HRP20171720T1 - Derivati pirolo [3,2-d] pirimidina za liječenje virusnih infekcija i drugih bolesti - Google Patents
Derivati pirolo [3,2-d] pirimidina za liječenje virusnih infekcija i drugih bolesti Download PDFInfo
- Publication number
- HRP20171720T1 HRP20171720T1 HRP20171720TT HRP20171720T HRP20171720T1 HR P20171720 T1 HRP20171720 T1 HR P20171720T1 HR P20171720T T HRP20171720T T HR P20171720TT HR P20171720 T HRP20171720 T HR P20171720T HR P20171720 T1 HRP20171720 T1 HR P20171720T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- alkyl
- pharmaceutically acceptable
- formula
- solvate
- Prior art date
Links
- KCTZOTUQSGYWLV-UHFFFAOYSA-N N1C=NC=C2N=CC=C21 Chemical class N1C=NC=C2N=CC=C21 KCTZOTUQSGYWLV-UHFFFAOYSA-N 0.000 title 1
- 208000036142 Viral infection Diseases 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 230000009385 viral infection Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 150000001408 amides Chemical class 0.000 claims 3
- 125000004104 aryloxy group Chemical group 0.000 claims 3
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 3
- 150000001733 carboxylic acid esters Chemical class 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 150000002825 nitriles Chemical class 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 150000003456 sulfonamides Chemical class 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 101000669402 Homo sapiens Toll-like receptor 7 Proteins 0.000 claims 1
- 102100039390 Toll-like receptor 7 Human genes 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
Claims (8)
1. Spoj s formulom (I)
[image]
i njegova farmaceutski prihvatljiva sol, solvat ili njihov polimorf naznačen time da
R1 je H, fluor ili metil;
R2 je H, halogen ili C1-3 alkil;
R3 je C1-6 alkil proizvoljno supstituiran s jednim ili više supstituenata koji su neovisno odabrani iz niza koji sadrži ariloksi, heterocikal, halogen, aril, alkilamino, dialkilamino, C1-6 alkil, karboksilnu kiselinu, karboksilni ester, karboksilni amid, nitril, ili C1-6alkoksi;
ili pri čemu
R3 je alkilaril proizvoljno supstituiran s jednim ili više supstituenata koji se neovisno biraju iz niza koji sadrži halogen, ariloksi, aril, alkilamino, dialkilamino, C1-6 alkil, karboksilnu kiselinu, karboksilni ester, karboksilni amid, sulfonamid, nitril, ili C1-6 alkoksi;
R4 je C1-6 alkil proizvoljno supstituiran s jednim ili više supstituenata koji se neovisno biraju iz niza koji sadrži hidroksil, C1-6 alkil, C3-7 cikloalkil, C2-6 alkenil ili aril proizvoljno dalje supstituirani s C1-6 alkilom, i C3-7 cikloalkil proizvoljno dalje supstituiran s C1-6 alkilom;
ili pri čemu
R4 je alkilaril proizvoljno supstituiran s jednim ili više supstituenata koji se neovisno biraju iz niza koji sadrži halogen, ariloksi, aril, alkilamino, dialkilamino, C1-6 alkil, karboksilnu kiselinu, karboksilni ester, karboksilni amid, sulfonamid, nitril, ili C1-6alkoksi.
2. Spoj prema zahtjevu 1 naznačen time da R3 je skupina CH2-aril (supstituirana ili nesupstituirana), i R1, R2, i R4 su opisani kao u zahtjevu 1.
3. Spoj s formulom (I) naznačen time da R3 i R4 su oba skupine CH2-aril proizvoljno dodatno supstituirani kako je opisano u zahtjevu 1, te pri čemu R1 i R2 su opisani kao u zahtjevu 1.
4. Spoj prema zahtjevu 1 naznačen time da R1 je fluor, R2 je vodik, i R3 i R4 su opisani kao u zahtjevu 1.
5. Spoj prema zahtjevu 1 naznačen time da ima slijedeću kemijsku strukturu:
[image]
6. Farmaceutski pripravak naznačen time da sadrži spoj s formulom (I) ili (II) ili njegovu farmaceutski prihvatljivu sol, solvat ili polimorf prema zahtjevu 1 ili 5 zajedno s jednim ili više farmaceutski prihvatljivih pomoćnih tvari, razrjeđivačima ili nosačima.
7. Spoj s formulom (I) ili (II) ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf prema zahtjevu 1 ili 5, ili farmaceutski pripravak koji sadrži navedeni spoj s formulom (I) ili (II) ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf prema zahtjevu 6 naznačen time da je za upotrebu kao lijek.
8. Spoj s formulom (I) ili (II) ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf prema zahtjevu 1 ili zahtjevu 5 ili navedeni farmaceutski pripravak koji sadrži navedeni spoj s formulom (I) ili (II) ili njegova farmaceutski prihvatljiva sol, solvat ili polimorf prema zahtjevu 6 naznačen time da je za upotrebu za liječenje bilo kojeg poremećaja u kojem je uključena modulacija TLR7.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP13174108 | 2013-06-27 | ||
EP14738751.8A EP3030563B1 (en) | 2013-06-27 | 2014-06-26 | Pyrrolo [3,2-d] pyrimidine derivatives for the treatment of viral infections and other diseases |
PCT/EP2014/063467 WO2014207082A1 (en) | 2013-06-27 | 2014-06-26 | Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20171720T1 true HRP20171720T1 (hr) | 2017-12-29 |
Family
ID=48692351
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20171720TT HRP20171720T1 (hr) | 2013-06-27 | 2017-11-09 | Derivati pirolo [3,2-d] pirimidina za liječenje virusnih infekcija i drugih bolesti |
Country Status (26)
Country | Link |
---|---|
US (2) | US10385054B2 (hr) |
EP (1) | EP3030563B1 (hr) |
JP (2) | JP6763769B2 (hr) |
KR (1) | KR102311234B1 (hr) |
CN (2) | CN109369643B (hr) |
AU (2) | AU2014301089B2 (hr) |
BR (1) | BR112015032546B1 (hr) |
CA (1) | CA2913028C (hr) |
CL (1) | CL2015003686A1 (hr) |
DK (1) | DK3030563T3 (hr) |
EA (2) | EA034893B1 (hr) |
ES (1) | ES2645950T3 (hr) |
HK (1) | HK1218116A1 (hr) |
HR (1) | HRP20171720T1 (hr) |
HU (1) | HUE037125T2 (hr) |
IL (3) | IL242655B (hr) |
MX (1) | MX361527B (hr) |
MY (1) | MY176142A (hr) |
NO (1) | NO3030563T3 (hr) |
PH (1) | PH12015502780B1 (hr) |
PL (1) | PL3030563T3 (hr) |
PT (1) | PT3030563T (hr) |
SG (2) | SG10201803331PA (hr) |
SI (1) | SI3030563T1 (hr) |
UA (1) | UA117590C2 (hr) |
WO (1) | WO2014207082A1 (hr) |
Families Citing this family (24)
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EP2694484B1 (en) | 2011-04-08 | 2018-07-18 | Janssen Sciences Ireland UC | Pyrimidine derivatives for the treatment of viral infections |
WO2014207082A1 (en) * | 2013-06-27 | 2014-12-31 | Janssen R&D Ireland | Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases |
JOP20150177B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
MA44334A (fr) | 2015-10-29 | 2018-09-05 | Novartis Ag | Conjugués d'anticorps comprenant un agoniste du récepteur de type toll |
CA3003962A1 (en) | 2015-12-18 | 2017-06-22 | Janssen Pharmaceutica Nv | Radiolabelled mglur2/3 pet ligands |
EP3389727B1 (en) | 2015-12-18 | 2020-08-12 | Janssen Pharmaceutica NV | Radiolabelled mglur2/3 pet ligands |
EP3519406B1 (en) | 2016-09-29 | 2022-02-23 | Janssen Sciences Ireland Unlimited Company | Pyrimidine prodrugs for the treatment of viral infections and further diseases |
TW201945003A (zh) * | 2018-03-01 | 2019-12-01 | 愛爾蘭商健生科學愛爾蘭無限公司 | 2,4-二胺基喹唑啉衍生物及其醫學用途 |
WO2019209811A1 (en) | 2018-04-24 | 2019-10-31 | Bristol-Myers Squibb Company | Macrocyclic toll-like receptor 7 (tlr7) agonists |
US11554120B2 (en) | 2018-08-03 | 2023-01-17 | Bristol-Myers Squibb Company | 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor |
WO2020162705A1 (ko) | 2019-02-08 | 2020-08-13 | 성균관대학교산학협력단 | 톨-유사 수용체 7 또는 8 작용자와 콜레스테롤의 결합체 및 그 용도 |
CN115151547A (zh) | 2020-01-27 | 2022-10-04 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
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CN115135655A (zh) | 2020-01-27 | 2022-09-30 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
WO2021154667A1 (en) | 2020-01-27 | 2021-08-05 | Bristol-Myers Squibb Company | C3-SUBSTITUTED 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
EP4097105A1 (en) | 2020-01-27 | 2022-12-07 | Bristol-Myers Squibb Company | 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists |
CN115643805A (zh) | 2020-01-27 | 2023-01-24 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
JP2023512205A (ja) | 2020-01-27 | 2023-03-24 | ブリストル-マイヤーズ スクイブ カンパニー | トール様受容体7(TLR7)アゴニストとしての1H-ピラゾロ[4,3-d]ピリミジン化合物 |
CN115279765A (zh) | 2020-01-27 | 2022-11-01 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
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