AR098534A1 - Terapias para tratar trastornos mieloproliferativos - Google Patents
Terapias para tratar trastornos mieloproliferativosInfo
- Publication number
- AR098534A1 AR098534A1 ARP140104419A ARP140104419A AR098534A1 AR 098534 A1 AR098534 A1 AR 098534A1 AR P140104419 A ARP140104419 A AR P140104419A AR P140104419 A ARP140104419 A AR P140104419A AR 098534 A1 AR098534 A1 AR 098534A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbonitrile
- pyrimidine
- oxo
- diamino
- dihydroquinazolin
- Prior art date
Links
- 208000014767 Myeloproliferative disease Diseases 0.000 title abstract 2
- 238000002560 therapeutic procedure Methods 0.000 title 1
- -1 cyanomethyl Chemical group 0.000 abstract 13
- XVIAPHVAGFEFFN-UHFFFAOYSA-N pyrimidine-5-carbonitrile Chemical compound N#CC1=CN=CN=C1 XVIAPHVAGFEFFN-UHFFFAOYSA-N 0.000 abstract 13
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 abstract 7
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 4
- JCINBYQJBYJGDM-UHFFFAOYSA-N bms-911543 Chemical compound CCN1C(C(=O)N(C2CC2)C2CC2)=CC(C=2N(C)C=NC=22)=C1N=C2NC=1C=C(C)N(C)N=1 JCINBYQJBYJGDM-UHFFFAOYSA-N 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 abstract 3
- 229940122245 Janus kinase inhibitor Drugs 0.000 abstract 3
- 239000012828 PI3K inhibitor Substances 0.000 abstract 3
- 229950003628 buparlisib Drugs 0.000 abstract 3
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 abstract 3
- JEGHXKRHKHPBJD-UHFFFAOYSA-N 5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine Chemical compound CS(=O)(=O)N1CCC2=C1N=C(N1CCOCC1)N=C2C1=CN=C(N)N=C1 JEGHXKRHKHPBJD-UHFFFAOYSA-N 0.000 abstract 2
- SJVQHLPISAIATJ-ZDUSSCGKSA-N 8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]-1-isoquinolinone Chemical compound C1([C@@H](NC=2C=3N=CNC=3N=CN=2)C)=CC2=CC=CC(Cl)=C2C(=O)N1C1=CC=CC=C1 SJVQHLPISAIATJ-ZDUSSCGKSA-N 0.000 abstract 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 abstract 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 229940126401 izorlisib Drugs 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- ASUGUQWIHMTFJL-QGZVFWFLSA-N (2r)-2-methyl-2-[[2-(1h-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]-n-(2,2,2-trifluoroethyl)butanamide Chemical compound FC(F)(F)CNC(=O)[C@@](C)(CC)NC1=CC=NC(C=2C3=CC=CN=C3NC=2)=N1 ASUGUQWIHMTFJL-QGZVFWFLSA-N 0.000 abstract 1
- YOVVNQKCSKSHKT-HNNXBMFYSA-N (2s)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one Chemical compound C1CN(C(=O)[C@@H](O)C)CCN1CC1=C(C)C2=NC(C=3C=NC(N)=NC=3)=NC(N3CCOCC3)=C2S1 YOVVNQKCSKSHKT-HNNXBMFYSA-N 0.000 abstract 1
- ISOCDPQFIXDIMS-QHCPKHFHSA-N (2s)-n-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide Chemical compound O=C([C@H]1NCCC1)NC(C=C1)=CC=C1C(N=1)=CC=NC=1NC(C=C1)=CC=C1N1CCOCC1 ISOCDPQFIXDIMS-QHCPKHFHSA-N 0.000 abstract 1
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 abstract 1
- CBOKMGGXRIPHEU-NSHDSACASA-N 2,4-diamino-6-[[(1s)-1-(8-chloro-4-oxo-3-phenylquinazolin-2-yl)ethyl]amino]pyrimidine-5-carbonitrile Chemical compound N([C@@H](C)C=1N(C(=O)C2=CC=CC(Cl)=C2N=1)C=1C=CC=CC=1)C1=NC(N)=NC(N)=C1C#N CBOKMGGXRIPHEU-NSHDSACASA-N 0.000 abstract 1
- ACLLAWULMDEEMO-INIZCTEOSA-N 2,4-diamino-6-[[(1s)-1-[3-(3,5-difluorophenyl)-4-oxoquinazolin-2-yl]propyl]amino]pyrimidine-5-carbonitrile Chemical compound N([C@@H](CC)C=1N(C(=O)C2=CC=CC=C2N=1)C=1C=C(F)C=C(F)C=1)C1=NC(N)=NC(N)=C1C#N ACLLAWULMDEEMO-INIZCTEOSA-N 0.000 abstract 1
- NSIHPICIDJNIQQ-QMMMGPOBSA-N 2,4-diamino-6-[[(1s)-1-[3-(3,5-difluorophenyl)-5,6-difluoro-4-oxoquinazolin-2-yl]ethyl]amino]pyrimidine-5-carbonitrile Chemical compound N([C@@H](C)C=1N(C(=O)C2=C(F)C(F)=CC=C2N=1)C=1C=C(F)C=C(F)C=1)C1=NC(N)=NC(N)=C1C#N NSIHPICIDJNIQQ-QMMMGPOBSA-N 0.000 abstract 1
- WDHFKDGIVIKECH-QMMMGPOBSA-N 2,4-diamino-6-[[(1s)-1-[5,8-dichloro-3-(5-fluoropyridin-3-yl)-4-oxoquinazolin-2-yl]ethyl]amino]pyrimidine-5-carbonitrile Chemical compound N([C@@H](C)C=1N(C(=O)C2=C(Cl)C=CC(Cl)=C2N=1)C=1C=C(F)C=NC=1)C1=NC(N)=NC(N)=C1C#N WDHFKDGIVIKECH-QMMMGPOBSA-N 0.000 abstract 1
- FYLACRXGVZXOJG-NSHDSACASA-N 2,4-diamino-6-[[(1s)-1-[5-chloro-3-(3-cyanophenyl)-4-oxoquinazolin-2-yl]ethyl]amino]pyrimidine-5-carbonitrile Chemical compound N([C@@H](C)C=1N(C(=O)C2=C(Cl)C=CC=C2N=1)C=1C=C(C=CC=1)C#N)C1=NC(N)=NC(N)=C1C#N FYLACRXGVZXOJG-NSHDSACASA-N 0.000 abstract 1
- IUVCFHHAEHNCFT-INIZCTEOSA-N 2-[(1s)-1-[4-amino-3-(3-fluoro-4-propan-2-yloxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)chromen-4-one Chemical compound C1=C(F)C(OC(C)C)=CC=C1C(C1=C(N)N=CN=C11)=NN1[C@@H](C)C1=C(C=2C=C(F)C=CC=2)C(=O)C2=CC(F)=CC=C2O1 IUVCFHHAEHNCFT-INIZCTEOSA-N 0.000 abstract 1
- KTBSXLIQKWEBRB-UHFFFAOYSA-N 2-[1-[1-[3-fluoro-2-(trifluoromethyl)pyridine-4-carbonyl]piperidin-4-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile Chemical compound C1=CN=C(C(F)(F)F)C(F)=C1C(=O)N1CCC(N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CC1 KTBSXLIQKWEBRB-UHFFFAOYSA-N 0.000 abstract 1
- MCIDWGZGWVSZMK-UHFFFAOYSA-N 2-[6-(1h-indol-4-yl)-1h-indazol-4-yl]-5-[(4-propan-2-ylpiperazin-1-yl)methyl]-1,3-oxazole Chemical compound C1CN(C(C)C)CCN1CC1=CN=C(C=2C=3C=NNC=3C=C(C=2)C=2C=3C=CNC=3C=CC=2)O1 MCIDWGZGWVSZMK-UHFFFAOYSA-N 0.000 abstract 1
- QINPEPAQOBZPOF-UHFFFAOYSA-N 2-amino-n-[3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide Chemical compound COC1=CC=C(Cl)C(NC=2C(=NC3=CC=CC=C3N=2)NS(=O)(=O)C=2C=C(NC(=O)C(C)(C)N)C=CC=2)=C1 QINPEPAQOBZPOF-UHFFFAOYSA-N 0.000 abstract 1
- XTKLTGBKIDQGQL-UHFFFAOYSA-N 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-morpholin-4-ylbenzimidazole-4-carboxylic acid Chemical compound CC1=NC2=C(C(O)=O)C=C(N3CCOCC3)C=C2N1CC1=CC=CC(C(F)(F)F)=C1C XTKLTGBKIDQGQL-UHFFFAOYSA-N 0.000 abstract 1
- CVICEEPAFUYBJG-UHFFFAOYSA-N 5-chloro-2,2-difluoro-1,3-benzodioxole Chemical group C1=C(Cl)C=C2OC(F)(F)OC2=C1 CVICEEPAFUYBJG-UHFFFAOYSA-N 0.000 abstract 1
- PDOQBOJDRPLBQU-QMMMGPOBSA-N 5-chloro-2-n-[(1s)-1-(5-fluoropyrimidin-2-yl)ethyl]-4-n-(5-methyl-1h-pyrazol-3-yl)pyrimidine-2,4-diamine Chemical compound N([C@@H](C)C=1N=CC(F)=CN=1)C(N=1)=NC=C(Cl)C=1NC=1C=C(C)NN=1 PDOQBOJDRPLBQU-QMMMGPOBSA-N 0.000 abstract 1
- CPRAGQJXBLMUEL-UHFFFAOYSA-N 9-(1-anilinoethyl)-7-methyl-2-(4-morpholinyl)-4-pyrido[1,2-a]pyrimidinone Chemical compound C=1C(C)=CN(C(C=C(N=2)N3CCOCC3)=O)C=2C=1C(C)NC1=CC=CC=C1 CPRAGQJXBLMUEL-UHFFFAOYSA-N 0.000 abstract 1
- 229960005531 AMG 319 Drugs 0.000 abstract 1
- SQSZANZGUXWJEA-UHFFFAOYSA-N Gandotinib Chemical compound N1C(C)=CC(NC2=NN3C(CC=4C(=CC(Cl)=CC=4)F)=C(C)N=C3C(CN3CCOCC3)=C2)=N1 SQSZANZGUXWJEA-UHFFFAOYSA-N 0.000 abstract 1
- 239000002144 L01XE18 - Ruxolitinib Substances 0.000 abstract 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 abstract 1
- JOOXLOJCABQBSG-UHFFFAOYSA-N N-tert-butyl-3-[[5-methyl-2-[4-[2-(1-pyrrolidinyl)ethoxy]anilino]-4-pyrimidinyl]amino]benzenesulfonamide Chemical compound N1=C(NC=2C=C(C=CC=2)S(=O)(=O)NC(C)(C)C)C(C)=CN=C1NC(C=C1)=CC=C1OCCN1CCCC1 JOOXLOJCABQBSG-UHFFFAOYSA-N 0.000 abstract 1
- 108091007960 PI3Ks Proteins 0.000 abstract 1
- QIUASFSNWYMDFS-NILGECQDSA-N PX-866 Chemical compound CC(=O)O[C@@H]1C[C@]2(C)C(=O)CC[C@H]2C2=C1[C@@]1(C)[C@@H](COC)OC(=O)\C(=C\N(CC=C)CC=C)C1=C(O)C2=O QIUASFSNWYMDFS-NILGECQDSA-N 0.000 abstract 1
- 239000004012 Tofacitinib Substances 0.000 abstract 1
- HGVNLRPZOWWDKD-UHFFFAOYSA-N ZSTK-474 Chemical compound FC(F)C1=NC2=CC=CC=C2N1C(N=1)=NC(N2CCOCC2)=NC=1N1CCOCC1 HGVNLRPZOWWDKD-UHFFFAOYSA-N 0.000 abstract 1
- 208000017733 acquired polycythemia vera Diseases 0.000 abstract 1
- 229950000971 baricitinib Drugs 0.000 abstract 1
- XUZMWHLSFXCVMG-UHFFFAOYSA-N baricitinib Chemical compound C1N(S(=O)(=O)CC)CC1(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 XUZMWHLSFXCVMG-UHFFFAOYSA-N 0.000 abstract 1
- PZBCKZWLPGJMAO-UHFFFAOYSA-N copanlisib Chemical compound C1=CC=2C3=NCCN3C(NC(=O)C=3C=NC(N)=NC=3)=NC=2C(OC)=C1OCCCN1CCOCC1 PZBCKZWLPGJMAO-UHFFFAOYSA-N 0.000 abstract 1
- 229950006418 dactolisib Drugs 0.000 abstract 1
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical compound O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 abstract 1
- 229950008830 decernotinib Drugs 0.000 abstract 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229950003487 fedratinib Drugs 0.000 abstract 1
- 229950008908 gandotinib Drugs 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 206010028537 myelofibrosis Diseases 0.000 abstract 1
- KWRYMZHCQIOOEB-LBPRGKRZSA-N n-[(1s)-1-(7-fluoro-2-pyridin-2-ylquinolin-3-yl)ethyl]-7h-purin-6-amine Chemical compound C1([C@@H](NC=2C=3N=CNC=3N=CN=2)C)=CC2=CC=C(F)C=C2N=C1C1=CC=CC=N1 KWRYMZHCQIOOEB-LBPRGKRZSA-N 0.000 abstract 1
- 229950011410 pacritinib Drugs 0.000 abstract 1
- HWXVIOGONBBTBY-ONEGZZNKSA-N pacritinib Chemical compound C=1C=C(C=2)NC(N=3)=NC=CC=3C(C=3)=CC=CC=3COC\C=C\COCC=2C=1OCCN1CCCC1 HWXVIOGONBBTBY-ONEGZZNKSA-N 0.000 abstract 1
- LHNIIDJUOCFXAP-UHFFFAOYSA-N pictrelisib Chemical compound C1CN(S(=O)(=O)C)CCN1CC1=CC2=NC(C=3C=4C=NNC=4C=CC=3)=NC(N3CCOCC3)=C2S1 LHNIIDJUOCFXAP-UHFFFAOYSA-N 0.000 abstract 1
- 208000037244 polycythemia vera Diseases 0.000 abstract 1
- 208000003476 primary myelofibrosis Diseases 0.000 abstract 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 229960000215 ruxolitinib Drugs 0.000 abstract 1
- HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical group C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 abstract 1
- BLGWHBSBBJNKJO-UHFFFAOYSA-N serabelisib Chemical compound C=1C=C2OC(N)=NC2=CC=1C(=CN12)C=CC1=NC=C2C(=O)N1CCOCC1 BLGWHBSBBJNKJO-UHFFFAOYSA-N 0.000 abstract 1
- 229960001350 tofacitinib Drugs 0.000 abstract 1
- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 abstract 1
Classifications
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
En la presente se proporcionan métodos, composiciones, y kits para tratar trastornos mieloproliferativos o neoplasmas, inclusive policitemia vera, mielofibrosis primaria, trombocitemia y trombocitemia esencial. Reivindicación 1: Un método para tratar un trastorno hiperproliferativo, que comprende administrar a un paciente una cantidad terapéuticamente eficaz de inhibidor de JAK y una cantidad terapéuticamente eficaz de inhibidor de PI3K. Reivindicación 2: El método de la reivindicación 1, donde el inhibidor de JAK se selecciona del grupo que consiste en ruxolitinib, fedratinib, tofacitinib, baricitinib, Iestaurtinib, pacritinib, decernotinib, XL019, AZD1480, INCB039110, LY2784544, BMS911543, NS018, GLPG0634, GLPG0788 o N-(cianometil)-4-[2-(4-morfolinoanilino)pirimidin-4-iI]benzamida; o sus sales farmacéuticamente aceptables. Reivindicación 3: El método de cualquiera de las reivindicaciones 1 - 2, donde el inhibidor de JAK se administra con una dosis entre 15 y 300 mg. Reivindicación 4: El método de cualquiera de las reivindicaciones 1 - 3, donde el inhibidor de PI3K se selecciona del grupo de XL147, BKM120, GDC-0941, BAY80-6946, PX-866, CH5132799, XL756, BEZ235, y GDC-0980, wortmanina, LY294002, PI3K II, TGR-1202, AMG-319, GSK2269557, X-339, X-414, RP5090, KAR4141, XL499, OXY111A, IPI-145, IPI-443, GSK2636771, BAY 10824391, buparlisib, BYL719, RG7604, MLN1117, WX-037, AEZS-129, PA799, ZSTK474, AS252424, TGX221, TG100115, IC87114, (S)-2-(1-((9H-purin-6-iI)amino)propil)-5-flúor-3-fenilquinazolin-4(3H)-ona, (S)-2-(1-((9H-purin-6-il)amino)etil)-6-flúor-3-fenilquinazolin-4(3H)-ona, (S)-2,4-diamino-6-(((5-cloro-8-flúor-4-oxo-3-(piridin-3-il)-3,4-dihidroquinazolin-2-il)(ciclopropil)metil)amino)pirimidina-5-carbonitrilo, (S)-3-(1-((9H-purin-6-il)amino)etil)-8-cloro-2-fenilisoquinolin-1(2H)-ona, (S)-2,4-diamino-6-(ciclopropil(5,8-dicloro-4-oxo-3-(piridin-3-il)-3,4-dihidroquinazolin-2-il)metilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5-cloro-3-(4-metiIpiridin-3-iI)-4-oxo-3,4-dihidroquinazolin-2-il)etilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5-cloro-3-(5-flúor-4-metilpiridin-3-il)-4-oxo-3,4-dihidroquinazolin-2-iI)etilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5-cloro-4-oxo-3-(piridin-3-il)-3,4-dihidroquinazolin-2-iI)etilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5-cloro-3-(5-fluoropiridin-3-il)-4-oxo-3,4-dihidroquinazolin-2-iI)etilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5-metil-4-oxo-3-(piridin-3-il)-3,4-dihidroquinazolin-2-iI)etilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5-cloro-3-(5-metilpiridin-3-il)-4-oxo-3,4-dihidroquinazoIin-2-iI)etiIamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-((5-cloro-3-(5-fluoropiridin-3-il)-4-oxo-3,4-dihidroquinazolin-2-il)(ciclopropil)metilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5-cloro-8-flúor-4-oxo-3-(piridin-3-il)-3,4-dihidroquinazolin-2-iI)-2-ciclopropiletilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5,8-dicloro-4-oxo-3-(piridin-3-il)-3,4-dihidroquinazoIin-2-il)etilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5,8-dicloro-3-(5-fluoropiridin-3-il)-4-oxo-3,4-dihidroquinazolin-2-il)etilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-(1-(5-cloro-8-flúor-3-(5-fluoropiridin-3-il)-4-oxo-3,4-dihidroquinazolin-2-il)etilamino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-((1-(5-cloro-3-(3-cianofenil)-4-oxo-3,4-dihidroquinazolin-2-il)etil)amino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-((1-(3-(3-cianofenil)-6-flúor-4-oxo-3,4-dihidroquinazolin-2-iI)etil)amino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-((1-(8-cloro-4-oxo-3-fenil-3,4-dihidroquinazolin-2-il)etil)amino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-((1-(3-(3,5-difluorofenil)-5,6-diflúor-4-oxo-3,4-dihidroquinazolin-2-il)etil)amino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-((1-(3-(3,5-difluorofenil)-4-oxo-3,4-dihidroquinazolin-2-il)propil)amino)pirimidina-5-carbonitrilo, (S)-2,4-diamino-6-((1-(3-(3-cianofenil)-5-(difluorometil)-4-oxo-3,4-dihidroquinazoIin-2-iI)etil)amino)pirimidina-5-carbonitrilo; o una de sus sales farmacéuticamente aceptables. Reivindicación 5: El método de cualquiera de las reivindicaciones 1 - 4, donde e inhibidor de PI3K se administra con una dosis entre 10 mg y 300 mg.
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| US201361909072P | 2013-11-26 | 2013-11-26 |
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| TW (1) | TW201609105A (es) |
| WO (1) | WO2015081127A2 (es) |
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-
2014
- 2014-11-25 US US14/553,825 patent/US20150148345A1/en not_active Abandoned
- 2014-11-25 JP JP2016554833A patent/JP2016537433A/ja active Pending
- 2014-11-25 WO PCT/US2014/067472 patent/WO2015081127A2/en not_active Ceased
- 2014-11-25 CA CA2931615A patent/CA2931615A1/en not_active Abandoned
- 2014-11-25 AU AU2014354769A patent/AU2014354769A1/en not_active Abandoned
- 2014-11-25 EP EP14819169.5A patent/EP3074016A2/en not_active Withdrawn
- 2014-11-26 TW TW103141006A patent/TW201609105A/zh unknown
- 2014-11-26 AR ARP140104419A patent/AR098534A1/es unknown
-
2016
- 2016-06-08 US US15/177,031 patent/US20160279135A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20160279135A1 (en) | 2016-09-29 |
| EP3074016A2 (en) | 2016-10-05 |
| AU2014354769A1 (en) | 2016-05-26 |
| CA2931615A1 (en) | 2015-06-04 |
| JP2016537433A (ja) | 2016-12-01 |
| WO2015081127A2 (en) | 2015-06-04 |
| WO2015081127A3 (en) | 2015-09-03 |
| TW201609105A (zh) | 2016-03-16 |
| US20150148345A1 (en) | 2015-05-28 |
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