JP2018520161A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018520161A5 JP2018520161A5 JP2018500585A JP2018500585A JP2018520161A5 JP 2018520161 A5 JP2018520161 A5 JP 2018520161A5 JP 2018500585 A JP2018500585 A JP 2018500585A JP 2018500585 A JP2018500585 A JP 2018500585A JP 2018520161 A5 JP2018520161 A5 JP 2018520161A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocyclyl
- heteroaryl
- cycloalkyl
- aryl
- 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
- 125000000623 heterocyclic group Chemical group 0.000 claims 86
- 125000006545 (C1-C9) alkyl group Chemical group 0.000 claims 73
- 125000001072 heteroaryl group Chemical group 0.000 claims 72
- 125000003118 aryl group Chemical group 0.000 claims 65
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 62
- 150000001875 compounds Chemical class 0.000 claims 52
- 125000006647 (C3-C15) cycloalkyl group Chemical group 0.000 claims 47
- 150000003839 salts Chemical class 0.000 claims 34
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 30
- 125000001475 halogen functional group Chemical group 0.000 claims 30
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 29
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 125000004093 cyano group Chemical group *C#N 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- 125000001188 haloalkyl group Chemical group 0.000 claims 21
- 125000001424 substituent group Chemical group 0.000 claims 21
- 239000000203 mixture Substances 0.000 claims 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims 18
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 17
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 13
- 150000002431 hydrogen Chemical class 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 9
- 206010009887 colitis Diseases 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- -1 —N 3 Chemical group 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- 125000000464 thioxo group Chemical group S=* 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000004232 Enteritis Diseases 0.000 claims 2
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 208000004998 Abdominal Pain Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 206010073128 Anaplastic oligodendroglioma Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 208000006820 Arthralgia Diseases 0.000 claims 1
- 206010003267 Arthritis reactive Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 206010005003 Bladder cancer 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
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009895 Colitis ischaemic Diseases 0.000 claims 1
- 206010056979 Colitis microscopic Diseases 0.000 claims 1
- 102000008186 Collagen Human genes 0.000 claims 1
- 108010035532 Collagen Proteins 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 208000000059 Dyspnea Diseases 0.000 claims 1
- 206010013975 Dyspnoeas Diseases 0.000 claims 1
- 206010058838 Enterocolitis infectious Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000010201 Exanthema Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010018634 Gouty Arthritis Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 1
- 208000000616 Hemoptysis Diseases 0.000 claims 1
- 206010019728 Hepatitis alcoholic Diseases 0.000 claims 1
- 208000004044 Hypesthesia Diseases 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010023232 Joint swelling Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010024648 Livedo reticularis Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000008771 Lymphadenopathy Diseases 0.000 claims 1
- 102100030412 Matrix metalloproteinase-9 Human genes 0.000 claims 1
- 108010015302 Matrix metalloproteinase-9 Proteins 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000037039 Monarthritis Diseases 0.000 claims 1
- 206010028116 Mucosal inflammation Diseases 0.000 claims 1
- 201000010927 Mucositis Diseases 0.000 claims 1
- 206010028813 Nausea Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 201000010133 Oligodendroglioma Diseases 0.000 claims 1
- 206010031009 Oral pain Diseases 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
- 206010034719 Personality change Diseases 0.000 claims 1
- 208000001280 Prediabetic State Diseases 0.000 claims 1
- 206010036774 Proctitis 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
- 208000020410 Psoriasis-related juvenile idiopathic arthritis Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010049416 Short-bowel syndrome Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 102100025750 Sphingosine 1-phosphate receptor 1 Human genes 0.000 claims 1
- 101710155454 Sphingosine 1-phosphate receptor 1 Proteins 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010047571 Visual impairment Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000005856 abnormality Effects 0.000 claims 1
- 208000002552 acute disseminated encephalomyelitis Diseases 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 208000002353 alcoholic hepatitis Diseases 0.000 claims 1
- 206010002224 anaplastic astrocytoma Diseases 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 201000008240 chemical colitis Diseases 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- 208000019902 chronic diarrheal disease Diseases 0.000 claims 1
- 229920001436 collagen Polymers 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 201000003146 cystitis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000007784 diverticulitis Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000010227 enterocolitis Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 201000005884 exanthem Diseases 0.000 claims 1
- 206010016256 fatigue Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 230000002641 glycemic effect Effects 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000003676 hair loss Effects 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 208000034783 hypoesthesia Diseases 0.000 claims 1
- 208000009326 ileitis Diseases 0.000 claims 1
- 201000008254 ileocolitis Diseases 0.000 claims 1
- 208000027138 indeterminate colitis Diseases 0.000 claims 1
- 208000027139 infectious colitis Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 201000008222 ischemic colitis Diseases 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000018555 lymphatic system disease Diseases 0.000 claims 1
- 208000004341 lymphocytic colitis Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000008275 microscopic colitis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 230000008693 nausea Effects 0.000 claims 1
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 231100000862 numbness Toxicity 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 208000035824 paresthesia Diseases 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 206010037844 rash Diseases 0.000 claims 1
- 208000002574 reactive arthritis Diseases 0.000 claims 1
- 230000035945 sensitivity Effects 0.000 claims 1
- 231100000046 skin rash Toxicity 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 208000029257 vision disease Diseases 0.000 claims 1
- 230000004393 visual impairment Effects 0.000 claims 1
- 230000008673 vomiting Effects 0.000 claims 1
- QJOXCEGGCSBIIE-VWLOTQADSA-N CC(C)(C)CNc(c(cc(C[C@H](C1=CN(C2CC2)NN1)c1cccc2c1ccnc2)cc1Cl)c1nc1)c1C#N Chemical compound CC(C)(C)CNc(c(cc(C[C@H](C1=CN(C2CC2)NN1)c1cccc2c1ccnc2)cc1Cl)c1nc1)c1C#N QJOXCEGGCSBIIE-VWLOTQADSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562189158P | 2015-07-06 | 2015-07-06 | |
| US62/189,158 | 2015-07-06 | ||
| US201562269060P | 2015-12-17 | 2015-12-17 | |
| US62/269,060 | 2015-12-17 | ||
| PCT/US2016/040520 WO2017007689A1 (en) | 2015-07-06 | 2016-06-30 | Cot modulators and methods of use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018171794A Division JP6781221B2 (ja) | 2015-07-06 | 2018-09-13 | Ｃｏｔモジュレーターおよびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018520161A JP2018520161A (ja) | 2018-07-26 |
| JP2018520161A5 true JP2018520161A5 (enExample) | 2018-09-06 |
| JP6430060B2 JP6430060B2 (ja) | 2018-11-28 |
Family
ID=56411943
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018500585A Active JP6430060B2 (ja) | 2015-07-06 | 2016-06-30 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2018171794A Active JP6781221B2 (ja) | 2015-07-06 | 2018-09-13 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2019137759A Active JP6906021B2 (ja) | 2015-07-06 | 2019-07-26 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2020208330A Active JP7138155B2 (ja) | 2015-07-06 | 2020-12-16 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2022065168A Withdrawn JP2022082816A (ja) | 2015-07-06 | 2022-04-11 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2024081151A Withdrawn JP2024100865A (ja) | 2015-07-06 | 2024-05-17 | Ｃｏｔモジュレーターおよびその使用方法 |
Family Applications After (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018171794A Active JP6781221B2 (ja) | 2015-07-06 | 2018-09-13 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2019137759A Active JP6906021B2 (ja) | 2015-07-06 | 2019-07-26 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2020208330A Active JP7138155B2 (ja) | 2015-07-06 | 2020-12-16 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2022065168A Withdrawn JP2022082816A (ja) | 2015-07-06 | 2022-04-11 | Ｃｏｔモジュレーターおよびその使用方法 |
| JP2024081151A Withdrawn JP2024100865A (ja) | 2015-07-06 | 2024-05-17 | Ｃｏｔモジュレーターおよびその使用方法 |
Country Status (41)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012278976B2 (en) | 2011-07-06 | 2017-05-11 | Gilead Sciences, Inc. | Compounds for the treatment of HIV |
| US10118890B2 (en) | 2014-10-10 | 2018-11-06 | The Research Foundation For The State University Of New York | Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration |
| MX370984B (es) | 2015-07-06 | 2020-01-09 | Gilead Sciences Inc | Moduladores de cáncer de tiroides de osaka (cot) y métodos de uso de los mismos. |
| KR20200022527A (ko) | 2015-07-06 | 2020-03-03 | 길리애드 사이언시즈, 인코포레이티드 | Cot 조정제로서의 6-아미노-퀴놀린-3-카르보니트릴 |
| JP6776378B2 (ja) | 2016-06-30 | 2020-10-28 | ギリアード サイエンシーズ， インコーポレイテッド | Ｃｏｔモジュレーターとしての４，６−ジアミノキナゾリン類およびその使用方法 |
| KR20200131351A (ko) * | 2016-08-19 | 2020-11-23 | 길리애드 사이언시즈, 인코포레이티드 | Hiv 바이러스 감염의 예방적 또는 치유적 치료에 유용한 치료 화합물 |
| EA036921B1 (ru) * | 2017-02-10 | 2021-01-15 | Джилид Сайэнс, Инк. | Терапевтические соединения, которые можно применять для профилактического или терапевтического лечения инфекции вирусом вич |
| CN108794516A (zh) * | 2017-04-26 | 2018-11-13 | 上海时莱生物技术有限公司 | 硼酸和硼酸酯类化合物及其制备方法和用途 |
| AR112412A1 (es) | 2017-08-17 | 2019-10-23 | Gilead Sciences Inc | Formas de sal de colina de un inhibidor de la cápside del vih |
| AR112413A1 (es) | 2017-08-17 | 2019-10-23 | Gilead Sciences Inc | Formas sólidas de un inhibidor de la cápside del vih |
| EP3689866A4 (en) * | 2017-09-26 | 2021-07-07 | Nippon Soda Co., Ltd. | QUINOLINE COMPOUND AND BACTERICIDAL AGENT FOR AGRICULTURE AND HORTICULTURE |
| PL3752495T3 (pl) | 2018-02-15 | 2024-01-15 | Gilead Sciences, Inc. | Pochodne pirydynowe i ich zastosowanie do leczenia infekcji hiv |
| KR102587504B1 (ko) | 2018-02-16 | 2023-10-11 | 길리애드 사이언시즈, 인코포레이티드 | 레트로비리다에 바이러스 감염의 치료에 유용한 치료 화합물을 제조하기 위한 방법 및 중간체 |
| WO2019168874A1 (en) | 2018-02-27 | 2019-09-06 | The Research Foundation For The State University Of New York | Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same |
| CN110294660B (zh) * | 2018-03-23 | 2021-09-24 | 中国农业大学 | 一种含碳碳三键和/或碳氮三键的不饱和有机化合物的还原氘化方法 |
| CN108658996A (zh) * | 2018-06-25 | 2018-10-16 | 中国药科大学 | 一种氘代Fiduxosin的制备方法 |
| KR20230141905A (ko) | 2018-07-16 | 2023-10-10 | 길리애드 사이언시즈, 인코포레이티드 | Hiv의 치료를 위한 캡시드 억제제 |
| TWI770527B (zh) * | 2019-06-14 | 2022-07-11 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| ES2974680T3 (es) | 2019-08-09 | 2024-07-01 | Idorsia Pharmaceuticals Ltd | Derivados de (2-acetamidil)tio-beta-D-galactopiranósidos |
| WO2021028336A1 (en) | 2019-08-09 | 2021-02-18 | Idorsia Pharmaceuticals Ltd | (hetero)aryl-methyl-thio-beta-d-galactopyranoside derivatives |
| RS66695B1 (sr) | 2019-08-15 | 2025-05-30 | Idorsia Pharmaceuticals Ltd | 2-hidroksicikloalkan-1-karbamoil derivati |
| EP4021904B1 (en) | 2019-08-29 | 2024-01-03 | Idorsia Pharmaceuticals Ltd | Alpha-d-galactopyranoside derivatives |
| AU2020391466B2 (en) | 2019-11-26 | 2024-05-23 | Gilead Sciences, Inc. | Capsid inhibitors for the prevention of HIV |
| EP4126231A1 (en) | 2020-03-30 | 2023-02-08 | Gilead Sciences, Inc. | Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound |
| WO2021202688A1 (en) * | 2020-04-02 | 2021-10-07 | Gilead Sciences, Inc. | Process for preparing a cot inhibitor compound |
| AU2021296607B2 (en) | 2020-06-25 | 2024-07-25 | Gilead Sciences, Inc. | Capsid inhibitors for the treatment of HIV |
| EP4225752B1 (en) | 2020-10-06 | 2024-12-11 | Idorsia Pharmaceuticals Ltd | Spiro derivatives of alpha-d-galactopyranosides |
| KR20230104190A (ko) | 2020-11-02 | 2023-07-07 | 이도르시아 파마슈티컬스 리미티드 | 갈렉틴-3 억제 2-히드록시시클로알칸-1-카르바모일 유도체 |
| ES3032987T3 (en) | 2021-02-09 | 2025-07-29 | Idorsia Pharmaceuticals Ltd | Hydroxyheterocycloalkane-carbamoyl derivatives |
| WO2022184755A1 (en) | 2021-03-03 | 2022-09-09 | Idorsia Pharmaceuticals Ltd | Triazolyl-methyl substituted alpha-d-galactopyranoside derivatives |
| TW202345826A (zh) * | 2021-06-04 | 2023-12-01 | 美商基利科學股份有限公司 | 治療nash之方法 |
| CA3220429A1 (en) * | 2021-06-11 | 2022-12-15 | Neuronascent, Inc. | Methods and compositions for lipid formulation of lipophilic small molecule therapies of the heterocyclic type |
| HRP20250928T1 (hr) | 2021-12-03 | 2025-09-26 | Gilead Sciences, Inc. | TERAPIJSKI SPOJEVI ZA INFEKCIJU VIRUSOM HIV-a |
| EP4440700A1 (en) | 2021-12-03 | 2024-10-09 | Gilead Sciences, Inc. | Therapeutic compounds for hiv virus infection |
| WO2023102523A1 (en) | 2021-12-03 | 2023-06-08 | Gilead Sciences, Inc. | Therapeutic compounds for hiv virus infection |
| WO2024245157A1 (zh) * | 2023-05-30 | 2024-12-05 | 浙江星浩澎博医药有限公司 | 氮杂喹啉环衍生物 |
| AU2024282281A1 (en) * | 2023-06-02 | 2026-01-15 | Westol, Llc | 2,8-dihydroxyquinoline glucuronide derivatives with enhanced properties for use as anticancer, antiviral, antimicrobial, and other therapeutic applications |
| WO2025020886A1 (zh) * | 2023-07-27 | 2025-01-30 | 浙江星浩澎博医药有限公司 | 氮杂喹唑啉环衍生物及其用途 |
| KR102732584B1 (ko) | 2024-03-28 | 2024-11-21 | (주)신한티이씨 | 전기 배전반의 화재 위험 감지 및 진압용 소화 장치 |
Family Cites Families (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3930837A (en) | 1971-12-31 | 1976-01-06 | Ici Australia Limited | 3-chloro-5-acetamidaisoquinoline as a herbicide |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| IT7819093A0 (it) | 1977-01-10 | 1978-01-06 | Ciba Geigy | Prodotti antielmintici e loro impiego. |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4902514A (en) | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| JP2634438B2 (ja) | 1988-07-26 | 1997-07-23 | 三井東圧化学株式会社 | 不斉ビスオキサゾリルピリジン誘導体およびその製造方法 |
| DE4014171A1 (de) | 1990-05-03 | 1991-11-07 | Basf Ag | Cyanochinolinverbindungen |
| GB9310700D0 (en) | 1993-05-24 | 1993-07-07 | Zeneca Ltd | Novel composition |
| UA73073C2 (uk) * | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| KR20010022781A (ko) | 1997-08-28 | 2001-03-26 | 도쿠시마 히데이치 | 시아노아크릴레이트 화합물을 함유하는 공업용 항균·항진균제, 살조제(殺藻劑) 및 생물 부착 방지제 |
| DE69935933T2 (de) | 1998-07-10 | 2008-01-10 | Massachusetts Institute Of Technology, Cambridge | Liganden für Metalle und verbesserte Metall-katalysierte Verfahren, die darauf basieren |
| WO2000018740A1 (en) * | 1998-09-29 | 2000-04-06 | American Cyanamid Company | Substituted 3-cyanoquinolines as protein tyrosine kinases inhibitors |
| BR0308737A (pt) | 2002-03-20 | 2005-01-11 | Bristol Myers Squibb Co | Pró-drogas de fosfato de fluoroxindóis |
| JP2006515341A (ja) | 2003-03-03 | 2006-05-25 | エフ．ホフマン−ラ ロシュ アーゲー | ５−ｈｔ６調節物質として使用するための２，５−および２，６−置換テトラヒドロイソキノリン |
| CA2535385A1 (en) | 2003-08-19 | 2005-03-03 | Wyeth Holdings Corporation | Process for the preparation of 4-amino-3-quinolinecarbonitriles |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| TW200529846A (en) * | 2004-02-20 | 2005-09-16 | Wyeth Corp | 3-quinolinecarbonitrile protein kinase inhibitors |
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| BRPI0609928A2 (pt) | 2005-05-18 | 2010-05-11 | Wyeth Corp | inibidores de quinase tpl-2 de 3-cianoquinolina e métodos de fabricação e uso dos mesmos |
| WO2006124944A1 (en) | 2005-05-18 | 2006-11-23 | Wyeth | 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of tpl2 kinase and methods of making and using the same |
| WO2007050732A1 (en) | 2005-10-28 | 2007-05-03 | Abbott Laboratories | INDAZOLE DERIVATIVES THAT INHIBIT TRPVl RECEPTOR |
| EP2001480A4 (en) | 2006-03-31 | 2011-06-15 | Abbott Lab | Indazole CONNECTIONS |
| WO2008055950A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | Novel inhibitors of glutaminyl cyclase |
| WO2008092292A1 (en) | 2007-01-17 | 2008-08-07 | The Hong Kong University Of Science And Technology | Isoquinolone compounds as subtype-selective agonists for melatonin receptors mt1 and mt2 |
| GB0820856D0 (en) | 2008-11-14 | 2008-12-24 | Univ Leuven Kath | Novel inhibitors of flavivirus replication |
| TWI491606B (zh) | 2009-07-13 | 2015-07-11 | Gilead Sciences Inc | 調節細胞凋亡信號之激酶的抑制劑 |
| GB0922302D0 (en) | 2009-12-22 | 2010-02-03 | Imp Innovations Ltd | Compounds |
| WO2011112678A1 (en) | 2010-03-09 | 2011-09-15 | Dana-Farber Cancer Institute, Inc. | Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy |
| BR112012031340B1 (pt) * | 2010-06-09 | 2021-09-14 | Tianjin Hemay Bio-Tech Co., Ltd | Derivados de cianoquinolina, composição farmacêutica compreendendo os mesmos, e seu uso |
| EP2708540B1 (en) | 2011-05-10 | 2018-07-25 | Kyowa Hakko Kirin Co., Ltd. | Pyrimido-diazepinone compound |
| US9173395B2 (en) | 2011-07-04 | 2015-11-03 | Bayer Intellectual Property Gmbh | Use of substituted isoquinolinones, isoquinolindiones, isoquinolintriones and dihydroisoquinolinones or in each case salts thereof as active agents against abiotic stress in plants |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| CA2853227C (en) | 2011-10-27 | 2019-05-14 | Taisho Pharmaceutical Co., Ltd. | Azole derivative |
| TWI701253B (zh) | 2011-11-11 | 2020-08-11 | 美商基利阿波羅有限責任公司 | Ａｃｃ抑制劑及彼等之用途 |
| UY34573A (es) | 2012-01-27 | 2013-06-28 | Gilead Sciences Inc | Inhibidor de la quinasa que regula la señal de la apoptosis |
| CN103483363B (zh) | 2012-06-13 | 2016-12-21 | 上海赛迦化工产品有限公司 | 多样性的手性氨基硼酸及其制备方法和应用 |
| IN2015DN03795A (enExample) | 2012-10-24 | 2015-10-02 | Inserm Inst Nat De La Santé Et De La Rech Médicale | |
| CN103408572B (zh) | 2013-07-12 | 2015-12-02 | 上海工程技术大学 | 手性氨基硼酸衍生物及其制备方法和应用 |
| US10189780B2 (en) | 2013-12-12 | 2019-01-29 | Zeno Royalties & Milestones, LLC | Bicyclic alkyl compounds and synthesis |
| WO2015134710A1 (en) | 2014-03-07 | 2015-09-11 | Kalyra Pharmaceuticals, Inc. | Propellane derivates and synthesis |
| US9701661B2 (en) * | 2014-07-11 | 2017-07-11 | Northwestern University | 2-imidazolyl-pyrimidine scaffolds as potent and selective inhibitors of neuronal nitric oxide synthase |
| EP3193855B1 (en) | 2014-09-17 | 2021-05-19 | Recurium IP Holdings, LLC | Bicyclic compounds |
| SG11201701723XA (en) | 2014-09-24 | 2017-04-27 | Gilead Sciences Inc | Methods of treating liver disease |
| WO2016106384A1 (en) | 2014-12-23 | 2016-06-30 | Gilead Sciences, Inc. | Processes for preparing ask1 inhibitors |
| MA41252A (fr) | 2014-12-23 | 2017-10-31 | Gilead Sciences Inc | Formes solides d'un inhibiteur d'ask 1 |
| CN107106873A (zh) | 2015-01-09 | 2017-08-29 | 吉利德阿波罗公司 | 用于治疗非酒精性脂肪肝病的acc抑制剂组合治疗 |
| CA2974004A1 (en) | 2015-01-16 | 2016-07-21 | 3M Innovative Properties Company | Systems and methods for selecting grid actions to improve grid outcomes |
| MX370984B (es) | 2015-07-06 | 2020-01-09 | Gilead Sciences Inc | Moduladores de cáncer de tiroides de osaka (cot) y métodos de uso de los mismos. |
| KR20200022527A (ko) * | 2015-07-06 | 2020-03-03 | 길리애드 사이언시즈, 인코포레이티드 | Cot 조정제로서의 6-아미노-퀴놀린-3-카르보니트릴 |
| AU2016382372B2 (en) | 2015-12-31 | 2019-09-19 | Hitgen Inc. | Sulfonamide derivative and preparation method and use thereof |
| US10183951B2 (en) | 2016-03-02 | 2019-01-22 | Gilead Apollo, Llc | Solid forms of a thienopyrimidinedione ACC inhibitor and methods for production thereof |
| JP6738895B2 (ja) | 2016-06-21 | 2020-08-12 | Ｐｈｃホールディングス株式会社 | カタラーゼ阻害剤及びカタラーゼ阻害剤を用いるアナライトの測定方法 |
| JP6776378B2 (ja) | 2016-06-30 | 2020-10-28 | ギリアード サイエンシーズ， インコーポレイテッド | Ｃｏｔモジュレーターとしての４，６−ジアミノキナゾリン類およびその使用方法 |
| CN106512014A (zh) | 2016-10-27 | 2017-03-22 | 武汉大学 | 肿瘤进展位点2在治疗脂肪肝和ⅱ型糖尿病中的功能和应用 |
| CN110382503B (zh) | 2017-03-03 | 2022-07-19 | 吉利德科学公司 | 制备acc抑制剂及其固体形式的方法 |
| JP6906626B2 (ja) | 2017-03-28 | 2021-07-21 | ギリアード サイエンシーズ， インコーポレイテッド | 肝疾患を処置するための治療的組み合わせ |
| JP2020516627A (ja) | 2017-04-12 | 2020-06-11 | ギリアード サイエンシーズ， インコーポレイテッド | 肝疾患を処置する方法 |
| CN111182904A (zh) | 2017-10-06 | 2020-05-19 | 吉利德科学公司 | 包含acc抑制剂的组合治疗 |
| US11524005B2 (en) | 2019-02-19 | 2022-12-13 | Gilead Sciences, Inc. | Solid forms of FXR agonists |
| EP3934615A4 (en) | 2019-03-08 | 2023-01-25 | The Regents Of The University Of California | ACNE TREATMENT COMPOSITIONS AND METHODS |
| TWI770527B (zh) | 2019-06-14 | 2022-07-11 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| AR119594A1 (es) | 2019-08-09 | 2021-12-29 | Gilead Sciences Inc | Derivados de tienopirimidina como inhibidores acc y usos de los mismos |
| EP4126231A1 (en) | 2020-03-30 | 2023-02-08 | Gilead Sciences, Inc. | Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound |
| WO2021202688A1 (en) | 2020-04-02 | 2021-10-07 | Gilead Sciences, Inc. | Process for preparing a cot inhibitor compound |
| TW202345826A (zh) | 2021-06-04 | 2023-12-01 | 美商基利科學股份有限公司 | 治療nash之方法 |
-
2016
- 2016-06-30 MX MX2017004737A patent/MX370984B/es active IP Right Grant
- 2016-06-30 CA CA2971640A patent/CA2971640C/en active Active
- 2016-06-30 KR KR1020187003221A patent/KR101974793B1/ko active Active
- 2016-06-30 PL PL16738976T patent/PL3191470T3/pl unknown
- 2016-06-30 CN CN202210008753.1A patent/CN114380799B/zh active Active
- 2016-06-30 JP JP2018500585A patent/JP6430060B2/ja active Active
- 2016-06-30 AU AU2016290820A patent/AU2016290820B2/en active Active
- 2016-06-30 MA MA39422A patent/MA39422B1/fr unknown
- 2016-06-30 HU HUE16738976A patent/HUE043310T2/hu unknown
- 2016-06-30 MY MYPI2018700007A patent/MY196173A/en unknown
- 2016-06-30 PT PT181865684T patent/PT3456717T/pt unknown
- 2016-06-30 NZ NZ738525A patent/NZ738525A/en unknown
- 2016-06-30 HR HRP20190853TT patent/HRP20190853T1/hr unknown
- 2016-06-30 KR KR1020227031078A patent/KR20220129667A/ko not_active Ceased
- 2016-06-30 ES ES18186568T patent/ES2872076T3/es active Active
- 2016-06-30 IL IL274568A patent/IL274568B/en unknown
- 2016-06-30 ME MEP-2019-117A patent/ME03425B/me unknown
- 2016-06-30 PT PT211623939T patent/PT3896064T/pt unknown
- 2016-06-30 PE PE2017002804A patent/PE20180462A1/es unknown
- 2016-06-30 DK DK16738976.6T patent/DK3191470T3/en active
- 2016-06-30 KR KR1020207002878A patent/KR102443575B1/ko active Active
- 2016-06-30 RS RS20190498A patent/RS58639B1/sr unknown
- 2016-06-30 CU CUP2017000172A patent/CU20170172A7/xx unknown
- 2016-06-30 SM SM20190244T patent/SMT201900244T1/it unknown
- 2016-06-30 SI SI201630202T patent/SI3191470T1/sl unknown
- 2016-06-30 US US15/199,534 patent/US20170008905A1/en not_active Abandoned
- 2016-06-30 KR KR1020197011792A patent/KR102073641B1/ko active Active
- 2016-06-30 SG SG11201702041PA patent/SG11201702041PA/en unknown
- 2016-06-30 EP EP25176778.6A patent/EP4613332A3/en active Pending
- 2016-06-30 EP EP16738976.6A patent/EP3191470B1/en active Active
- 2016-06-30 EP EP18186568.4A patent/EP3456717B1/en active Active
- 2016-06-30 UA UAA201712984A patent/UA123010C2/uk unknown
- 2016-06-30 EA EA201792613A patent/EA036788B1/ru unknown
- 2016-06-30 NZ NZ750707A patent/NZ750707A/en unknown
- 2016-06-30 ES ES16738976T patent/ES2734713T3/es active Active
- 2016-06-30 CN CN201680050602.5A patent/CN107922390B/zh active Active
- 2016-06-30 SI SI201631907T patent/SI3896064T1/sl unknown
- 2016-06-30 ES ES21162393T patent/ES3034100T3/es active Active
- 2016-06-30 CR CR20170599A patent/CR20170599A/es unknown
- 2016-06-30 CN CN201910292757.5A patent/CN109879859B/zh active Active
- 2016-06-30 PL PL18186568T patent/PL3456717T3/pl unknown
- 2016-06-30 IL IL293770A patent/IL293770B2/en unknown
- 2016-06-30 KR KR1020247000058A patent/KR20240008398A/ko not_active Ceased
- 2016-06-30 PL PL21162393.9T patent/PL3896064T3/pl unknown
- 2016-06-30 SI SI201631197T patent/SI3456717T1/sl unknown
- 2016-06-30 PT PT16738976T patent/PT3191470T/pt unknown
- 2016-06-30 CN CN202411260421.8A patent/CN119143730A/zh active Pending
- 2016-06-30 EP EP21162393.9A patent/EP3896064B1/en active Active
- 2016-06-30 LT LTEP16738976.6T patent/LT3191470T/lt unknown
- 2016-06-30 WO PCT/US2016/040520 patent/WO2017007689A1/en not_active Ceased
- 2016-07-04 BR BR102016015656-4A patent/BR102016015656B1/pt active IP Right Grant
- 2016-07-05 TW TW105121281A patent/TWI634112B/zh active
- 2016-07-05 TW TW107117905A patent/TWI699361B/zh active
- 2016-07-05 TW TW109122003A patent/TWI748539B/zh active
- 2016-07-06 UY UY0001036771A patent/UY36771A/es not_active Application Discontinuation
-
2017
- 2017-02-09 US US15/429,086 patent/US9878995B2/en active Active
- 2017-04-18 SA SA517381350A patent/SA517381350B1/ar unknown
- 2017-12-20 IL IL256433A patent/IL256433B/en active IP Right Grant
- 2017-12-22 EC ECIEPI201784635A patent/ECSP17084635A/es unknown
- 2017-12-22 CO CONC2017/0013351A patent/CO2017013351A2/es unknown
- 2017-12-22 SV SV2017005605A patent/SV2017005605A/es unknown
- 2017-12-22 CL CL2017003356A patent/CL2017003356A1/es unknown
- 2017-12-26 DO DO2017000311A patent/DOP2017000311A/es unknown
-
2018
- 2018-01-03 PH PH12018500031A patent/PH12018500031A1/en unknown
- 2018-02-07 US US15/891,163 patent/US20180237455A1/en not_active Abandoned
- 2018-09-13 JP JP2018171794A patent/JP6781221B2/ja active Active
-
2019
- 2019-04-23 US US16/391,673 patent/US20190248807A1/en not_active Abandoned
- 2019-05-03 AU AU2019203122A patent/AU2019203122B2/en active Active
- 2019-05-20 CY CY20191100535T patent/CY1121750T1/el unknown
- 2019-05-29 IL IL266995A patent/IL266995B/en active IP Right Grant
- 2019-07-26 JP JP2019137759A patent/JP6906021B2/ja active Active
- 2019-12-17 US US16/717,074 patent/US11066414B2/en active Active
-
2020
- 2020-09-06 PH PH12020551397A patent/PH12020551397A1/en unknown
- 2020-10-20 AU AU2020257055A patent/AU2020257055B2/en active Active
- 2020-12-16 JP JP2020208330A patent/JP7138155B2/ja active Active
-
2021
- 2021-05-11 US US17/317,041 patent/US11905299B2/en active Active
-
2022
- 2022-04-11 JP JP2022065168A patent/JP2022082816A/ja not_active Withdrawn
- 2022-06-10 AU AU2022204050A patent/AU2022204050B2/en active Active
-
2023
- 2023-12-11 US US18/534,800 patent/US20240254137A1/en not_active Abandoned
-
2024
- 2024-05-17 JP JP2024081151A patent/JP2024100865A/ja not_active Withdrawn
- 2024-07-17 AU AU2024204902A patent/AU2024204902A1/en not_active Abandoned
-
2025
- 2025-04-14 US US19/177,702 patent/US20250346609A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2018520161A5 (enExample) | ||
| HRP20190853T1 (hr) | Cot modulatori i postupci za njihovu upotrebu | |
| AU2020205294B2 (en) | 2-aminopyrimidin-6-ones and analogs exhibiting anti-cancer and anti-proliferative activities | |
| JP2013533884A5 (enExample) | ||
| JP2013533883A5 (enExample) | ||
| JP2013525433A5 (enExample) | ||
| AU2021414253A9 (en) | Series of piperidine-substituted benzoic acid compounds, and use thereof | |
| AU2019217320B2 (en) | Steroid derivative regulators, method for preparing the same, and uses thereof | |
| JP2013530238A5 (enExample) | ||
| JP2018511647A5 (enExample) | ||
| JP2018504437A5 (enExample) | ||
| PT2794604T (pt) | Novas di-hidropirimidinoisoquinolinonas e as suas composições farmacêuticas para o tratamento de doenças inflamatórias | |
| RU2015149767A (ru) | Дейтерированные диаминопиримидиновые соединения и фармацевтические композиции, содержащие такие соединения | |
| JP2008520744A (ja) | 抗炎症性ピラゾロピリミジン | |
| CA2797533A1 (en) | Compounds that modulate intracellular calcium | |
| JP2013536259A5 (enExample) | ||
| JP2018510131A5 (enExample) | ||
| JP2018537480A5 (enExample) | ||
| JP2010534670A5 (enExample) | ||
| JPWO2015129821A1 (ja) | オートタキシン阻害活性を有する縮合ピラゾール誘導体 | |
| JPWO2021185256A5 (enExample) | ||
| JPWO2020025517A5 (enExample) | ||
| JP2013530239A5 (enExample) | ||
| JPWO2021071802A5 (enExample) | ||
| JPWO2021092246A5 (enExample) |