JP6783230B2 - ヒストンデメチラーゼのインヒビターとしてのピロリドンアミド化合物 - Google Patents
ヒストンデメチラーゼのインヒビターとしてのピロリドンアミド化合物 Download PDFInfo
- Publication number
- JP6783230B2 JP6783230B2 JP2017518802A JP2017518802A JP6783230B2 JP 6783230 B2 JP6783230 B2 JP 6783230B2 JP 2017518802 A JP2017518802 A JP 2017518802A JP 2017518802 A JP2017518802 A JP 2017518802A JP 6783230 B2 JP6783230 B2 JP 6783230B2
- Authority
- JP
- Japan
- Prior art keywords
- membered
- carbocyclyl
- alkyl
- compound according
- salt
- 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.)
- Expired - Fee Related
Links
- 0 Cc1cc(Oc2ccccc2)cc(*=C)n1 Chemical compound Cc1cc(Oc2ccccc2)cc(*=C)n1 0.000 description 20
- UECKGIBZRAQRNT-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CC1N(C=CC=C1C)C1=O)=O Chemical compound CC(C)(C)OC(N(CC1)CC1N(C=CC=C1C)C1=O)=O UECKGIBZRAQRNT-UHFFFAOYSA-N 0.000 description 1
- APCBTRDHCDOPNY-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CC1O)=O Chemical compound CC(C)(C)OC(N(CC1)CC1O)=O APCBTRDHCDOPNY-UHFFFAOYSA-N 0.000 description 1
- DZUBTKLPIBEHSR-JTQLQIEISA-N CC(C)(C)OC(N(CC1)C[C@H]1NC(C1CC1)=O)=O Chemical compound CC(C)(C)OC(N(CC1)C[C@H]1NC(C1CC1)=O)=O DZUBTKLPIBEHSR-JTQLQIEISA-N 0.000 description 1
- HDIGBKXZIAJVFB-UHFFFAOYSA-N CC(C)C(C1)=NNC1C(N(CC1)CC1NC(NC)=O)=O Chemical compound CC(C)C(C1)=NNC1C(N(CC1)CC1NC(NC)=O)=O HDIGBKXZIAJVFB-UHFFFAOYSA-N 0.000 description 1
- BNBACRJYRCHOJC-UHFFFAOYSA-N CC(C)c1n[nH]c(C(N(CC2)CC2Nc2ncccc2)=O)c1 Chemical compound CC(C)c1n[nH]c(C(N(CC2)CC2Nc2ncccc2)=O)c1 BNBACRJYRCHOJC-UHFFFAOYSA-N 0.000 description 1
- DMNBHKDYAMCUIV-UHFFFAOYSA-N CC(C)c1n[nH]c(C(N(CC2)CC2c2cc(OC)cc(C)n2)=O)c1 Chemical compound CC(C)c1n[nH]c(C(N(CC2)CC2c2cc(OC)cc(C)n2)=O)c1 DMNBHKDYAMCUIV-UHFFFAOYSA-N 0.000 description 1
- HOHNWNOHHOMLDU-UHFFFAOYSA-N CC(C)c1nc(C)cc(-c2c[n](C)nc2)c1 Chemical compound CC(C)c1nc(C)cc(-c2c[n](C)nc2)c1 HOHNWNOHHOMLDU-UHFFFAOYSA-N 0.000 description 1
- HFBWRCZRDIVAMQ-UHFFFAOYSA-N CC(c1n[nH]c(C(O)=O)c1)=O Chemical compound CC(c1n[nH]c(C(O)=O)c1)=O HFBWRCZRDIVAMQ-UHFFFAOYSA-N 0.000 description 1
- LTBGAGHQQLYBFD-UHFFFAOYSA-N CCC(C1)N=C(C)C=C1NCc1ccccc1 Chemical compound CCC(C1)N=C(C)C=C1NCc1ccccc1 LTBGAGHQQLYBFD-UHFFFAOYSA-N 0.000 description 1
- BVNIREPGHLFKNZ-UHFFFAOYSA-N CNC(C1CC1)=O Chemical compound CNC(C1CC1)=O BVNIREPGHLFKNZ-UHFFFAOYSA-N 0.000 description 1
- SCWKRWCUMCMVPW-UHFFFAOYSA-N CNC(Oc1ccccc1)=O Chemical compound CNC(Oc1ccccc1)=O SCWKRWCUMCMVPW-UHFFFAOYSA-N 0.000 description 1
- CRSQCKSFDSBUPQ-UHFFFAOYSA-N Cc1cc(-c2c[n](C)nc2)cc(C)n1 Chemical compound Cc1cc(-c2c[n](C)nc2)cc(C)n1 CRSQCKSFDSBUPQ-UHFFFAOYSA-N 0.000 description 1
- NNOGVLOFSVCMBY-UHFFFAOYSA-N Cc1cc(-c2ccccn2)cc(C)n1 Chemical compound Cc1cc(-c2ccccn2)cc(C)n1 NNOGVLOFSVCMBY-UHFFFAOYSA-N 0.000 description 1
- CFIHITRYALVMCY-UHFFFAOYSA-N Cc1cc(C(N(C)C)=O)cc(C)n1 Chemical compound Cc1cc(C(N(C)C)=O)cc(C)n1 CFIHITRYALVMCY-UHFFFAOYSA-N 0.000 description 1
- MLDMYLXCMZTSHX-UHFFFAOYSA-N Cc1cc(C(OC)=O)cc(C)n1 Chemical compound Cc1cc(C(OC)=O)cc(C)n1 MLDMYLXCMZTSHX-UHFFFAOYSA-N 0.000 description 1
- TXRZXFOOTYXLOQ-QGRYRQEDSA-N N/C(/C(N(CC1)CC1NC(C1CC1)=O)=O)=C\C(Cc1ccccc1)=N Chemical compound N/C(/C(N(CC1)CC1NC(C1CC1)=O)=O)=C\C(Cc1ccccc1)=N TXRZXFOOTYXLOQ-QGRYRQEDSA-N 0.000 description 1
Classifications
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- 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
-
- 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
- A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/04—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2014088309 | 2014-10-10 | ||
| CNPCT/CN2014/088309 | 2014-10-10 | ||
| PCT/US2015/054949 WO2016057924A1 (en) | 2014-10-10 | 2015-10-09 | Pyrrolidine amide compounds as histone demethylase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017530984A JP2017530984A (ja) | 2017-10-19 |
| JP2017530984A5 JP2017530984A5 (enExample) | 2018-11-22 |
| JP6783230B2 true JP6783230B2 (ja) | 2020-11-11 |
Family
ID=54337935
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017518802A Expired - Fee Related JP6783230B2 (ja) | 2014-10-10 | 2015-10-09 | ヒストンデメチラーゼのインヒビターとしてのピロリドンアミド化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10022354B2 (enExample) |
| EP (1) | EP3204379B1 (enExample) |
| JP (1) | JP6783230B2 (enExample) |
| CN (1) | CN107912040B (enExample) |
| WO (1) | WO2016057924A1 (enExample) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2018014377A (es) | 2016-05-27 | 2019-03-14 | Gilead Sciences Inc | Metodos para tratar infecciones por virus de hepatitis b usando inhibidores de proteina no estructural 5a (ns5a), proteina no estructural 5b (ns5b) o proteina no estructural 3 (ns3). |
| BR102017010009A2 (pt) | 2016-05-27 | 2017-12-12 | Gilead Sciences, Inc. | Compounds for the treatment of hepatitis b virus infection |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| PT3507276T (pt) | 2016-09-02 | 2022-01-11 | Gilead Sciences Inc | Compostos moduladores do recetor de tipo toll |
| WO2018045150A1 (en) | 2016-09-02 | 2018-03-08 | Gilead Sciences, Inc. | 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators |
| MA46535A (fr) | 2016-10-14 | 2019-08-21 | Prec Biosciences Inc | Méganucléases modifiées spécifiques de séquences de reconnaissance dans le génome du virus de l'hépatite b |
| TW201822637A (zh) | 2016-11-07 | 2018-07-01 | 德商拜耳廠股份有限公司 | 用於控制動物害蟲的經取代磺醯胺類 |
| AU2018209164B2 (en) | 2017-01-17 | 2021-11-04 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| TWI714820B (zh) | 2017-01-31 | 2021-01-01 | 美商基利科學股份有限公司 | 替諾福韋艾拉酚胺(tenofovir alafenamide)之晶型 |
| JOP20180008A1 (ar) | 2017-02-02 | 2019-01-30 | Gilead Sciences Inc | مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b |
| JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
| KR20190063745A (ko) * | 2017-11-30 | 2019-06-10 | (주)인핸스드바이오 | p34 단백질 및 NEDD4-1 단백질의 결합 억제제로서의 신규 화합물 및 이의 용도 |
| WO2019123339A1 (en) | 2017-12-20 | 2019-06-27 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| AU2018392213B2 (en) | 2017-12-20 | 2021-03-04 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein |
| SI3752501T1 (sl) | 2018-02-13 | 2023-08-31 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
| JP7050165B2 (ja) | 2018-02-26 | 2022-04-07 | ギリアード サイエンシーズ, インコーポレイテッド | Hbv複製阻害剤としての置換ピロリジン化合物 |
| EP3774883A1 (en) | 2018-04-05 | 2021-02-17 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis b virus protein x |
| TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
| TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | 2,2,─環二核苷酸 |
| TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
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| SI3820572T1 (sl) | 2018-07-13 | 2023-12-29 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
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| JP7158577B2 (ja) | 2018-10-24 | 2022-10-21 | ギリアード サイエンシーズ, インコーポレイテッド | Pd-1/pd-l1阻害剤 |
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| CA3117556A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds as hpk1 inhibitors |
| CN109852662B (zh) * | 2018-12-25 | 2021-02-19 | 华南农业大学 | 组蛋白甲基化H3K4me3在猪卵巢颗粒细胞中的应用 |
| WO2020178770A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| JP7350871B2 (ja) | 2019-03-07 | 2023-09-26 | インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール,ヴイ.ヴイ.アイ. | 2’3’-環状ジヌクレオチドおよびそのプロドラッグ |
| EP3935065A1 (en) | 2019-03-07 | 2022-01-12 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
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| WO2021010492A1 (en) * | 2019-07-17 | 2021-01-21 | Ono Pharmaceutical Co., Ltd. | Compound having kdm5 inhibitory activity and pharmaceutical use thereof |
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| UY38934A (es) * | 2019-10-29 | 2021-05-31 | Biogen Ma Inc | Inhibidores de o-glucoproteína-2-acetamido-2-deoxi-3-d-glucopiranosidasa espirocíclica |
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| CN107912040A (zh) | 2018-04-13 |
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| EP3204379B1 (en) | 2019-03-06 |
| EP3204379A1 (en) | 2017-08-16 |
| WO2016057924A1 (en) | 2016-04-14 |
| CN107912040B (zh) | 2021-04-06 |
| US20170312252A1 (en) | 2017-11-02 |
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