DK2509950T3 - 5-amino-4-hydroxypentoylamider - Google Patents

5-amino-4-hydroxypentoylamider Download PDF

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Publication number
DK2509950T3
DK2509950T3 DK10790938.4T DK10790938T DK2509950T3 DK 2509950 T3 DK2509950 T3 DK 2509950T3 DK 10790938 T DK10790938 T DK 10790938T DK 2509950 T3 DK2509950 T3 DK 2509950T3
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Denmark
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mmol
solution
formula
added
compound
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DK10790938.4T
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English (en)
Inventor
Genadiy Kalayanov
Bart Rudolf Romanie Kesteleyn
Kevin Parkes
Bengt Bertil Samuelsson
Wim Bert Griet Schepens
Johannes Wilhelmus J Thuring
Hans Kristian Wallberg
Jörg Kurt Wegner
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Janssen Sciences Ireland Uc
Medivir Ab
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    • 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
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • C07D277/30Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Claims (19)

1. Forbindelse med formlen I:
hvor R1 er halogen, Ci_4alkoxy, trifluormethoxy; R2 er en gruppe med formlen:
R3 er en gruppe med formlen:
R4 er en gruppe med formlen:
n er 0 eller 1; hvert A uafhængigt er CH eller N; R5 og R6 uafhængigt er hydrogen, Ci-4alkyl eller halogen; R7 er Ci-4alkyl eller Ci-4alkoxyCi-4alkyl; R8 er Ci-4alkyl eller Ci-4alkoxyCi-4alkyl; hvert R9 uafhængigt er Ci-4alkyl, cyclopropyl, trifluormethyl, Ci_4alkoxy eller dimethylamino; R10 er hydrogen, C^alkyl, cyclopropyl, trif luormethyl, Ci_ 4alkoxy eller dimethylamino; R11 er hydrogen eller Ci_4alkyl; de farmaceutisk acceptable additionssalte og de farmaceutisk acceptable solvater deraf.
2. Forbindelse ifølge krav 1, hvor R1 er halogen eller methoxy.
3. Forbindelse ifølge krav 1, hvor R1 er fluor eller chlor; hvilket fluor eller chlor er indsubstitueret i ortho-stillingen; eller R1 er methoxy; hvilket methoxy er indsubstitueret i meta-stillingen.
4. Forbindelse ifølge et hvilket som helst af kravene 1-3, hvor R2 er en gruppe med formlen
5. Forbindelse ifølge et hvilket som helst af kravene 1-3, hvor R2 er en gruppe med formlen
6. Forbindelse ifølge et hvilket som helst af kravene 1-5, hvor R5 er hydrogen, og R6 er halogen eller Ci_4alkyl; R5 er halogen, og R6 er hydrogen; R5 er halogen eller Ci-4alkyl, og R6 er hydrogen; eller R5 og R6 begge er hydrogen eller begge er halogen; R11 er Ci_4alkyl.
7. Forbindelse ifølge et hvilket som helst af kravene 1-5, hvor R5 er hydrogen, og R6 er fluor eller chlor; R5 er fluor eller chlor, og R6 er hydrogen; R5 er hydrogen, og R6 er methyl; R5 og R6 begge er hydrogen, eller R5 er chlor, og R6 er fluor; især hvor R5 er hydrogen, og R6 er fluor; R5 er chlor, og R6 er hydrogen; R5 er hydrogen, og R6 er methyl; R5 og R5 begge er hydrogen, eller R5 er chlor, og R6 er fluor; og R11 er methyl.
8. Forbindelse ifølge et hvilket som helst af kravene 1-7, hvor R3 er en gruppe med formlen
9. Forbindelse ifølge et hvilket som helst af kravene 1-7, hvor R3 er en gruppe med formlen
10. Forbindelse ifølge krav 9, hvor R8 er methyl eller 2- methoxyethyl.
11. Forbindelse ifølge krav 1-10, hvor R9 er Ci_2alkoxy eller dimethylamino.
12. Forbindelse ifølge et hvilket som helst af kravene 1-11, hvor R4 er en gruppe med den kemiske struktur, som er specificeret i krav 1, men hvor R9 er R9a i den første gruppe, R9 er R9b i den anden gruppe, R9 er R9c i den tredje gruppe, R9 er R9d i den fjerde gruppe, og R9 er R9e i den femte og i den sjette gruppe; hvilke grupper kan repræsenteres som følger:
hvor hvert A uafhængigt er CH eller N; eller hvor hvert A er CH; R9a er Ci_4alkoxy eller dimethylamino; R9b er Ci-4alkoxy eller dimethylamino; R9c er Ci-4alkoxy eller dimethylamino; R9d er Ci-4alkyl, cyclopropyl, trifluormethyl; R10 er hydrogen, Ci-4alkyl, cyclopropyl eller trifluormethyl; eller R10 er hydrogen, methyl, cyclopropyl eller trifluormethyl; hvert R9e uafhængigt er Ci-4alkyl, cyclopropyl, Ci_4alkoxy eller dimethylamino.
13. Forbindelse ifølge krav 12, hvor, i R9a, R9b, R9c, R9d eller R9e, Ci_4alkoxy er methoxy, og Ci_4alkyl er methyl.
14. Forbindelse ifølge et hvilket som helst af kravene 1-7, hvor R4 er: R9a A'"'" 4;'N * hvor A er CH, og R9a er methoxy eller dimethylamino.
15. Forbindelse ifølge krav 1, som har formlen
16. Forbindelse ifølge krav 1, som har formlen
17. Forbindelse ifølge krav 1, som har formlen
18. Forbindelse ifølge et hvilket som helst af kravene 1-17 til anvendelse som et lægemiddel.
19. Farmaceutisk sammensætning, som omfatter en effektiv mængde af en forbindelse med formlen I ifølge et hvilket som helst af kravene 1-17 og en bærer.
DK10790938.4T 2009-12-11 2010-12-10 5-amino-4-hydroxypentoylamider DK2509950T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09178979 2009-12-11
EP10162370 2010-05-10
PCT/EP2010/069328 WO2011070131A1 (en) 2009-12-11 2010-12-10 5-amino- 4-hydroxypentoyl amides

Publications (1)

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DK2509950T3 true DK2509950T3 (da) 2015-05-18

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DK10790938.4T DK2509950T3 (da) 2009-12-11 2010-12-10 5-amino-4-hydroxypentoylamider

Country Status (24)

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US (1) US8592429B2 (da)
EP (1) EP2509950B1 (da)
JP (1) JP5797662B2 (da)
KR (1) KR101771698B1 (da)
CN (1) CN102770413B (da)
AP (1) AP3217A (da)
AR (1) AR079354A1 (da)
AU (1) AU2010329867B2 (da)
BR (1) BR112012013493B1 (da)
CA (1) CA2783929C (da)
DK (1) DK2509950T3 (da)
EA (1) EA020758B1 (da)
ES (1) ES2536774T3 (da)
HK (1) HK1177454A1 (da)
IL (1) IL219272A (da)
JO (1) JO3090B1 (da)
MX (1) MX2012006613A (da)
NZ (1) NZ599916A (da)
PL (1) PL2509950T3 (da)
PT (1) PT2509950E (da)
SG (1) SG181609A1 (da)
TW (1) TWI485149B (da)
UY (1) UY33098A (da)
WO (1) WO2011070131A1 (da)

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Publication number Priority date Publication date Assignee Title
JP7111733B2 (ja) 2017-03-16 2022-08-02 江蘇恒瑞医薬股▲ふん▼有限公司 ヘテロアリール[4,3-c]ピリミジン-5-アミン誘導体、その製造方法、およびその医薬の使用

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IL89900A0 (en) * 1988-04-12 1989-12-15 Merck & Co Inc Hiv protease inhibitors useful for the treatment of aids and pharmaceutical compositions containing them
EP0534511A1 (en) * 1991-08-16 1993-03-31 Merck & Co. Inc. HIV protease inhibitors useful for the treatment of aids
CN1089269A (zh) * 1993-01-04 1994-07-13 希巴-盖吉股份公司 新颖的作为治疗剂的5-氨基-4-羟基己酸衍生物
US5733882A (en) * 1994-01-17 1998-03-31 Smithkline Beecham Corporation Retroviral protease inhibitors
PT708085E (pt) * 1994-10-19 2002-11-29 Novartis Ag Eteres antivirais de isosteros de substrato de aspartato protease
HU229224B1 (en) * 2001-02-14 2013-09-30 Tibotec Pharmaceuticals Ltd Little Island 2-(substituted-amino)-benzothiazole sulfonamide compounds having broadspectrum hiv protease inhibitor activity and medicaments containing them
TWI286476B (en) * 2001-12-12 2007-09-11 Tibotec Pharm Ltd Combination of cytochrome P450 dependent protease inhibitors
US7834043B2 (en) * 2003-12-11 2010-11-16 Abbott Laboratories HIV protease inhibiting compounds
CN101115713A (zh) * 2005-02-10 2008-01-30 美迪维尔公司 人类免疫缺陷性病毒蛋白酶抑制剂
EP1851193B1 (en) * 2005-02-10 2009-04-22 Medivir AB Hiv protease inhibitors
WO2007048557A1 (en) * 2005-10-25 2007-05-03 Medivir Ab Protease inhibitors
JO2841B1 (en) * 2006-06-23 2014-09-15 تيبوتيك فارماسيوتيكالز ليمتد 2-(substituted-amino) -benzothiazole sulfonamide as protease inhibitors HIV (HIV)
NZ573887A (en) * 2006-07-21 2012-02-24 Gilead Sciences Inc Antiviral protease inhibitors

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Publication number Publication date
EA201290487A1 (ru) 2012-11-30
AU2010329867A1 (en) 2012-05-24
KR20120107104A (ko) 2012-09-28
SG181609A1 (en) 2012-07-30
EP2509950A1 (en) 2012-10-17
AP3217A (en) 2015-04-30
JP5797662B2 (ja) 2015-10-21
EP2509950B1 (en) 2015-02-25
BR112012013493B1 (pt) 2020-12-08
PT2509950E (pt) 2015-06-08
AU2010329867B2 (en) 2016-01-28
ES2536774T3 (es) 2015-05-28
CA2783929A1 (en) 2011-06-16
UY33098A (es) 2011-06-30
HK1177454A1 (en) 2013-08-23
IL219272A (en) 2014-09-30
CN102770413B (zh) 2015-08-26
TW201130823A (en) 2011-09-16
CA2783929C (en) 2020-04-07
JO3090B1 (ar) 2017-03-15
TWI485149B (zh) 2015-05-21
JP2013513576A (ja) 2013-04-22
WO2011070131A1 (en) 2011-06-16
CN102770413A (zh) 2012-11-07
BR112012013493A2 (pt) 2016-05-31
AP2012006228A0 (en) 2012-04-30
KR101771698B1 (ko) 2017-08-25
US20120295920A1 (en) 2012-11-22
AR079354A1 (es) 2012-01-18
EA020758B1 (ru) 2015-01-30
MX2012006613A (es) 2012-07-10
PL2509950T3 (pl) 2015-10-30
US8592429B2 (en) 2013-11-26
NZ599916A (en) 2013-10-25
BR112012013493A8 (pt) 2017-12-26
IL219272A0 (en) 2012-06-28

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