JPWO2020061046A5 - - Google Patents
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- Publication number
- JPWO2020061046A5 JPWO2020061046A5 JP2021514532A JP2021514532A JPWO2020061046A5 JP WO2020061046 A5 JPWO2020061046 A5 JP WO2020061046A5 JP 2021514532 A JP2021514532 A JP 2021514532A JP 2021514532 A JP2021514532 A JP 2021514532A JP WO2020061046 A5 JPWO2020061046 A5 JP WO2020061046A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- pharmaceutically acceptable
- hydrogen
- 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
- 229910052739 hydrogen Inorganic materials 0.000 claims 56
- 239000001257 hydrogen Substances 0.000 claims 56
- 125000000217 alkyl group Chemical group 0.000 claims 55
- 150000002431 hydrogen Chemical class 0.000 claims 30
- 150000003839 salts Chemical class 0.000 claims 30
- 125000004093 cyano group Chemical group *C#N 0.000 claims 29
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 29
- 239000012453 solvate Substances 0.000 claims 29
- 239000000203 mixture Substances 0.000 claims 28
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 27
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 26
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 23
- 125000000623 heterocyclic group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000002367 halogens Chemical class 0.000 claims 17
- 125000000753 cycloalkyl group Chemical group 0.000 claims 16
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 14
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000002950 monocyclic group Chemical group 0.000 claims 12
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000004429 atom Chemical group 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 7
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 7
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims 6
- 229910052794 bromium Inorganic materials 0.000 claims 5
- 229910052801 chlorine Inorganic materials 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052731 fluorine Inorganic materials 0.000 claims 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 2
- ICSNLGPSRYBMBD-UHFFFAOYSA-N 2-aminopyridine Chemical compound NC1=CC=CC=N1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 claims 2
- 108010051696 Growth Hormone Proteins 0.000 claims 2
- 101000599951 Homo sapiens Insulin-like growth factor I Proteins 0.000 claims 2
- 102100037852 Insulin-like growth factor I Human genes 0.000 claims 2
- 102100038803 Somatotropin Human genes 0.000 claims 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 2
- 239000000122 growth hormone Substances 0.000 claims 2
- 229940088597 hormone Drugs 0.000 claims 2
- 239000005556 hormone Substances 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 208000020016 psychiatric disease Diseases 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 2
- 230000001228 trophic effect Effects 0.000 claims 2
- XWCLWYVYMUTYNP-UHFFFAOYSA-N 2-[2-amino-4-(4-aminopiperidin-1-yl)-5-(3-chloro-5-fluorophenyl)pyridin-3-yl]-7-methoxy-3H-benzimidazole-5-carbonitrile Chemical compound NC1=NC=C(C(=C1C1=NC2=C(N1)C=C(C=C2OC)C#N)N1CCC(CC1)N)C1=CC(=CC(=C1)F)Cl XWCLWYVYMUTYNP-UHFFFAOYSA-N 0.000 claims 1
- GWXXLUISNRRCDH-UHFFFAOYSA-N 2-[2-amino-4-(4-aminopiperidin-1-yl)-5-(3-fluoro-5-methylphenyl)pyridin-3-yl]-7-methoxy-3H-benzimidazole-5-carbonitrile Chemical compound NC1=NC=C(C(=C1C1=NC2=C(N1)C=C(C=C2OC)C#N)N1CCC(CC1)N)C1=CC(=CC(=C1)C)F GWXXLUISNRRCDH-UHFFFAOYSA-N 0.000 claims 1
- MNTYWCOOZNFBOW-UHFFFAOYSA-N 2-[4-(4-aminopiperidin-1-yl)-2-(dimethylamino)-5-(3-fluoro-5-methylphenyl)pyridin-3-yl]-7-methoxy-3H-benzimidazole-5-carbonitrile Chemical compound NC1CCN(CC1)C1=C(C(=NC=C1C1=CC(=CC(=C1)C)F)N(C)C)C1=NC2=C(N1)C=C(C=C2OC)C#N MNTYWCOOZNFBOW-UHFFFAOYSA-N 0.000 claims 1
- TXQQISIPFAYEPW-UHFFFAOYSA-N 4-(4-aminopiperidin-1-yl)-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methylphenyl)-N-methylpyridine-2-carboxamide Chemical compound NC1CCN(CC1)C1=C(C(=NC=C1C1=CC(=CC(=C1)C)F)C(=O)NC)C1=NC2=C(N1)C=C(C=C2OC)F TXQQISIPFAYEPW-UHFFFAOYSA-N 0.000 claims 1
- LIEKIPDHLZCKJD-UHFFFAOYSA-N 4-(4-aminopiperidin-1-yl)-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methylphenyl)pyridine-2-carbonitrile Chemical compound NC1CCN(CC1)C1=C(C(=NC=C1C1=CC(=CC(=C1)C)F)C#N)C1=NC2=C(N1)C=C(C=C2OC)F LIEKIPDHLZCKJD-UHFFFAOYSA-N 0.000 claims 1
- NQPBTXCQNMNVLD-UHFFFAOYSA-N 4-(4-aminopiperidin-1-yl)-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methylphenyl)pyridine-2-carboxamide Chemical compound NC1CCN(CC1)C1=C(C(=NC=C1C1=CC(=CC(=C1)C)F)C(=O)N)C1=NC2=C(N1)C=C(C=C2OC)F NQPBTXCQNMNVLD-UHFFFAOYSA-N 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 206010000599 Acromegaly Diseases 0.000 claims 1
- 102000051325 Glucagon Human genes 0.000 claims 1
- 108060003199 Glucagon Proteins 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000022873 Ocular disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 102100024819 Prolactin Human genes 0.000 claims 1
- 108010057464 Prolactin Proteins 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 1
- 229960004666 glucagon Drugs 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- XPRFCBRXEPLAPJ-UHFFFAOYSA-N methyl 4-(4-aminopiperidin-1-yl)-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methylphenyl)pyridine-2-carboxylate Chemical compound NC1CCN(CC1)C1=C(C(=NC=C1C1=CC(=CC(=C1)C)F)C(=O)OC)C1=NC2=C(N1)C=C(C=C2OC)F XPRFCBRXEPLAPJ-UHFFFAOYSA-N 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000011519 neuroendocrine tumor Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229940097325 prolactin Drugs 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862732735P | 2018-09-18 | 2018-09-18 | |
| US62/732,735 | 2018-09-18 | ||
| PCT/US2019/051514 WO2020061046A1 (en) | 2018-09-18 | 2019-09-17 | Somatostatin modulators and uses thereof |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022501342A JP2022501342A (ja) | 2022-01-06 |
| JPWO2020061046A5 true JPWO2020061046A5 (https=) | 2022-09-27 |
| JP2022501342A5 JP2022501342A5 (https=) | 2022-09-27 |
| JP7431813B2 JP7431813B2 (ja) | 2024-02-15 |
Family
ID=69772634
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021514532A Active JP7431813B2 (ja) | 2018-09-18 | 2019-09-17 | ソマトスタチンモジュレーターとその使用 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US10696689B2 (https=) |
| EP (2) | EP3853218B1 (https=) |
| JP (1) | JP7431813B2 (https=) |
| AR (1) | AR116424A1 (https=) |
| DK (1) | DK3853218T3 (https=) |
| ES (1) | ES3022912T3 (https=) |
| FI (1) | FI3853218T3 (https=) |
| HR (1) | HRP20250425T1 (https=) |
| HU (1) | HUE071203T2 (https=) |
| LT (1) | LT3853218T (https=) |
| PL (1) | PL3853218T3 (https=) |
| PT (1) | PT3853218T (https=) |
| RS (1) | RS66720B1 (https=) |
| SI (1) | SI3853218T1 (https=) |
| SM (1) | SMT202500155T1 (https=) |
| TW (1) | TWI852944B (https=) |
| WO (1) | WO2020061046A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20221279T1 (hr) | 2016-07-14 | 2022-12-23 | Crinetics Pharmaceuticals, Inc. | Modulatori somatostatina i njihove uporabe |
| WO2018170284A1 (en) | 2017-03-16 | 2018-09-20 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| EP3752498B1 (en) | 2018-02-12 | 2023-06-28 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| AR116424A1 (es) | 2018-09-18 | 2021-05-05 | Crinetics Pharmaceuticals Inc | Moduladores de la somatostatina y usos de los mismos |
| TWI841768B (zh) | 2019-08-14 | 2024-05-11 | 美商克林提克斯醫藥股份有限公司 | 非肽生長抑制素(somatostatin)5型受體激動劑及其用途 |
| FI4210700T3 (fi) | 2020-09-09 | 2025-09-16 | Crinetics Pharmaceuticals Inc | Somatostatiinimodulaatorin formulaatioita |
| EP4294797A1 (en) * | 2021-02-17 | 2023-12-27 | Crinetics Pharmaceuticals, Inc. | Crystalline forms of a somatostatin modulator |
| JP2026500913A (ja) | 2022-12-13 | 2026-01-09 | クリネティックス ファーマシューティカルズ，インク． | ソマトスタチンサブタイプ－２受容体（ｓｓｔ２ｒ）標的化治療薬及びその使用 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6127343A (en) * | 1996-05-14 | 2000-10-03 | Novo Nordisk A/S | Somatostatin agonists and antagonists |
| US6025372A (en) | 1997-04-04 | 2000-02-15 | Merck & Co., Inc. | Somatostatin agonists |
| FR2802206B1 (fr) | 1999-12-14 | 2005-04-22 | Sod Conseils Rech Applic | Derives de 4-aminopiperidine et leur utilisation en tant que medicament |
| US20060281764A1 (en) | 2005-06-10 | 2006-12-14 | Gaul Michael D | Aminopyrimidines as kinase modulators |
| CA2644929A1 (en) | 2006-03-13 | 2008-05-02 | Merck & Co., Inc. | Somatostatin agonists |
| EP2054385A2 (en) | 2006-08-15 | 2009-05-06 | F. Hoffmann-Roche AG | Phenyl, pyridine and quinoline derivatives |
| EP2211619A1 (en) | 2007-10-18 | 2010-08-04 | Merck Sharp & Dohme Corp. | Substituted 1,2,4-oxadiazoles and analogs thereof as cb2 receptor modulators, useful in the treatment of pain, respiratory and non-respiratory diseases |
| CA2729220A1 (en) | 2008-06-25 | 2009-12-30 | Envivo Pharmaceuticals, Inc. | Di-substituted phenyl compounds |
| GB0818241D0 (en) | 2008-10-06 | 2008-11-12 | Cancer Res Technology | Compounds and their use |
| CA2772194A1 (en) | 2009-09-01 | 2011-03-10 | Pfizer Inc. | Benzimidazole derivatives |
| CA2799414A1 (en) * | 2010-05-18 | 2011-11-24 | Merck Sharp & Dohme Corp. | Spiro isoxazoline compounds as sstr5 antagonists |
| GB201008290D0 (en) | 2010-05-18 | 2010-06-30 | Syngenta Ltd | Chemical compounds |
| WO2014007228A1 (ja) | 2012-07-03 | 2014-01-09 | 小野薬品工業株式会社 | ソマトスタチン受容体作動活性を有する化合物およびその医薬用途 |
| AU2014325078B2 (en) | 2013-09-30 | 2018-10-25 | Ono Pharmaceutical Co., Ltd. | Compound having agonistic activity to somatostatin receptor and medicinal use thereof |
| CN105579524B (zh) | 2013-10-02 | 2018-05-04 | 株式会社可乐丽 | 树脂组合物、多层片、包装材料和容器 |
| HRP20221279T1 (hr) | 2016-07-14 | 2022-12-23 | Crinetics Pharmaceuticals, Inc. | Modulatori somatostatina i njihove uporabe |
| JP6838387B2 (ja) * | 2016-12-21 | 2021-03-03 | トヨタ紡織株式会社 | 内装部品の取付構造 |
| CN110300749A (zh) | 2017-02-08 | 2019-10-01 | 小野药品工业株式会社 | 具有生长抑素受体激动活性的化合物及其医药用途 |
| WO2018170284A1 (en) | 2017-03-16 | 2018-09-20 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| US11028068B2 (en) | 2017-07-25 | 2021-06-08 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| EP3752498B1 (en) | 2018-02-12 | 2023-06-28 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| AR116424A1 (es) | 2018-09-18 | 2021-05-05 | Crinetics Pharmaceuticals Inc | Moduladores de la somatostatina y usos de los mismos |
| TWI841768B (zh) | 2019-08-14 | 2024-05-11 | 美商克林提克斯醫藥股份有限公司 | 非肽生長抑制素(somatostatin)5型受體激動劑及其用途 |
-
2019
- 2019-09-17 AR ARP190102640A patent/AR116424A1/es unknown
- 2019-09-17 PT PT198633950T patent/PT3853218T/pt unknown
- 2019-09-17 WO PCT/US2019/051514 patent/WO2020061046A1/en not_active Ceased
- 2019-09-17 RS RS20250348A patent/RS66720B1/sr unknown
- 2019-09-17 HU HUE19863395A patent/HUE071203T2/hu unknown
- 2019-09-17 DK DK19863395.0T patent/DK3853218T3/da active
- 2019-09-17 JP JP2021514532A patent/JP7431813B2/ja active Active
- 2019-09-17 EP EP19863395.0A patent/EP3853218B1/en active Active
- 2019-09-17 HR HRP20250425TT patent/HRP20250425T1/hr unknown
- 2019-09-17 LT LTEPPCT/US2019/051514T patent/LT3853218T/lt unknown
- 2019-09-17 EP EP25151398.2A patent/EP4548974A3/en active Pending
- 2019-09-17 US US16/572,921 patent/US10696689B2/en active Active
- 2019-09-17 ES ES19863395T patent/ES3022912T3/es active Active
- 2019-09-17 FI FIEP19863395.0T patent/FI3853218T3/fi active
- 2019-09-17 TW TW108133468A patent/TWI852944B/zh active
- 2019-09-17 PL PL19863395.0T patent/PL3853218T3/pl unknown
- 2019-09-17 SI SI201930927T patent/SI3853218T1/sl unknown
- 2019-09-17 SM SM20250155T patent/SMT202500155T1/it unknown
-
2020
- 2020-05-19 US US16/877,947 patent/US11186590B2/en active Active
-
2021
- 2021-10-26 US US17/511,326 patent/US20220048924A1/en not_active Abandoned
-
2022
- 2022-04-06 US US17/714,825 patent/US11834462B2/en active Active
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