JPWO2019126085A5 - - Google Patents
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- JPWO2019126085A5 JPWO2019126085A5 JP2020533674A JP2020533674A JPWO2019126085A5 JP WO2019126085 A5 JPWO2019126085 A5 JP WO2019126085A5 JP 2020533674 A JP2020533674 A JP 2020533674A JP 2020533674 A JP2020533674 A JP 2020533674A JP WO2019126085 A5 JPWO2019126085 A5 JP WO2019126085A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- amino
- oxy
- pyrazole
- cyclohexane
- 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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- NZNMSOFKMUBTKW-UHFFFAOYSA-N cyclohexanecarboxylic acid Chemical compound OC(=O)C1CCCCC1 NZNMSOFKMUBTKW-UHFFFAOYSA-N 0.000 claims 61
- -1 cyano, hydroxyl Chemical group 0.000 claims 38
- 125000000217 alkyl group Chemical group 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 26
- 150000003839 salts Chemical class 0.000 claims 26
- 239000012453 solvate Substances 0.000 claims 25
- 125000003545 alkoxy group Chemical group 0.000 claims 22
- 125000001188 haloalkyl group Chemical group 0.000 claims 18
- 125000004994 halo alkoxy alkyl group Chemical group 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 14
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 13
- 125000004103 aminoalkyl group Chemical group 0.000 claims 13
- 125000005843 halogen group Chemical group 0.000 claims 13
- 125000003282 alkyl amino group Chemical group 0.000 claims 11
- 125000004438 haloalkoxy group Chemical group 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 206010016654 Fibrosis Diseases 0.000 claims 8
- 230000004761 fibrosis Effects 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000008338 non-alcoholic fatty liver disease Diseases 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- GSBYCHUVIAIDRI-YJBOKZPZSA-N FC1=C(COC(=O)NCC2=C(C=NN2C)C2=CC=C(C=N2)O[C@@H]2C[C@H](CCC2)C(=O)O)C=C(C=C1)F Chemical compound FC1=C(COC(=O)NCC2=C(C=NN2C)C2=CC=C(C=N2)O[C@@H]2C[C@H](CCC2)C(=O)O)C=C(C=C1)F GSBYCHUVIAIDRI-YJBOKZPZSA-N 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 208000020832 chronic kidney disease Diseases 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 210000004072 lung Anatomy 0.000 claims 3
- IVSIYBXNSGHEIT-KBPBESRZSA-N (1S,3S)-3-[4-methyl-2-[1-methyl-5-[(2-methylpropan-2-yl)oxycarbonylamino]pyrazol-4-yl]pyrimidin-5-yl]oxycyclohexane-1-carboxylic acid Chemical compound C(C)(C)(C)OC(=O)NC1=C(C=NN1C)C1=NC=C(C(=N1)C)O[C@@H]1C[C@H](CCC1)C(=O)O IVSIYBXNSGHEIT-KBPBESRZSA-N 0.000 claims 2
- BWGYKJRRIMLVJC-IRXDYDNUSA-N (1S,3S)-3-[6-[5-[(butoxycarbonylamino)methyl]-1-methylpyrazol-4-yl]-2-methylpyridin-3-yl]oxycyclohexane-1-carboxylic acid Chemical compound C(CCC)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C(=N1)C)O[C@@H]1C[C@H](CCC1)C(=O)O BWGYKJRRIMLVJC-IRXDYDNUSA-N 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- CPLNEDJDVKFMJE-HOTGVXAUSA-N C(C(C)C)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O Chemical compound C(C(C)C)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O CPLNEDJDVKFMJE-HOTGVXAUSA-N 0.000 claims 2
- FHGCDKFMVKGHBV-OALUTQOASA-N C(C1=CC=CC=C1)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O Chemical compound C(C1=CC=CC=C1)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O FHGCDKFMVKGHBV-OALUTQOASA-N 0.000 claims 2
- IEDAWVLMSWGZHO-IRXDYDNUSA-N C(CCC)OC(=O)N(C)CC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O Chemical compound C(CCC)OC(=O)N(C)CC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O IEDAWVLMSWGZHO-IRXDYDNUSA-N 0.000 claims 2
- LDTAIINMBIJQJO-GJZGRUSLSA-N C(CCC)OC(=O)NC1=C(C=NN1C)C1=NC=C(C(=N1)C)O[C@@H]1C[C@H](CCC1)C(=O)O Chemical compound C(CCC)OC(=O)NC1=C(C=NN1C)C1=NC=C(C(=N1)C)O[C@@H]1C[C@H](CCC1)C(=O)O LDTAIINMBIJQJO-GJZGRUSLSA-N 0.000 claims 2
- LMOPIWVUWLXYKK-HOTGVXAUSA-N C(CCC)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O Chemical compound C(CCC)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O LMOPIWVUWLXYKK-HOTGVXAUSA-N 0.000 claims 2
- AQVFUUCKVGAVAT-HOTGVXAUSA-N C(CCC)OC(=O)NCC1=C(C=NN1C)C=1N=C(C(=NC=1)O[C@@H]1C[C@H](CCC1)C(=O)O)C Chemical compound C(CCC)OC(=O)NCC1=C(C=NN1C)C=1N=C(C(=NC=1)O[C@@H]1C[C@H](CCC1)C(=O)O)C AQVFUUCKVGAVAT-HOTGVXAUSA-N 0.000 claims 2
- XYEYPRROBGENEH-ROUUACIJSA-N C(CCCCC)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O Chemical compound C(CCCCC)OC(=O)NCC1=C(C=NN1C)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O XYEYPRROBGENEH-ROUUACIJSA-N 0.000 claims 2
- YAGRIXYKDPDDKZ-HOTGVXAUSA-N CC1=NC(=CC=C1O[C@@H]1C[C@H](CCC1)C(=O)O)C=1C=NN(C=1CNC(=O)OCCC)C Chemical compound CC1=NC(=CC=C1O[C@@H]1C[C@H](CCC1)C(=O)O)C=1C=NN(C=1CNC(=O)OCCC)C YAGRIXYKDPDDKZ-HOTGVXAUSA-N 0.000 claims 2
- LFHZOUDMAGPSSQ-IRXDYDNUSA-N CN1N=CC(=C1CNC(=O)OCCCCC)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O Chemical compound CN1N=CC(=C1CNC(=O)OCCCCC)C1=CC=C(C=N1)O[C@@H]1C[C@H](CCC1)C(=O)O LFHZOUDMAGPSSQ-IRXDYDNUSA-N 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- NPYVDYJNYPFSEH-PXNSSMCTSA-N FC=1C=C(COC(=O)NCC2=C(C=NN2C)C2=CC=C(C(=N2)C)O[C@@H]2C[C@H](CCC2)C(=O)O)C=C(C=1)F Chemical compound FC=1C=C(COC(=O)NCC2=C(C=NN2C)C2=CC=C(C(=N2)C)O[C@@H]2C[C@H](CCC2)C(=O)O)C=C(C=1)F NPYVDYJNYPFSEH-PXNSSMCTSA-N 0.000 claims 2
- QWDBIIXZERKDJB-LPHOPBHVSA-N FC=1C=C(COC(=O)NCC2=C(C=NN2C)C2=CC=C(C=N2)O[C@@H]2C[C@H](CCC2)C(=O)O)C=C(C=1)F Chemical compound FC=1C=C(COC(=O)NCC2=C(C=NN2C)C2=CC=C(C=N2)O[C@@H]2C[C@H](CCC2)C(=O)O)C=C(C=1)F QWDBIIXZERKDJB-LPHOPBHVSA-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
- 241000124008 Mammalia Species 0.000 claims 2
- 125000003342 alkenyl group Chemical group 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
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- VZFUCHSFHOYXIS-UHFFFAOYSA-N cycloheptane carboxylic acid Natural products OC(=O)C1CCCCCC1 VZFUCHSFHOYXIS-UHFFFAOYSA-N 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia 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
- 208000031422 Lymphocytic Chronic B-Cell Leukemia 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
- 208000002193 Pain 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
- 208000012322 Raynaud phenomenon Diseases 0.000 claims 1
- 206010039710 Scleroderma 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
- 230000001154 acute effect Effects 0.000 claims 1
- 230000001476 alcoholic effect Effects 0.000 claims 1
- 125000000033 alkoxyamino group Chemical group 0.000 claims 1
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 210000000941 bile Anatomy 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
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 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
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 210000004207 dermis Anatomy 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000008482 dysregulation Effects 0.000 claims 1
- 230000002357 endometrial effect Effects 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- 239000000835 fiber Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 210000004392 genitalia 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
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 210000002216 heart Anatomy 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 210000002429 large intestine Anatomy 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 210000002200 mouth mucosa Anatomy 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 210000002850 nasal mucosa Anatomy 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 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
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 210000003800 pharynx Anatomy 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 239000002904 solvent Substances 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
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762607541P | 2017-12-19 | 2017-12-19 | |
| US62/607,541 | 2017-12-19 | ||
| PCT/US2018/066110 WO2019126085A1 (en) | 2017-12-19 | 2018-12-18 | Pyrazole n-linked carbamoyl cyclohexyl acids as lpa antagonists |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021507895A JP2021507895A (ja) | 2021-02-25 |
| JPWO2019126085A5 true JPWO2019126085A5 (https=) | 2022-02-01 |
| JP2021507895A5 JP2021507895A5 (https=) | 2022-02-01 |
| JP7301839B2 JP7301839B2 (ja) | 2023-07-03 |
Family
ID=65003575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020533674A Active JP7301839B2 (ja) | 2017-12-19 | 2018-12-18 | Ｌｐａアンタゴニストとしてのピラゾールｎ－連結のカルバモイルシクロヘキシル酸 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11384067B2 (https=) |
| EP (1) | EP3728216B1 (https=) |
| JP (1) | JP7301839B2 (https=) |
| KR (1) | KR102698386B1 (https=) |
| CN (1) | CN111699180B (https=) |
| AU (1) | AU2018388482A1 (https=) |
| BR (1) | BR112020011953A2 (https=) |
| CA (1) | CA3085347A1 (https=) |
| EA (1) | EA202091500A1 (https=) |
| ES (1) | ES2962367T3 (https=) |
| IL (1) | IL275361A (https=) |
| MX (1) | MX2020005874A (https=) |
| SG (1) | SG11202005701VA (https=) |
| WO (1) | WO2019126085A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR108838A1 (es) | 2016-06-21 | 2018-10-03 | Bristol Myers Squibb Co | Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa |
| EP4011875A1 (en) | 2017-12-19 | 2022-06-15 | Bristol-Myers Squibb Company | Triazole n-linked carbamoyl cyclohexyl acids as lpa antagonists |
| US11447475B2 (en) * | 2017-12-19 | 2022-09-20 | Bristol-Myers Squibb Company | Isoxazole N-linked carbamoyl cyclohexyl acids as LPA antagonists |
| KR102788997B1 (ko) | 2018-09-18 | 2025-03-28 | 브리스톨-마이어스 스큅 컴퍼니 | Lpa 길항제로서의 옥사비시클로 산 |
| ES2946657T3 (es) | 2018-09-18 | 2023-07-24 | Bristol Myers Squibb Co | Acidos ciclopentílicos como antagonistas de LPA |
| CN111434655A (zh) * | 2019-01-15 | 2020-07-21 | 武汉朗来科技发展有限公司 | 溶血磷脂酸受体拮抗剂及其制备方法 |
| 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 |
| CN114456157A (zh) * | 2020-11-10 | 2022-05-10 | 武汉人福创新药物研发中心有限公司 | 氮取代氨基碳酸酯噻吩类化合物及其用途 |
| WO2022174882A1 (en) * | 2021-02-16 | 2022-08-25 | Chiesi Farmaceutici S.P.A. | 5-membered heterocyclyl carbamate derivatives as dual lpa receptor 1 and lpa receptor 2 inhibitors |
| 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 |
| 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 |
| CN121773091A (zh) * | 2023-09-08 | 2026-03-31 | 西藏海思科制药有限公司 | 杂芳环衍生物的lpar1拮抗剂及其用途 |
| CN117024409A (zh) * | 2023-10-10 | 2023-11-10 | 药康众拓(北京)医药科技有限公司 | 氘代lpa1抑制剂化合物及其用途 |
| WO2026061483A1 (zh) * | 2024-09-19 | 2026-03-26 | 西藏海思科制药有限公司 | 一种lpar1拮抗剂及其用途 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002062389A1 (en) | 2001-02-08 | 2002-08-15 | Ono Pharmaceutical Co., Ltd. | Remedies for urinary diseases comprising lpa receptor controlling agents |
| US7432271B2 (en) * | 2003-09-02 | 2008-10-07 | Bristol-Myers Squibb Company | Pyrazolyl inhibitors of 15-lipoxygenase |
| DE102004038403B4 (de) | 2004-08-07 | 2006-08-31 | Sanofi-Aventis Deutschland Gmbh | Verfahren zur Herstellung der enantiomeren Formen von cis-konfigurierten 3-Hydroxycyclohexancarbonsäure-Derivaten |
| WO2011017350A2 (en) | 2009-08-04 | 2011-02-10 | 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 |
| GB2474120B (en) | 2009-10-01 | 2011-12-21 | Amira Pharmaceuticals Inc | Compounds as Lysophosphatidic acid receptor antagonists |
| EA201390821A1 (ru) | 2010-12-07 | 2013-10-30 | Амира Фармасьютикалс, Инк. | Антагонисты рецепторов лизофосфатидной кислоты и их применение |
| US8785442B2 (en) | 2011-01-30 | 2014-07-22 | Curegenix, Inc. | Compound as antagonist of lysophosphatidic acid receptor, composition, and use thereof |
| 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 |
| US20140329871A1 (en) | 2011-12-04 | 2014-11-06 | Angion Biomedica Corp. | Small molecule anti-fibrotic compounds and uses thereof |
| SG11201407229UA (en) * | 2012-06-20 | 2014-12-30 | Hoffmann La Roche | Substituted pyrazole compounds as lpar antagonists |
| 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) |
| DK2988743T3 (da) | 2013-03-15 | 2021-03-01 | Epigen Biosciences Inc | Heterocykliske forbindelser, der kan anvendes til behandling af sygdom |
| US20170283400A1 (en) * | 2014-09-17 | 2017-10-05 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| 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 |
| 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 |
| US11180488B2 (en) * | 2017-12-19 | 2021-11-23 | Bristol-Myers Squibb Company | Isoxazole o-linked carbamoyl cyclohexyl acids as LPA antagonists |
| EP4011875A1 (en) | 2017-12-19 | 2022-06-15 | Bristol-Myers Squibb Company | Triazole n-linked carbamoyl cyclohexyl acids as lpa antagonists |
-
2018
- 2018-12-18 CN CN201880089037.2A patent/CN111699180B/zh active Active
- 2018-12-18 SG SG11202005701VA patent/SG11202005701VA/en unknown
- 2018-12-18 KR KR1020207020528A patent/KR102698386B1/ko active Active
- 2018-12-18 EP EP18830676.5A patent/EP3728216B1/en active Active
- 2018-12-18 JP JP2020533674A patent/JP7301839B2/ja active Active
- 2018-12-18 US US16/954,310 patent/US11384067B2/en active Active
- 2018-12-18 MX MX2020005874A patent/MX2020005874A/es unknown
- 2018-12-18 ES ES18830676T patent/ES2962367T3/es active Active
- 2018-12-18 EA EA202091500A patent/EA202091500A1/ru unknown
- 2018-12-18 CA CA3085347A patent/CA3085347A1/en not_active Abandoned
- 2018-12-18 BR BR112020011953-9A patent/BR112020011953A2/pt not_active Application Discontinuation
- 2018-12-18 AU AU2018388482A patent/AU2018388482A1/en not_active Abandoned
- 2018-12-18 WO PCT/US2018/066110 patent/WO2019126085A1/en not_active Ceased
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2020
- 2020-06-14 IL IL275361A patent/IL275361A/en unknown
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