JP2017512779A5 - - Google Patents
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- JP2017512779A5 JP2017512779A5 JP2016557602A JP2016557602A JP2017512779A5 JP 2017512779 A5 JP2017512779 A5 JP 2017512779A5 JP 2016557602 A JP2016557602 A JP 2016557602A JP 2016557602 A JP2016557602 A JP 2016557602A JP 2017512779 A5 JP2017512779 A5 JP 2017512779A5
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- Japan
- Prior art keywords
- het
- group
- substituents
- alkyl
- oxo
- 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.)
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- 125000001424 substituent group Chemical group 0.000 claims 38
- 150000001875 compounds Chemical class 0.000 claims 24
- -1 Het Chemical group 0.000 claims 23
- 125000004043 oxo group Chemical group O=* 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000002367 halogens Chemical class 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 206010025135 lupus erythematosus Diseases 0.000 claims 6
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 5
- 208000010668 atopic eczema Diseases 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 3
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 3
- 206010012434 Dermatitis allergic Diseases 0.000 claims 3
- 208000005777 Lupus Nephritis Diseases 0.000 claims 3
- 206010039085 Rhinitis allergic Diseases 0.000 claims 3
- 201000010105 allergic rhinitis Diseases 0.000 claims 3
- 208000006673 asthma Diseases 0.000 claims 3
- 201000008937 atopic dermatitis Diseases 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- 206010012442 Dermatitis contact Diseases 0.000 claims 2
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 2
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 2
- 206010006451 bronchitis Diseases 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 208000010247 contact dermatitis Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000004343 1-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000028185 Angioedema Diseases 0.000 claims 1
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010065687 Bone loss Diseases 0.000 claims 1
- 229940124003 CRTH2 antagonist Drugs 0.000 claims 1
- RRXSYZFVDIRTFB-UHFFFAOYSA-N C[CH]C1=CC=C(OC)C=C1 Chemical group C[CH]C1=CC=C(OC)C=C1 RRXSYZFVDIRTFB-UHFFFAOYSA-N 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 208000004332 Evans syndrome Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000024869 Goodpasture syndrome Diseases 0.000 claims 1
- 206010018690 Granulocytosis Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 206010018910 Haemolysis Diseases 0.000 claims 1
- 201000004331 Henoch-Schoenlein purpura Diseases 0.000 claims 1
- 206010019617 Henoch-Schonlein purpura Diseases 0.000 claims 1
- 208000031814 IgA Vasculitis Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 208000034624 Leukocytoclastic Cutaneous Vasculitis Diseases 0.000 claims 1
- 208000032514 Leukocytoclastic vasculitis Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome 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
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000024780 Urticaria Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 208000007502 anemia Diseases 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000003454 betamimetic effect Effects 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 230000008588 hemolysis Effects 0.000 claims 1
- 208000007475 hemolytic anemia Diseases 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 201000006362 hypersensitivity vasculitis Diseases 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 208000015446 immunoglobulin a vasculitis Diseases 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000010901 lateral sclerosis Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 208000005264 motor neuron disease Diseases 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000004235 neutropenia Diseases 0.000 claims 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 230000000010 osteolytic effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl 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
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- GUSDJDARKXWLBJ-UHFFFAOYSA-N CCBc1cc(O)c2[s]c(C)nc2c1 Chemical compound CCBc1cc(O)c2[s]c(C)nc2c1 GUSDJDARKXWLBJ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461955487P | 2014-03-19 | 2014-03-19 | |
| US61/955,487 | 2014-03-19 | ||
| PCT/EP2015/055237 WO2015140054A1 (en) | 2014-03-19 | 2015-03-12 | Heteroaryl syk inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017512779A JP2017512779A (ja) | 2017-05-25 |
| JP2017512779A5 true JP2017512779A5 (OSRAM) | 2018-04-12 |
| JP6535022B2 JP6535022B2 (ja) | 2019-06-26 |
Family
ID=52706148
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016557952A Active JP6416275B2 (ja) | 2014-03-19 | 2015-03-12 | ヘテロアリールｓｙｋ阻害剤 |
| JP2016557602A Active JP6535022B2 (ja) | 2014-03-19 | 2015-03-12 | ヘテロアリールｓｙｋ阻害剤 |
| JP2016557587A Active JP6599884B2 (ja) | 2014-03-19 | 2015-03-12 | 新規なヘテロアリール化合物及び医薬としてのその使用 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016557952A Active JP6416275B2 (ja) | 2014-03-19 | 2015-03-12 | ヘテロアリールｓｙｋ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016557587A Active JP6599884B2 (ja) | 2014-03-19 | 2015-03-12 | 新規なヘテロアリール化合物及び医薬としてのその使用 |
Country Status (32)
| Country | Link |
|---|---|
| US (4) | US9914735B2 (OSRAM) |
| EP (3) | EP3119765B1 (OSRAM) |
| JP (3) | JP6416275B2 (OSRAM) |
| KR (1) | KR102431017B1 (OSRAM) |
| CN (3) | CN110183440B (OSRAM) |
| AP (1) | AP2016009373A0 (OSRAM) |
| AR (1) | AR099785A1 (OSRAM) |
| AU (1) | AU2015233654B2 (OSRAM) |
| CA (1) | CA2942997C (OSRAM) |
| CL (1) | CL2016001963A1 (OSRAM) |
| CY (1) | CY1121937T1 (OSRAM) |
| DK (1) | DK3119772T3 (OSRAM) |
| EA (1) | EA032097B1 (OSRAM) |
| ES (1) | ES2738416T3 (OSRAM) |
| HR (1) | HRP20191364T1 (OSRAM) |
| HU (1) | HUE046061T2 (OSRAM) |
| IL (1) | IL247057B (OSRAM) |
| LT (1) | LT3119772T (OSRAM) |
| ME (1) | ME03472B (OSRAM) |
| MX (1) | MX2016011784A (OSRAM) |
| MY (1) | MY185837A (OSRAM) |
| PE (1) | PE20161427A1 (OSRAM) |
| PH (1) | PH12016501796A1 (OSRAM) |
| PL (1) | PL3119772T3 (OSRAM) |
| PT (1) | PT3119772T (OSRAM) |
| RS (1) | RS59110B1 (OSRAM) |
| SG (1) | SG11201607794QA (OSRAM) |
| SI (1) | SI3119772T1 (OSRAM) |
| TW (1) | TWI680967B (OSRAM) |
| UA (1) | UA119667C2 (OSRAM) |
| UY (1) | UY36037A (OSRAM) |
| WO (3) | WO2015140054A1 (OSRAM) |
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| ME03472B (me) | 2014-03-19 | 2020-01-20 | Boehringer Ingelheim Int | Heteroarilni sik inhibitori |
| MX2018003008A (es) | 2015-09-11 | 2018-04-11 | Boehringer Ingelheim Int | Heteroarilos sustituidos con pirazolilo y su uso como medicamentos. |
| EP3371188B1 (en) | 2015-11-02 | 2019-10-23 | Janssen Pharmaceutica NV | [1,2,4]triazolo[1,5-a]pyrimidin-7-yl compound |
| CN105503730B (zh) * | 2015-12-25 | 2018-06-22 | 山东大学 | 吡唑类衍生物及其制备方法与应用 |
| CN109890824B (zh) | 2016-11-02 | 2022-05-24 | 詹森药业有限公司 | 作为pde2抑制剂的[1,2,4]三唑并[1,5-a]嘧啶化合物 |
| AU2017353315B2 (en) | 2016-11-02 | 2021-09-16 | Janssen Pharmaceutica Nv | (1,2,4)triazolo(1,5-a)pyrimidine compounds as PDE2 inhibitors |
| TWI764950B (zh) | 2016-11-02 | 2022-05-21 | 比利時商健生藥品公司 | Ｐｄｅ２抑制劑 |
| EP3824906A1 (en) | 2016-12-21 | 2021-05-26 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| US11833156B2 (en) | 2017-09-22 | 2023-12-05 | Jubilant Epipad LLC | Heterocyclic compounds as pad inhibitors |
| WO2019077631A1 (en) | 2017-10-18 | 2019-04-25 | Jubilant Biosys Limited | IMIDAZO-PYRIDINE COMPOUNDS FOR USE AS PAD INHIBITORS |
| KR20200085836A (ko) | 2017-11-06 | 2020-07-15 | 주빌런트 프로델 엘엘씨 | Pd1/pd-l1 활성화 억제제로서의 피리미딘 유도체 |
| BR112020010322A2 (pt) | 2017-11-24 | 2020-11-17 | Jubilant Episcribe Llc | composto da fórmula i; composto da fórmula ia; composto da fórmula ib; processo de preparação de compostos da fórmula i; composição farmacêutica; método para o tratamento e/ou prevenção de várias doenças; uso dos compostos; método para o tratamento de câncer; e método para o tratamento e/ou prevenção de uma afecção mediada por prmt5 ou um distúrbio proliferativo ou câncer |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| CN112105610B (zh) | 2018-03-13 | 2024-01-26 | 朱比连特普罗德尔有限责任公司 | 作为pd1/pd-l1相互作用/活化的抑制剂的双环化合物 |
| EP3817822A4 (en) | 2018-07-06 | 2022-07-27 | Kymera Therapeutics, Inc. | PROTEIN DEGRADANTS AND USES THEREOF |
| EP4371987B9 (en) | 2018-10-31 | 2025-11-26 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds as hpk1 inhibitors |
| KR102658602B1 (ko) | 2018-10-31 | 2024-04-19 | 길리애드 사이언시즈, 인코포레이티드 | Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물 |
| CA3119773A1 (en) | 2018-11-30 | 2020-06-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| US11633399B2 (en) | 2018-12-25 | 2023-04-25 | Sol-Gel Technologies Ltd. | Treatment of skin disorders with compositions comprising an EGFR inhibitor |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子 |
| WO2020237025A1 (en) | 2019-05-23 | 2020-11-26 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| WO2020264490A1 (en) * | 2019-06-28 | 2020-12-30 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| EP4076524A4 (en) | 2019-12-17 | 2023-11-29 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
| JP2023509366A (ja) | 2019-12-17 | 2023-03-08 | カイメラ セラピューティクス， インコーポレイテッド | Ｉｒａｋ分解剤およびそれらの使用 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| US20220213086A1 (en) * | 2020-12-25 | 2022-07-07 | Eternity Bioscience Inc. | Azole compounds as irak inhibitors, preparation methods and medicinal uses thereof |
| TW202241891A (zh) | 2020-12-30 | 2022-11-01 | 美商凱麥拉醫療公司 | Irak降解劑及其用途 |
| MX2023009178A (es) | 2021-02-15 | 2023-08-21 | Kymera Therapeutics Inc | Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos. |
| US12171768B2 (en) | 2021-02-15 | 2024-12-24 | Kymera Therapeutics, Inc. | IRAK4 degraders and uses thereof |
| KR20220138655A (ko) * | 2021-04-06 | 2022-10-13 | 주식회사 온코크로스 | 신장 질환의 예방 또는 치료용 화합물 |
| KR20220138654A (ko) * | 2021-04-06 | 2022-10-13 | 주식회사 온코크로스 | 당뇨병의 예방 또는 치료용 화합물 |
| AR127505A1 (es) | 2021-10-29 | 2024-01-31 | Kymera Therapeutics Inc | Degradadores irak-4 y síntesis de los mismos |
| WO2023147594A2 (en) | 2022-01-31 | 2023-08-03 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CN115215803B (zh) * | 2022-09-19 | 2022-12-30 | 苏州美诺医药科技有限公司 | 一种4-卤代-1-(二氟甲基)-1h-咪唑的制备方法 |
| WO2024081889A1 (en) | 2022-10-14 | 2024-04-18 | Genesis Therapeutics, Inc. | 4h-pyrido[1,2-a]pyrimidin-4-one derivatives for treating cancer |
| CN116836162B (zh) * | 2023-05-24 | 2025-09-05 | 南方医科大学 | 吡唑[4,3-c]吡啶类化合物或其药学上可接受的盐及其应用 |
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