CN109071544A - 三并环类化合物及其应用 - Google Patents
三并环类化合物及其应用 Download PDFInfo
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- CN109071544A CN109071544A CN201880001646.8A CN201880001646A CN109071544A CN 109071544 A CN109071544 A CN 109071544A CN 201880001646 A CN201880001646 A CN 201880001646A CN 109071544 A CN109071544 A CN 109071544A
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- alkyl
- 400mhz
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- 238000002360 preparation method Methods 0.000 claims abstract description 10
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 6
- -1 3- azabicyclo [3.1.0] hexyl Chemical group 0.000 claims description 101
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 56
- 125000000217 alkyl group Chemical group 0.000 claims description 43
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- 125000005842 heteroatom Chemical group 0.000 claims description 27
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
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- 229910002027 silica gel Inorganic materials 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 150000003413 spiro compounds Chemical class 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 125000001273 sulfonato group Chemical group [O-]S(*)(=O)=O 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 125000006253 t-butylcarbonyl group Chemical group [H]C([H])([H])C(C(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 238000003419 tautomerization reaction Methods 0.000 description 1
- ISIJQEHRDSCQIU-UHFFFAOYSA-N tert-butyl 2,7-diazaspiro[4.5]decane-7-carboxylate Chemical compound C1N(C(=O)OC(C)(C)C)CCCC11CNCC1 ISIJQEHRDSCQIU-UHFFFAOYSA-N 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- DZLFLBLQUQXARW-UHFFFAOYSA-N tetrabutylammonium Chemical compound CCCC[N+](CCCC)(CCCC)CCCC DZLFLBLQUQXARW-UHFFFAOYSA-N 0.000 description 1
- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
- GVIJJXMXTUZIOD-UHFFFAOYSA-N thianthrene Chemical group C1=CC=C2SC3=CC=CC=C3SC2=C1 GVIJJXMXTUZIOD-UHFFFAOYSA-N 0.000 description 1
- 125000002769 thiazolinyl group Chemical group 0.000 description 1
- 125000002053 thietanyl group Chemical group 0.000 description 1
- 125000005309 thioalkoxy group Chemical group 0.000 description 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 229960005371 tolbutamide Drugs 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
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- 230000001988 toxicity Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 125000004417 unsaturated alkyl group Chemical group 0.000 description 1
- 238000011144 upstream manufacturing Methods 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
-
- 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
-
- 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
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
Claims (18)
- PCT国内申请,权利要求书已公开。
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CN2017101003091 | 2017-02-23 | ||
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CN201710648155X | 2017-08-01 | ||
CN201810008592 | 2018-01-04 | ||
CN201810008592X | 2018-01-04 | ||
PCT/CN2018/075995 WO2018153285A1 (zh) | 2017-02-23 | 2018-02-09 | 三并环类化合物及其应用 |
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
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CN110872307A (zh) * | 2019-06-05 | 2020-03-10 | 河南科技大学第一附属医院 | 一种医院妇科所用噻唑类药物分子及其制备方法和应用 |
CN112334137A (zh) * | 2018-05-03 | 2021-02-05 | 埃默里大学 | 用于nash和其他代谢紊乱的孤儿核受体调节剂 |
TWI746110B (zh) * | 2019-08-15 | 2021-11-11 | 大陸商福建廣生堂藥業股份有限公司 | 氧氮雜卓類化合物的製備方法 |
CN114456099A (zh) * | 2022-02-21 | 2022-05-10 | 八叶草健康产业研究院(厦门)有限公司 | 一种4-氯吡咯-2-羧酸的制备方法 |
Families Citing this family (3)
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JP7118354B2 (ja) | 2018-08-23 | 2022-08-16 | 福建▲広▼生中霖生物科技有限公司 | 三環式化合物の結晶形及びその使用 |
WO2021213445A1 (zh) * | 2020-04-22 | 2021-10-28 | 南京明德新药研发有限公司 | 内磺酰胺衍生物及其应用 |
CN115515596A (zh) * | 2020-05-15 | 2022-12-23 | 福建广生中霖生物科技有限公司 | 包含三并环类化合物的组合及其在制备治疗hbv药物中的应用 |
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CN106413402A (zh) * | 2014-03-13 | 2017-02-15 | 美国印第安纳大学研究和技术公司 | 乙型肝炎核心蛋白变构调节剂 |
CN106459032A (zh) * | 2014-05-13 | 2017-02-22 | 豪夫迈·罗氏有限公司 | 治疗和预防乙型肝炎病毒感染的新的二氢喹嗪酮类 |
WO2017069279A1 (ja) * | 2015-10-23 | 2017-04-27 | 武田薬品工業株式会社 | 複素環化合物 |
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CN102060786A (zh) | 2011-01-20 | 2011-05-18 | 天津大学 | 4-(取代-1,3-二炔基)-4-(三氟甲基)-3,4-二氢取代喹唑啉-2-酮类化合物及其制备方法和应用 |
ES2640063T3 (es) | 2013-04-03 | 2017-10-31 | Janssen Sciences Ireland Uc | Derivados de n-fenil-carboxamida y su uso como medicamentos para el tratamiento de la hepatitis B |
ES2777248T3 (es) | 2013-11-14 | 2020-08-04 | Novira Therapeutics Inc | Derivados de azepano y métodos de tratar infecciones por hepatitis B |
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CN106413402A (zh) * | 2014-03-13 | 2017-02-15 | 美国印第安纳大学研究和技术公司 | 乙型肝炎核心蛋白变构调节剂 |
CN106459032A (zh) * | 2014-05-13 | 2017-02-22 | 豪夫迈·罗氏有限公司 | 治疗和预防乙型肝炎病毒感染的新的二氢喹嗪酮类 |
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CN112334137A (zh) * | 2018-05-03 | 2021-02-05 | 埃默里大学 | 用于nash和其他代谢紊乱的孤儿核受体调节剂 |
CN110872307A (zh) * | 2019-06-05 | 2020-03-10 | 河南科技大学第一附属医院 | 一种医院妇科所用噻唑类药物分子及其制备方法和应用 |
TWI746110B (zh) * | 2019-08-15 | 2021-11-11 | 大陸商福建廣生堂藥業股份有限公司 | 氧氮雜卓類化合物的製備方法 |
CN114456099A (zh) * | 2022-02-21 | 2022-05-10 | 八叶草健康产业研究院(厦门)有限公司 | 一种4-氯吡咯-2-羧酸的制备方法 |
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CN109071544B (zh) | 2020-03-17 |
CA3054324A1 (en) | 2018-08-30 |
LT3587420T (lt) | 2021-07-12 |
EP3587420A1 (en) | 2020-01-01 |
SG11201907725SA (en) | 2019-09-27 |
RS61913B1 (sr) | 2021-06-30 |
JP2020508342A (ja) | 2020-03-19 |
KR102085497B1 (ko) | 2020-03-05 |
PT3587420T (pt) | 2021-06-04 |
HUE054822T2 (hu) | 2021-10-28 |
AU2018223435A1 (en) | 2019-10-10 |
MX2019010042A (es) | 2020-01-13 |
DK3587420T3 (da) | 2021-06-07 |
AU2018223435B2 (en) | 2020-12-24 |
KR20190120300A (ko) | 2019-10-23 |
IL268827A (en) | 2019-11-03 |
EP3587420B1 (en) | 2021-03-31 |
SI3587420T1 (sl) | 2021-09-30 |
CA3054324C (en) | 2020-12-01 |
ZA201906135B (en) | 2021-04-28 |
US20200247819A1 (en) | 2020-08-06 |
ES2874656T3 (es) | 2021-11-05 |
US11053260B2 (en) | 2021-07-06 |
JP6764039B2 (ja) | 2020-09-30 |
PH12019501955A1 (en) | 2020-07-06 |
WO2018153285A1 (zh) | 2018-08-30 |
PL3587420T3 (pl) | 2021-10-11 |
BR112019017603A2 (pt) | 2020-03-24 |
EP3587420A4 (en) | 2020-02-19 |
MY175445A (en) | 2020-06-29 |
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Effective date of registration: 20220214 Address after: 355300 building 1-7, Fuyuan Industrial Park, Zherong County, Ningde City, Fujian Province Patentee after: Fujian Guangsheng Zhonglin Biotechnology Co.,Ltd. Address before: 355399 Fuyuan Industrial Zone, Dongyuan Township, Zherong County, Ningde City, Fujian Province Patentee before: FUJIAN COSUNTER PHARMACEUTICAL Co.,Ltd. |