HRP20211220T1 - Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba - Google Patents
Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba Download PDFInfo
- Publication number
- HRP20211220T1 HRP20211220T1 HRP20211220TT HRP20211220T HRP20211220T1 HR P20211220 T1 HRP20211220 T1 HR P20211220T1 HR P20211220T T HRP20211220T T HR P20211220TT HR P20211220 T HRP20211220 T HR P20211220T HR P20211220 T1 HRP20211220 T1 HR P20211220T1
- Authority
- HR
- Croatia
- Prior art keywords
- image
- compound
- iii
- nitrogen
- membered
- Prior art date
Links
- 108010038555 Phosphoglycerate dehydrogenase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 229910052717 sulfur Chemical group 0.000 claims 9
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 8
- 239000001301 oxygen Chemical group 0.000 claims 8
- 239000011593 sulfur Chemical group 0.000 claims 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 125000001931 aliphatic group Chemical group 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- -1 -OR Chemical group 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 102100037579 D-3-phosphoglycerate dehydrogenase Human genes 0.000 claims 1
- 101000739890 Homo sapiens D-3-phosphoglycerate dehydrogenase Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 101150009274 nhr-1 gene Proteins 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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
- C07D405/12—Heterocyclic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/14—Heterocyclic 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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/02—Heterocyclic 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 two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (15)
1. Spoj formule I:
[image]
ili njegova farmaceutski prihvatljiva sol, gdje je:
R1 is C1-4 alkil,
svaki od R2 i R3 neovisno je halogen, -OR, -CN, C1-6 alifatska skupina koja može biti supstituirana s 1, 2 ili 3 halogena ili -L-R’, ili R2 i R3 se mogu uzeti zajedno s ugljikovim atomima na koje su vezani i s bilo kojim brojem atoma između njih tvoreći petero- do osmeročlani djelomično nezasićeni prsten koji ima 0-2 heteroatoma neovisno odabranih od dušika, kisika ili sumpora,
R4 je vodik, halogen, -OR5, -CN, C1-6 alifatska skupina koja može biti supstituirana s 1, 2 ili 3 halogena ili -L-R’,
svaki R je neovisno vodik ili skupina koja može biti supstituirana odabrana od sljedećih: C1-6 alifatska skupina, tro- do osmeročlani zasićeni ili djelomično nezasićeni monociklički karbociklički prsten, fenil, osmero- do deseteročlani biciklički aromatski karbociklički prsten, četvero- do osmeročlani zasićeni ili djelomično nezasićeni monociklički heterociklički prsteni koji ima 1-2 heteroatoma neovisno odabranih od dušika, kisika ili sumpora, petero- do šesteročlani monociklički heteroaromatski prsten koji ima 1-4 heteroatoma neovisno odabranih dušika, kisika ili sumpora, ili osmero- do deseteročlani biciklički heteroaromatski prsten koji ima 1-5 heteroatoma neovisno odabranih od dušika, kisika ili sumpora,
R5 je vodik, -(CH2)n-fenil, -(CH2)n-Cy’ ili C1-6 alkil koji može biti supstituiran s 1, 2 ili 3 halogena,
svaki L neovisno jest C1-6 bivalentni ravnolančani ili razgranati ugljikovodični lanac u kojem su 1-4 metilnskih skupina zamijenjeni sa sljedećim: -O-, -C(O)-, -C(O)O-, -OC(O)-, -OC(O)N(R)-, -(R)NC(O)O-, -C(O)N(R)-, -(R)NC(O)-, -N(R)-, -N(R)C(O)N(R)-, -S-, -SO- ili -SO2-,
svaki R’ neovisno jest vodik, C1-6 alifatska skupina ili četvero- do osmeročlani člani zasićeni ili djelomično nezasićeni moguće supstituirani monociklički heterociklički psten koji ima 1-3 heteroatoma neovisno odabranih od dušika, kisika ili sumpora,
R6 je vodik ili C1-4 alkil,
R7 je vodik, -CO2R, C1-6 alifatska skupina koja može biti supstituirana, -Cy- ili bivalentni tro- do sedmeričlani prsten,
L1 je kovalentna veza ili C1-8 bivalentni ravnolančani ili razgranati ugljikovodični lanac u kojem su 1-5 metilenskih skupina lanca su neovisno i opcionalno zamijenjeni sa sljedećim: -O-, -C(O)-, -C(O)O-, -OC(O)-, -N(R)-, -C(O)N(R)-, -(R)NC(O)-, -OC(O)N(R)-, -R)NC(O)O-, -N(R)C(O)N(R)-, -S-, -SO-, -SO2-, -SO2N(R)-, -(R)NSO2-, -C(S)-, -C(S)O-, -OC(S)-, -C(S)N(R)-, -(R)NC(S)-, -(R)NC(S)N(R)- ili -Cy-,
svaki -Cy- neovisno je bivalentni šesteročlani arilenski prsten koji sadrži 0-2 dušikovih atoma ili bivalentni peteročlani heteroarilni prsten s 1-4 heteroatoma neovisno odabranih od dušika, kisika ili sumpora, ili bivalentni djelomično nezasićeni osmero- do deseteročlani biciklički heterociklenski prsten s 1-4 heteroatoma neovisno odabranih od dušika, kisika ili sumpora, pri čemu -Cy- može biti supstituiran s 1 ili 2 supstituenata neovisno odabranih od sljedećih: C1-4 alkil ili -OR, -Cy’ je četvero- do osmeročlani zasićeni ili djelomično nezasićeni monociklički heterociklički prsten koji ima 1-2 heteroatoma neovisno odabranih od dušika, kisika ili sumpora,
R10 je C1-6 alifatska skupina koja može biti supstituarana sa sljedećim: 1, 2 ili 3 halogena, -C(O)CH3, ili -SO2-N(R1)(R11),
R11 je -C(O)CH3, -C(O)NHR1 ili pirazinil,
n je neovisno 0, 1, 2, 3, 4 ili 5,
m je neovisno 0, 1 ili 2,
X je O, S ili -N(R10)-, te
svaki od Y1 i Y2 neovisno je =N- ili =C(R4)-.
2. Spoj prema patentom zahtjevu 1, naznačen time da R1 jest metil.
3. Spoj prema patentom zahtjevu 2, naznačen time da (I) R2 jest halogen, -OR-CN ili -L-R’, može biti naznačen time da oba R2 i R3 jesi halogeni, ili
naznačen time da (II) R2 jest F, Cl, -CF3, -OCF3, -OCHF2, -OCH2Ph, -OCH3, -CN, -CH3,
[image]
ili
[image]
ili:
naznačen time da (III) R3 jest halogen ili -OR, ili:
naznačen time da (IV) R4 jest vodik.
4. Spoj prema patentom zahtjevu 2, naznačen time da L1 jest SO2NH-,
[image]
moguće naznačen time da (i) L1 jest
[image]
[image]
ili
[image]
ili naznačen time da (ii) R7 jest vodik, metl, etiil, cikclopropil, ciklobutil, tetrazolil ili -CO2H.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time da X jest O, ili naznačen time da X jest S, ili naznačen time da X jest -N(R10)-.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5, naznačen time da Y1 jest N te Y2 jest =(CH)-, , ili naznačen time da Y1 jest =(CH)- te Y2 jest N.
7. Spoj prema patentom zahtjevu 1, naznačen time da je spomenuti spoj odabran od formula II-a, II-b, II-c, II-d, or II-e:
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentom zahtjevu 1, naznačen time da je spomenuti spoj ima bilo koju od formula III-a, III-b, III-c, III-d, III-e, III-f, IIIg, III-h, ili III-i:
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema patentom zahtjevu 1, naznačen time da spoj jest odabran od sljedećih:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Farmaceutski pripravak sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9 ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljiv adjuvans, nosač ili vezikul.
11. Spoj iz bilo kojeg od patentnih zahtjeva 1 do 9 ili njegov farmaceutski pripravak za upotrebu u liječenju poremećaja posredovanog s PHGDH.
12. Spoj iz bilo kojeg od patentnih zahtjeva 1 do 9, za upotrebu u liječenju karcinoma.
13. Spoj za upotrebu iz patentnog zahtjeva 12, naznačen time da karcinom jest melanom ili karcinom dojke.
14. Spoj iz bilo kojeg od patentnih zahtjeva 1 do 9, naznačen time da je za upotrebu u liječenju tumora.
15. Spoj za upotrebu iz patentnog zahtjeva 14, naznačen time da tumori jesu sljedeći: melanom, ili karcinom dojke, ili naznačen time da jest karcinom malih stanica pluća (SCLC) ili karcinom ne-malih stanica pluća (NSCLC).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662305930P | 2016-03-09 | 2016-03-09 | |
| PCT/US2017/021420 WO2017156165A1 (en) | 2016-03-09 | 2017-03-08 | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
| EP17764026.5A EP3426243B1 (en) | 2016-03-09 | 2017-03-08 | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211220T1 true HRP20211220T1 (hr) | 2021-10-29 |
Family
ID=59789738
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211220TT HRP20211220T1 (hr) | 2016-03-09 | 2021-07-28 | Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US10954220B2 (hr) |
| EP (2) | EP3426243B1 (hr) |
| CY (1) | CY1124338T1 (hr) |
| DK (1) | DK3426243T3 (hr) |
| ES (2) | ES2883328T3 (hr) |
| HR (1) | HRP20211220T1 (hr) |
| HU (1) | HUE055197T2 (hr) |
| LT (1) | LT3426243T (hr) |
| PL (2) | PL3884939T3 (hr) |
| PT (1) | PT3426243T (hr) |
| RS (1) | RS62271B1 (hr) |
| SI (1) | SI3426243T1 (hr) |
| WO (1) | WO2017156165A1 (hr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3884939T3 (pl) | 2016-03-09 | 2024-02-26 | Raze Therapeutics, Inc. | Inhibitory dehydrogenazy 3-fosfoglicerynianowej i ich zastosowania |
| US11014882B2 (en) * | 2016-03-09 | 2021-05-25 | Raze Therapeutics, Inc. | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
| EP3694506B1 (en) * | 2017-10-09 | 2023-08-02 | Merck Sharp & Dohme LLC | Novel substituted phenyloxetane and phenyltetrahydrofuran compounds as indoleamine 2,3-dioxygenase (ido) inhibitors |
| WO2019099294A1 (en) * | 2017-11-14 | 2019-05-23 | Merck Sharp & Dohme Corp. | Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors |
| EP3886854A4 (en) | 2018-11-30 | 2022-07-06 | Nuvation Bio Inc. | PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THERE |
| TW202227447A (zh) * | 2020-08-18 | 2022-07-16 | 大陸商和記黃埔醫藥（上海）有限公司 | 嘧啶酮類化合物及其用途 |
| EP4355729A1 (en) | 2021-06-16 | 2024-04-24 | Celgene Corporation | Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases |
| WO2024132767A1 (en) | 2022-12-19 | 2024-06-27 | Chiesi Farmaceutici S.P.A. | Phosphoglicerate dehydrogenase inhibitors for the treatment of fibrosis |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR901228A (fr) | 1943-01-16 | 1945-07-20 | Deutsche Edelstahlwerke Ag | Système d'aimant à entrefer annulaire |
| US5639600A (en) | 1994-08-05 | 1997-06-17 | The Regents Of The University Of California | Diagnosis and treatment of cell proliferative disease having clonal macrophage involvement |
| US7087648B1 (en) | 1997-10-27 | 2006-08-08 | The Regents Of The University Of California | Methods for modulating macrophage proliferation using polyamine analogs |
| BR0007532A (pt) | 1999-01-13 | 2001-11-20 | Univ New York State Res Found | Métodos para identificar inibidores de proteìnaquinase, para testar compostos para umacapacidade de inibir a atividade de proteìnaquinase e para inibir uma proteìna quinase, inibidorde proteìna tirosina quinase não peptìdica, e,método de tratar uma condição responsiva a uminibidor de proteìna quinase em um paciente |
| JP4078074B2 (ja) | 1999-12-10 | 2008-04-23 | ファイザー・プロダクツ・インク | ピロロ［２，３−ｄ］ピリミジン化合物 |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| JP3836436B2 (ja) | 2001-04-27 | 2006-10-25 | 全薬工業株式会社 | 複素環式化合物及びそれを有効成分とする抗腫瘍剤 |
| AR034897A1 (es) | 2001-08-07 | 2004-03-24 | Hoffmann La Roche | Derivados n-monoacilados de o-fenilendiaminas, sus analogos heterociclicos de seis miembros y su uso como agentes farmaceuticos |
| JP4623962B2 (ja) | 2001-10-22 | 2011-02-02 | ザ・リサーチ・ファウンデーション・オブ・ステイト・ユニバーシティ・オブ・ニューヨーク | タンパク質キナーゼおよびホスファターゼ阻害剤、それらを設計する方法、ならびにそれらを使用する方法 |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| DE60325740D1 (de) | 2002-08-14 | 2009-02-26 | Silence Therapeutics Ag | Verwendung von protein-kinase-n-beta |
| WO2004089925A1 (en) | 2003-04-03 | 2004-10-21 | Semafore Pharmaceuticals, Inc. | Pi-3 kinase inhibitor prodrugs |
| DK1644363T3 (da) | 2003-05-30 | 2012-05-29 | Gemin X Pharmaceuticals Canada Inc | Triheterocykliske forbindelser, sammensætninger og fremgangsmåder til behandling af cancer eller virussygdomme |
| EP1692153A4 (en) | 2003-07-03 | 2007-03-21 | Univ Pennsylvania | INHIBITION OF EXPRESSION OF SYK-KINASE |
| LT2612862T (lt) | 2004-05-13 | 2017-01-25 | Icos Corporation | Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai |
| WO2006067445A2 (en) | 2004-12-22 | 2006-06-29 | Astrazeneca Ab | Csf-1r kinase inhibitors |
| UY29300A1 (es) | 2004-12-22 | 2006-07-31 | Astrazeneca Ab | Compuestos quimicos |
| DK1856135T3 (da) | 2005-01-19 | 2010-04-12 | Rigel Pharmaceuticals Inc | Prodrugs af 2,4-pyrimidindiamin-forbindelser og deres anvendelser |
| WO2007040650A2 (en) | 2005-05-12 | 2007-04-12 | Abbott Laboratories | Apoptosis promoters |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| US7402325B2 (en) | 2005-07-28 | 2008-07-22 | Phoenix Biotechnology, Inc. | Supercritical carbon dioxide extract of pharmacologically active components from Nerium oleander |
| EP2388263A1 (en) | 2005-08-04 | 2011-11-23 | Sirtris Pharmaceuticals, Inc. | Imidazo[2,1-b]thiazole derivatives as sirtuin modulators |
| EA024305B1 (ru) | 2005-10-07 | 2016-09-30 | Экселиксис, Инк. | Ингибиторы фосфатидилинозит-3-киназы и их применение |
| BR122021011788B1 (pt) | 2005-11-01 | 2022-01-25 | Impact Biomedicines, Inc | Inibidores de biaril meta pirimidina de cinases, composição farmacêutica e processo para preparar uma composição farmacêutica |
| MY159449A (en) | 2005-12-13 | 2017-01-13 | Incyte Holdings Corp | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| NZ572812A (en) | 2006-04-26 | 2010-09-30 | Hoffmann La Roche | THIENO [3, 2-D] PYRIMIDINE Indazole DERIVATIVE USEFUL AS PI3K INHIBITOR |
| US7838542B2 (en) | 2006-06-29 | 2010-11-23 | Kinex Pharmaceuticals, Llc | Bicyclic compositions and methods for modulating a kinase cascade |
| EP2532235A1 (en) | 2006-09-22 | 2012-12-12 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| EP2079729A1 (en) | 2006-11-03 | 2009-07-22 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| KR101566840B1 (ko) | 2007-03-12 | 2015-11-06 | 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 | 페닐 아미노 피리미딘 화합물 및 이의 용도 |
| US8394794B2 (en) | 2007-03-23 | 2013-03-12 | Regents Of The University Of Minnesota | Therapeutic compounds |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| EP2158183A2 (en) | 2007-05-25 | 2010-03-03 | Vertex Pharmaceuticals Incorporated | Ion channel modulators and methods of use |
| UA101493C2 (ru) | 2008-03-11 | 2013-04-10 | Инсайт Корпорейшн | Производные азетидина и циклобутана как ингибиторы jak |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| NO2344478T3 (hr) * | 2008-11-03 | 2018-02-24 | ||
| US9096579B2 (en) | 2012-04-20 | 2015-08-04 | Boehringer Ingelheim International Gmbh | Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments |
| EP3125883B1 (en) * | 2014-04-04 | 2020-08-12 | Iomet Pharma Ltd. | Indole derivatives for use in medicine |
| US11014882B2 (en) | 2016-03-09 | 2021-05-25 | Raze Therapeutics, Inc. | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
| PL3884939T3 (pl) | 2016-03-09 | 2024-02-26 | Raze Therapeutics, Inc. | Inhibitory dehydrogenazy 3-fosfoglicerynianowej i ich zastosowania |
-
2017
- 2017-03-08 PL PL21167434.6T patent/PL3884939T3/pl unknown
- 2017-03-08 US US16/082,659 patent/US10954220B2/en active Active
- 2017-03-08 EP EP17764026.5A patent/EP3426243B1/en active Active
- 2017-03-08 SI SI201730882T patent/SI3426243T1/sl unknown
- 2017-03-08 ES ES17764026T patent/ES2883328T3/es active Active
- 2017-03-08 LT LTEP17764026.5T patent/LT3426243T/lt unknown
- 2017-03-08 WO PCT/US2017/021420 patent/WO2017156165A1/en active Application Filing
- 2017-03-08 PT PT177640265T patent/PT3426243T/pt unknown
- 2017-03-08 PL PL17764026T patent/PL3426243T3/pl unknown
- 2017-03-08 DK DK17764026.5T patent/DK3426243T3/da active
- 2017-03-08 EP EP21167434.6A patent/EP3884939B1/en active Active
- 2017-03-08 ES ES21167434T patent/ES2965264T3/es active Active
- 2017-03-08 HU HUE17764026A patent/HUE055197T2/hu unknown
- 2017-03-08 RS RS20211023A patent/RS62271B1/sr unknown
-
2021
- 2021-01-15 US US17/150,669 patent/US11634412B2/en active Active
- 2021-07-19 CY CY20211100651T patent/CY1124338T1/el unknown
- 2021-07-28 HR HRP20211220TT patent/HRP20211220T1/hr unknown
-
2023
- 2023-03-01 US US18/115,942 patent/US20230312536A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US10954220B2 (en) | 2021-03-23 |
| LT3426243T (lt) | 2021-08-10 |
| WO2017156165A1 (en) | 2017-09-14 |
| EP3884939B1 (en) | 2023-10-25 |
| DK3426243T3 (da) | 2021-07-19 |
| EP3426243B1 (en) | 2021-05-19 |
| ES2883328T3 (es) | 2021-12-07 |
| HUE055197T2 (hu) | 2021-11-29 |
| RS62271B1 (sr) | 2021-09-30 |
| PL3884939T3 (pl) | 2024-02-26 |
| US11634412B2 (en) | 2023-04-25 |
| ES2965264T3 (es) | 2024-04-11 |
| PT3426243T (pt) | 2021-08-19 |
| PL3426243T3 (pl) | 2021-10-04 |
| EP3884939C0 (en) | 2023-10-25 |
| US20190071431A1 (en) | 2019-03-07 |
| EP3884939A1 (en) | 2021-09-29 |
| CY1124338T1 (el) | 2022-07-22 |
| US20230312536A1 (en) | 2023-10-05 |
| EP3426243A4 (en) | 2019-07-03 |
| EP3426243A1 (en) | 2019-01-16 |
| SI3426243T1 (sl) | 2021-11-30 |
| US20230009122A1 (en) | 2023-01-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20211220T1 (hr) | Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba | |
| HRP20191579T1 (hr) | Spojevi kao modulatori za ror gama | |
| HRP20200107T1 (hr) | Novi derivati hidroksiestera, postupak za njihovu pripravu i farmaceutski pripravci koji ih sadrže | |
| AR106863A1 (es) | Compuestos de bencimidazol inhibidores de pad4 | |
| HRP20191901T1 (hr) | Ciklizirani derivati sulfamoilarilamida i njihova uporaba kao lijekova za liječenje hepatitisa b | |
| RS54708B1 (en) | ARYLETINYL DERIVATIVES | |
| HRP20230537T1 (hr) | Supstituirani derivati tieno[2,3-d]pirimidina kao inhibitori za menin-mll i postupci za uporabu | |
| AR060316A1 (es) | Azaindoles de utilidad como inhibidores de janus quinasas | |
| AR064416A1 (es) | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. | |
| ECSP11011200A (es) | Derivados de oxadiazale como agonista de los receptores s1p1 | |
| HRP20220502T1 (hr) | Kombinacije koje sadrže derivate 5-fenoksi-3h-pirimidin-4-ona i njihova uporaba za profilaksu ili liječenje infekcije hiv-om | |
| AR076486A1 (es) | Inhibidores de fosfoinositida 3 kinasa y composiciones farmaceuticas que los contienen. | |
| AR107042A1 (es) | Inhibidores de la tirosina quinasa de bruton y métodos de su uso | |
| AR056198A1 (es) | Un proceso para la fabricacion de una composicion farmaceutica tipo tableta | |
| AR087052A1 (es) | Derivados de amina ciclica como antagonistas del receptor ep4 | |
| AR096748A1 (es) | Compuestos heteroaromáticos y su uso como ligandos d1 de dopamina | |
| AR096979A1 (es) | Derivados de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen | |
| EA201170099A1 (ru) | Замещенные пиримидин-4-оновые производные | |
| AR072171A1 (es) | Derivados de nicotinamida, composicion farmaceutica que los comprende y su uso en combinaciones y en la preparacion de un medicamento para el tratamiento del asma. | |
| AR037288A1 (es) | Compuestos derivados de sulfonamidas, procedimiento para la obtencion, composicion farmaceutica y uso para la elaboracion de un medicamento | |
| HRP20192041T1 (hr) | [derivati 7-(morfolinil)-2-(n-piperazinil) metil tieno [2, 3-c]piridina kao lijekovi protiv raka] | |
| RU2012125971A (ru) | Новые химические соединения производные 2,4-диамино-1,3,5-триазина для профилактики и лечения заболеваний человека и животных | |
| AR088474A1 (es) | Derivados de alcoholes de 1-fenil-2-piridinilalquilo como inhibidores de la fosfodiesterasa | |
| CO6321168A2 (es) | Nuevos derivados de 2-amidotiadiazol | |
| AR098432A1 (es) | Compuestos heterocíclicos |