JPWO2020033955A5 - - Google Patents
Download PDFInfo
- Publication number
- JPWO2020033955A5 JPWO2020033955A5 JP2021531626A JP2021531626A JPWO2020033955A5 JP WO2020033955 A5 JPWO2020033955 A5 JP WO2020033955A5 JP 2021531626 A JP2021531626 A JP 2021531626A JP 2021531626 A JP2021531626 A JP 2021531626A JP WO2020033955 A5 JPWO2020033955 A5 JP WO2020033955A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- disease
- cycloalkyl
- formula
- pruritus
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 37
- 208000003251 Pruritus Diseases 0.000 claims 33
- 206010047642 Vitiligo Diseases 0.000 claims 26
- 229910052799 carbon Inorganic materials 0.000 claims 24
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 23
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 201000004384 Alopecia Diseases 0.000 claims 13
- 230000001363 autoimmune Effects 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 230000001684 chronic effect Effects 0.000 claims 10
- 206010016654 Fibrosis Diseases 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 9
- 231100000360 alopecia Toxicity 0.000 claims 9
- 150000001602 bicycloalkyls Chemical group 0.000 claims 8
- 208000035475 disorder Diseases 0.000 claims 8
- 230000004761 fibrosis Effects 0.000 claims 8
- 230000001404 mediated effect Effects 0.000 claims 8
- 206010025323 Lymphomas Diseases 0.000 claims 7
- 206010000496 acne Diseases 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 206010025135 lupus erythematosus Diseases 0.000 claims 7
- 208000017520 skin disease Diseases 0.000 claims 7
- 208000011580 syndromic disease Diseases 0.000 claims 7
- 208000002874 Acne Vulgaris Diseases 0.000 claims 6
- 208000023275 Autoimmune disease Diseases 0.000 claims 6
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 6
- 230000001154 acute effect Effects 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 208000006673 asthma Diseases 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 6
- 208000017169 kidney disease Diseases 0.000 claims 6
- 206010028537 myelofibrosis Diseases 0.000 claims 6
- 230000037390 scarring Effects 0.000 claims 6
- 201000004681 Psoriasis Diseases 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 208000003476 primary myelofibrosis Diseases 0.000 claims 5
- 206010003645 Atopy Diseases 0.000 claims 4
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 4
- 206010061218 Inflammation Diseases 0.000 claims 4
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 4
- 206010040070 Septic Shock Diseases 0.000 claims 4
- 102100023345 Tyrosine-protein kinase ITK/TSK Human genes 0.000 claims 4
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 4
- 206010047115 Vasculitis Diseases 0.000 claims 4
- 206010003246 arthritis Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 230000002496 gastric effect Effects 0.000 claims 4
- 230000002757 inflammatory effect Effects 0.000 claims 4
- 230000004054 inflammatory process Effects 0.000 claims 4
- 230000003448 neutrophilic effect Effects 0.000 claims 4
- 208000035824 paresthesia Diseases 0.000 claims 4
- 230000009885 systemic effect Effects 0.000 claims 4
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 4
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 206010012442 Dermatitis contact Diseases 0.000 claims 3
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 3
- 208000017604 Hodgkin disease Diseases 0.000 claims 3
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 3
- 206010020751 Hypersensitivity Diseases 0.000 claims 3
- 208000009525 Myocarditis Diseases 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 3
- 206010039710 Scleroderma Diseases 0.000 claims 3
- 206010040047 Sepsis Diseases 0.000 claims 3
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 3
- 206010052779 Transplant rejections Diseases 0.000 claims 3
- 208000024780 Urticaria Diseases 0.000 claims 3
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 3
- 206010068168 androgenetic alopecia Diseases 0.000 claims 3
- 201000002996 androgenic alopecia Diseases 0.000 claims 3
- 201000008937 atopic dermatitis Diseases 0.000 claims 3
- 208000010668 atopic eczema Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 208000019425 cirrhosis of liver Diseases 0.000 claims 3
- 208000010247 contact dermatitis Diseases 0.000 claims 3
- 201000001981 dermatomyositis Diseases 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 208000033679 diabetic kidney disease Diseases 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 230000003176 fibrotic effect Effects 0.000 claims 3
- 208000002557 hidradenitis Diseases 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 230000036210 malignancy Effects 0.000 claims 3
- 208000037244 polycythemia vera Diseases 0.000 claims 3
- 230000035935 pregnancy Effects 0.000 claims 3
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 201000005671 spondyloarthropathy Diseases 0.000 claims 3
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 3
- 206010063409 Acarodermatitis Diseases 0.000 claims 2
- 206010000748 Acute febrile neutrophilic dermatosis Diseases 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 206010001767 Alopecia universalis Diseases 0.000 claims 2
- 206010050245 Autoimmune thrombocytopenia Diseases 0.000 claims 2
- 208000037157 Azotemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 2
- 206010013774 Dry eye Diseases 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 208000010201 Exanthema Diseases 0.000 claims 2
- 201000008808 Fibrosarcoma Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 208000024869 Goodpasture syndrome Diseases 0.000 claims 2
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000006877 Insect Bites and Stings Diseases 0.000 claims 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 2
- 208000002260 Keloid Diseases 0.000 claims 2
- 201000002795 Muckle-Wells syndrome Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 2
- 201000002481 Myositis Diseases 0.000 claims 2
- 206010058105 Neutrophilic dermatosis Diseases 0.000 claims 2
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- 208000030852 Parasitic disease Diseases 0.000 claims 2
- 206010034277 Pemphigoid Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 206010065159 Polychondritis Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
- 206010063837 Reperfusion injury Diseases 0.000 claims 2
- 241000447727 Scabies Species 0.000 claims 2
- 206010039705 Scleritis Diseases 0.000 claims 2
- 208000010265 Sweet syndrome Diseases 0.000 claims 2
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 206010042953 Systemic sclerosis Diseases 0.000 claims 2
- 208000024799 Thyroid disease Diseases 0.000 claims 2
- 206010044248 Toxic shock syndrome Diseases 0.000 claims 2
- 231100000650 Toxic shock syndrome Toxicity 0.000 claims 2
- 206010069351 acute lung injury Diseases 0.000 claims 2
- 208000032775 alopecia universalis congenita Diseases 0.000 claims 2
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 2
- 210000000013 bile duct Anatomy 0.000 claims 2
- 206010006451 bronchitis Diseases 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 206010009887 colitis Diseases 0.000 claims 2
- 208000018631 connective tissue disease Diseases 0.000 claims 2
- 208000022993 cryopyrin-associated periodic syndrome Diseases 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 206010014910 enthesopathy Diseases 0.000 claims 2
- 201000005884 exanthem Diseases 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 210000004209 hair Anatomy 0.000 claims 2
- 230000003676 hair loss Effects 0.000 claims 2
- 210000003128 head Anatomy 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 201000007162 hidradenitis suppurativa Diseases 0.000 claims 2
- 208000030603 inherited susceptibility to asthma Diseases 0.000 claims 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 230000007803 itching Effects 0.000 claims 2
- 210000001117 keloid Anatomy 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 208000028454 lice infestation Diseases 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 210000005036 nerve Anatomy 0.000 claims 2
- 201000005737 orchitis Diseases 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 229960001592 paclitaxel Drugs 0.000 claims 2
- 201000001245 periodontitis Diseases 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 239000008177 pharmaceutical agent Substances 0.000 claims 2
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 2
- 230000001823 pruritic effect Effects 0.000 claims 2
- 208000009954 pyoderma gangrenosum Diseases 0.000 claims 2
- 206010037844 rash Diseases 0.000 claims 2
- 208000002574 reactive arthritis Diseases 0.000 claims 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 2
- 208000005687 scabies Diseases 0.000 claims 2
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 2
- 210000003491 skin Anatomy 0.000 claims 2
- 208000020431 spinal cord injury Diseases 0.000 claims 2
- 230000007863 steatosis Effects 0.000 claims 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 2
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 2
- 208000009852 uremia Diseases 0.000 claims 2
- KWYNRYCEOIQZBK-HZLRFILRSA-N (E)-1-[(2S,5R)-5-[[5-[(1R)-2,2-difluorocyclopropyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-methylpiperidin-1-yl]-4-(dimethylamino)but-2-en-1-one Chemical compound FC1([C@H](C1)C1=CNC=2N=CN=C(C=21)N[C@@H]1CC[C@@H](N(C1)C(\C=C\CN(C)C)=O)C)F KWYNRYCEOIQZBK-HZLRFILRSA-N 0.000 claims 1
- DNHWQEMJLPZUQI-QWHCGFSZSA-N 1-[(2S,5R)-5-[[5-(1-hydroxycyclobutyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-methylpiperidin-1-yl]prop-2-en-1-one Chemical compound OC1(CCC1)C1=CNC=2N=CN=C(C=21)N[C@@H]1CC[C@@H](N(C1)C(C=C)=O)C DNHWQEMJLPZUQI-QWHCGFSZSA-N 0.000 claims 1
- PWLBOGZWJVTIRY-GXTWGEPZSA-N 1-[(2S,5R)-5-[[5-(cyclobutanecarbonyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-methylpiperidin-1-yl]prop-2-en-1-one Chemical compound C1(CCC1)C(=O)C1=CNC=2N=CN=C(C=21)N[C@@H]1CC[C@@H](N(C1)C(C=C)=O)C PWLBOGZWJVTIRY-GXTWGEPZSA-N 0.000 claims 1
- JQGKRVBGJDIOSH-SWLSCSKDSA-N 1-[(2S,5R)-5-[[5-(cyclopropylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-methylpiperidin-1-yl]prop-2-en-1-one Chemical compound C1(CC1)CC1=CNC=2N=CN=C(C=21)N[C@@H]1CC[C@@H](N(C1)C(C=C)=O)C JQGKRVBGJDIOSH-SWLSCSKDSA-N 0.000 claims 1
- KULMFWJHZABAFA-DMDPSCGWSA-N 1-[(2S,5R)-5-[[5-[(1R)-2,2-difluorocyclopropyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-methylpiperidin-1-yl]prop-2-en-1-one Chemical compound FC1([C@H](C1)C1=CNC=2N=CN=C(C=21)N[C@@H]1CC[C@@H](N(C1)C(C=C)=O)C)F KULMFWJHZABAFA-DMDPSCGWSA-N 0.000 claims 1
- JOOXGONBYJJLOS-DYEKYZERSA-N 1-[(2S,5R)-5-[[5-[(1S)-2,2-difluorocyclopropyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-ethylpiperidin-1-yl]prop-2-en-1-one Chemical compound FC1([C@@H](C1)C1=CNC=2N=CN=C(C=21)N[C@@H]1CC[C@@H](N(C1)C(C=C)=O)CC)F JOOXGONBYJJLOS-DYEKYZERSA-N 0.000 claims 1
- UVMRUUAXXSEKBU-HFZMZTSTSA-N 1-[(2S,5R)-5-[[5-[(3S,6S)-2,2-difluorospiro[2.4]heptan-6-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-methylpiperidin-1-yl]prop-2-en-1-one Chemical compound FC1(C[C@]11C[C@H](CC1)C1=CNC=2N=CN=C(C=21)N[C@@H]1CC[C@@H](N(C1)C(C=C)=O)C)F UVMRUUAXXSEKBU-HFZMZTSTSA-N 0.000 claims 1
- WGWWIVYXVXQCLC-IACUBPJLSA-N 1-[(2S,5R)-5-[[5-[[(1R)-2,2-difluorocyclopropyl]methyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-methylpiperidin-1-yl]prop-2-en-1-one Chemical compound FC1([C@@H](C1)CC1=CNC=2N=CN=C(C=21)N[C@@H]1CC[C@@H](N(C1)C(C=C)=O)C)F WGWWIVYXVXQCLC-IACUBPJLSA-N 0.000 claims 1
- BMTKJPSVZZUNBN-CFVMTHIKSA-N 1-[(2S,5S)-5-[[5-[(1R)-2,2-difluorocyclopropyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2-propan-2-ylpiperidin-1-yl]prop-2-en-1-one Chemical compound FC1([C@H](C1)C1=CNC=2N=CN=C(C=21)N[C@H]1CC[C@H](N(C1)C(C=C)=O)C(C)C)F BMTKJPSVZZUNBN-CFVMTHIKSA-N 0.000 claims 1
- OTLLEIBWKHEHGU-UHFFFAOYSA-N 2-[5-[[5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy]-3,4-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,5-dihydroxy-4-phosphonooxyhexanedioic acid Chemical compound C1=NC=2C(N)=NC=NC=2N1C(C(C1O)O)OC1COC1C(CO)OC(OC(C(O)C(OP(O)(O)=O)C(O)C(O)=O)C(O)=O)C(O)C1O OTLLEIBWKHEHGU-UHFFFAOYSA-N 0.000 claims 1
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims 1
- JHNLZOVBAQWGQU-UHFFFAOYSA-N 380814_sial Chemical compound CS(O)(=O)=O.O=P(=O)OP(=O)=O JHNLZOVBAQWGQU-UHFFFAOYSA-N 0.000 claims 1
- -1 5-((3R,5R)-1,1-difluorospiro[2.4]heptan-5-yl)-7H-pyrrolo[2,3-d]pyrimidine Chemical compound 0.000 claims 1
- 208000007122 AIDS-Associated Nephropathy Diseases 0.000 claims 1
- 206010000503 Acne cystic Diseases 0.000 claims 1
- HGINCPLSRVDWNT-UHFFFAOYSA-N Acrolein Chemical compound C=CC=O HGINCPLSRVDWNT-UHFFFAOYSA-N 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010033646 Acute and chronic pancreatitis Diseases 0.000 claims 1
- 206010000830 Acute leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 208000026326 Adult-onset Still disease Diseases 0.000 claims 1
- 208000032671 Allergic granulomatous angiitis Diseases 0.000 claims 1
- 206010001766 Alopecia totalis Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002198 Anaphylactic reaction Diseases 0.000 claims 1
- 206010059245 Angiopathy Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 200000000007 Arterial disease Diseases 0.000 claims 1
- 206010003267 Arthritis reactive Diseases 0.000 claims 1
- 208000000104 Arthus reaction Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000004300 Atrophic Gastritis Diseases 0.000 claims 1
- 208000022715 Autoinflammatory syndrome Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 208000009299 Benign Mucous Membrane Pemphigoid Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010006448 Bronchiolitis Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 206010073960 CANDLE syndrome Diseases 0.000 claims 1
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010062746 Carditis Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 201000006082 Chickenpox Diseases 0.000 claims 1
- 206010008635 Cholestasis Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000006344 Churg-Strauss Syndrome Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000026372 Congenital cystic kidney disease Diseases 0.000 claims 1
- 206010056489 Coronary artery restenosis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000026292 Cystic Kidney disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 239000012623 DNA damaging agent Substances 0.000 claims 1
- 208000001840 Dandruff Diseases 0.000 claims 1
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 1
- 206010011878 Deafness Diseases 0.000 claims 1
- 206010012434 Dermatitis allergic Diseases 0.000 claims 1
- 206010048768 Dermatosis Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000003024 Diffuse alopecia Diseases 0.000 claims 1
- 208000019872 Drug Eruptions Diseases 0.000 claims 1
- 208000017701 Endocrine disease Diseases 0.000 claims 1
- 208000004232 Enteritis Diseases 0.000 claims 1
- 208000018428 Eosinophilic granulomatosis with polyangiitis Diseases 0.000 claims 1
- 206010015084 Episcleritis Diseases 0.000 claims 1
- 206010015150 Erythema Diseases 0.000 claims 1
- 206010016207 Familial Mediterranean fever Diseases 0.000 claims 1
- 208000007659 Fibroadenoma Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- 206010016936 Folliculitis Diseases 0.000 claims 1
- 206010017533 Fungal infection Diseases 0.000 claims 1
- 206010058872 Fungal sepsis Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 208000036495 Gastritis atrophic Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010051920 Glomerulonephropathy Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 206010070737 HIV associated nephropathy Diseases 0.000 claims 1
- 208000004547 Hallucinations Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 206010019668 Hepatic fibrosis Diseases 0.000 claims 1
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 206010019939 Herpes gestationis Diseases 0.000 claims 1
- 241000238631 Hexapoda Species 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010058490 Hyperoxia Diseases 0.000 claims 1
- 201000002980 Hyperparathyroidism Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010020843 Hyperthermia Diseases 0.000 claims 1
- 206010062767 Hypophysitis Diseases 0.000 claims 1
- 241000248486 Hypotrichia Species 0.000 claims 1
- 201000009495 Hypotrichosis Diseases 0.000 claims 1
- XQFRJNBWHJMXHO-RRKCRQDMSA-N IDUR Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(I)=C1 XQFRJNBWHJMXHO-RRKCRQDMSA-N 0.000 claims 1
- XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 claims 1
- XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 208000024934 IgG4-related mediastinitis Diseases 0.000 claims 1
- 208000014919 IgG4-related retroperitoneal fibrosis Diseases 0.000 claims 1
- 208000004575 Infectious Arthritis Diseases 0.000 claims 1
- 206010061217 Infestation Diseases 0.000 claims 1
- 108010050904 Interferons Proteins 0.000 claims 1
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- 208000015710 Iron-Deficiency Anemia Diseases 0.000 claims 1
- 206010023126 Jaundice Diseases 0.000 claims 1
- 208000012528 Juvenile dermatomyositis Diseases 0.000 claims 1
- 206010023330 Keloid scar Diseases 0.000 claims 1
- 206010023347 Keratoacanthoma Diseases 0.000 claims 1
- 208000009319 Keratoconjunctivitis Sicca Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010048649 Koebner phenomenon Diseases 0.000 claims 1
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 1
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims 1
- 201000010743 Lambert-Eaton myasthenic syndrome Diseases 0.000 claims 1
- 206010024434 Lichen sclerosus Diseases 0.000 claims 1
- 208000012309 Linear IgA disease Diseases 0.000 claims 1
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims 1
- 208000004852 Lung Injury Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 208000016604 Lyme disease Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 229940124647 MEK inhibitor Drugs 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000002805 Mediastinal fibrosis Diseases 0.000 claims 1
- 208000027530 Meniere disease Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010054949 Metaplasia Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000003250 Mixed connective tissue disease Diseases 0.000 claims 1
- 208000012192 Mucous membrane pemphigoid Diseases 0.000 claims 1
- 206010028372 Muscular weakness Diseases 0.000 claims 1
- 208000000112 Myalgia Diseases 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 1
- 208000001738 Nervous System Trauma Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 201000009053 Neurodermatitis Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 206010030216 Oesophagitis Diseases 0.000 claims 1
- 208000003435 Optic Neuritis Diseases 0.000 claims 1
- 206010031149 Osteitis Diseases 0.000 claims 1
- 206010033165 Ovarian failure Diseases 0.000 claims 1
- 206010033554 Palmoplantar keratoderma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010033733 Papule Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 241000517324 Pediculidae Species 0.000 claims 1
- 241000517307 Pediculus humanus Species 0.000 claims 1
- 208000008223 Pemphigoid Gestationis Diseases 0.000 claims 1
- 201000011152 Pemphigus Diseases 0.000 claims 1
- 208000031845 Pernicious anaemia Diseases 0.000 claims 1
- 208000037581 Persistent Infection Diseases 0.000 claims 1
- 241001674048 Phthiraptera Species 0.000 claims 1
- 206010036805 Progressive massive fibrosis Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000001818 Pseudofolliculitis barbae Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010037549 Purpura Diseases 0.000 claims 1
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 claims 1
- 206010037876 Rash papular Diseases 0.000 claims 1
- 208000033464 Reiter syndrome Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 208000004756 Respiratory Insufficiency Diseases 0.000 claims 1
- 206010038748 Restrictive cardiomyopathy Diseases 0.000 claims 1
- 201000001949 Retinal Vasculitis Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 206010038979 Retroperitoneal fibrosis Diseases 0.000 claims 1
- 208000027066 STING-associated vasculopathy with onset in infancy Diseases 0.000 claims 1
- 206010039580 Scar Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 206010039793 Seborrhoeic dermatitis Diseases 0.000 claims 1
- 206010070834 Sensitisation Diseases 0.000 claims 1
- 206010053879 Sepsis syndrome Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010040880 Skin irritation Diseases 0.000 claims 1
- 208000006045 Spondylarthropathies Diseases 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010042496 Sunburn Diseases 0.000 claims 1
- 206010042742 Sympathetic ophthalmia Diseases 0.000 claims 1
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims 1
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 229940123237 Taxane Drugs 0.000 claims 1
- 206010043276 Teratoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010043866 Tinea capitis Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010069363 Traumatic lung injury Diseases 0.000 claims 1
- 108060008683 Tumor Necrosis Factor Receptor Proteins 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010054000 Type II hypersensitivity Diseases 0.000 claims 1
- 206010053614 Type III immune complex mediated reaction Diseases 0.000 claims 1
- 206010053613 Type IV hypersensitivity reaction Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010046750 Urticaria papular Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010046980 Varicella Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 206010057295 Vocal cord inflammation Diseases 0.000 claims 1
- 208000000208 Wet Macular Degeneration Diseases 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 206010048222 Xerosis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 230000001476 alcoholic effect Effects 0.000 claims 1
- 201000009961 allergic asthma Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 208000004631 alopecia areata Diseases 0.000 claims 1
- 230000036783 anaphylactic response Effects 0.000 claims 1
- 208000003455 anaphylaxis Diseases 0.000 claims 1
- 208000007502 anemia Diseases 0.000 claims 1
- 230000002491 angiogenic effect Effects 0.000 claims 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 229940100197 antimetabolite Drugs 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- 206010003230 arteritis Diseases 0.000 claims 1
- 229960003852 atezolizumab Drugs 0.000 claims 1
- 230000003143 atherosclerotic effect Effects 0.000 claims 1
- 208000010216 atopic IgE responsiveness Diseases 0.000 claims 1
- 230000001746 atrial effect Effects 0.000 claims 1
- 230000006472 autoimmune response Effects 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 230000005784 autoimmunity Effects 0.000 claims 1
- 229950002916 avelumab Drugs 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 208000018339 bone inflammation disease Diseases 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 208000019664 bone resorption disease Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 201000003149 breast fibroadenoma Diseases 0.000 claims 1
- 208000000594 bullous pemphigoid Diseases 0.000 claims 1
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 1
- 229940127093 camptothecin Drugs 0.000 claims 1
- 208000035269 cancer or benign tumor Diseases 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 190000008236 carboplatin Chemical compound 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 201000010415 childhood type dermatomyositis Diseases 0.000 claims 1
- 230000007870 cholestasis Effects 0.000 claims 1
- 231100000359 cholestasis Toxicity 0.000 claims 1
- 208000016644 chronic atrophic gastritis Diseases 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000024207 chronic leukemia Diseases 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims 1
- 201000010002 cicatricial pemphigoid Diseases 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 230000019771 cognition Effects 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 210000002777 columnar cell Anatomy 0.000 claims 1
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims 1
- 229960002448 dasatinib Drugs 0.000 claims 1
- 231100000895 deafness Toxicity 0.000 claims 1
- 208000010643 digestive system disease Diseases 0.000 claims 1
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 208000000718 duodenal ulcer Diseases 0.000 claims 1
- 229950009791 durvalumab Drugs 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 206010014599 encephalitis Diseases 0.000 claims 1
- 201000002491 encephalomyelitis Diseases 0.000 claims 1
- 201000010048 endomyocardial fibrosis Diseases 0.000 claims 1
- 230000002327 eosinophilic effect Effects 0.000 claims 1
- 201000001561 eosinophilic gastritis Diseases 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 231100000321 erythema Toxicity 0.000 claims 1
- 210000003743 erythrocyte Anatomy 0.000 claims 1
- 208000006881 esophagitis Diseases 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 239000002095 exotoxin Substances 0.000 claims 1
- 231100000776 exotoxin Toxicity 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 210000004709 eyebrow Anatomy 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 206010016629 fibroma Diseases 0.000 claims 1
- 230000002344 fibroplastic effect Effects 0.000 claims 1
- 206010016766 flatulence Diseases 0.000 claims 1
- 229960002949 fluorouracil Drugs 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
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 208000007565 gingivitis Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 201000010912 granulomatous dermatitis Diseases 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000035876 healing Effects 0.000 claims 1
- 208000016354 hearing loss disease Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 230000002949 hemolytic effect Effects 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 210000005260 human cell Anatomy 0.000 claims 1
- 230000000222 hyperoxic effect Effects 0.000 claims 1
- 206010020718 hyperplasia Diseases 0.000 claims 1
- 230000036031 hyperthermia Effects 0.000 claims 1
- 229960000908 idarubicin Drugs 0.000 claims 1
- 229960002411 imatinib Drugs 0.000 claims 1
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 230000036039 immunity Effects 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 208000021646 inflammation of heart layer Diseases 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 230000000968 intestinal effect Effects 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 208000001024 intrahepatic cholestasis Diseases 0.000 claims 1
- 230000007872 intrahepatic cholestasis Effects 0.000 claims 1
- 208000037906 ischaemic injury Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 230000000366 juvenile effect Effects 0.000 claims 1
- 206010023332 keratitis Diseases 0.000 claims 1
- 206010023365 keratopathy Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 230000001418 larval effect Effects 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 201000010260 leiomyoma Diseases 0.000 claims 1
- 201000011486 lichen planus Diseases 0.000 claims 1
- 208000006132 lipodystrophy Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 231100000515 lung injury Toxicity 0.000 claims 1
- 208000019420 lymphoid neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000006512 mast cell neoplasm Diseases 0.000 claims 1
- 208000008585 mastocytosis Diseases 0.000 claims 1
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 1
- 230000009245 menopause Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 239000002184 metal Substances 0.000 claims 1
- 229910052751 metal Inorganic materials 0.000 claims 1
- 230000015689 metaplastic ossification Effects 0.000 claims 1
- 230000001394 metastastic effect Effects 0.000 claims 1
- 206010061289 metastatic neoplasm Diseases 0.000 claims 1
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 1
- 230000036473 myasthenia Effects 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000005962 mycosis fungoides Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 230000002988 nephrogenic effect Effects 0.000 claims 1
- 230000007383 nerve stimulation Effects 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 208000028412 nervous system injury Diseases 0.000 claims 1
- 230000001537 neural effect Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000007538 neurilemmoma Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000018360 neuromuscular disease Diseases 0.000 claims 1
- 230000005015 neuronal process Effects 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 229960001346 nilotinib Drugs 0.000 claims 1
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims 1
- 229960003301 nivolumab Drugs 0.000 claims 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000002674 obstructive nephropathy Diseases 0.000 claims 1
- 229940005483 opioid analgesics Drugs 0.000 claims 1
- 210000003300 oropharynx Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000004535 ovarian dysfunction Diseases 0.000 claims 1
- 231100000539 ovarian failure Toxicity 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 229960001756 oxaliplatin Drugs 0.000 claims 1
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims 1
- 230000036407 pain Effects 0.000 claims 1
- 201000008743 palmoplantar keratosis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 208000012963 papular rash Diseases 0.000 claims 1
- 208000008664 papular urticaria Diseases 0.000 claims 1
- 230000024241 parasitism Effects 0.000 claims 1
- 230000001936 parietal effect Effects 0.000 claims 1
- 229960002621 pembrolizumab Drugs 0.000 claims 1
- 201000001976 pemphigus vulgaris Diseases 0.000 claims 1
- 230000000737 periodic effect Effects 0.000 claims 1
- 206010034674 peritonitis Diseases 0.000 claims 1
- 230000002085 persistent effect Effects 0.000 claims 1
- 206010034754 petechiae Diseases 0.000 claims 1
- 210000003800 pharynx Anatomy 0.000 claims 1
- 208000017983 photosensitivity disease Diseases 0.000 claims 1
- 201000006292 polyarteritis nodosa Diseases 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 229920001296 polysiloxane Polymers 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000002028 premature Effects 0.000 claims 1
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 201000001474 proteinuria Diseases 0.000 claims 1
- 208000017502 proteosome-associated autoinflammatory syndrome Diseases 0.000 claims 1
- 208000017940 prurigo nodularis Diseases 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 230000001107 psychogenic effect Effects 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 201000004193 respiratory failure Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 210000001525 retina Anatomy 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 231100000241 scar Toxicity 0.000 claims 1
- 206010039667 schwannoma Diseases 0.000 claims 1
- 208000008742 seborrheic dermatitis Diseases 0.000 claims 1
- 230000008313 sensitization Effects 0.000 claims 1
- 230000001953 sensory effect Effects 0.000 claims 1
- 201000001223 septic arthritis Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 206010040400 serum sickness Diseases 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 201000009890 sinusitis Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 231100000475 skin irritation Toxicity 0.000 claims 1
- 230000036556 skin irritation Effects 0.000 claims 1
- 231100000046 skin rash Toxicity 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims 1
- 201000001297 telogen effluvium Diseases 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000021510 thyroid gland disease Diseases 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 208000037816 tissue injury Diseases 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 229950007217 tremelimumab Drugs 0.000 claims 1
- 102000003298 tumor necrosis factor receptor Human genes 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000008026 type II hypersensitivity Effects 0.000 claims 1
- 208000025883 type III hypersensitivity disease Diseases 0.000 claims 1
- 208000027930 type IV hypersensitivity disease Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
- 229960004528 vincristine Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 229960000237 vorinostat Drugs 0.000 claims 1
- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
- JCTMNJJUFWXAMM-MRXNPFEDSA-N 1-[(3R)-3-[[5-(cyclopentylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]prop-2-en-1-one Chemical compound C1(CCCC1)CC1=CNC=2N=CN=C(C=21)N[C@H]1CN(CCC1)C(C=C)=O JCTMNJJUFWXAMM-MRXNPFEDSA-N 0.000 description 2
- YTLFCXVESGQVHK-UONOGXRCSA-N 2-methylpropyl 4-[[(3R,6S)-6-methyl-1-prop-2-enoylpiperidin-3-yl]amino]-7H-pyrrolo[2,3-d]pyrimidine-5-carboxylate Chemical compound C(C=C)(=O)N1C[C@@H](CC[C@@H]1C)NC=1C2=C(N=CN=1)NC=C2C(=O)OCC(C)C YTLFCXVESGQVHK-UONOGXRCSA-N 0.000 description 2
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024200937A JP2025037892A (ja) | 2018-08-10 | 2024-11-18 | ピロロピリミジンitk阻害剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862717400P | 2018-08-10 | 2018-08-10 | |
| US62/717,400 | 2018-08-10 | ||
| PCT/US2019/046182 WO2020033955A1 (en) | 2018-08-10 | 2019-08-12 | Pyrrolopyrimidine itk inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024200937A Division JP2025037892A (ja) | 2018-08-10 | 2024-11-18 | ピロロピリミジンitk阻害剤 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021534244A JP2021534244A (ja) | 2021-12-09 |
| JP2021534244A5 JP2021534244A5 (https=) | 2022-08-29 |
| JPWO2020033955A5 true JPWO2020033955A5 (https=) | 2022-08-29 |
| JP7591500B2 JP7591500B2 (ja) | 2024-11-28 |
Family
ID=69405523
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021531626A Active JP7591500B2 (ja) | 2018-08-10 | 2019-08-12 | ピロロピリミジンitk阻害剤 |
| JP2024200937A Pending JP2025037892A (ja) | 2018-08-10 | 2024-11-18 | ピロロピリミジンitk阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024200937A Pending JP2025037892A (ja) | 2018-08-10 | 2024-11-18 | ピロロピリミジンitk阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (4) | US11021482B2 (https=) |
| EP (1) | EP3833350A4 (https=) |
| JP (2) | JP7591500B2 (https=) |
| KR (1) | KR102849047B1 (https=) |
| CN (2) | CN119080779A (https=) |
| AU (1) | AU2019317625B2 (https=) |
| BR (1) | BR112021002479A2 (https=) |
| CA (1) | CA3109192A1 (https=) |
| IL (1) | IL280593A (https=) |
| MX (1) | MX2021001558A (https=) |
| PH (1) | PH12021550187A1 (https=) |
| SG (1) | SG11202100525SA (https=) |
| WO (1) | WO2020033955A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| EP3710431A4 (en) | 2017-11-03 | 2021-07-07 | Aclaris Therapeutics, Inc. | SUBSTITUTED PYRROLOPYRIMIDINE-BASED JAK INHIBITORS AND THEIR MANUFACTURING AND USE PROCEDURES |
| WO2020033955A1 (en) * | 2018-08-10 | 2020-02-13 | Aclaris Therapeutics, Inc. | Pyrrolopyrimidine itk inhibitors |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| WO2020223728A1 (en) | 2019-05-02 | 2020-11-05 | Aclaris Therapeutics, Inc. | Substituted pyrrolopyridines as jak inhibitors |
| CN114787363A (zh) | 2019-10-01 | 2022-07-22 | 恩派瑞安神经科学公司 | 对真菌进行遗传工程化以调节色胺表达 |
| TW202207918A (zh) * | 2020-05-14 | 2022-03-01 | 美商施萬生物製藥研發Ip有限責任公司 | 腸道選擇性jak3抑制劑的投與 |
| KR102560138B1 (ko) * | 2020-06-15 | 2023-07-27 | 경북대학교 산학협력단 | 신경교세포 표현형 기반의 siRNA 다중 스크리닝을 통해 선별된 신경교세포 인산화효소의 신경염증 조절 용도 |
| CN114887080B (zh) * | 2020-12-08 | 2023-10-31 | 深圳瑞吉生物科技有限公司 | 一种mRNA剂型的免疫抑制剂及其在制备肿瘤治疗药物中的应用 |
| CN113350346B (zh) * | 2021-06-01 | 2023-06-27 | 广西医科大学第一附属医院 | 长春新碱在预防或治疗心肌纤维化中的应用 |
| KR20230019801A (ko) * | 2021-08-02 | 2023-02-09 | 한국화학연구원 | 신규한 피롤로 피리미딘 유도체 화합물, 이의 제조방법, 및 이를 유효성분으로 포함하는 대사성 간질환의 예방 또는 치료용 약학적 조성물 |
| CN113571191A (zh) * | 2021-08-31 | 2021-10-29 | 复旦大学附属中山医院 | 免疫检查点抑制剂相关mace发生风险的预测方法 |
| WO2023110843A1 (en) * | 2021-12-15 | 2023-06-22 | Almirall, S.A. | Heterobicyclic derivatives as itk inhibitors |
| EP4457336A4 (en) | 2021-12-31 | 2026-01-14 | Empyrean Neuroscience Inc | ORGANISMS GENETICALLY MODIFIED TO PRODUCE PSYCHOTROPIC ALKALOIDS |
| EP4615440A1 (en) * | 2022-11-08 | 2025-09-17 | Aclaris Therapeutics, Inc. | Pyrrolopyrimidine compositions for treatment of itk mediated conditions |
| CN116115760A (zh) * | 2022-12-15 | 2023-05-16 | 浙江大学 | Eed抑制剂在制备治疗神经免疫性疾病药物中的应用 |
| WO2025144781A1 (en) * | 2023-12-28 | 2025-07-03 | Aclaris Therapeutics, Inc. | Crystalline polymorph of an itk inhibitor |
| WO2025144783A1 (en) * | 2023-12-28 | 2025-07-03 | Aclaris Therapeutics, Inc. | Methods of synthesizing substituted pyrrolopyrimidine compounds |
| CN117982685B (zh) * | 2024-01-26 | 2025-05-30 | 北京大学人民医院 | 用于骨肉瘤检测的光学分子成像探针及其制备方法和应用 |
| WO2025181247A1 (en) * | 2024-02-28 | 2025-09-04 | Almirall, S.A. | Heterobicyclic derivatives as itk inhibitors |
| WO2025235366A1 (en) * | 2024-05-07 | 2025-11-13 | Aclaris Therapeutics, Inc. | Pyrrolopyrimidine compositions for treatment of atopic dermatitis |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2141916T3 (es) | 1993-11-30 | 2000-04-01 | Searle & Co | Pirazolil-bencenosulfonamidas sustituidas para el tratamiento de la inflamacion. |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| WO2000000202A1 (en) | 1998-06-30 | 2000-01-06 | Parker Hughes Institute | Method for inhibiting c-jun expression using jak-3 inhibitors |
| US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| SE0301372D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
| AR054416A1 (es) | 2004-12-22 | 2007-06-27 | Incyte Corp | Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas. |
| WO2006127587A1 (en) | 2005-05-20 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
| WO2007007919A2 (en) | 2005-07-14 | 2007-01-18 | Astellas Pharma Inc. | Heterocyclic janus kinase 3 inhibitors |
| EP2251341A1 (en) | 2005-07-14 | 2010-11-17 | Astellas Pharma Inc. | Heterocyclic Janus kinase 3 inhibitors |
| EP2455382B1 (en) | 2005-12-13 | 2016-10-26 | Incyte Holdings Corporation | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors |
| US8071779B2 (en) | 2006-12-18 | 2011-12-06 | Inspire Pharmaceuticals, Inc. | Cytoskeletal active rho kinase inhibitor compounds, composition and use |
| EP2123651A4 (en) | 2007-01-12 | 2011-05-04 | Astellas Pharma Inc | CONDENSED PYRIDINE COMPOUND |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| 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. |
| SG176111A1 (en) | 2009-05-22 | 2011-12-29 | Incyte Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| JP5775070B2 (ja) | 2009-05-22 | 2015-09-09 | インサイト・コーポレイションIncyte Corporation | ヤヌスキナーゼ阻害剤としてのピラゾール−4−イル−ピロロ[2,3−d]ピリミジンおよびピロール−3−イル−ピロロ[2,3−d]ピリミジンのN−(ヘテロ)アリール−ピロリジン誘導体 |
| US9273028B2 (en) | 2010-10-29 | 2016-03-01 | Biogen Ma Inc. | Heterocyclic tyrosine kinase inhibitors |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| AU2012295802B2 (en) | 2011-08-12 | 2017-03-30 | Nissan Chemical Industries, Ltd. | Tricyclic heterocyclic compounds and JAK inhibitors |
| EP2788000B1 (en) | 2011-12-06 | 2018-05-30 | Merck Sharp & Dohme Corp. | Pyrrolopyrimidines as janus kinase inhibitors |
| PL2892927T3 (pl) | 2012-09-07 | 2018-11-30 | Regeneron Pharmaceuticals, Inc. | Sposoby leczenia atopowego zapalenia skóry przez podawanie antagonisty IL-4R |
| US9206188B2 (en) * | 2013-04-18 | 2015-12-08 | Arrien Pharmaceuticals Llc | Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors |
| GB2515785A (en) * | 2013-07-03 | 2015-01-07 | Redx Pharma Ltd | Compounds |
| MX368464B (es) * | 2013-12-05 | 2019-10-02 | Pfizer | Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinil o y pirrolo[2,3-d]piridinilo. |
| EP2924026A1 (en) | 2014-03-28 | 2015-09-30 | Novartis Tiergesundheit AG | Aminosulfonylmethylcyclohexanes as JAK inhibitors |
| CR20160525A (es) | 2014-05-14 | 2016-12-20 | Pfizer | Pirazolopiridinas y pirazolopirimidinas |
| WO2016000615A1 (en) * | 2014-07-02 | 2016-01-07 | Sunshine Lake Pharma Co., Ltd. | Heteroaryl compounds and pharmaceutical applications thereof |
| CN105712998B (zh) * | 2014-12-05 | 2019-12-13 | 上海润诺生物科技有限公司 | 氮杂吲哚类衍生物、其制备方法及其在医药上的应用 |
| CA2973597A1 (en) * | 2015-01-23 | 2016-07-28 | Confluence Life Sciences, Inc. | Heterocyclic itk inhibitors for treating inflammation and cancer |
| US10703756B2 (en) * | 2015-05-01 | 2020-07-07 | Pfizer Inc. | Pyrrolo[2,3-D]pyrimidinyl, pyrrolo[2,3-B]pyrazinyl, pyrrolo[2,3-B]pyridinyl acrylamides and epoxides thereof |
| WO2017097224A1 (zh) | 2015-12-11 | 2017-06-15 | 四川科伦博泰生物医药股份有限公司 | 氮杂环丁烷衍生物、其制备方法及用途 |
| RU2714206C1 (ru) * | 2016-06-30 | 2020-02-13 | Даевунг Фармасьютикал Ко., Лтд. | Пиразолопиримидиновые производные в качестве ингибитора киназы |
| TW201811795A (zh) * | 2016-08-24 | 2018-04-01 | 美商亞闊股份有限公司 | 胺基-吡咯并嘧啶酮化合物及其用途 |
| EP3710431A4 (en) | 2017-11-03 | 2021-07-07 | Aclaris Therapeutics, Inc. | SUBSTITUTED PYRROLOPYRIMIDINE-BASED JAK INHIBITORS AND THEIR MANUFACTURING AND USE PROCEDURES |
| US10800775B2 (en) | 2017-11-03 | 2020-10-13 | Aclaris Therapeutics, Inc. | Pyrazolyl pyrrolo[2,3-b]pyrmidine-5-carboxylate analogs and methods of making the same |
| WO2020033955A1 (en) * | 2018-08-10 | 2020-02-13 | Aclaris Therapeutics, Inc. | Pyrrolopyrimidine itk inhibitors |
| CA3123596A1 (en) | 2018-12-19 | 2020-06-25 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of gastrointestinal disease |
| WO2020223728A1 (en) | 2019-05-02 | 2020-11-05 | Aclaris Therapeutics, Inc. | Substituted pyrrolopyridines as jak inhibitors |
| CA3150975A1 (en) | 2019-06-10 | 2020-12-17 | Incyte Corporation | Topical treatment of vitiligo by a jak inhibitor |
| WO2021022178A1 (en) | 2019-07-31 | 2021-02-04 | Aclaris Therapeutics, Inc. | Substituted sulfonamide pyrrolopyridines as jak inhibitors |
-
2019
- 2019-08-12 WO PCT/US2019/046182 patent/WO2020033955A1/en not_active Ceased
- 2019-08-12 EP EP19846283.0A patent/EP3833350A4/en active Pending
- 2019-08-12 KR KR1020217007377A patent/KR102849047B1/ko active Active
- 2019-08-12 CA CA3109192A patent/CA3109192A1/en active Pending
- 2019-08-12 JP JP2021531626A patent/JP7591500B2/ja active Active
- 2019-08-12 CN CN202411055491.XA patent/CN119080779A/zh active Pending
- 2019-08-12 US US16/538,354 patent/US11021482B2/en active Active
- 2019-08-12 SG SG11202100525SA patent/SG11202100525SA/en unknown
- 2019-08-12 CN CN201980066579.2A patent/CN112823005B/zh active Active
- 2019-08-12 BR BR112021002479-4A patent/BR112021002479A2/pt not_active IP Right Cessation
- 2019-08-12 AU AU2019317625A patent/AU2019317625B2/en active Active
- 2019-08-12 MX MX2021001558A patent/MX2021001558A/es unknown
-
2021
- 2021-01-25 PH PH12021550187A patent/PH12021550187A1/en unknown
- 2021-02-02 IL IL280593A patent/IL280593A/en unknown
- 2021-04-21 US US17/236,531 patent/US11820775B2/en active Active
-
2023
- 2023-10-24 US US18/383,301 patent/US12297203B2/en active Active
-
2024
- 2024-11-18 JP JP2024200937A patent/JP2025037892A/ja active Pending
-
2025
- 2025-04-18 US US19/182,994 patent/US20260035373A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JPWO2020033955A5 (https=) | ||
| JP2021534244A5 (https=) | ||
| AU2019280356B2 (en) | ERK inhibitor and use thereof | |
| JP7591500B2 (ja) | ピロロピリミジンitk阻害剤 | |
| AU2017378943B2 (en) | FGFR4 inhibitor, preparation method therefor and pharmaceutical use thereof | |
| AU2015304883B2 (en) | Aminopyrimidinyl compounds as JAK inhibitors | |
| AU2017281228B2 (en) | Positive allosteric modulators of the muscarinic acetylcholine receptor M4 | |
| AU2019323035B2 (en) | Pyrazine compounds and uses thereof | |
| CN103269704B (zh) | 杂环化合物和其用途 | |
| WO2008124085A2 (en) | Methods of using combinations of mek and jak-2 inhibitors | |
| AU2020301437B2 (en) | Heterocyclic compounds for mediating tyrosine kinase 2 activity | |
| JP2019514903A5 (https=) | ||
| JP2025540958A (ja) | 蕁麻疹の治療のための野生型c-kitキナーゼ阻害剤としてのN-フェニル-ピラゾロ[1,5-A]ピリジン-3-カルボキサミド誘導体 | |
| EP2063896A2 (en) | Kinase inhibitors useful for the treatment of proliferative diseases | |
| WO2014095774A1 (de) | Bet-proteininhibitorische dihydropyridopyrazinone | |
| CN111801328A (zh) | 自分泌运动因子抑制剂及其用途 | |
| AU2021295413A1 (en) | Amidopyrimidone derivatives | |
| JP2021500380A (ja) | P2x3阻害剤としての新規なピラゾロ−ピロロ−ピリミジン−ジオン誘導体 | |
| JP2023554596A (ja) | 化合物、組成物及び方法 | |
| JPWO2021022186A5 (https=) | ||
| JPWO2020223728A5 (https=) | ||
| AU2018329047B2 (en) | Cycloolefin substituted heteroaromatic compounds and their use | |
| AU2010334804B2 (en) | Aminoalkylpyrimidine derivatives as histamine H4 receptor antagonists | |
| AU2020300689B2 (en) | Chemical compounds | |
| CN114008044A (zh) | 吡啶基或嘧啶基mtor激酶抑制剂 |