DK2858499T3 - Pyrimidinyl-tyrosin-kinaseinhibitorer - Google Patents
Pyrimidinyl-tyrosin-kinaseinhibitorer Download PDFInfo
- Publication number
- DK2858499T3 DK2858499T3 DK13800042.7T DK13800042T DK2858499T3 DK 2858499 T3 DK2858499 T3 DK 2858499T3 DK 13800042 T DK13800042 T DK 13800042T DK 2858499 T3 DK2858499 T3 DK 2858499T3
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- DK
- Denmark
- Prior art keywords
- compound
- amino
- chloro
- oxo
- bipiperidine
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Classifications
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
-
- 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
-
- 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
- A61P37/08—Antiallergic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Claims (14)
- 1. Forbindelse af formel I:I eller et farmaceutisk acceptabelt salt deraf, hvor: hvert R1 er uafhængigt hydrogen, en eventuelt substitueret Ci-6 alifatisk gruppe, en eventuelt substitueret 3-7-leddet monocyklisk heterocyklisk gruppe, eller en eventuelt substitueret heterocyclylalkylgruppe, som har 3-7 kulstofatomer og 1-3 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl; eller to R1 grupper er taget sammen med deres mellemliggende atomer for at danne en eventuelt substitueret 3-7-leddet mættet eller delvist umættet monocyklisk heterocyklisk ring, som har 1-2 heteroatomer uafhængigt valgt fra nitrogen, oxygen, eller svovl; hvor eventuelt substituerede grupper kan substitueres med halogen, -NO2, -CN, -OR, -SR, -N(R)2, -C(O)R, -CO2R, -N(R)C(O)OR, -C(O)N(R)2, -OC(O)R, -N(R)C(O)R, -S(O)R, -S(O)2R, eller -S(O)2N(R)2; hvert R er uafhængigt hydrogen eller C1-6 alifatisk; eller to R grupper bundet til det samme nitrogen er taget sammen med deres mellemliggende atomer for at danne en eventuelt substitueret 3-7-leddet mættet eller delvist umættet monocyklisk heterocyklisk ring, som har 1-2 heteroatomer, i hvilken et hvilket som helst andet heteroatom er uafhængigt valgt fra nitrogen, oxygen, eller svovl;Ring A erR2 er -Cl eller-F; og R3 er -CF3, -OCF3, eller -F.
- 2. Forbindelsen ifølge krav 1, hvor forbindelsen er af formel Il-a:eller et farmaceutisk acceptabelt salt deraf, eller: hvor forbindelsen er af formel Il-b:ll-b eller et farmaceutisk acceptabelt salt deraf, eller: hvor forbindelsen er af formel III:Ill
- 3. Forbindelsen ifølge krav 1, hvor forbindelsen er formel IV:
- 4. Forbindelsen ifølge krav 3, hvor R3 er -CF3, eller hvor R3 er -F.
- 5. Forbindelsen ifølge krav 3, hvor begge R1 er hydrogen.
- 6. Forbindelsen ifølge krav 3, hvor et R1 er hydrogen og det andet R1 er en eventuelt substitueret C1-6 alifatisk, fortrinsvis hvor et R1 er hydrogen og det andet R1 er methyl.
- 7. Forbindelsen ifølge krav 3, hvor (i) begge R1 er eventuelt substituerede C1-6 alifatiske grupper, eller: hvor (ii) et R1 er hydrogen og det andet er eventuelt substitueret C1-6 alifatisk, eller: hvor (iii) begge R1 er eventuelt substituerede Ci-6 alifatiske grupper, eller: hvor (iv) begge R1 er hydrogen.
- 8. Forbindelsen ifølge krav 1, hvor R2 er -Cl, eller hvor R2 er -F.
- 9. Forbindelsen ifølge krav 1, hvor R3 er -CF3, eller hvor R3 er -OCF3, eller hvor R3 er -F.
- 10. Forbindelsen ifølge krav 1, valgt fra gruppen bestående af: 1 1 1
- 11. Forbindelse ifølge et hvilket som helst af kravene 1-10 eller en sammensætning deraf til anvendelse i reduktion af den enzymatiske aktivitet af Brutons tyrosin-kinase.
- 12. Forbindelse ifølge et hvilket som helst af kravene 1-10 eller en sammensætning deraf til anvendelse i behandlingen afen lidelse responsiv over for inhibition af Brutons tyrosin-kinase.
- 13. Forbindelse ifølge et hvilket som helst af kravene 1-10 afen sammensætning deraf til anvendelse i behandlingen afen lidelse valgt fra gruppen bestående af autoimmune lidelser, inflammatoriske lidelser, og cancere.
- 14. Forbindelsen til anvendelse ifølge krav 13, hvor lidelsen er rheumatoid arthritis, eller hvor lidelsen er systemisk lupus erythematosus, eller hvor lidelsen er atopisk dermatitis, eller hvor lidelsen er leukæmi eller lymfom.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261657360P | 2012-06-08 | 2012-06-08 | |
PCT/US2013/044800 WO2013185084A1 (en) | 2012-06-08 | 2013-06-07 | Pyrimidinyl tyrosine kinase inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2858499T3 true DK2858499T3 (da) | 2018-08-20 |
Family
ID=49712704
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK13800042.7T DK2858499T3 (da) | 2012-06-08 | 2013-06-07 | Pyrimidinyl-tyrosin-kinaseinhibitorer |
Country Status (30)
Country | Link |
---|---|
US (5) | US9394277B2 (da) |
EP (3) | EP3753934A1 (da) |
JP (6) | JP6214643B2 (da) |
KR (4) | KR102102587B1 (da) |
CN (3) | CN109305959B (da) |
AR (1) | AR091273A1 (da) |
AU (5) | AU2013271407B2 (da) |
BR (2) | BR122021002178B1 (da) |
CA (2) | CA3108186A1 (da) |
CY (1) | CY1120638T1 (da) |
DK (1) | DK2858499T3 (da) |
EA (2) | EA027823B1 (da) |
ES (2) | ES2834333T3 (da) |
HK (1) | HK1209284A1 (da) |
HR (1) | HRP20181294T1 (da) |
HU (1) | HUE039897T2 (da) |
IL (2) | IL235938B (da) |
IN (1) | IN2014DN10576A (da) |
LT (1) | LT2858499T (da) |
MX (2) | MX363672B (da) |
NZ (1) | NZ702715A (da) |
PH (2) | PH12014502699B1 (da) |
PL (1) | PL2858499T3 (da) |
PT (1) | PT2858499T (da) |
RS (1) | RS57978B1 (da) |
SG (2) | SG11201408173WA (da) |
SI (1) | SI2858499T1 (da) |
TW (3) | TWI719209B (da) |
WO (1) | WO2013185084A1 (da) |
ZA (1) | ZA201409255B (da) |
Families Citing this family (19)
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ES2711936T3 (es) | 2009-09-04 | 2019-05-08 | Biogen Ma Inc | Inhibidores de la tirosina cinasa de Bruton |
US9273028B2 (en) | 2010-10-29 | 2016-03-01 | Biogen Ma Inc. | Heterocyclic tyrosine kinase inhibitors |
AR091273A1 (es) * | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | Inhibidores de pirimidinil tirosina quinasa |
WO2013185082A2 (en) | 2012-06-08 | 2013-12-12 | Biogen Idec Ma Inc. | Inhibitors of bruton's tyrosine kinase |
TWI675833B (zh) * | 2013-12-11 | 2019-11-01 | 美商百健Ma公司 | 布魯頓氏(bruton’s)酪胺酸激酶之聯芳基抑制劑 |
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