ES2568909T3 - Novedosos compuestos antagonistas del receptor de la neuroquinina 1 - Google Patents

Novedosos compuestos antagonistas del receptor de la neuroquinina 1 Download PDF

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Publication number
ES2568909T3
ES2568909T3 ES13720801T ES13720801T ES2568909T3 ES 2568909 T3 ES2568909 T3 ES 2568909T3 ES 13720801 T ES13720801 T ES 13720801T ES 13720801 T ES13720801 T ES 13720801T ES 2568909 T3 ES2568909 T3 ES 2568909T3
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Prior art keywords
alkyl
nr8r9
optionally substituted
hydrogen
novel
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ES13720801T
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Inventor
Morten Dahl Sørensen
Romano Di Fabio
Alfonso Pozzan
Maria Pia Catalani
Haakon BLADH
Jakob Felding
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Leo Pharma AS
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Leo Pharma AS
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20Spiro-condensed systems
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/20Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un compuesto de formula general A**Fórmula** en donde n es 1 o 2; R1 y R2 son independientemente hidrógeno, C1-4 alquilo, C1-4 haloalquilo, C1-4 alcoxi, CD3 o halógeno; R3 es hidrógeno, C(>=O)OR7 o C1-4 alquilo opcionalmente sustituido con hidroxi o NR8R9; R4 es hidrógeno u oxo; R5 y R6 son independientemente hidrógeno, hidroxi, NR8R9, C(>=O)R7, C(>=O)OR7, C(>=O)NR8R9, C1-4 alquilo, en donde dicho C1-4 alquilo es opcionalmente sustituido con hidroxi, NR8R9 o un anillo heterocíclico de 5 o 6 miembros en donde dicho anillo heterocíclico de 5 o 6 miembros es opcionalmente sustituido con C1-4 alquilo o C(>=O)R7; o R5 y R6, junto con el átomo de carbono al que están unidos, forman >=CH2 o un heterocicloalquilo de 5 o 6 miembros, en donde dicho heterocicloalquilo es opcionalmente sustituido con C1-4 alquilo; R7 es hidrógeno o C1-4 alquilo; R8 y R9 son independientemente hidrógeno o C1-4 alquilo, o R8 y R9, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico de 5 o 6 miembros o una sal o solvato farmacéuticamente aceptable del mismo.
ES13720801T 2012-02-22 2013-02-20 Novedosos compuestos antagonistas del receptor de la neuroquinina 1 Active ES2568909T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261601902P 2012-02-22 2012-02-22
US201261601902P 2012-02-22
PCT/EP2013/053319 WO2013124286A1 (en) 2012-02-22 2013-02-20 Novel neurokinin 1 receptor antagonist compounds

Publications (1)

Publication Number Publication Date
ES2568909T3 true ES2568909T3 (es) 2016-05-05

Family

ID=48325586

Family Applications (1)

Application Number Title Priority Date Filing Date
ES13720801T Active ES2568909T3 (es) 2012-02-22 2013-02-20 Novedosos compuestos antagonistas del receptor de la neuroquinina 1

Country Status (17)

Country Link
US (1) US9181259B2 (es)
EP (1) EP2817312B1 (es)
JP (1) JP6111274B2 (es)
KR (1) KR20140122764A (es)
CN (1) CN104245702B (es)
AU (1) AU2013224181A1 (es)
CA (1) CA2864440A1 (es)
DK (1) DK2817312T3 (es)
ES (1) ES2568909T3 (es)
HK (1) HK1205104A1 (es)
MX (1) MX2014010012A (es)
PL (1) PL2817312T3 (es)
RU (1) RU2631319C2 (es)
SG (1) SG11201404880UA (es)
TW (1) TW201339161A (es)
WO (1) WO2013124286A1 (es)
ZA (1) ZA201405959B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2817312T3 (pl) * 2012-02-22 2016-08-31 Leo Pharma As Nowe związki będące antagonistami receptora neurokininy 1
SG11201501867UA (en) 2012-10-11 2015-04-29 Nerre Therapeutics Ltd Novel uses
US8906951B1 (en) 2013-06-24 2014-12-09 Tigercat Pharma, Inc. Use of NK-1 receptor antagonists in pruritus
US9198898B2 (en) 2013-06-24 2015-12-01 Tigercat Pharma, Inc. Use of NK-1 receptor antagonists in pruritus
WO2015024203A1 (en) * 2013-08-20 2015-02-26 Leo Pharma A/S Novel neurokinin 1 receptor antagonist compounds ii
US10744185B2 (en) * 2015-11-09 2020-08-18 Ngm Biopharmaceuticals, Inc. Methods of using variants of FGF19 polypeptides for the treatment of pruritus
JP2019519592A (ja) * 2016-06-29 2019-07-11 メンロ セラピューティクス インコーポレイテッド 様々な掻痒状態を処置するためのニューロキニン−1アンタゴニストの使用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9923748D0 (en) * 1999-10-07 1999-12-08 Glaxo Group Ltd Chemical compounds
GB0025354D0 (en) 2000-10-17 2000-11-29 Glaxo Group Ltd Chemical compounds
GB0108595D0 (en) 2001-04-05 2001-05-23 Glaxo Group Ltd Chemical compounds
GB0203020D0 (en) * 2002-02-08 2002-03-27 Glaxo Group Ltd Chemical compounds
UA77515C2 (en) * 2002-04-04 2006-12-15 Diazabicyclo alkane derivatives possessing neuroldnin-nk1 receptor antagonistic activity
CA2590039A1 (en) * 2004-12-14 2006-06-22 Merck & Co., Inc. Octahydropyrano[3,4-c]pyrrole tachykinin receptor antagonists
EP2129381A1 (en) 2007-01-24 2009-12-09 Glaxo Group Limited Pharmaceutical compositions comprising 3, 5-diamin0-6- (2, 3-dichl0phenyl) -l, 2, 4-triazine or r (-) -2, 4-diamino-5- (2, 3-dichlorophenyl) -6-fluoromethyl pyrimidine and an nk1
WO2009002770A1 (en) 2007-06-22 2008-12-31 Merck & Co., Inc. 6.5-pyrrolopiperidine tachykinin receptor antagonists
PL2817312T3 (pl) * 2012-02-22 2016-08-31 Leo Pharma As Nowe związki będące antagonistami receptora neurokininy 1

Also Published As

Publication number Publication date
KR20140122764A (ko) 2014-10-20
CN104245702B (zh) 2016-09-14
PL2817312T3 (pl) 2016-08-31
AU2013224181A1 (en) 2014-10-02
RU2014138032A (ru) 2016-04-10
EP2817312B1 (en) 2016-02-17
ZA201405959B (en) 2016-08-31
WO2013124286A1 (en) 2013-08-29
CN104245702A (zh) 2014-12-24
CA2864440A1 (en) 2013-08-29
EP2817312A1 (en) 2014-12-31
DK2817312T3 (en) 2016-04-11
US9181259B2 (en) 2015-11-10
SG11201404880UA (en) 2014-09-26
MX2014010012A (es) 2014-09-12
US20150018345A1 (en) 2015-01-15
HK1205104A1 (en) 2015-12-11
JP2015511240A (ja) 2015-04-16
TW201339161A (zh) 2013-10-01
RU2631319C2 (ru) 2017-09-21
JP6111274B2 (ja) 2017-04-05

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