DK3049417T3 - Pyridiner, pyrimidiner, og pyraziner, som btk-inhibitorer og anvendelser deraf - Google Patents
Pyridiner, pyrimidiner, og pyraziner, som btk-inhibitorer og anvendelser deraf Download PDFInfo
- Publication number
- DK3049417T3 DK3049417T3 DK14750672.9T DK14750672T DK3049417T3 DK 3049417 T3 DK3049417 T3 DK 3049417T3 DK 14750672 T DK14750672 T DK 14750672T DK 3049417 T3 DK3049417 T3 DK 3049417T3
- Authority
- DK
- Denmark
- Prior art keywords
- compound
- pyrrolo
- mmol
- pyrimidin
- optionally substituted
- Prior art date
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- 0 CC(C1)=C*=C(C=C*2CC(CCC3)C*3C(C=C)=O)C2=C1Oc(cc1)ccc1Oc1ccccc1 Chemical compound CC(C1)=C*=C(C=C*2CC(CCC3)C*3C(C=C)=O)C2=C1Oc(cc1)ccc1Oc1ccccc1 0.000 description 4
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- C07D471/02—Heterocyclic 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 two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07D487/02—Heterocyclic 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
- C07D487/04—Ortho-condensed systems
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- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Reproductive Health (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (18)
1. Forbindelse med formel I,
eller et farmaceutisk acceptabelt salt deraf, hvor: X er N eller CR2; XI er N eller CR2; X2 er N eller CR2; hver R2 er uafhængigt valgt fra -R, halogen, -haloalkyl, -OR, -SR, -CN, -NOz, -SO2R, -SOR, -C(O)R, -CO2R, -C(O)N(R)2, -NRC(O)R, -NRC(O)N(R)2, -NRSO2R, eller -N(R)2; hver R er uafhængigt hydrogen, C1-6 alifatisk, C3-10 aryl, en 3-8 leddet mættet eller delvist umættet carbocyklisk ring, en 3-7 leddet heterocyklisk ring med 1-4 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl, eller en 5-6 leddet monocyklisk heteroarylring med 1-4 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl; der hver eventuelt er substitueret; eller to R grupper på det samme atom taget sammen med det atom til hvilket de er bundet danner en C3-10 aryl, en 3-8 leddet mættet eller delvist umættet carbocyklisk ring, en 3-7 leddet heterocyklisk ring med 1-4 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl, eller en 5-6 leddet monocyklisk heteroaryl ring med 1-4 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl; der hver eventuelt er substitueret; L er en divalent gruppe valgt fra C3-10 aryl, en 3-8 leddet mættet eller delvist umættet carbocyklisk ring, en 3-7 leddet heterocyklisk ring med 1-4 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl og en 5-6
leddet monocyklisk heteroaryl ring med 1-4 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl; der hver eventuelt er substitueret; eller L er en divalent gruppe valgt fra Ci-6 alifatisk-C3-io aryl, Ci-6 alifatisk-3-8 leddet mættet eller delvist umættet carbocyklisk ring, Ci-6 alifatisk-3-7 leddet heterocyklisk ring med 1-4 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl og en Ci-6 alifatisk-5-6 leddet monocyklisk heteroaryl ring med 1-4 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl; der hver eventuelt er substitueret; Y er O, S, SO2, SO, C(O), CO2, C(O)N(R), -NRC(O), -NRC(O)N(R), -NRSO2, eller N(R); eller Y er fraværende; R1 er C2-6 alkenyl eller C2-6 alkynyl, der eventuelt er substitueret; eller R1 er CN.
2. Forbindelsen ifølge krav 1, hvor hver R2 er uafhængigt phenyl eller pyrazolyl.
3. Forbindelsen ifølge krav 1, hvor hver R2 er uafhængigt -OR eller -N(R)2.
4. Forbindelsen ifølge krav 1, hvor hver R2 er uafhængigt hydrogen,
5. Forbindelsen ifølge krav 1, hvor L er
6. Forbindelsen ifølge krav 1, hvor Y er NR,
7. Forbindelsen ifølge krav 1, hvorY er fraværende.
8. Forbindelsen ifølge krav 1, hvor R1 er -CN, -CH2CN,
9. Forbindelsen ifølge krav 1, med formel I-al,
eller et farmaceutisk acceptabelt salt deraf.
10. Forbindelsen ifølge krav 1, med formel I-a2,
eller et farmaceutisk acceptabelt salt deraf.
11. Forbindelsen ifølge krav 1, med formel I-bl,
eller et farmaceutisk acceptabelt salt deraf.
12. Forbindelsen ifølge krav 1, med formel I-b2,
I-b2; eller et farmaceutisk acceptabelt salt deraf.
13. Forbindelsen ifølge krav 1, med formel I-cl:
eller et farmaceutisk acceptabelt salt deraf.
14. Forbindelsen ifølge krav 1, med formel I-c2:
eller et farmaceutisk acceptabelt salt deraf.
15. Forbindelsen ifølge krav 1, valgt fra
16. Farmaceutisk sammensætning omfattende en forbindelse ifølge krav 1 og en farmaceutisk acceptabel adjuvans, bærer, eller vehikel.
17. Forbindelse ifølge et hvilket som helst af kravene 1 til 15 og/eller et fysiologisk acceptabelt salt deraf til anvendelse i behandlingen afen BTK-medieret lidelse , hvor den BTK-medierede lidelse er inflammatorisk tarmsygdom, arthritis, systemisk lupus erythematosus (SLE eller lupus), lupus nephritis, vasculitis, idiopathisk thrombocytopenisk purpura (ITP), rheumatoid arthritis, psoriatisk arthritis, osteoarthritis, Still's sygdom, juvenile arthritis, diabetes, myasthenia gravis, Hashimoto's thyroiditis, Ord's thyroiditis, Graves' sygdom, autoimmun thyroiditis, Sjogren's syndrom, multipel sclerose, systemisk sclerose, Lyme neuroborreliosis, Guillain-Barre syndrom, akut dissemineret encephalomyelitis, Addison's sygdom, opsoclonus-myoclonus syndrom, ankylosing spondylosis, antiphospholipid antistofsyndrom, aplastisk anæmi, autoimmun hepatitis, autoimmun gastritis, perniciøs anæmi, søliakisygdom, Goodpasture's syndrom, idiopatisk thrombocytopænisk purpura, optisk neuritis, scleroderma, primær biliær cirrhose, Reiter's syndrom, Takayasu's arteritis, temporal arteritis, varm
autoimmun hæmolytisk anæmi, Wegener's granulomatose, psoriasis, alopecia universalis, Behcet's sygdom, kronisk fedme, dysautonomi, membranøs glomerulonephropati, endometriose, interstitial cystitis, pemphigus vulgaris, bulløs pemphigoid, neuromyotoni, scleroderma, eller vulvodyni.
18. Fremgangsmåde til fremstilling afen forbindelse med formel I ifølge krav 1, omfattende trinnene at: omsætte en forbindelse med formel (Il-a)
hvor X, X1 og X2, er som defineret i krav 1; med en forbindelse til at give en forbindelse med formel I:
hvor X, X1, X2, R1, L og Y er som defineret i krav 1.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361860401P | 2013-07-31 | 2013-07-31 | |
PCT/US2014/048810 WO2015017502A1 (en) | 2013-07-31 | 2014-07-30 | Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof |
Publications (1)
Publication Number | Publication Date |
---|---|
DK3049417T3 true DK3049417T3 (da) | 2019-01-14 |
Family
ID=51303133
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK14750672.9T DK3049417T3 (da) | 2013-07-31 | 2014-07-30 | Pyridiner, pyrimidiner, og pyraziner, som btk-inhibitorer og anvendelser deraf |
Country Status (24)
Country | Link |
---|---|
US (2) | US9738648B2 (da) |
EP (1) | EP3049417B1 (da) |
JP (1) | JP6612751B2 (da) |
KR (1) | KR20160036053A (da) |
CN (1) | CN105814057B (da) |
AU (1) | AU2014296261B2 (da) |
BR (1) | BR112016001600A8 (da) |
CA (1) | CA2918242C (da) |
DK (1) | DK3049417T3 (da) |
ES (1) | ES2706150T3 (da) |
HR (1) | HRP20190054T1 (da) |
HU (1) | HUE042111T2 (da) |
IL (1) | IL243844B (da) |
LT (1) | LT3049417T (da) |
MX (1) | MX367085B (da) |
NZ (1) | NZ715838A (da) |
PL (1) | PL3049417T3 (da) |
PT (1) | PT3049417T (da) |
RS (1) | RS58361B1 (da) |
RU (1) | RU2712220C2 (da) |
SG (2) | SG10201900025UA (da) |
SI (1) | SI3049417T1 (da) |
WO (1) | WO2015017502A1 (da) |
ZA (1) | ZA201600564B (da) |
Families Citing this family (64)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
EP3280708B1 (en) | 2015-04-10 | 2021-09-01 | Araxes Pharma LLC | Substituted quinazoline compounds and methods of use thereof |
MX2017013275A (es) | 2015-04-15 | 2018-01-26 | Araxes Pharma Llc | Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos. |
US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
WO2017058805A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
US10875842B2 (en) | 2015-09-28 | 2020-12-29 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
CA3005089A1 (en) | 2015-11-16 | 2017-05-26 | Araxes Pharma Llc | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
FI3377484T3 (fi) * | 2015-11-17 | 2023-11-30 | Merck Patent Gmbh | Menetelmiä multippeliskleroosin hoitoon käyttämällä pyrimidiini- ja pyridiiniyhdisteitä, joilla on BTK inhiboiva vaikutus |
CN107021963A (zh) | 2016-01-29 | 2017-08-08 | 北京诺诚健华医药科技有限公司 | 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用 |
CN108884068B (zh) | 2016-03-24 | 2021-02-26 | 特殊治疗有限公司 | 作为dub抑制剂的1-氰基-吡咯烷衍生物 |
US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
WO2018035080A1 (en) * | 2016-08-16 | 2018-02-22 | Merck Patent Gmbh | 2-oxo-imidazopyridines as reversible btk inhibitors and uses thereof |
WO2018064510A1 (en) | 2016-09-29 | 2018-04-05 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
GB201616511D0 (en) | 2016-09-29 | 2016-11-16 | Mission Therapeutics Limited | Novel compounds |
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