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1. RS54180 - FUSED HETEROAROMATIC PYRROLIDINONES AS SYK INHIBITORS

Office
Serbia
Application Number 20150544
Application Date 17.12.2010
Publication Number 54180
Publication Date 31.12.2015
Grant Number 54180
Grant Date 31.12.2015
Publication Kind B1
IPC
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/437
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 7/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7Drugs for disorders of the blood or the extracellular fluid
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
CPC
A61K 31/437
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/527
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
527spiro-condensed
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Applicants TAKEDA PHARMACEUTICAL
Inventors ARIKAWA YASUYOSHI
JONES BENJAMIN
LAM BETTY
NIE ZHE
SMITH CHRISTOPHER
TAKAHASHI MASASHI
DONG QING
FEHER VICTORIA
Title
(EN) FUSED HETEROAROMATIC PYRROLIDINONES AS SYK INHIBITORS
(SR) FUZIONISANI HETEROAROMATSKI PIROLIDINONI KAO SYK INHIBITORI
Abstract
(SR) Jedinjenje, naznačeno time, što ima Formulu 1, ili neka njegova farmaceutski prihvatljiva so, pri čemu: G je C(R5); L1 i L2 su svaki nezavisno izabrani iz -NH- i neke veze; R1 i R2 su svaki nezavisno izabrani iz vodonika, halo, C1-3alkila, i C1-3haloalkila, ili R1 i R2, zajedno sa atomom na kojeg su spojeni, formiraju C3-6cikloalkil; R3 je izabran iz C2-6alkila, C3-8cikloalkila, C2-5heterociklila, i C1-9heteroarila, pri čemu je svaki ponekad supstituisan sa jednim do pet supstituenata nezavisno izabranih iz halo. okso, -NO2, -CN, R6, i R7; R4 je izabran iz C3-8cikloalkila, C2-5heterociklila, C6-14arila, i C1-9heteroarila, pri čemu je svaki ponekad supstituisan sa jednim do pet supstituenata nezavisno izabranih iz halo, okso, -CN, R6, i R7; R3 je izabran iz vodonika, halo, -CN, C1-4alkila, C2-4alkenila, C2-4alkinila, C2-5heterociklila, C1-5heteroarila, i R10, pri čemu su alkil, alkenil, alkinil (svaki) ponekad supstituisani sa jednim od supstituenata nezavisno izabranih iz halo, -CN, okso, i R10, a gde heterociklilni ostatak ima 3 do 6 atoma u prstenu, a heteroarilni ostatak ima 5 ili 6 atoma u prstenu, a svaki heterociklil i heteroaril je ponekad supstituisan sa jednim do četiri supstituenta nezavisno izabrana iz halo, -NO2, -CN, C1-4alkila, C2-4alkenila, C2-4alkinila, C1-4haloalkila, i R10; svaki R6 je nezavisno izabran iz -OR8, -N(R8)R9, -NR8C(O)R9, -C(O)R8 -C(O)OR8, -C(O)N(R8)R9, -C(O)N(R8)OR9, -C(O)N(R8)S(O)2R9, -N(R8)S(O)2R9, -S(O)nR8, i -S(O)2N(R8)R9; svaki R7 je nezavisno izabran iz C1-6alkila, C2-6alkenila, C2-6alkinila, C3-6cikloalkil-(CH2)m-, C6-14aril-(CH2)m-, C2-5heterociklil-(CH2)m-, i C1-9heteroaril-(CH2)m-. pri čemu je svaki ponekad supstituisan sa jednim do pet supstituenata nezavisno izabranih iz halo, okso, -NO2, -CN, C1-6alkila, C1-6haloalkila, i R10; svaki R8 i R9 je nezavisno izabran iz vodonika ili iz C1-6alkila, C2-6alkenila, C2-6alkinila, C3-6cikloalkil-(CH2)m-, C6-14aril-(CH2)m-, C2-5heterociklil-(CH2)m-, i C1-9heteroaril-(CH2)m-, pri čemu je svaki ponekad supstituisan sa jednim do pet supstituenata nezavisno izabranih iz halo, okso, -NO2, -CN, C1-6alkila, C1-6haloalkila. i R10; svaki R10 je nezavisno izabran iz -OR11, -N(R11)R12, -N(R11)C(O)R12, -C(O)R11, -C(O)OR11, -C(O)N(R11)R12, -C(O)N(R11)OR12, -C(O)N(R11)S(O)2R12, NR11S(O)2R12, -S(O)nR11, i -S(O)2N(R11)R12; svaki R11 i R12 je nezavisno izabran iz vodonika i C1-6alkila; svaki n je nezavisno izabran iz 0, 1 i 2; a svaki m je nezavisno izabran iz 0, 1, 2, 3, i 4; pri čemu svaki malopre pomenuti heteroarilni ostatak sadrži jedan do četiri heteroatoma koja su nezavisno izabrana iz N, O, i S. a svaki od malopre pomenutih heterociklilnih ostataka je zasićen ili delomično nezasićen i ima jedan ili dva heteroatoma nezavisno izabrana iz N, O, i S. Prijava sadrži još 24 patentnih zahteva.
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