HRP20221221T1 - Pirimidinski spoj kao inhibitor jak kinaze - Google Patents
Pirimidinski spoj kao inhibitor jak kinaze Download PDFInfo
- Publication number
- HRP20221221T1 HRP20221221T1 HRP20221221TT HRP20221221T HRP20221221T1 HR P20221221 T1 HRP20221221 T1 HR P20221221T1 HR P20221221T T HRP20221221T T HR P20221221TT HR P20221221 T HRP20221221 T HR P20221221T HR P20221221 T1 HRP20221221 T1 HR P20221221T1
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- Prior art keywords
- compound
- pharmaceutically acceptable
- formula
- image
- acceptable salt
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- -1 Pyrimidine compound Chemical class 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 9
- 239000000825 pharmaceutical preparation Substances 0.000 claims 8
- 206010012438 Dermatitis atopic Diseases 0.000 claims 4
- 201000008937 atopic dermatitis Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 3
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 208000037896 autoimmune cutaneous disease Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 201000011486 lichen planus Diseases 0.000 claims 2
- 206010001764 Alopecia scarring Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 229910010084 LiAlH4 Inorganic materials 0.000 claims 1
- 208000011738 Lichen planopilaris Diseases 0.000 claims 1
- 206010024434 Lichen sclerosus Diseases 0.000 claims 1
- 239000012448 Lithium borohydride Substances 0.000 claims 1
- 201000009053 Neurodermatitis Diseases 0.000 claims 1
- 206010034277 Pemphigoid Diseases 0.000 claims 1
- 208000031709 Skin Manifestations Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 208000004631 alopecia areata Diseases 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 230000021615 conjugation Effects 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 239000006071 cream Substances 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 239000012280 lithium aluminium hydride Substances 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 208000017940 prurigo nodularis Diseases 0.000 claims 1
- 208000037851 severe atopic dermatitis Diseases 0.000 claims 1
- 239000012279 sodium borohydride Substances 0.000 claims 1
- 229910000033 sodium borohydride Inorganic materials 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Dental Preparations (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Claims (29)
1. Spoj, naznačen time što ima formulu (I):
[image]
,
ili njegova farmaceutski prihvatljiva sol.
2. Slobodni oblik, naznačen time što je slobodni oblik spoja u skladu s patentnim zahtjevom 1.
3. Kristalni oblik spoja formule (I):
[image]
,
gdje je kristalni oblik naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu koji sadrži vrhunce difrakcije pri vrijednostima 2θ od 11,4 ± 0,2, 16,2 ± 0,2, 16,6 ± 0,2, 17,7 ± 0,2, te 21,9 ± 0,2.
4. Kristalni oblik u skladu s patentnim zahtjevom 3, gdje je uzorak difrakcije rendgenskih zraka na prahu naznačen time što dodatno ima dodatne vrhunce difrakcije pri vrijednostima 2θ od 8,9 ± 0,2, 9,5 ± 0,2, te 10,2 ± 0,2.
5. Kristalni oblik u skladu s patentnim zahtjevom 4, gdje je uzorak difrakcije rendgenskih zraka na prahu naznačen time što dodatno ima dva ili više dodatnih vrhunaca difrakcije pri vrijednostima 2θ, koje se bira između 14,4 ± 0,2, 19,0 ± 0,2, 19,2 ± 0,2, 19,8 ± 0,2, 20,1 ± 0,2, 20,4 ± 0,2, 20,6 ± 0,2, 20,8 ± 0,2, 21,3 ± 0,2, 25,9 ± 0,2, 30,1 ± 0,2, 30,5 ± 0,2, 30,9 ± 0,2, 32,6 ± 0,2, te 33,8 ± 0,2.
6. Kristalni oblik u skladu s patentnim zahtjevom 3, gdje je kristalni oblik naznačen time što ima diferencijalnu skenirajuću kalorimetriju tragova zabilježenu pri brzini grijanja od 10 °C u minuti, koja pokazuje maksimum u endotermnom toplinskom toku s vrhuncem na 238,1 °C ± 2 °C.
7. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 ili 2, kao i farmaceutski prihvatljivi nosač.
8. Farmaceutski pripravak, naznačen time što sadrži kristalni oblik u skladu s bilo kojim od patentnih zahtjeva 3 to 6, te farmaceutski prihvatljivi nosač.
9. Farmaceutski pripravak u skladu s patentnim zahtjevom 7, naznačen time što dodatno sadrži jedno ili više dodatnih terapijskih sredstava.
10. Farmaceutski pripravak u skladu s patentnim zahtjevom 7, naznačen time što je farmaceutski pripravak mast ili krema.
11. Farmaceutski pripravak u skladu s patentnim zahtjevom 7, naznačen time što je spoj (I), ili njegova farmaceutski prihvatljiva sol, prisutan u količini između 0,1 i 10 %, težinski.
12. Farmaceutski pripravak u skladu s patentnim zahtjevom 7, naznačen time što je spoj (I), ili njegova farmaceutski prihvatljiva sol, prisutan u količini između 0,25 i 5%, težinski.
13. Farmaceutski pripravak u skladu s patentnim zahtjevom 7, naznačen time što je spoj (I), ili njegova farmaceutski prihvatljiva sol, prisutan u količini između 0,05 i 0,5%, težinski.
14. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je namijenjen upotrebi u liječenju upalne ili autoimune kožne bolesti kod sisavca.
15. Spoj u skladu s patentnim zahtjevom 14, naznačen time što je namijenjen upotrebi u liječenju upalne kožne bolesti kod sisavca.
16. Spoj u skladu s patentnim zahtjevom 15, naznačen time što je namijenjen upotrebi u liječenju atopičnog dermatitisa.
17. Spoj u skladu s patentnim zahtjevom 16, naznačen time što je atopični dermatitis umjereni do teški atopični dermatitis.
18. Spoj u skladu s patentnim zahtjevom 16, naznačen time što je atopični dermatitis blagi do umjereni atopični dermatitis.
19. Spoj u skladu s patentnim zahtjevom 14, naznačen time što je namijenjen upotrebi u liječenju alopecije areate.
20. Spoj u skladu s patentnim zahtjevom 14, naznačen time što je namijenjen upotrebi u liječenju upalne ili autoimune kožne bolesti koju se bira iz skupine koju čine: vitiligo, prurigo nodularis, lihen planus, kontaktni dermatitis, kožne manifestacije reakcije presatka prema domaćinu, pemfigoid, diskoidni lupus, sklerozni lišaj, lihen planopilaris, psorijaza, te folikulitis dekalvans.
21. Spoj u skladu s patentnim zahtjevom 14, naznačen time što je namijenjen upotrebi u liječenju psorijaze.
22. Postupak priprave spoja formule (I):
[image]
,
ili njegove farmaceutski prihvatljive soli, naznačen time što se sastoji u:
(a) reakciji spoja formule (II):
[image]
,
gdje je R C1-12 alkilna skupina, s reducensom; i
(b) uz izborno dobivanje farmaceutski prihvatljive soli, kako bi se dobilo spoj formule (I), ili njegovu farmaceutski prihvatljivu sol.
23. Postupak u skladu s patentnim zahtjevom 22, naznačen time što se reducens bira iz skupine koju čine LiAlH4, NaBH4, te LiBH4.
24. Postupak u skladu s patentnim zahtjevom 22, naznačen time što je R etil.
25. Postupak u skladu s patentnim zahtjevom 22, naznačen time što se spoj formule (II) dobiva konjugiranjem spoja formule (III)
[image]
,
gdje je X halogen, sa spojem formule 1-9
[image]
.
26. Spoj formule (II):
[image]
,
ili njegova farmaceutski prihvatljiva sol,
naznačen time što je R C1-12 alkilna skupina.
27. Spoj u skladu s patentnim zahtjevom 26, naznačen time što je R etil.
28. Spoj formule (III):
[image]
,
ili njegova farmaceutski prihvatljiva sol,
naznačen time što je R C1-12 alkilna skupina, a X je halogen.
29. Spoj u skladu s patentnim zahtjevom 28, naznačen time što je R etil, a X je klor.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762577852P | 2017-10-27 | 2017-10-27 | |
| PCT/US2018/057682 WO2019084383A1 (en) | 2017-10-27 | 2018-10-26 | PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS |
| EP18801171.2A EP3672965B1 (en) | 2017-10-27 | 2018-10-26 | Pyrimidine compound as jak kinase inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20221221T1 true HRP20221221T1 (hr) | 2022-12-09 |
Family
ID=64277858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20221221TT HRP20221221T1 (hr) | 2017-10-27 | 2018-10-26 | Pirimidinski spoj kao inhibitor jak kinaze |
Country Status (37)
| Country | Link |
|---|---|
| US (7) | US10308646B2 (hr) |
| EP (1) | EP3672965B1 (hr) |
| JP (1) | JP7218364B2 (hr) |
| KR (1) | KR102613503B1 (hr) |
| CN (1) | CN111247142B (hr) |
| AR (1) | AR113803A1 (hr) |
| AU (1) | AU2018354370B2 (hr) |
| BR (1) | BR112020008015A2 (hr) |
| CA (1) | CA3074034A1 (hr) |
| CL (1) | CL2020001090A1 (hr) |
| CR (1) | CR20200180A (hr) |
| CU (1) | CU24671B1 (hr) |
| DK (1) | DK3672965T3 (hr) |
| DO (1) | DOP2020000083A (hr) |
| EA (1) | EA202091016A1 (hr) |
| EC (1) | ECSP20023795A (hr) |
| ES (1) | ES2932526T3 (hr) |
| GE (1) | GEP20227344B (hr) |
| HR (1) | HRP20221221T1 (hr) |
| HU (1) | HUE060401T2 (hr) |
| IL (1) | IL274037B2 (hr) |
| LT (1) | LT3672965T (hr) |
| MA (1) | MA49956B1 (hr) |
| MD (1) | MD3672965T2 (hr) |
| MX (1) | MX2020004255A (hr) |
| NI (1) | NI202000032A (hr) |
| PE (1) | PE20201495A1 (hr) |
| PH (1) | PH12020500528A1 (hr) |
| PL (1) | PL3672965T3 (hr) |
| PT (1) | PT3672965T (hr) |
| RS (1) | RS63608B1 (hr) |
| SG (1) | SG11202001706RA (hr) |
| SI (1) | SI3672965T1 (hr) |
| TW (1) | TWI789446B (hr) |
| UA (1) | UA125130C2 (hr) |
| WO (1) | WO2019084383A1 (hr) |
| ZA (1) | ZA202001641B (hr) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7218364B2 (ja) | 2017-10-27 | 2023-02-06 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋキナーゼ阻害剤としてのピリミジン化合物 |
| CN115925705A (zh) * | 2018-11-30 | 2023-04-07 | 江苏豪森药业集团有限公司 | 杂芳类衍生物调节剂、其制备方法和应用 |
| JP7482152B2 (ja) | 2019-04-24 | 2024-05-13 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | 皮膚疾患の処置のためのピリミジンｊａｋ阻害剤 発明の背景 |
| CA3135383A1 (en) | 2019-04-24 | 2020-10-29 | Theravance Biopharma R&D Ip, Llc | Ester and carbonate pyrimidine compounds as jak kinase inhibitors |
| KR20230054682A (ko) * | 2020-07-28 | 2023-04-25 | 아큐티스 바이오테라퓨틱스, 인크. | Jak 저해제 및 라우레스-4를 함유하는 국소 제형 |
| JP2023543670A (ja) * | 2020-08-26 | 2023-10-18 | ナロ・セラピューティクス | Ｍｙｃファミリー癌原遺伝子タンパク質のモジュレーター |
| EP4225438A1 (en) * | 2020-10-08 | 2023-08-16 | Icahn School of Medicine at Mount Sinai | Compositions for treatment alopecia areata, biomarkers for treatment success, and methods of use thereof |
| CA3236262A1 (en) | 2021-10-25 | 2023-05-04 | Isaac Marx | Tyk2 degraders and uses thereof |
| CN114246938A (zh) * | 2022-01-25 | 2022-03-29 | 中山大学中山眼科中心 | Il-4在制备用于治疗视网膜变性疾病药物中的应用 |
| CN115487301B (zh) * | 2022-11-08 | 2023-07-07 | 四川大学华西医院 | Il-13抑制剂在制备延缓或治疗视网膜色素变性的药物中的用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4919934A (en) | 1989-03-02 | 1990-04-24 | Richardson-Vicks Inc. | Cosmetic sticks |
| HUP0302173A2 (hu) | 2000-09-15 | 2003-09-29 | Vertex Pharmaceuticals Incorporated | Protein kináz inhibitorokként alkalmazható pirazolvegyületek |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ES2265452T3 (es) | 2000-12-21 | 2007-02-16 | Vertex Pharmaceuticals Incorporated | Compuestos de pirazol utiles como inhibidores de la proteina quinasa. |
| EP1831216A2 (en) | 2004-12-23 | 2007-09-12 | Pfizer Products Inc. | Heteroaromatic derivatives useful as anticancer agents |
| WO2007059299A1 (en) | 2005-11-16 | 2007-05-24 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| MX2008016523A (es) | 2006-06-30 | 2009-01-19 | Astrazeneca Ab | Derivados de pirimidina utiles en el tratamiento de cancer. |
| CA2656290A1 (en) | 2006-07-05 | 2008-01-10 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| BR112014015549A8 (pt) | 2011-12-22 | 2017-07-04 | Hoffmann La Roche | composto, método de inibição da atividade pak1, método para o tratamento, processo, composição, utilização de um composto e invenção |
| WO2015094803A1 (en) * | 2013-12-16 | 2015-06-25 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| NO2721710T3 (hr) * | 2014-08-21 | 2018-03-31 | ||
| JP2017535520A (ja) * | 2014-09-30 | 2017-11-30 | ハンミ・ファイン・ケミカル・カンパニー・リミテッドＨａｎｍｉ Ｆｉｎｅ Ｃｈｅｍｉｃａｌ Ｃｏ．， Ｌｔｄ． | 高純度の（ｒ）−９−［２−（ホスホノメトキシ）プロピル］アデニンの製造方法 |
| EP3303348B1 (en) * | 2015-05-28 | 2019-08-07 | Theravance Biopharma R&D IP, LLC | Naphthyridine compounds as jak kinase inhibitors |
| WO2017044434A1 (en) | 2015-09-11 | 2017-03-16 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| EA035226B1 (ru) | 2016-04-28 | 2020-05-19 | ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи | Пиримидиновые соединения в качестве ингибиторов jak киназы |
| JP7218364B2 (ja) * | 2017-10-27 | 2023-02-06 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋキナーゼ阻害剤としてのピリミジン化合物 |
| JP7482152B2 (ja) | 2019-04-24 | 2024-05-13 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | 皮膚疾患の処置のためのピリミジンｊａｋ阻害剤 発明の背景 |
| CA3135383A1 (en) | 2019-04-24 | 2020-10-29 | Theravance Biopharma R&D Ip, Llc | Ester and carbonate pyrimidine compounds as jak kinase inhibitors |
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