PE20120575A1 - Derivados de pirazolopirimidina como inhibidores de jak quinasas - Google Patents
Derivados de pirazolopirimidina como inhibidores de jak quinasasInfo
- Publication number
- PE20120575A1 PE20120575A1 PE2012000003A PE2012000003A PE20120575A1 PE 20120575 A1 PE20120575 A1 PE 20120575A1 PE 2012000003 A PE2012000003 A PE 2012000003A PE 2012000003 A PE2012000003 A PE 2012000003A PE 20120575 A1 PE20120575 A1 PE 20120575A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- carboxamide
- pyrazole
- pyrimidine
- inhibitors
- Prior art date
Links
- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical class C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 title abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- XMRIUEGHBZTNND-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine-3-carboxamide Chemical compound C1=CC=NC2=C(C(=O)N)C=NN21 XMRIUEGHBZTNND-UHFFFAOYSA-N 0.000 abstract 2
- LPCQBTAOTIZGAE-UHFFFAOYSA-N 2h-pyrimidine-1-carboxamide Chemical compound NC(=O)N1CN=CC=C1 LPCQBTAOTIZGAE-UHFFFAOYSA-N 0.000 abstract 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 abstract 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 1
- 108010024121 Janus Kinases Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 206010028537 myelofibrosis Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
REFERIDA A UN COMPUESTO DERIVADO DE PIRAZOLOPIRIMIDINA DE FORMULA (I), DONDE R1 ES H, ALQUILO C1-C6, OR6, NR6R7 O HALOGENO; R2 ES UN HETEROARILO DE 5 O 6 MIEMBROS OPCIONALMENTE SUSTITUIDO CON R4; R3 ES FENILO, CICLOALQUILO C3-C6, HETEROCICLILO DE 3 A 10 MIEMBROS, ENTRE OTROS; R4 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R6 Y R7 SON H, ALQUILO C1-C6, ALQUINILO C2-C6, CN, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(3-(5-CLORO-2-METOXIFENIL)-1-METIL-1H-PIRAZOL-4-IL)PIRAZOLO[1,5-a]PIRIMIDINA-3-CARBOXAMIDA, N-(5-(5-CLORO-2-METOXIFENIL)-1-METIL-1H-PIRAZOL-4-IL)PIRAZOLO[1,5-a]PIRIMIDINA-3-CARBOXAMIDA, N-(3-(2,5-DIMETILOFENIL)-1-METIL-1H-PIRAZOL-4-IL)PIRAZOLO[1,5-a]PIRIMIDINA-3-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN UNA O MAS JANUS QUINASAS Y SON UTILES EN EL TRATAMIENTO DE CANCER, POLICITEMIA VERA, MIELOFIBROSIS, ENFERMEDAD DE CHRON, ARTRITIS REUMATOIDE, TROMBOCITOSIS PRIMARIA, ENTRE OTROS
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22291809P | 2009-07-02 | 2009-07-02 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20120575A1 true PE20120575A1 (es) | 2012-05-25 |
Family
ID=43411778
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2015000692A PE20151249A1 (es) | 2009-07-02 | 2010-07-02 | Derivados de pirazolopirimidina como inhibidores de jak quinasas |
PE2012000003A PE20120575A1 (es) | 2009-07-02 | 2010-07-02 | Derivados de pirazolopirimidina como inhibidores de jak quinasas |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2015000692A PE20151249A1 (es) | 2009-07-02 | 2010-07-02 | Derivados de pirazolopirimidina como inhibidores de jak quinasas |
Country Status (35)
Country | Link |
---|---|
US (6) | US8999998B2 (es) |
EP (3) | EP2448941B1 (es) |
JP (4) | JP5769261B2 (es) |
KR (3) | KR20180108858A (es) |
CN (2) | CN102482284B (es) |
AU (1) | AU2010266188B2 (es) |
BR (1) | BRPI1010197A2 (es) |
CA (1) | CA2767097A1 (es) |
CL (1) | CL2012000001A1 (es) |
CO (1) | CO6491081A2 (es) |
CR (2) | CR20170115A (es) |
DK (1) | DK2448941T3 (es) |
EC (1) | ECSP12011645A (es) |
ES (1) | ES2657839T3 (es) |
HR (1) | HRP20180157T1 (es) |
HU (1) | HUE035537T2 (es) |
IL (3) | IL217224B (es) |
IN (1) | IN2012DN00755A (es) |
LT (1) | LT2448941T (es) |
MA (1) | MA33502B1 (es) |
MX (1) | MX2012000169A (es) |
MY (1) | MY160156A (es) |
NO (1) | NO2448941T3 (es) |
NZ (4) | NZ706218A (es) |
PE (2) | PE20151249A1 (es) |
PH (1) | PH12015500666A1 (es) |
PL (1) | PL2448941T3 (es) |
PT (1) | PT2448941T (es) |
RS (1) | RS56671B1 (es) |
RU (2) | RU2567238C2 (es) |
SG (2) | SG10201509607XA (es) |
SI (1) | SI2448941T1 (es) |
UA (1) | UA110324C2 (es) |
WO (1) | WO2011003065A2 (es) |
ZA (2) | ZA201200490B (es) |
Families Citing this family (122)
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RS53245B2 (sr) | 2007-06-13 | 2022-10-31 | Incyte Holdings Corp | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila |
AU2009308675A1 (en) | 2008-10-31 | 2010-05-06 | Genentech, Inc. | Pyrazolopyrimidine JAK inhibitor compounds and methods |
LT2432472T (lt) | 2009-05-22 | 2020-02-10 | Incyte Holdings Corporation | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai |
UA110324C2 (en) * | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
AU2011224484A1 (en) | 2010-03-10 | 2012-09-27 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
EA201290957A1 (ru) | 2010-04-07 | 2013-04-30 | Ф.Хоффманн-Ля Рош Аг | Пиразол-4-илгетероциклилкарбоксамидные соединения и способы их применения |
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MX340490B (es) | 2010-07-13 | 2016-07-11 | F Hoffmann-La Roche Ag * | Derivados de pirazolo [1, 5a] pirimidina y de tieno [3, 2b] pirimidina como moduladores de la cinasa asociada al receptor de la interleucina 4 (irak4). |
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US8609669B2 (en) | 2010-11-16 | 2013-12-17 | Abbvie Inc. | Potassium channel modulators |
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BR112014007622A2 (pt) | 2011-09-30 | 2017-04-04 | Oncodesign Sa | inibidores de flt3 cinase macrocíclicos |
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- 2015-02-06 US US14/615,873 patent/US20150152117A1/en not_active Abandoned
- 2015-03-25 PH PH12015500666A patent/PH12015500666A1/en unknown
- 2015-06-17 JP JP2015122441A patent/JP6312634B2/ja active Active
- 2015-12-09 IL IL242999A patent/IL242999B/en not_active IP Right Cessation
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2017
- 2017-06-20 US US15/627,847 patent/US20170283424A1/en not_active Abandoned
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2018
- 2018-01-04 JP JP2018000305A patent/JP2018083828A/ja not_active Withdrawn
- 2018-01-15 IL IL256921A patent/IL256921A/en unknown
- 2018-01-26 HR HRP20180157TT patent/HRP20180157T1/hr unknown
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2019
- 2019-06-07 JP JP2019106948A patent/JP2019194199A/ja active Pending
- 2019-09-05 US US16/561,432 patent/US20200002345A1/en not_active Abandoned
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2022
- 2022-01-14 US US17/648,045 patent/US20220389020A1/en not_active Abandoned
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2023
- 2023-11-13 US US18/507,678 patent/US20240150364A1/en active Pending
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