HRP20171795T1 - Dvojni selektivni inhibitori pi3 delta i gamma kinaze - Google Patents

Dvojni selektivni inhibitori pi3 delta i gamma kinaze Download PDF

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HRP20171795T1
HRP20171795T1 HRP20171795TT HRP20171795T HRP20171795T1 HR P20171795 T1 HRP20171795 T1 HR P20171795T1 HR P20171795T T HRP20171795T T HR P20171795TT HR P20171795 T HRP20171795 T HR P20171795T HR P20171795 T1 HRP20171795 T1 HR P20171795T1
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compound
disease
compound according
intended
lymphoma
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HRP20171795TT
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Swaroop Kumar V.S. Vakkalanka
Prashant K. Bhavar
Srikant Viswanadha
Govindarajulu Babu
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Rhizen Pharmaceuticals S.A.
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Publication of HRP20171795T1 publication Critical patent/HRP20171795T1/hr

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    • CCHEMISTRY; METALLURGY
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A61P17/00Drugs for dermatological disorders
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
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    • AHUMAN NECESSITIES
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    • 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
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    • A61P3/00Drugs for disorders of the metabolism
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    • A61P35/00Antineoplastic agents
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms

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  • Organic Chemistry (AREA)
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  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Claims (19)

1. Spoj, naznačen time što se bira između 2-(1-(9H-purin-6-ilamino)propil)-3-(3-fluorfenil)-4H-kromen-4-ona i njegovih farmaceutski prihvatljivih soli.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što se spoj bira između (S)-2-(1-(9H-purin-6-ilamino)propil)-3-(3-fluorfenil)-4H-kromen-4-ona i njegovih farmaceutski prihvatljivih soli.
3. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je spoj (S)-2-(1-(9H-purin-6-ilamino)propil)-3-(3-fluorfenil)-4H-kromen-4-on.
4. Spoj u skladu s patentnim zahtjevom 2 ili patentnim zahtjevom 3, naznačen time što spoj uglavnom ne sadrži (R)-2-(1-(9H-purin-6-ilamino)propil)-3-(3-fluorfenil)-4H-kromen-4-on i njegove farmaceutski prihvatljive soli.
5. Spoj u skladu s patentnim zahtjevom 2 ili patentnim zahtjevom 3, naznačen time što spoj ima enantiomerni suvišak veći od otprilike 95%.
6. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-5 i najmanje jednu farmaceutski prihvatljivu podlogu.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u inhibiranju katalitičke aktivnosti PI3 δ kinaze prisutne u stanici stavljanjem u kontakt stanice s djelotvornom količinom navedenog spoja.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u inhibiranju katalitičke aktivnosti PI3 γ kinaze prisutne u stanici, stavljanjem u kontakt stanice s djelotvornom količinom navedenog spoja.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u inhibiranju katalitičke aktivnosti PI3 δ kinaze i PI3 γ kinaze prisutne u stanici, stavljanjem u kontakt stanice s djelotvornom količinom navedenog spoja.
10. Spoj namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 7-9, naznačen time što se inhibiranje provodi kod subjekta koji boluje od bolesti, poremećaja ili stanja koje se bira između raka, poremećaja kostiju, upalne bolesti, imunosne bolesti, bolesti živčanog sustava, metaboličke bolesti, dišne bolesti, tromboze i srčane bolesti.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u liječenju leukemije kod pacijenta kojem je to potrebno, koje se sastoji u primjeni djelotvorne količine navedenog spoja.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u liječenju astme ili kronične opstruktivne plućne bolesti kod pacijenta kojem je to potrebno, koje se sastoji u primjeni djelotvorne količine navedenog spoja.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u liječenju reumatoidnog artritisa, psorijaze, lupusa ili eksperimentalnog autoimunog encefalomijelitisa (EAE) kod pacijenta kojem je to potrebno, koje se sastoji u primjeni djelotvorne količine navedenog spoja.
14. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u liječenju kronične limfocitne leukemije (CLL), nehodgkinovskog limfoma (NHL), Hodgkinovog limfoma (HL), akutne mijeloidne leukemije (AML), multiplog mijeloma (MM), limfoma malih limfocita (SLL) ili bezbolnog nehodgkinovskog limfoma (I-NHL) kao bolesti kod pacijenta kojem je to potrebno, koje se sastoji u primjeni djelotvorne količine navedenog spoja.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u liječenju bolesti, poremećaja ili stanja kojem bi pogodovalo inhibiranje katalitičke aktivnosti PI3 δ/γ kinaze.
16. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je namijenjen upotrebi u liječenju bolesti, poremećaja ili stanja povezanog s PI3K koje se sastoji u primjeni na subjektu kojem je to potrebno djelotvorne količine navedenog spoja.
17. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 16, naznačen time što se upotreba dodatno sastoji u primjeni dodatnog aktivnog sredstva, koje se bira između sredstava protiv raka, protuupalnih sredstava, imunosupresivnih sredstava, steroida, nesteroidnih protuupalnih sredstava, antihistaminika, analgetika i njihovih smjesa.
18. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 16, naznačen time što je bolest, poremećaj ili stanje povezano s PI3K bolest povezana s imunosnim sustavom, bolest ili poremećaj koji uključuje upalu, rak ili koju drugu proliferativnu bolest, bolest ili poremećaj jetre, ili bolest ili poremećaj bubrega.
19. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 16, naznačen time što se bolest, poremećaj ili stanje povezano s PI3K bira između leukemije, akutne limfocitne leukemije, akutne limfoblastične leukemije, limfoma B-stanica, limfoma T-stanica, Hodgkinovog limfoma, nehodgkinovskog limfoma, limfoma vlasastih stanica, Burkettovog limfoma, akutne i kronične mijelogene leukemije, mijelodisplastičnog sindroma i promijelocitne leukemije, psorijaze, reumatoidnog artritisa, osteoartritisa, astme, COPD, alergijskog rinitisa i eritematoznog lupusa.
HRP20171795TT 2013-06-07 2017-11-20 Dvojni selektivni inhibitori pi3 delta i gamma kinaze HRP20171795T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN2501CH2013 2013-06-07
IN5567CH2013 2013-12-03
PCT/IB2014/061954 WO2014195888A1 (en) 2013-06-07 2014-06-04 Dual selective pi3 delta and gamma kinase inhibitors
EP14732019.6A EP3004106B1 (en) 2013-06-07 2014-06-04 Dual selective pi3 delta and gamma kinase inhibitors

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HRP20171795T1 true HRP20171795T1 (hr) 2018-01-26

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US (3) US9790224B2 (hr)
EP (1) EP3004106B1 (hr)
JP (1) JP6499165B2 (hr)
KR (1) KR102292853B1 (hr)
CN (1) CN105358560B (hr)
AP (1) AP2015008888A0 (hr)
AR (1) AR096543A1 (hr)
AU (1) AU2014276476B2 (hr)
BR (1) BR112015030385B1 (hr)
CA (1) CA2913226C (hr)
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EA (1) EA029017B1 (hr)
ES (1) ES2648094T3 (hr)
HK (1) HK1217949A1 (hr)
HR (1) HRP20171795T1 (hr)
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IL (1) IL242761B (hr)
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PT (1) PT3004106T (hr)
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SI (1) SI3004106T1 (hr)
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WO (1) WO2014195888A1 (hr)
ZA (1) ZA201508708B (hr)

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MX2015001081A (es) 2012-07-24 2015-10-14 Pharmacyclics Inc Mutaciones asociadas a resistencia a inhibidores de la tirosina cinasa de bruton (btk).
JP6501270B2 (ja) 2013-03-14 2019-04-17 ザ カリフォルニア インスティテュート フォー バイオメディカル リサーチ 標的化剤抗体抱合体およびその使用
SG11201509992RA (en) * 2013-06-07 2016-01-28 Rhizen Pharmaceuticals Sa Dual selective pi3 delta and gamma kinase inhibitors
SG11201510011VA (en) 2013-06-07 2016-01-28 California Inst Biomedical Res Small molecule inhibitors of fibrosis
EP3250036B1 (en) 2014-12-10 2021-05-12 The Scripps Research Institute Small molecule inhibitors of fibrosis
MX2017008486A (es) * 2014-12-23 2017-09-19 Pharmacyclics Llc Combinaciones del inhibidor de tirosina cinasa de bruton (btk) y regimenes de dosificacion.
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WO2021229452A1 (en) 2020-05-14 2021-11-18 Rhizen Pharmaceuticals Ag Purine derivatives as sik-3 inhibitors
WO2023125418A1 (zh) * 2021-12-31 2023-07-06 同润生物医药(上海)有限公司 一种苯磺酸盐结晶及其制备方法
WO2023125419A1 (zh) * 2021-12-31 2023-07-06 同润生物医药(上海)有限公司 一种己二酸盐结晶及其制备方法
TW202328132A (zh) * 2021-12-31 2023-07-16 大陸商同潤生物醫藥(上海)有限公司 PI3Kδ/γ雙重抑制劑化合物的半富馬酸鹽結晶及其製備方法
WO2023130334A1 (zh) * 2022-01-07 2023-07-13 同润生物医药(上海)有限公司 一种色烯-4-酮化合物及其中间体的制备方法
WO2023209634A1 (en) 2022-04-29 2023-11-02 Rhizen Pharmaceuticals Ag A dual selective pi3k delta and gamma inhibitors and/or a salt-inducible kinase 3 inhibitor for treating solid tumors

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AR084366A1 (es) 2010-12-20 2013-05-08 Incyte Corp N-(1-(fenil sustituido)etil)-9h-purin-6-aminas como inhibidores de pi3k
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SG11201509992RA (en) * 2013-06-07 2016-01-28 Rhizen Pharmaceuticals Sa Dual selective pi3 delta and gamma kinase inhibitors
US20200289520A1 (en) * 2017-12-06 2020-09-17 Rhizen Pharmaceuticals Sa Composition and method for treating peripheral t-cell lymphoma and cutaneous t-cell lymphoma

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PH12015502698B1 (en) 2016-03-14
EA029017B1 (ru) 2018-01-31
EA201592113A1 (ru) 2016-05-31
US20140364447A1 (en) 2014-12-11
CN105358560B (zh) 2017-03-08
ES2648094T3 (es) 2017-12-28
PL3004106T3 (pl) 2018-01-31
AU2014276476A1 (en) 2015-12-10
LT3004106T (lt) 2018-02-26
JP6499165B2 (ja) 2019-04-10
US11466006B2 (en) 2022-10-11
IL242761B (en) 2018-11-29
NO3004106T3 (hr) 2018-01-27
SI3004106T1 (en) 2018-03-30
NZ714465A (en) 2021-03-26
US20170334914A1 (en) 2017-11-23
MX2015016741A (es) 2016-11-14
AR096543A1 (es) 2016-01-13
BR112015030385B1 (pt) 2020-08-18
EP3004106B1 (en) 2017-08-30
CY1119615T1 (el) 2018-04-04
RS56606B1 (sr) 2018-02-28
AP2015008888A0 (en) 2015-11-30
SG11201509992RA (en) 2016-01-28
KR20160017047A (ko) 2016-02-15
PT3004106T (pt) 2017-11-27
TWI615144B (zh) 2018-02-21
BR112015030385A2 (pt) 2017-07-25
JP2016520644A (ja) 2016-07-14
US9790224B2 (en) 2017-10-17
KR102292853B1 (ko) 2021-08-24
BR112015030385A8 (pt) 2019-12-24
MX366449B (es) 2019-07-09
AU2014276476B2 (en) 2018-05-10
HK1217949A1 (zh) 2017-01-27
HUE035237T2 (hu) 2018-05-02
CA2913226C (en) 2023-01-03
DK3004106T3 (en) 2017-12-04
TW201517908A (zh) 2015-05-16
US20210032248A1 (en) 2021-02-04
PH12015502698A1 (en) 2016-03-14
CN105358560A (zh) 2016-02-24
CL2015003562A1 (es) 2016-08-05
WO2014195888A1 (en) 2014-12-11
EP3004106A1 (en) 2016-04-13
ZA201508708B (en) 2017-02-22
CA2913226A1 (en) 2014-12-11
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