas skābes sāļiem, tā stereoķīmisko izomēru formām, tā kvaternizētām formām un tā Ņ-oksidiem.
    6. Farmaceitisks sastāvs, kas kā aktīvo sastāvdaļu satur savienojuma, saskaņā ar jebkuru no 1. līdz 5. punktiem, terapeitiski efektīvu daudzumu un farmaceitiski saderīgu nesēju. 1 Farmaceitisks sastāvs, saskaņā ar 6. punktu, atšķirīgs ar to, ka tas bez tam satur terapeitiski efektīvu daudzumu protonu sūkņa inhibitora vai terapeitiski efektīvu daudzumu bismuta savienojuma, vai terapeitiski efektīvu daudzumu protonu sūkņa inhibitora un bismuta savienojuma kombinācijas. 3 LV 10951
    8. Metode sastāva, saskaņā ar 6. punktu, iegūšanai, atšķirīga ar to, ka aktīvā ingredienta terapeitiski efektīvu daudzumu rūpīgi samaisa ar farmaceitiski saderīgu nesēju.
    9. Savienojums, saskaņā ar 1. punktu, ko izmanto, kā medikamentu.
    10. Metode savienojuma, saskaņā ar jebkuru no 1. līdz 5. punktiem, iegūšanai, atšķirīga ar to, ka a) Ņ-alkilē azolu ar formulu (II) ar starpproduktu ar formulu (III) reakcijas apstākļos inertā šķīdinātājā,
    kur A un R1 - R7 ir, kā norādīts 1. punktā, un W ir reaģējoša atšķeļama grupa, b) liek reaģēt azolam ar formulu (II) ar starpproduktu ar formulu (IV) reakcijas apstākļos inertā šķīdinātājā un reaģenta klātbūtnē, kas transformē hidroksilgrupu starpproduktā (IV) vieglāk atšķeļamā grupā,
  4. 4 c) liek reaģēt starpproduktam ar formulu (V) ar reaģentu ar formulu (VI), kurā W' ir reaģējoša atšķeļama grupa, tā iegūstot savienojumu ar formulu (l-b), 4
    d) liek reaģēt starpproduktam ar formulu (VII) ar metānimidamidu vai tā atvasinājumu reakcijas apstākļos inertā šķīdinātājā, tā iegūstot savienojumu ar formulu (l-c), o
    nh=ch-nh2 N-NH
    un, ja nepieciešams, pārvērš savienojumus ar formulu (I) vienu otrai sekojošās praksē pazīstamās funkcionālo grupu transformēšanas reakcijās un, ja nepieciešams, pārvērš savienojumus ar formulu (I) terapeitiski aktīvā netoksiskā pievienotas skābes sālī, apstrādājot ar skābi, vai pretēji, pārvērš sāls formu brīvā bāzē, apstrādājot ar sārmu; un/vai gatavo to stereoķīmisko izomēru formas; un/vai gatavo to kvaternizētas formas; un/vai gatavo to Ņ-oksīdus.
LVP-95-143A 1992-10-27 1995-05-26 4-quinolinyl derivatives with anti-helicobacter activity LV10951B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US96700892A 1992-10-27 1992-10-27
US6980493A 1993-06-01 1993-06-01
PCT/EP1993/002884 WO1994010164A1 (en) 1992-10-27 1993-10-19 4-quinolinyl derivatives with anti-helicobacter activity

Publications (2)

Publication Number Publication Date
LV10951A LV10951A (lv) 1995-12-20
LV10951B true LV10951B (en) 1996-08-20

Family

ID=26750446

Family Applications (1)

Application Number Title Priority Date Filing Date
LVP-95-143A LV10951B (en) 1992-10-27 1995-05-26 4-quinolinyl derivatives with anti-helicobacter activity

Country Status (22)

Country Link
US (1) US5589484A (lv)
EP (1) EP0666855B1 (lv)
JP (1) JPH08502503A (lv)
KR (1) KR100239003B1 (lv)
AT (1) ATE143013T1 (lv)
AU (1) AU675087B2 (lv)
BG (1) BG99566A (lv)
CA (1) CA2146651A1 (lv)
CZ (1) CZ287159B6 (lv)
DE (1) DE69304930T2 (lv)
DK (1) DK0666855T3 (lv)
ES (1) ES2094567T3 (lv)
FI (1) FI951996A (lv)
GR (1) GR3021690T3 (lv)
HU (1) HUT71895A (lv)
LV (1) LV10951B (lv)
NO (1) NO951588L (lv)
NZ (1) NZ256871A (lv)
PL (1) PL175679B1 (lv)
RU (1) RU2130933C1 (lv)
SK (1) SK53495A3 (lv)
WO (1) WO1994010164A1 (lv)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1086094A1 (en) 1998-05-23 2001-03-28 Byk Gulden Lomberg Chemische Fabrik GmbH Quinoline-aminomethyl-pyridyl derivatives with anti-helicobacter activity
GB9819382D0 (en) * 1998-09-04 1998-10-28 Cerebrus Ltd Chemical compounds I
TW200803855A (en) * 2006-02-24 2008-01-16 Kalypsys Inc Quinolones useful as inducible nitric oxide synthase inhibitors
US8987315B2 (en) 2009-12-31 2015-03-24 Innocrin Pharmaceuticals, Inc. Metalloenzyme inhibitor compounds
US9302992B2 (en) 2013-04-02 2016-04-05 Annji Pharmaceutical Co., Ltd. Multifunctional quinoline derivatives as anti-neurodegenerative agents
EP2981525A4 (en) * 2013-04-02 2016-12-21 Annji Pharm Co Ltd MULTIFUNCTIONAL QUINOLINE DERIVATIVES AS ANTI-NEURODEGENERATIVE AGENTS
JP6254239B2 (ja) 2016-02-29 2017-12-27 大日精化工業株式会社 ポリマーの製造方法
JP6245719B1 (ja) 2017-03-24 2017-12-13 大日精化工業株式会社 ポリマーの製造方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8827820D0 (en) * 1988-11-29 1988-12-29 Janssen Pharmaceutica Nv (1h-azol-1-ylmethyl)substituted quinoline derivatives
US5185346A (en) * 1988-11-29 1993-02-09 Hanssen Pharmaceutica (1H-azol-1-ylmethyl)substituted quinoline derivatives
CA2002864C (en) * 1988-11-29 1999-11-16 Eddy J. E. Freyne (1h-azol-1-ylmethyl) substituted quinoline, quinazoline or quinoxaline derivatives
GB8827822D0 (en) * 1988-11-29 1988-12-29 Janssen Pharmaceutica Nv (1h-azol-1-ylmethyl)substituted quinoline derivatives

Also Published As

Publication number Publication date
EP0666855A1 (en) 1995-08-16
CZ83795A3 (en) 1995-09-13
PL308550A1 (en) 1995-08-21
NZ256871A (en) 1995-09-26
HU9501207D0 (en) 1995-06-28
ES2094567T3 (es) 1997-01-16
CZ287159B6 (en) 2000-10-11
NO951588D0 (no) 1995-04-26
FI951996A0 (fi) 1995-04-26
CA2146651A1 (en) 1994-05-11
HUT71895A (en) 1996-02-28
KR950704297A (ko) 1995-11-17
AU675087B2 (en) 1997-01-23
LV10951A (lv) 1995-12-20
RU95109440A (ru) 1997-03-10
GR3021690T3 (en) 1997-02-28
WO1994010164A1 (en) 1994-05-11
DE69304930D1 (de) 1996-10-24
JPH08502503A (ja) 1996-03-19
ATE143013T1 (de) 1996-10-15
EP0666855B1 (en) 1996-09-18
US5589484A (en) 1996-12-31
KR100239003B1 (ko) 2000-02-01
NO951588L (no) 1995-06-27
RU2130933C1 (ru) 1999-05-27
DE69304930T2 (de) 1997-02-27
AU5178293A (en) 1994-05-24
PL175679B1 (pl) 1999-01-29
FI951996A (fi) 1995-04-26
DK0666855T3 (da) 1996-10-07
BG99566A (en) 1996-01-31
SK53495A3 (en) 1995-09-13

Similar Documents

Publication Publication Date Title
RU2152392C1 (ru) Ацильные производные азолонов, способ их получения, фармацевтическая композиция на их основе и способ ее получения
DE69620445T2 (de) (imidazol-5-yl)methyl-2-chinolinoderivate als farnesyl protein transferase inhibitoren
NZ289853A (en) 4(sulphonyl)piperazine azolone derivatives for anti-helicobacter compositions
EP0232937B1 (en) Anti-histaminic compositions containing n-heterocyclyl-4-piperidinamines
NZ290117A (en) Anti-helicobacter agents comprising 4[2-(1-substituted)-propyl]-2,3-dihydro-3-oxo-4h-1,2,4-triazol-4-yl]- (het)ring-1-carboxamide or -carbothiamide derivatives
IL175512A (en) A pure crystalline form of aripiprazole
US4835161A (en) Anti-histaminic compositions containing n-heterocyclyl-4-piperidinamines
AP435A (en) Substituted azolone derivatives.
AU2002233706C1 (en) Pyridopyrimidine or naphthyridine derivative
LV10951B (en) 4-quinolinyl derivatives with anti-helicobacter activity
KR100593395B1 (ko) 광범위-스펙트럼 항진균제로서의 수용성 아졸
NO310289B1 (no) Heterocykliske azolonderivater med anti-Helicobacteraktivitet
EP0398426A1 (en) Antirhinoviral (thio)morpholinyl and piperazinyl alkylphenol ethers
EP0364943B1 (en) Benzoheterocyclic compounds
KR100497942B1 (ko) 광학활성을 유발하는 7-피롤리딘 치환체를 갖는 광학활성의 퀴놀린 카르복실산 유도체 및 그의 제조방법