JPWO2020060914A5 - - Google Patents
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- JPWO2020060914A5 JPWO2020060914A5 JP2021515046A JP2021515046A JPWO2020060914A5 JP WO2020060914 A5 JPWO2020060914 A5 JP WO2020060914A5 JP 2021515046 A JP2021515046 A JP 2021515046A JP 2021515046 A JP2021515046 A JP 2021515046A JP WO2020060914 A5 JPWO2020060914 A5 JP WO2020060914A5
- Authority
- JP
- Japan
- Prior art keywords
- independently
- alkyl
- haloalkyl
- cycloalkyl
- stereoisomer
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 43
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 26
- 125000003545 alkoxy group Chemical group 0.000 claims description 21
- 150000001875 compounds Chemical class 0.000 claims description 19
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 17
- -1 cyano, hydroxyl Chemical group 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
- 239000001257 hydrogen Substances 0.000 claims description 17
- 150000003839 salts Chemical class 0.000 claims description 17
- 239000012453 solvate Substances 0.000 claims description 17
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 14
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 9
- 125000003282 alkyl amino group Chemical group 0.000 claims description 8
- 125000002947 alkylene group Chemical group 0.000 claims description 7
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims 15
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 7
- 206010016654 Fibrosis Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 230000004761 fibrosis Effects 0.000 claims 6
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 5
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 5
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 208000020832 chronic kidney disease Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 102100040607 Lysophosphatidic acid receptor 1 Human genes 0.000 claims 2
- 101710149745 Lysophosphatidic acid receptor 1 Proteins 0.000 claims 2
- 206010064930 age-related macular degeneration Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 208000004296 neuralgia Diseases 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 210000003491 skin Anatomy 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 208000009304 Acute Kidney Injury Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010058019 Cancer Pain Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000005016 Intestinal Neoplasms Diseases 0.000 claims 1
- 206010072877 Intestinal fibrosis Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000001132 Osteoporosis 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
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000033626 Renal failure acute Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010050207 Skin fibrosis Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 201000011040 acute kidney failure Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000008482 dysregulation Effects 0.000 claims 1
- 210000004696 endometrium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 210000002216 heart Anatomy 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 210000002429 large intestine Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 208000026037 malignant tumor of neck Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 210000002850 nasal mucosa Anatomy 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000005443 oral cavity cancer Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 230000001850 reproductive effect Effects 0.000 claims 1
- 230000002784 sclerotic effect Effects 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 210000000952 spleen Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 description 9
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 7
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862732588P | 2018-09-18 | 2018-09-18 | |
| US62/732,588 | 2018-09-18 | ||
| PCT/US2019/051272 WO2020060914A1 (en) | 2018-09-18 | 2019-09-16 | Oxabicyclo acids as lpa antagonists |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022500473A JP2022500473A (ja) | 2022-01-04 |
| JP2022500473A5 JP2022500473A5 (https=) | 2023-11-08 |
| JPWO2020060914A5 true JPWO2020060914A5 (https=) | 2023-11-08 |
| JP7412424B2 JP7412424B2 (ja) | 2024-01-12 |
Family
ID=68073221
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021515046A Active JP7412424B2 (ja) | 2018-09-18 | 2019-09-16 | Ｌｐａアンタゴニストとしてのオキサビシクロ酸 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US12428430B2 (https=) |
| EP (1) | EP3853232B1 (https=) |
| JP (1) | JP7412424B2 (https=) |
| KR (1) | KR102788997B1 (https=) |
| CN (1) | CN113366000A (https=) |
| ES (1) | ES2941774T3 (https=) |
| WO (1) | WO2020060914A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20220041572A1 (en) * | 2018-09-18 | 2022-02-10 | Bristol-Myers Squibb Company | Cycloheptyl acids as lpa antagonists |
| ES2946657T3 (es) * | 2018-09-18 | 2023-07-24 | Bristol Myers Squibb Co | Acidos ciclopentílicos como antagonistas de LPA |
| AU2020384883B2 (en) | 2019-11-15 | 2023-11-16 | Gilead Sciences, Inc. | Triazole carbamate pyridyl sulfonamides as LPA receptor antagonists and uses thereof |
| TWI843503B (zh) | 2020-06-03 | 2024-05-21 | 美商基利科學股份有限公司 | Lpa受體拮抗劑及其用途 |
| CN115867556B (zh) | 2020-06-03 | 2025-05-06 | 吉利德科学公司 | Lpa受体拮抗剂及其用途 |
| TWI853704B (zh) | 2021-05-11 | 2024-08-21 | 美商基利科學股份有限公司 | Lpa受體拮抗劑及其用途 |
| KR20240007233A (ko) | 2021-05-13 | 2024-01-16 | 길리애드 사이언시즈, 인코포레이티드 | Lpa 수용체 길항제 및 이의 용도 |
| NO346587B1 (en) * | 2021-06-02 | 2022-10-17 | Axichem Ab | Capsaicin derivatives in the treatment of idiopathic pulmonary fibrosis |
| WO2023107938A1 (en) | 2021-12-08 | 2023-06-15 | Gilead Sciences, Inc. | Lpa receptor antagonists and uses thereof |
| AR128613A1 (es) | 2022-02-25 | 2024-05-29 | Lhotse Bio Inc | Compuestos y composiciones para el tratamiento de afecciones asociadas con la actividad del receptor de lpa |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100390178C (zh) | 1999-11-12 | 2008-05-28 | 拜奥根Idec马萨诸塞公司 | 作为腺苷受体拮抗剂的多环烷基嘌呤 |
| WO2002062389A1 (en) | 2001-02-08 | 2002-08-15 | Ono Pharmaceutical Co., Ltd. | Remedies for urinary diseases comprising lpa receptor controlling agents |
| US20080186971A1 (en) | 2007-02-02 | 2008-08-07 | Tarari, Inc. | Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic |
| WO2011017350A2 (en) | 2009-08-04 | 2011-02-10 | Amira Pharmaceuticals, Inc. | Compounds as lysophosphatidic acid receptor antagonists |
| GB2474120B (en) | 2009-10-01 | 2011-12-21 | Amira Pharmaceuticals Inc | Compounds as Lysophosphatidic acid receptor antagonists |
| GB2474748B (en) | 2009-10-01 | 2011-10-12 | Amira Pharmaceuticals Inc | Polycyclic compounds as lysophosphatidic acid receptor antagonists |
| TW201120016A (en) | 2009-12-08 | 2011-06-16 | Abbott Lab | Novel oxadiazole compounds |
| EP3360552A1 (en) * | 2010-12-07 | 2018-08-15 | Amira Pharmaceuticals, Inc. | Polycyclic lpa1 antagonist and uses thereof |
| EA201390821A1 (ru) | 2010-12-07 | 2013-10-30 | Амира Фармасьютикалс, Инк. | Антагонисты рецепторов лизофосфатидной кислоты и их применение |
| WO2012138648A1 (en) | 2011-04-06 | 2012-10-11 | Irm Llc | Compositions and methods for modulating lpa receptors |
| WO2013070879A1 (en) | 2011-11-10 | 2013-05-16 | Bristol-Myers Squibb Company | Methods for treating spinal cord injury with lpa receptor antagonists |
| SG11201406526WA (en) | 2012-04-27 | 2014-11-27 | Novartis Ag | Cyclic bridgehead ether dgat1 inhibitors |
| SG11201407228PA (en) | 2012-06-20 | 2014-12-30 | Hoffmann La Roche | N-aryltriazole compounds as lpar antagonists |
| UA109868C2 (ru) | 2012-06-20 | 2015-10-12 | Ф. Хоффманн-Ля Рош Аг | Соединения n-алкилтриазола как антагонисты лизофосфатидной кислоты (lpar) |
| WO2014113485A1 (en) | 2013-01-15 | 2014-07-24 | Intermune, Inc. | Lysophosphatidic acid receptor antagonists |
| US8962660B2 (en) * | 2013-03-14 | 2015-02-24 | Bristol-Myers Squibb Company | Oxabicyclo [2.2.2] acid GPR120 modulators |
| DK2988743T3 (da) | 2013-03-15 | 2021-03-01 | Epigen Biosciences Inc | Heterocykliske forbindelser, der kan anvendes til behandling af sygdom |
| AR108838A1 (es) | 2016-06-21 | 2018-10-03 | Bristol Myers Squibb Co | Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa |
| JP7212047B2 (ja) | 2017-12-19 | 2023-01-24 | ブリストル－マイヤーズ スクイブ カンパニー | Ｌｐａアンタゴニストとしてのシクロヘキシル酸ピラゾールアゾール |
| CN111699180B (zh) | 2017-12-19 | 2024-11-29 | 百时美施贵宝公司 | 作为lpa拮抗剂的吡唑n-连接的氨基甲酰基环己基酸 |
| WO2019126089A1 (en) | 2017-12-19 | 2019-06-27 | Bristol-Myers Squibb Company | Cyclohexyl acid pyrazole azines as lpa antagonists |
| US11180488B2 (en) | 2017-12-19 | 2021-11-23 | Bristol-Myers Squibb Company | Isoxazole o-linked carbamoyl cyclohexyl acids as LPA antagonists |
| EP3728209B1 (en) | 2017-12-19 | 2025-12-24 | Bristol-Myers Squibb Company | Cyclohexyl acid isoxazole azines as lpa antagonists |
| EP4011875A1 (en) | 2017-12-19 | 2022-06-15 | Bristol-Myers Squibb Company | Triazole n-linked carbamoyl cyclohexyl acids as lpa antagonists |
| KR102756639B1 (ko) | 2017-12-19 | 2025-01-16 | 브리스톨-마이어스 스큅 컴퍼니 | Lpa 길항제로서의 시클로헥실 산 이속사졸 아졸 |
| US11447475B2 (en) | 2017-12-19 | 2022-09-20 | Bristol-Myers Squibb Company | Isoxazole N-linked carbamoyl cyclohexyl acids as LPA antagonists |
| CN112041302B (zh) | 2017-12-19 | 2024-11-19 | 百时美施贵宝公司 | 作为lpa拮抗剂的吡唑o-连接的氨基甲酰基环己基酸 |
| ES2946657T3 (es) | 2018-09-18 | 2023-07-24 | Bristol Myers Squibb Co | Acidos ciclopentílicos como antagonistas de LPA |
| US20220041572A1 (en) | 2018-09-18 | 2022-02-10 | Bristol-Myers Squibb Company | Cycloheptyl acids as lpa antagonists |
-
2019
- 2019-09-16 KR KR1020217011085A patent/KR102788997B1/ko active Active
- 2019-09-16 US US17/276,173 patent/US12428430B2/en active Active
- 2019-09-16 CN CN201980074322.1A patent/CN113366000A/zh active Pending
- 2019-09-16 EP EP19779297.1A patent/EP3853232B1/en active Active
- 2019-09-16 WO PCT/US2019/051272 patent/WO2020060914A1/en not_active Ceased
- 2019-09-16 JP JP2021515046A patent/JP7412424B2/ja active Active
- 2019-09-16 ES ES19779297T patent/ES2941774T3/es active Active
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