KR20170090478A - Cd38 억제제 및 치료 방법 - Google Patents
Cd38 억제제 및 치료 방법 Download PDFInfo
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- KR20170090478A KR20170090478A KR1020177018180A KR20177018180A KR20170090478A KR 20170090478 A KR20170090478 A KR 20170090478A KR 1020177018180 A KR1020177018180 A KR 1020177018180A KR 20177018180 A KR20177018180 A KR 20177018180A KR 20170090478 A KR20170090478 A KR 20170090478A
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- Prior art keywords
- mmol
- cyclohexyl
- reaction
- indole
- added
- Prior art date
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- NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical compound [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 description 1
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- 102000020233 phosphotransferase Human genes 0.000 description 1
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- 102000054765 polymorphisms of proteins Human genes 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229920005990 polystyrene resin Polymers 0.000 description 1
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- 239000002243 precursor Substances 0.000 description 1
- VVWRJUBEIPHGQF-MDZDMXLPSA-N propan-2-yl (ne)-n-propan-2-yloxycarbonyliminocarbamate Chemical compound CC(C)OC(=O)\N=N\C(=O)OC(C)C VVWRJUBEIPHGQF-MDZDMXLPSA-N 0.000 description 1
- VVWRJUBEIPHGQF-UHFFFAOYSA-N propan-2-yl n-propan-2-yloxycarbonyliminocarbamate Chemical compound CC(C)OC(=O)N=NC(=O)OC(C)C VVWRJUBEIPHGQF-UHFFFAOYSA-N 0.000 description 1
- 208000005069 pulmonary fibrosis Diseases 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
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- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 150000003222 pyridines Chemical class 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
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- 229910000033 sodium borohydride Inorganic materials 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- FQENQNTWSFEDLI-UHFFFAOYSA-J sodium diphosphate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]P([O-])(=O)OP([O-])([O-])=O FQENQNTWSFEDLI-UHFFFAOYSA-J 0.000 description 1
- JVBXVOWTABLYPX-UHFFFAOYSA-L sodium dithionite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])=O JVBXVOWTABLYPX-UHFFFAOYSA-L 0.000 description 1
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- 229940048086 sodium pyrophosphate Drugs 0.000 description 1
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- GWAXLDLPPZPQLO-UHFFFAOYSA-N tert-butyl 2,3-dihydroindole-1-carboxylate Chemical compound C1=CC=C2N(C(=O)OC(C)(C)C)CCC2=C1 GWAXLDLPPZPQLO-UHFFFAOYSA-N 0.000 description 1
- DHHKPEUQJIEKOA-UHFFFAOYSA-N tert-butyl 2-[6-(nitromethyl)-6-bicyclo[3.2.0]hept-3-enyl]acetate Chemical compound C1C=CC2C(CC(=O)OC(C)(C)C)(C[N+]([O-])=O)CC21 DHHKPEUQJIEKOA-UHFFFAOYSA-N 0.000 description 1
- FEYLUKDSKVSMSZ-UHFFFAOYSA-N tert-butyl n-(4-aminocyclohexyl)carbamate Chemical compound CC(C)(C)OC(=O)NC1CCC(N)CC1 FEYLUKDSKVSMSZ-UHFFFAOYSA-N 0.000 description 1
- 125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 210000001550 testis Anatomy 0.000 description 1
- FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 1
- 235000019818 tetrasodium diphosphate Nutrition 0.000 description 1
- 239000001577 tetrasodium phosphonato phosphate Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- MWKJTNBSKNUMFN-UHFFFAOYSA-N trifluoromethyltrimethylsilane Chemical compound C[Si](C)(C)C(F)(F)F MWKJTNBSKNUMFN-UHFFFAOYSA-N 0.000 description 1
- CWMFRHBXRUITQE-UHFFFAOYSA-N trimethylsilylacetylene Chemical group C[Si](C)(C)C#C CWMFRHBXRUITQE-UHFFFAOYSA-N 0.000 description 1
- 201000008827 tuberculosis Diseases 0.000 description 1
- 239000000439 tumor marker Substances 0.000 description 1
- 102000003390 tumor necrosis factor Human genes 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462086844P | 2014-12-03 | 2014-12-03 | |
| US62/086,844 | 2014-12-03 | ||
| PCT/IB2015/058965 WO2016087975A1 (en) | 2014-12-03 | 2015-11-19 | Cd38 inhibitors and methods of treatment |
Publications (1)
| Publication Number | Publication Date |
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| KR20170090478A true KR20170090478A (ko) | 2017-08-07 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020177018180A Withdrawn KR20170090478A (ko) | 2014-12-03 | 2015-11-19 | Cd38 억제제 및 치료 방법 |
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| US (1) | US9840496B2 (enExample) |
| EP (1) | EP3227275B1 (enExample) |
| JP (1) | JP6550132B2 (enExample) |
| KR (1) | KR20170090478A (enExample) |
| CN (1) | CN107428733A (enExample) |
| AU (1) | AU2015356721B2 (enExample) |
| BR (1) | BR112017011642A2 (enExample) |
| CA (1) | CA2969178A1 (enExample) |
| ES (1) | ES2717260T3 (enExample) |
| RU (1) | RU2017121002A (enExample) |
| WO (1) | WO2016087975A1 (enExample) |
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| EP3544612A4 (en) | 2016-11-23 | 2020-05-13 | Acetylon Pharmaceuticals, Inc. | PHARMACEUTICAL COMBINATIONS COMPRISING A HISTONE DEACETYLASE INHIBITOR AND A CD38 INHIBITOR AND METHODS OF USING THE SAME |
| WO2020146795A1 (en) | 2019-01-11 | 2020-07-16 | Omeros Corporation | Methods and compositions for treating cancer |
| US11535621B2 (en) * | 2019-07-31 | 2022-12-27 | Ribon Therapeutics, Inc. | Heterobicyclic amides as inhibitors of CD38 |
| US20230025807A1 (en) * | 2019-10-30 | 2023-01-26 | Mitobridge Inc. | Cd38 inhibitors |
| KR20230051425A (ko) * | 2020-04-07 | 2023-04-18 | 미토브리지, 인크. | Cd38 억제제 |
| IL301991A (en) * | 2020-10-09 | 2023-06-01 | Napa Therapeutics Ltd | Heteroaryl amide inhibitors for CD38 |
| EP4263524A1 (en) | 2020-12-21 | 2023-10-25 | Cytokinetics, Inc. | Pyrazole derivatives useful as nampt modulators |
| AR124718A1 (es) | 2021-01-29 | 2023-04-26 | Ribon Therapeutics Inc | Quinolinas y azaquinolinas como inhibidores de cd38 |
| EP4288053A4 (en) | 2021-02-08 | 2024-12-18 | Ohio State Innovation Foundation | Small molecule inhibitors of cd38 as immunosuppressants |
| CN117715897A (zh) * | 2021-04-30 | 2024-03-15 | 南京艾美斐生物医药科技有限公司 | 化合物及其作为cd38抑制剂的用途 |
| US20230116972A1 (en) * | 2021-07-12 | 2023-04-20 | Cytokinetics, Inc. | Cd38 modulators and methods of use thereof |
| EP4724430A1 (en) * | 2023-06-07 | 2026-04-15 | Flagship Pioneering Innovations VI, LLC | Condensed azines as inhibitors of cyclic adp ribose hydrolase |
| WO2026000074A1 (en) * | 2024-06-25 | 2026-01-02 | Welnx Company Inc. | Use of cd38 inhibitors for reducing th2 inflammation |
| WO2026075971A1 (en) | 2024-10-01 | 2026-04-09 | Neolaia Inc. | Combination therapy for treatment of metabolic disorders and inflamation related disorders using incretin compounds and cd38 inhibitors |
| WO2026090190A1 (en) * | 2024-10-22 | 2026-04-30 | Aeovian Pharmaceuticals, Inc. | Cd38 modulators and uses thereof |
| CN119775288B (zh) * | 2024-12-31 | 2025-10-10 | 浙江工业大学 | 一种cd38抑制化合物及应用 |
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| EP1370139A4 (en) * | 2001-01-04 | 2010-09-22 | Einstein Coll Med | INHIBITORS OF ADP-RIBOSYLTRANSFERASES, CYCLASES AND HYDROLASES AND THEIR USE |
| US7022680B2 (en) * | 2002-05-30 | 2006-04-04 | Albert Einstein College Of Medicine Of Yeshiva University | Inhibitors of ADP-ribosyl transferases, cyclases, and hydrolases |
| WO2010025235A1 (en) * | 2008-08-29 | 2010-03-04 | Regents Of The University Of Michigan | Selective ligands for the dopamine 3 (d3) receptor and methods of using the same |
| EP2801573A1 (en) * | 2013-05-09 | 2014-11-12 | Sanofi | Hydantoine derivatives as CD38 inhibitors |
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2015
- 2015-11-19 CN CN201580073761.2A patent/CN107428733A/zh active Pending
- 2015-11-19 ES ES15801951T patent/ES2717260T3/es active Active
- 2015-11-19 AU AU2015356721A patent/AU2015356721B2/en not_active Ceased
- 2015-11-19 KR KR1020177018180A patent/KR20170090478A/ko not_active Withdrawn
- 2015-11-19 WO PCT/IB2015/058965 patent/WO2016087975A1/en not_active Ceased
- 2015-11-19 CA CA2969178A patent/CA2969178A1/en not_active Abandoned
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- 2015-11-19 JP JP2017529357A patent/JP6550132B2/ja active Active
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Also Published As
| Publication number | Publication date |
|---|---|
| BR112017011642A2 (pt) | 2018-03-06 |
| US20170260164A1 (en) | 2017-09-14 |
| EP3227275A1 (en) | 2017-10-11 |
| WO2016087975A1 (en) | 2016-06-09 |
| RU2017121002A3 (enExample) | 2019-03-15 |
| ES2717260T3 (es) | 2019-06-20 |
| AU2015356721B2 (en) | 2018-03-15 |
| AU2015356721A1 (en) | 2017-06-08 |
| CA2969178A1 (en) | 2016-06-09 |
| RU2017121002A (ru) | 2019-01-11 |
| US9840496B2 (en) | 2017-12-12 |
| EP3227275B1 (en) | 2019-01-02 |
| CN107428733A (zh) | 2017-12-01 |
| JP2018501215A (ja) | 2018-01-18 |
| JP6550132B2 (ja) | 2019-07-24 |
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