JP2019535812A5 - - Google Patents
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- JP2019535812A5 JP2019535812A5 JP2019543185A JP2019543185A JP2019535812A5 JP 2019535812 A5 JP2019535812 A5 JP 2019535812A5 JP 2019543185 A JP2019543185 A JP 2019543185A JP 2019543185 A JP2019543185 A JP 2019543185A JP 2019535812 A5 JP2019535812 A5 JP 2019535812A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- nhc
- compound according
- cycloalkyl
- substituted
- 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
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- 150000001875 compounds Chemical class 0.000 claims 24
- -1 -OH Chemical group 0.000 claims 21
- 125000000753 cycloalkyl group Chemical group 0.000 claims 17
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000005843 halogen group Chemical group 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 8
- 208000032839 leukemia Diseases 0.000 claims 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 8
- 125000000018 nitroso group Chemical group N(=O)* 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims 4
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 4
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 4
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 3
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 3
- 102000001253 Protein Kinase Human genes 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 230000003176 fibrotic effect Effects 0.000 claims 3
- 108060006633 protein kinase Proteins 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 2
- ROSDSFDQCJNGOL-UHFFFAOYSA-N Dimethylamine Chemical compound CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 claims 2
- 206010015150 Erythema Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000029726 Neurodevelopmental disease Diseases 0.000 claims 2
- 208000027190 Peripheral T-cell lymphomas Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims 2
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims 2
- 208000031672 T-Cell Peripheral Lymphoma Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 206010064930 age-related macular degeneration Diseases 0.000 claims 2
- 230000033115 angiogenesis Effects 0.000 claims 2
- 206010002449 angioimmunoblastic T-cell lymphoma Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 2
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims 2
- 125000004981 cycloalkylmethyl group Chemical group 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000004850 cyclobutylmethyl group Chemical group C1(CCC1)C* 0.000 claims 2
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004851 cyclopentylmethyl group Chemical group C1(CCCC1)C* 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 201000011190 diabetic macular edema Diseases 0.000 claims 2
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000004064 dysfunction Effects 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 231100000321 erythema Toxicity 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 208000030533 eye disease Diseases 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 208000020968 mature T-cell and NK-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 210000002464 muscle smooth vascular Anatomy 0.000 claims 2
- 201000005962 mycosis fungoides Diseases 0.000 claims 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 230000001613 neoplastic effect Effects 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 1
- 101000669917 Homo sapiens Rho-associated protein kinase 1 Proteins 0.000 claims 1
- 101000669921 Homo sapiens Rho-associated protein kinase 2 Proteins 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- LIWAQLJGPBVORC-UHFFFAOYSA-N N-ethyl-N-methylamine Natural products CCNC LIWAQLJGPBVORC-UHFFFAOYSA-N 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease 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
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006289 Rett Syndrome Diseases 0.000 claims 1
- 102100039313 Rho-associated protein kinase 1 Human genes 0.000 claims 1
- 102100039314 Rho-associated protein kinase 2 Human genes 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 230000002491 angiogenic effect Effects 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000001286 intracranial vasospasm Diseases 0.000 claims 1
- 230000000366 juvenile effect Effects 0.000 claims 1
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000004060 metabolic process Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000002071 myeloproliferative effect Effects 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 210000000440 neutrophil Anatomy 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 201000006845 reticulosarcoma Diseases 0.000 claims 1
- 208000029922 reticulum cell sarcoma Diseases 0.000 claims 1
- 201000003068 rheumatic fever Diseases 0.000 claims 1
- 208000012201 sexual and gender identity disease Diseases 0.000 claims 1
- 208000015891 sexual disease Diseases 0.000 claims 1
- 208000002320 spinal muscular atrophy Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 0 CC(C1=C(C)C=C(CC=*)CC1)=N Chemical compound CC(C1=C(C)C=C(CC=*)CC1)=N 0.000 description 9
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662411908P | 2016-10-24 | 2016-10-24 | |
| US62/411,908 | 2016-10-24 | ||
| PCT/US2017/058071 WO2018081108A1 (en) | 2016-10-24 | 2017-10-24 | Amide compounds as kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019535812A JP2019535812A (ja) | 2019-12-12 |
| JP2019535812A5 true JP2019535812A5 (enExample) | 2020-12-03 |
| JP6948398B2 JP6948398B2 (ja) | 2021-10-13 |
Family
ID=62023980
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019543185A Active JP6948398B2 (ja) | 2016-10-24 | 2017-10-24 | キナーゼ阻害剤としてのアミド化合物 |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP3532479B1 (enExample) |
| JP (1) | JP6948398B2 (enExample) |
| CN (2) | CN110099906B (enExample) |
| AU (1) | AU2017351216C1 (enExample) |
| CA (1) | CA3078347A1 (enExample) |
| IL (2) | IL266150B2 (enExample) |
| WO (1) | WO2018081108A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019201296A1 (zh) * | 2018-04-18 | 2019-10-24 | 南京明德新药研发有限公司 | 作为rho激酶抑制剂的吡唑类化合物 |
| WO2019201297A1 (zh) * | 2018-04-18 | 2019-10-24 | 南京明德新药研发有限公司 | 作为rho激酶抑制剂的苯并吡唑类化合物 |
| WO2020142745A1 (en) * | 2019-01-04 | 2020-07-09 | Translational Drug Development, Llc | Methods of treating graft versus host disease and neoplastic disease with amide compounds |
| EP3784226B1 (en) | 2018-04-24 | 2024-08-14 | Translational Drug Development Llc | Pyrazole-phenylamide derivatives as inhibitors of the rho-associated protein kinase rock1 and rock2 for the treatment of cancer |
| WO2021262250A1 (en) * | 2020-06-25 | 2021-12-30 | Woolsey Pharmaceuticals, Inc | Methods of treating neurodevelopmental disorders |
| KR20240035820A (ko) | 2021-07-09 | 2024-03-18 | 플렉시움 인코포레이티드 | Ikzf2를 조절하는 아릴 화합물 및 약학 조성물 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| WO2010024903A1 (en) * | 2008-08-29 | 2010-03-04 | Yangbo Feng | BENZO[d]OXAZOLES AND BENZO[d]THIAZOLES AS KINASE INHIBITORS |
| WO2011106632A1 (en) * | 2010-02-26 | 2011-09-01 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| US9079880B2 (en) * | 2010-07-07 | 2015-07-14 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| US8697911B2 (en) * | 2010-07-07 | 2014-04-15 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| TW201444798A (zh) * | 2013-02-28 | 2014-12-01 | 必治妥美雅史谷比公司 | 作爲強效ｒｏｃｋ１及ｒｏｃｋ２抑制劑之苯基吡唑衍生物 |
-
2017
- 2017-10-24 IL IL266150A patent/IL266150B2/en unknown
- 2017-10-24 CN CN201780079730.7A patent/CN110099906B/zh not_active Expired - Fee Related
- 2017-10-24 CN CN202210797866.4A patent/CN115160295A/zh active Pending
- 2017-10-24 EP EP17863621.3A patent/EP3532479B1/en active Active
- 2017-10-24 WO PCT/US2017/058071 patent/WO2018081108A1/en not_active Ceased
- 2017-10-24 AU AU2017351216A patent/AU2017351216C1/en not_active Ceased
- 2017-10-24 JP JP2019543185A patent/JP6948398B2/ja active Active
- 2017-10-24 CA CA3078347A patent/CA3078347A1/en active Pending
-
2023
- 2023-07-18 IL IL304547A patent/IL304547A/en unknown
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