JP2017531624A5 - - Google Patents
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- JP2017531624A5 JP2017531624A5 JP2017513748A JP2017513748A JP2017531624A5 JP 2017531624 A5 JP2017531624 A5 JP 2017531624A5 JP 2017513748 A JP2017513748 A JP 2017513748A JP 2017513748 A JP2017513748 A JP 2017513748A JP 2017531624 A5 JP2017531624 A5 JP 2017531624A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- nhc
- nhnh
- heteroaryl
- 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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- 125000001072 heteroaryl group Chemical group 0.000 claims 55
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 52
- 125000000217 alkyl group Chemical group 0.000 claims 48
- 125000003118 aryl group Chemical group 0.000 claims 48
- 125000000753 cycloalkyl group Chemical group 0.000 claims 48
- 125000004404 heteroalkyl group Chemical group 0.000 claims 48
- 229910052736 halogen Inorganic materials 0.000 claims 43
- 150000002367 halogens Chemical class 0.000 claims 43
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 38
- 150000001875 compounds Chemical class 0.000 claims 35
- 125000004474 heteroalkylene group Chemical group 0.000 claims 27
- -1 —OH Inorganic materials 0.000 claims 18
- 125000005549 heteroarylene group Chemical group 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 125000002947 alkylene group Chemical group 0.000 claims 12
- 125000000732 arylene group Chemical group 0.000 claims 12
- 125000002993 cycloalkylene group Chemical group 0.000 claims 12
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 9
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 8
- 101150065749 Churc1 gene Proteins 0.000 claims 8
- 102100038239 Protein Churchill Human genes 0.000 claims 8
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000005647 linker group Chemical group 0.000 claims 6
- GYLDXIAOMVERTK-UHFFFAOYSA-N 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine Chemical compound C12=C(N)N=CN=C2N(C(C)C)N=C1C1=CC=C(OC(N)=N2)C2=C1 GYLDXIAOMVERTK-UHFFFAOYSA-N 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical class C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 4
- 229950009216 sapanisertib Drugs 0.000 claims 4
- 229960002930 sirolimus Drugs 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 102000008135 Mechanistic Target of Rapamycin Complex 1 Human genes 0.000 claims 3
- 108010035196 Mechanistic Target of Rapamycin Complex 1 Proteins 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- SVNJBEMPMKWDCO-KCHLEUMXSA-N (2s)-2-[[(2s)-3-carboxy-2-[[2-[[(2s)-5-(diaminomethylideneamino)-2-[[4-oxo-4-[[4-(4-oxo-8-phenylchromen-2-yl)morpholin-4-ium-4-yl]methoxy]butanoyl]amino]pentanoyl]amino]acetyl]amino]propanoyl]amino]-3-hydroxypropanoate Chemical compound C=1C(=O)C2=CC=CC(C=3C=CC=CC=3)=C2OC=1[N+]1(COC(=O)CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C([O-])=O)CCOCC1 SVNJBEMPMKWDCO-KCHLEUMXSA-N 0.000 claims 2
- 125000006587 (C5-C10) heteroarylene group Chemical group 0.000 claims 2
- DWZAEMINVBZMHQ-UHFFFAOYSA-N 1-[4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl]-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea Chemical compound C1CC(N(C)C)CCN1C(=O)C(C=C1)=CC=C1NC(=O)NC1=CC=C(C=2N=C(N=C(N=2)N2CCOCC2)N2CCOCC2)C=C1 DWZAEMINVBZMHQ-UHFFFAOYSA-N 0.000 claims 2
- RGJOJUGRHPQXGF-INIZCTEOSA-N 1-ethyl-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-7-(oxetan-3-yl)-6,8-dihydro-5h-pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea Chemical compound C1=CC(NC(=O)NCC)=CC=C1C(N=C1N2[C@H](COCC2)C)=NC2=C1CCN(C1COC1)C2 RGJOJUGRHPQXGF-INIZCTEOSA-N 0.000 claims 2
- XDLYKKIQACFMJG-UHFFFAOYSA-N 2-amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one Chemical compound C1=NC(OC)=CC=C1C(C1=O)=CC2=C(C)N=C(N)N=C2N1C1CCC(OCCO)CC1 XDLYKKIQACFMJG-UHFFFAOYSA-N 0.000 claims 2
- JUSFANSTBFGBAF-IRXDYDNUSA-N 3-[2,4-bis[(3s)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-n-methylbenzamide Chemical compound CNC(=O)C1=CC=CC(C=2N=C3N=C(N=C(C3=CC=2)N2[C@H](COCC2)C)N2[C@H](COCC2)C)=C1 JUSFANSTBFGBAF-IRXDYDNUSA-N 0.000 claims 2
- KVLFRAWTRWDEDF-IRXDYDNUSA-N AZD-8055 Chemical compound C1=C(CO)C(OC)=CC=C1C1=CC=C(C(=NC(=N2)N3[C@H](COCC3)C)N3[C@H](COCC3)C)C2=N1 KVLFRAWTRWDEDF-IRXDYDNUSA-N 0.000 claims 2
- YUXMAKUNSXIEKN-BTJKTKAUSA-N BGT226 Chemical compound OC(=O)\C=C/C(O)=O.C1=NC(OC)=CC=C1C1=CC=C(N=CC2=C3N(C=4C=C(C(N5CCNCC5)=CC=4)C(F)(F)F)C(=O)N2C)C3=C1 YUXMAKUNSXIEKN-BTJKTKAUSA-N 0.000 claims 2
- UFKLYTOEMRFKAD-SHTZXODSSA-N C1C[C@@H](OC)CC[C@@H]1N1C2=NC(C=3C=NC(=CC=3)C(C)(C)O)=CN=C2NCC1=O Chemical compound C1C[C@@H](OC)CC[C@@H]1N1C2=NC(C=3C=NC(=CC=3)C(C)(C)O)=CN=C2NCC1=O UFKLYTOEMRFKAD-SHTZXODSSA-N 0.000 claims 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- TUVCWJQQGGETHL-UHFFFAOYSA-N PI-103 Chemical compound OC1=CC=CC(C=2N=C3C4=CC=CN=C4OC3=C(N3CCOCC3)N=2)=C1 TUVCWJQQGGETHL-UHFFFAOYSA-N 0.000 claims 2
- NVRXTLZYXZNATH-UHFFFAOYSA-N PP121 Chemical compound N1=C(C=2C=C3C=CNC3=NC=2)C=2C(N)=NC=NC=2N1C1CCCC1 NVRXTLZYXZNATH-UHFFFAOYSA-N 0.000 claims 2
- 208000031481 Pathologic Constriction Diseases 0.000 claims 2
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000005874 benzothiadiazolyl group Chemical group 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 235000010290 biphenyl Nutrition 0.000 claims 2
- 239000004305 biphenyl Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 229950006418 dactolisib Drugs 0.000 claims 2
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical compound O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 claims 2
- 125000002720 diazolyl group Chemical group 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000005956 isoquinolyl group Chemical group 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 2
- VDOCQQKGPJENHJ-UHFFFAOYSA-N methyl n-[4-[4-morpholin-4-yl-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamate Chemical compound C1=CC(NC(=O)OC)=CC=C1C1=NC(N2CCOCC2)=C(C=NN2C3CCN(CC=4C=NC=CC=4)CC3)C2=N1 VDOCQQKGPJENHJ-UHFFFAOYSA-N 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000005493 quinolyl group Chemical group 0.000 claims 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 2
- 208000037804 stenosis Diseases 0.000 claims 2
- 230000036262 stenosis Effects 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- AKCRNFFTGXBONI-UHFFFAOYSA-N torin 1 Chemical compound C1CN(C(=O)CC)CCN1C1=CC=C(N2C(C=CC3=C2C2=CC(=CC=C2N=C3)C=2C=C3C=CC=CC3=NC=2)=O)C=C1C(F)(F)F AKCRNFFTGXBONI-UHFFFAOYSA-N 0.000 claims 2
- GUXXEUUYCAYESJ-UHFFFAOYSA-N torin 2 Chemical compound C1=NC(N)=CC=C1C1=CC=C(N=CC2=C3N(C=4C=C(C=CC=4)C(F)(F)F)C(=O)C=C2)C3=C1 GUXXEUUYCAYESJ-UHFFFAOYSA-N 0.000 claims 2
- MFAQYJIYDMLAIM-UHFFFAOYSA-N torkinib Chemical compound C12=C(N)N=CN=C2N(C(C)C)N=C1C1=CC2=CC(O)=CC=C2N1 MFAQYJIYDMLAIM-UHFFFAOYSA-N 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000026372 Congenital cystic kidney disease Diseases 0.000 claims 1
- 208000026292 Cystic Kidney disease Diseases 0.000 claims 1
- 206010017533 Fungal infection Diseases 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 230000005784 autoimmunity Effects 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical class N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000005559 triazolylene group Chemical group 0.000 claims 1
- VMXMBPPFDJEVAB-UHFFFAOYSA-P CC(CC(CCC1OCCOCC(N=N)=C[NH2+]CCOCCOCCOCCOCCOCCOCCOCCOCCC(NCCCC[NH2+]c2ncnc(N)c2C(c2ccc3[o]c(N)nc3c2)=N)=O)CC1OC)C(CC(C(C)C=C(C)C(C(C(C(C)CC(C)C=CC=CC=C(C)C(CC(CCC1C)OC1(C(C(N1C2CCCC1)=O)=O)O)OC)=O)OC)O)=O)OC2=O Chemical compound CC(CC(CCC1OCCOCC(N=N)=C[NH2+]CCOCCOCCOCCOCCOCCOCCOCCOCCC(NCCCC[NH2+]c2ncnc(N)c2C(c2ccc3[o]c(N)nc3c2)=N)=O)CC1OC)C(CC(C(C)C=C(C)C(C(C(C(C)CC(C)C=CC=CC=C(C)C(CC(CCC1C)OC1(C(C(N1C2CCCC1)=O)=O)O)OC)=O)OC)O)=O)OC2=O VMXMBPPFDJEVAB-UHFFFAOYSA-P 0.000 description 1
- 0 C[C@](C[C@](CC[C@@]1O)(C[C@]1OC)I#C)[C@](CC([C@](C)C=C(C)[C@@](*)[C@](C([C@](C)C[C@](C)C=CC=CC=C(C)[C@](C[C@@](CC[C@]1C)(C#C)OC1(C(C(*(CCCC1)[C@@]11C=C)=O)=O)OC)OC)=O)OC)=O)OC1=O Chemical compound C[C@](C[C@](CC[C@@]1O)(C[C@]1OC)I#C)[C@](CC([C@](C)C=C(C)[C@@](*)[C@](C([C@](C)C[C@](C)C=CC=CC=C(C)[C@](C[C@@](CC[C@]1C)(C#C)OC1(C(C(*(CCCC1)[C@@]11C=C)=O)=O)OC)OC)=O)OC)=O)OC1=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462049186P | 2014-09-11 | 2014-09-11 | |
| US62/049,186 | 2014-09-11 | ||
| PCT/US2015/049693 WO2016040806A1 (en) | 2014-09-11 | 2015-09-11 | mTORC1 INHIBITORS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020072118A Division JP7057798B2 (ja) | 2014-09-11 | 2020-04-14 | ｍＴＯＲＣ１阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017531624A JP2017531624A (ja) | 2017-10-26 |
| JP2017531624A5 true JP2017531624A5 (https=) | 2019-03-28 |
| JP6692798B2 JP6692798B2 (ja) | 2020-05-13 |
Family
ID=55459613
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017513748A Active JP6692798B2 (ja) | 2014-09-11 | 2015-09-11 | ｍＴＯＲＣ１阻害剤 |
| JP2020072118A Active JP7057798B2 (ja) | 2014-09-11 | 2020-04-14 | ｍＴＯＲＣ１阻害剤 |
| JP2022064349A Pending JP2022091995A (ja) | 2014-09-11 | 2022-04-08 | ｍＴＯＲＣ１阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020072118A Active JP7057798B2 (ja) | 2014-09-11 | 2020-04-14 | ｍＴＯＲＣ１阻害剤 |
| JP2022064349A Pending JP2022091995A (ja) | 2014-09-11 | 2022-04-08 | ｍＴＯＲＣ１阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (5) | US10117945B2 (https=) |
| EP (1) | EP3193902A4 (https=) |
| JP (3) | JP6692798B2 (https=) |
| CN (2) | CN107073066B (https=) |
| CA (1) | CA2960992C (https=) |
| MX (2) | MX2017001981A (https=) |
| WO (1) | WO2016040806A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016040806A1 (en) | 2014-09-11 | 2016-03-17 | The Regents Of The University Of California | mTORC1 INHIBITORS |
| WO2016094307A1 (en) | 2014-12-08 | 2016-06-16 | The Research Foundation For The State University Of New York | Anti-fungals targeting the synthesis of fungal shingolipids |
| US10683308B2 (en) * | 2015-09-11 | 2020-06-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
| CA3061907A1 (en) * | 2017-05-02 | 2018-11-08 | Revolution Medicines, Inc. | Rapamycin analogs as mtor inhibitors |
| WO2018232298A1 (en) | 2017-06-16 | 2018-12-20 | The Research Foundation For The State University Of New York | Anti-fungals compounds targeting the synthesis of fungal sphingolipids |
| JP6944584B2 (ja) * | 2017-07-20 | 2021-10-06 | キュリジン カンパニー，リミテッド | ＡＲ遺伝子及びｍＴＯＲ遺伝子の発現を同時に抑制する核酸 |
| WO2019178536A1 (en) * | 2018-03-16 | 2019-09-19 | The Regents Of The University Of California | Mtor inhibitors and uses thereof |
| CN112368289B (zh) * | 2018-05-01 | 2024-02-20 | 锐新医药公司 | 作为mtor抑制剂的c26-连接的雷帕霉素类似物 |
| IL300091A (en) | 2018-05-01 | 2023-03-01 | Revolution Medicines Inc | C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors |
| CN108676882B (zh) * | 2018-05-30 | 2022-02-22 | 中山大学肿瘤防治中心（中山大学附属肿瘤医院、中山大学肿瘤研究所） | NOP14基因及其蛋白作为肿瘤对mTOR抑制剂敏感性的标志物的应用 |
| IL314362A (en) | 2018-06-15 | 2024-09-01 | Janssen Pharmaceutica Nv | Rapamycin analogs and their uses |
| EP3914245A4 (en) * | 2019-01-22 | 2022-08-24 | Aeovian Pharmaceuticals, Inc. | MTORC-1 MODULATORS AND USES THEREOF |
| WO2020163594A1 (en) | 2019-02-07 | 2020-08-13 | The Regents Of The University Of California | Immunophilin binding agents and uses thereof |
| US20220193242A1 (en) * | 2019-02-07 | 2022-06-23 | The Regents Of The University Of California | Immunophilin-dependent inhibitors and uses thereof |
| CN110152004B (zh) * | 2019-07-08 | 2021-09-03 | 天津医科大学 | 甘氨酸在制备药物递送增强剂及细胞移植试剂方面的用途 |
| KR20220128345A (ko) | 2019-12-05 | 2022-09-20 | 아나쿠리아 테라퓨틱스, 인코포레이티드 | 라파마이신 유사체 및 이의 용도 |
| WO2021195599A1 (en) | 2020-03-27 | 2021-09-30 | Aeovian Pharmaceuticals, Inc. | Mtorc1 modulators and uses thereof |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| EP4185590A2 (en) * | 2020-07-21 | 2023-05-31 | Aeovian Pharmaceuticals, Inc. | Mtorc1 modulators and uses thereof |
| CN114507236A (zh) * | 2022-02-28 | 2022-05-17 | 山东中医药大学 | mTOR蛋白降解靶向嵌合体及其制备方法和应用 |
| AU2023275778A1 (en) | 2022-05-25 | 2024-12-12 | Revolution Medicines, Inc. | Methods of treating cancer with an mtor inhibitor |
| WO2026010866A1 (en) * | 2024-07-01 | 2026-01-08 | Apertor Pharmaceuticals, Inc. | Hetero-bifunctional molecules |
| CN119462690B (zh) * | 2024-11-08 | 2026-02-06 | 西安交通大学 | 一类基于自噬-溶酶体途径的选择性mTORC1降解剂及其制备方法和应用 |
Family Cites Families (101)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA737247B (en) | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
| US4316885A (en) | 1980-08-25 | 1982-02-23 | Ayerst, Mckenna And Harrison, Inc. | Acyl derivatives of rapamycin |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
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-
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