ME02763B - Derivati bipirazola kao inhibitori jak - Google Patents
Derivati bipirazola kao inhibitori jakInfo
- Publication number
- ME02763B ME02763B MEP-2017-116A MEP2017116A ME02763B ME 02763 B ME02763 B ME 02763B ME P2017116 A MEP2017116 A ME P2017116A ME 02763 B ME02763 B ME 02763B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- bipyrazol
- cyanomethyl
- Prior art date
Links
- YGAILVDTGIMZAB-UHFFFAOYSA-N 3-pyrazol-3-ylidenepyrazole Chemical class N1=NC=CC1=C1N=NC=C1 YGAILVDTGIMZAB-UHFFFAOYSA-N 0.000 title 1
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 93
- 150000003839 salts Chemical class 0.000 claims 33
- 125000004093 cyano group Chemical group *C#N 0.000 claims 28
- 150000001875 compounds Chemical class 0.000 claims 27
- 125000001424 substituent group Chemical group 0.000 claims 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 17
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 12
- 125000001309 chloro group Chemical group Cl* 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 9
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 8
- MSGYSFWCPOBHEV-AWEZNQCLSA-N 4-[3-(cyanomethyl)-3-[4-(3,5-dimethyl-1h-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-n-[(2s)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C1=C(F)C(C(=O)N[C@@H](C)C(F)(F)F)=CC(F)=C1N1CC(CC#N)(N2N=CC(=C2)C2=C(NN=C2C)C)C1 MSGYSFWCPOBHEV-AWEZNQCLSA-N 0.000 claims 7
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 7
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 206010028537 myelofibrosis Diseases 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- -1 C1-3 HaloAlkoxy Chemical group 0.000 claims 6
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 6
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 6
- 208000003476 primary myelofibrosis Diseases 0.000 claims 6
- 208000023275 Autoimmune disease Diseases 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 125000006601 (C1-C3) alkylcarbamyl group Chemical group 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims 4
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 208000017520 skin disease Diseases 0.000 claims 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical class OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 3
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 3
- 235000011007 phosphoric acid Nutrition 0.000 claims 3
- 208000037244 polycythemia vera Diseases 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 2
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 claims 2
- 125000006593 (C2-C3) alkynyl group Chemical group 0.000 claims 2
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 2
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 2
- 206010038272 Refractory anaemia with ringed sideroblasts Diseases 0.000 claims 2
- 208000033501 Refractory anemia with excess blasts Diseases 0.000 claims 2
- 206010072684 Refractory cytopenia with unilineage dysplasia Diseases 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 208000013685 acquired idiopathic sideroblastic anemia Diseases 0.000 claims 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 208000016586 myelodysplastic syndrome with excess blasts Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 1
- PKGWUYXTDWCQPT-ZDUSSCGKSA-N 4-[3-(cyanomethyl)-3-[3-(hydroxymethyl)-4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C[C@H](NC(=O)c1cc(F)c(cc1F)N1CC(CC#N)(C1)n1cc(c(CO)n1)-c1c[nH]nc1C)C(F)(F)F PKGWUYXTDWCQPT-ZDUSSCGKSA-N 0.000 claims 1
- YBWASPQEFFRUHU-LBPRGKRZSA-N 4-[3-(cyanomethyl)-3-[4-(1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C[C@H](NC(=O)c1cc(F)c(cc1F)N1CC(CC#N)(C1)n1cc(cn1)-c1cn[nH]c1)C(F)(F)F YBWASPQEFFRUHU-LBPRGKRZSA-N 0.000 claims 1
- XUQIWHXYCLHHCN-UQKRIMTDSA-N 4-[3-(cyanomethyl)-3-[4-(3,5-dimethyl-1h-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-n-[(2s)-1,1,1-trifluoropropan-2-yl]benzamide;phosphoric acid Chemical compound OP(O)(O)=O.C1=C(F)C(C(=O)N[C@@H](C)C(F)(F)F)=CC(F)=C1N1CC(CC#N)(N2N=CC(=C2)C2=C(NN=C2C)C)C1 XUQIWHXYCLHHCN-UQKRIMTDSA-N 0.000 claims 1
- PEDUBHMYSRBSPA-ZDUSSCGKSA-N 4-[3-(cyanomethyl)-3-[4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C[C@H](NC(=O)c1cc(F)c(cc1F)N1CC(CC#N)(C1)n1cc(cn1)-c1c[nH]nc1C)C(F)(F)F PEDUBHMYSRBSPA-ZDUSSCGKSA-N 0.000 claims 1
- IADHQAYOJSDLQB-UHFFFAOYSA-N 4-[3-(cyanomethyl)-3-[4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylbenzamide Chemical compound CC(C)NC(=O)c1ccc(cc1)N1CC(CC#N)(C1)n1cc(cn1)-c1c[nH]nc1C IADHQAYOJSDLQB-UHFFFAOYSA-N 0.000 claims 1
- QONJPRQDXVLSFV-LBPRGKRZSA-N 4-[3-(cyanomethyl)-3-[4-[5-(hydroxymethyl)-1H-pyrazol-4-yl]pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C[C@H](NC(=O)c1cc(F)c(cc1F)N1CC(CC#N)(C1)n1cc(cn1)-c1c[nH]nc1CO)C(F)(F)F QONJPRQDXVLSFV-LBPRGKRZSA-N 0.000 claims 1
- WDEZBQCRCIAJPW-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[3-methyl-4-(1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylpyrazine-2-carboxamide Chemical compound CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(c(C)n1)-c1cn[nH]c1 WDEZBQCRCIAJPW-UHFFFAOYSA-N 0.000 claims 1
- UVNZXZQWOUVYIS-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[3-methyl-4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylpyrazine-2-carboxamide Chemical compound CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(c(C)n1)-c1c[nH]nc1C UVNZXZQWOUVYIS-UHFFFAOYSA-N 0.000 claims 1
- IGEAGUKQINLFNW-AWEZNQCLSA-N 5-[3-(cyanomethyl)-3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]pyrazine-2-carboxamide Chemical compound C[C@H](NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(cn1)-c1c(C)n[nH]c1C)C(F)(F)F IGEAGUKQINLFNW-AWEZNQCLSA-N 0.000 claims 1
- JFFRGYYXQJTLOG-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylpyrazine-2-carboxamide Chemical compound CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(cn1)-c1c(C)n[nH]c1C JFFRGYYXQJTLOG-UHFFFAOYSA-N 0.000 claims 1
- WSFLFFVFSPLTTE-ZDUSSCGKSA-N 5-[3-(cyanomethyl)-3-[4-(5-ethyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]pyrazine-2-carboxamide Chemical compound CCc1n[nH]cc1-c1cnn(c1)C1(CC#N)CN(C1)c1cnc(cn1)C(=O)N[C@@H](C)C(F)(F)F WSFLFFVFSPLTTE-ZDUSSCGKSA-N 0.000 claims 1
- KJAVZRGMWQGUNS-ZDUSSCGKSA-N 5-[3-(cyanomethyl)-3-[4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]pyrazine-2-carboxamide Chemical compound C[C@H](NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(cn1)-c1c[nH]nc1C)C(F)(F)F KJAVZRGMWQGUNS-ZDUSSCGKSA-N 0.000 claims 1
- ZNDIFOVCUNVGNF-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylpyrazine-2-carboxamide Chemical compound CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(cn1)-c1c[nH]nc1C ZNDIFOVCUNVGNF-UHFFFAOYSA-N 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000006386 Bone Resorption Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 206010015150 Erythema Diseases 0.000 claims 1
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical class Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 208000034442 Refractory anemia with excess blasts type 1 Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010070834 Sensitisation Diseases 0.000 claims 1
- 206010040880 Skin irritation Diseases 0.000 claims 1
- 206010070835 Skin sensitisation Diseases 0.000 claims 1
- 208000024799 Thyroid disease Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 230000024279 bone resorption Effects 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 235000011167 hydrochloric acid Nutrition 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000012846 myelodysplastic syndrome with excess blasts-1 Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 150000003016 phosphoric acids Chemical class 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 206010067959 refractory cytopenia with multilineage dysplasia Diseases 0.000 claims 1
- 230000008313 sensitization Effects 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 230000036556 skin irritation Effects 0.000 claims 1
- 231100000475 skin irritation Toxicity 0.000 claims 1
- 231100000370 skin sensitisation Toxicity 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid group Chemical class S(O)(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
Classifications
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- C07D403/14—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 three or more hetero 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P19/08—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
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- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- 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
- A61P31/20—Antivirals for DNA 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
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
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Applications Claiming Priority (3)
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| EP14732705.0A EP2997023B9 (en) | 2013-05-17 | 2014-05-16 | Bipyrazole derivatives as jak inhibitors |
| PCT/US2014/038388 WO2014186706A1 (en) | 2013-05-17 | 2014-05-16 | Bipyrazole derivatives as jak inhibitors |
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| MEP-2019-79A ME03355B (me) | 2013-05-17 | 2014-05-16 | Soli bipirazola kao inhibitori jak |
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Country Status (36)
Families Citing this family (77)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| ES2487542T3 (es) | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| WO2010135621A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| PE20120493A1 (es) | 2009-06-29 | 2012-05-20 | Incyte Corp | Pirimidinonas como inhibidores de pi3k |
| WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2764848T3 (es) | 2010-12-20 | 2020-06-04 | Incyte Holdings Corp | N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| KR20230038593A (ko) | 2011-09-02 | 2023-03-20 | 인사이트 홀딩스 코포레이션 | Ｐｉ３ｋ 억제제로서 헤테로시클릴아민 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| US9181271B2 (en) | 2012-11-01 | 2015-11-10 | Incyte Holdings Corporation | Tricyclic fused thiophene derivatives as JAK inhibitors |
| PE20151157A1 (es) | 2012-11-15 | 2015-08-19 | Incyte Corp | Formas de dosificacion de ruxolitinib de liberacion sostenida |
| LT3489239T (lt) | 2013-03-06 | 2022-03-10 | Incyte Holdings Corporation | Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai |
| HRP20231048T1 (hr) * | 2013-05-17 | 2023-12-22 | Incyte Holdings Corporation | Derivati bipirazola kao jak inhibitori |
| UA120499C2 (uk) | 2013-08-07 | 2019-12-26 | Інсайт Корпорейшн | Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1 |
| CR20160449A (es) * | 2014-02-28 | 2016-12-20 | Incyte Corp | Inhibidores de la jak1 para el tratamiento de síndromes mielodisplásicos |
| MA39984B1 (fr) | 2014-04-08 | 2020-12-31 | Incyte Corp | Traitement d'affections malignes par lymphocytes b par un inhibiteur jak et pi3k combiné |
| MA39987A (fr) | 2014-04-30 | 2017-03-08 | Incyte Corp | Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées |
| WO2015184305A1 (en) * | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| WO2016172712A2 (en) | 2015-04-23 | 2016-10-27 | Sydnexis, Inc. | Ophthalmic composition |
| US9421199B2 (en) | 2014-06-24 | 2016-08-23 | Sydnexis, Inc. | Ophthalmic composition |
| US11382909B2 (en) | 2014-09-05 | 2022-07-12 | Sydnexis, Inc. | Ophthalmic composition |
| WO2016130501A1 (en) | 2015-02-09 | 2016-08-18 | Incyte Corporation | Aza-heteroaryl compounds as pi3k-gamma inhibitors |
| PH12017501538B1 (en) | 2015-02-27 | 2024-02-14 | Incyte Holdings Corp | Salts of p13k inhibitor and processes for their preparation |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| CN118453493A (zh) | 2015-05-29 | 2024-08-09 | 西德奈克西斯公司 | D2o稳定化的药物制剂 |
| SI3371190T1 (sl) | 2015-11-06 | 2022-08-31 | Incyte Corporation | Heterociklične spojine kot inhibitorji PI3K gama |
| WO2017120194A1 (en) | 2016-01-05 | 2017-07-13 | Incyte Corporation | Pyridine and pyridimine compounds as pi3k-gamma inhibitors |
| WO2017223414A1 (en) | 2016-06-24 | 2017-12-28 | Incyte Corporation | HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS |
| CN107759623B (zh) * | 2016-08-23 | 2020-08-14 | 苏州旺山旺水生物医药有限公司 | Jak抑制剂的中间体及其制备方法 |
| CN109890817B (zh) * | 2016-09-06 | 2022-06-17 | 豪夫迈·罗氏有限公司 | 8-(氮杂环丁烷-1-基)-[1,2,4]三唑并[1,5-a]吡啶基化合物、其组合物和应用方法 |
| SI3697789T1 (sl) | 2017-10-18 | 2022-04-29 | Incyte Corporation | Kondenzirani imidazolni derivati, substituirani s terciarnimi hidroksi skupinami, kot zaviralci PI3K-gama |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| IL276302B2 (en) | 2018-01-30 | 2023-11-01 | Incyte Corp | Procedures for preparing [1-(3-fluoro-2-(trifluoromethyl(isonicotinyl}piperidine-4-one) |
| CN118490690A (zh) | 2018-02-16 | 2024-08-16 | 因赛特公司 | 用于治疗细胞因子相关的病症的jak1通路抑制剂 |
| US11584961B2 (en) | 2018-03-30 | 2023-02-21 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| SMT202400306T1 (it) * | 2018-03-30 | 2024-09-16 | Incyte Corp | Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak. |
| AU2019252259A1 (en) | 2018-04-13 | 2020-12-03 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| CN108484468A (zh) * | 2018-05-11 | 2018-09-04 | 南京大学 | 芳基氮杂环丁烷类化合物的制备方法 |
| CN112469418A (zh) | 2018-06-01 | 2021-03-09 | 因赛特公司 | 治疗pi3k相关病症的给药方案 |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| CN113490484B (zh) | 2018-10-31 | 2024-08-23 | 因赛特公司 | 治疗血液疾病的组合疗法 |
| CN113692278A (zh) | 2018-12-19 | 2021-11-23 | 因赛特公司 | 用于治疗胃肠道疾病的jak1途径抑制剂 |
| KR20210137087A (ko) | 2019-03-05 | 2021-11-17 | 인사이트 코포레이션 | 만성 폐 동종이식 기능장애의 치료를 위한 jak1 경로 억제제 |
| TW202102222A (zh) * | 2019-03-19 | 2021-01-16 | 美商英塞特公司 | 白斑病之生物標記物 |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| US12360120B2 (en) | 2019-10-10 | 2025-07-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US12203942B2 (en) | 2019-10-10 | 2025-01-21 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US11992490B2 (en) | 2019-10-16 | 2024-05-28 | Incyte Corporation | Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP) |
| WO2021076124A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Use of jak1 inhibitors for the treatment of cutaneous lupus erythematosus and lichen planus (lp) |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| IL297437A (en) | 2020-05-13 | 2022-12-01 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| PE20231102A1 (es) * | 2020-06-02 | 2023-07-19 | Incyte Corp | Procesos para preparar un inhibidor de jak1 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| AU2021329301A1 (en) | 2020-08-18 | 2023-04-13 | Incyte Corporation | Process and intermediates for preparing a JAK1 inhibitor |
| KR20230096973A (ko) | 2020-08-18 | 2023-06-30 | 인사이트 코포레이션 | Jak 저해제를 제조하기 위한 방법 및 중간체 |
| CN112159394B (zh) * | 2020-10-09 | 2021-10-22 | 嘉兴特科罗生物科技有限公司 | 一种作为jak激酶抑制剂的小分子化合物及其用途 |
| MD4255442T2 (ro) | 2020-12-04 | 2025-08-31 | Incyte Corp | Inhibitor al JAK cu un analog al vitaminei D pentru tratamentul bolilor de piele |
| US11957661B2 (en) | 2020-12-08 | 2024-04-16 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of vitiligo |
| CN114099514A (zh) * | 2020-12-29 | 2022-03-01 | 上海岸阔医药科技有限公司 | 预防或治疗egfr功能异常相关的副作用的方法 |
| CA3207859A1 (en) | 2021-01-11 | 2022-07-14 | Incyte Corporation | Combination therapy comprising jak pathway inhibitor and rock inhibitor |
| IL308216A (en) | 2021-05-03 | 2024-01-01 | Incyte Corp | Jak1 pathway inhibitors for the treatment of prurigo nodularis |
| CN118317946A (zh) | 2021-07-12 | 2024-07-09 | 因赛特公司 | 用于制备巴瑞替尼的方法和中间体 |
| JP2025527297A (ja) | 2022-08-05 | 2025-08-20 | インサイト・コーポレイション | Ｊａｋ阻害剤を使用した蕁麻疹の処置 |
| US20240307353A1 (en) | 2023-03-16 | 2024-09-19 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of asthma |
| CN117186078A (zh) * | 2023-11-06 | 2023-12-08 | 药康众拓(北京)医药科技有限公司 | 氘代氮杂环丁烷类jak抑制剂药物及用途 |
| WO2025226637A1 (en) | 2024-04-22 | 2025-10-30 | Incyte Corporation | Combination therapy with an anti-colony stimulating factor 1 receptor antibody and a jak inhibitor |
Family Cites Families (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS60106847U (ja) | 1983-12-27 | 1985-07-20 | 富士重工業株式会社 | 室外後写鏡 |
| JP2650681B2 (ja) | 1987-07-10 | 1997-09-03 | 株式会社ブリヂストン | 空気ばね |
| JPH0515775Y2 (enExample) | 1987-07-13 | 1993-04-26 | ||
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| CN1152031C (zh) | 1998-08-11 | 2004-06-02 | 诺瓦提斯公司 | 具有血管生成抑制活性的异喹啉衍生物 |
| US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
| GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| PL202623B1 (pl) | 2000-06-28 | 2009-07-31 | Smithkline Beecham Plc | Sposób wytwarzania drobno zmielonego preparatu substancji leczniczej, drobno zmielona substancja lecznicza wytworzona tym sposobem i zawierająca ją kompozycja farmaceutyczna |
| AU2002337142B2 (en) | 2001-09-19 | 2007-10-11 | Aventis Pharma S.A. | Indolizines as kinase protein inhibitors |
| TWI302836B (en) | 2001-10-30 | 2008-11-11 | Novartis Ag | Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity |
| PE20040522A1 (es) | 2002-05-29 | 2004-09-28 | Novartis Ag | Derivados de diarilurea dependientes de la cinasa de proteina |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
| JP2008520612A (ja) | 2004-11-24 | 2008-06-19 | ノバルティス アクチエンゲゼルシャフト | ＪＡＫ阻害剤およびＢｃｒ−Ａｂｌ、Ｆｌｔ−３、ＦＡＫまたはＲＡＦキナーゼ阻害剤のうち少なくとも１個の組合せ |
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| BRPI0820544A2 (pt) * | 2007-11-16 | 2015-06-16 | Incyte Corp | 4-pirazolil-n-arilpirimidin-2-aminas e pirazolil-n-heteroarilpirimidin-2-aminas como inibidores de janus cinase |
| ES2602577T3 (es) * | 2008-03-11 | 2017-02-21 | Incyte Holdings Corporation | Derivados de azetidina y ciclobutano como inhibidores de JAK |
| CL2009001884A1 (es) | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| JOP20190231A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| WO2010135621A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| ES2487542T3 (es) | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| WO2011028685A1 (en) * | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| CA2777114C (en) | 2009-10-09 | 2018-10-23 | Incyte Corporation | Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| AU2011217961B2 (en) | 2010-02-18 | 2016-05-05 | Incyte Holdings Corporation | Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| KR20130094710A (ko) | 2010-04-14 | 2013-08-26 | 어레이 바이오파마 인크. | Ｊａｋ 키나아제의 억제제로서 5,7-치환된-이미다조［1,2-ｃ］피리미딘 |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| WO2012076063A1 (en) | 2010-12-10 | 2012-06-14 | Rottapharm S.P.A. | Pyridine amide derivatives as ep4 receptor antagonists |
| SG192910A1 (en) | 2011-02-24 | 2013-09-30 | Massachusetts Inst Technology | ALTERNATIVELY SPLICED mRNA ISOFORMS AS PROGNOSTIC INDICATORS FOR METASTATIC CANCER |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| ES2640911T3 (es) | 2011-09-22 | 2017-11-07 | Merck Sharp & Dohme Corp. | Cicloalquilnitrilpirazolcarboxamidas como inhibidores de la quinasa Janus |
| WO2013173720A1 (en) * | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| US9181271B2 (en) | 2012-11-01 | 2015-11-10 | Incyte Holdings Corporation | Tricyclic fused thiophene derivatives as JAK inhibitors |
| PE20151157A1 (es) | 2012-11-15 | 2015-08-19 | Incyte Corp | Formas de dosificacion de ruxolitinib de liberacion sostenida |
| LT3489239T (lt) | 2013-03-06 | 2022-03-10 | Incyte Holdings Corporation | Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai |
| US9266904B2 (en) | 2013-05-17 | 2016-02-23 | Hoffmann-La Roche Inc. | 6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection |
| HRP20231048T1 (hr) * | 2013-05-17 | 2023-12-22 | Incyte Holdings Corporation | Derivati bipirazola kao jak inhibitori |
| EP2803668A1 (en) | 2013-05-17 | 2014-11-19 | Boehringer Ingelheim International Gmbh | Novel (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles |
| JO3603B1 (ar) | 2013-05-17 | 2020-07-05 | Janssen Sciences Ireland Uc | مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي |
| US9371282B2 (en) | 2013-05-17 | 2016-06-21 | Centrexion Therapeutics Corporation | Somatostatin receptor subtype 4 (SSTR4) agonists |
| UA120499C2 (uk) | 2013-08-07 | 2019-12-26 | Інсайт Корпорейшн | Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1 |
| CR20160449A (es) | 2014-02-28 | 2016-12-20 | Incyte Corp | Inhibidores de la jak1 para el tratamiento de síndromes mielodisplásicos |
| MA39987A (fr) | 2014-04-30 | 2017-03-08 | Incyte Corp | Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| ES2756300T3 (es) | 2014-12-16 | 2020-04-27 | Novartis Ag | Compuestos de ácido isoxazol hidroxámico como inhibidores de LpxC |
| CN118490690A (zh) | 2018-02-16 | 2024-08-16 | 因赛特公司 | 用于治疗细胞因子相关的病症的jak1通路抑制剂 |
| PE20231102A1 (es) | 2020-06-02 | 2023-07-19 | Incyte Corp | Procesos para preparar un inhibidor de jak1 |
| MD4255442T2 (ro) | 2020-12-04 | 2025-08-31 | Incyte Corp | Inhibitor al JAK cu un analog al vitaminei D pentru tratamentul bolilor de piele |
| US11957661B2 (en) | 2020-12-08 | 2024-04-16 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of vitiligo |
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