CN103626752B - 二氢嘧啶类化合物及其在药物中的应用 - Google Patents
二氢嘧啶类化合物及其在药物中的应用 Download PDFInfo
- Publication number
- CN103626752B CN103626752B CN201310373003.5A CN201310373003A CN103626752B CN 103626752 B CN103626752 B CN 103626752B CN 201310373003 A CN201310373003 A CN 201310373003A CN 103626752 B CN103626752 B CN 103626752B
- Authority
- CN
- China
- Prior art keywords
- methyl
- esi
- independently
- thiazol
- dihydropyrimidine
- 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.)
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- 0 CCC(C1)C(C)(C(C)**)[N+]C=C1C(C)C Chemical compound CCC(C1)C(C)(C(C)**)[N+]C=C1C(C)C 0.000 description 10
- IDTNVGJHOHSVTM-UHFFFAOYSA-N C=[O]Nc1ccccc1 Chemical compound C=[O]Nc1ccccc1 IDTNVGJHOHSVTM-UHFFFAOYSA-N 0.000 description 1
- MRXDMKRNHOZUPH-YXSNPGODSA-N CC(C)/C=N\C(\C(C)C)=C/S Chemical compound CC(C)/C=N\C(\C(C)C)=C/S MRXDMKRNHOZUPH-YXSNPGODSA-N 0.000 description 1
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- HIOMIOFBGFGDHW-LURJTMIESA-N CC1(C)OC[C@@H](C(OC)=O)NC1 Chemical compound CC1(C)OC[C@@H](C(OC)=O)NC1 HIOMIOFBGFGDHW-LURJTMIESA-N 0.000 description 1
- XJYONJZVZMKDAC-UHFFFAOYSA-N CCOC(C1=C(CN(CCOC2)C2C(O)=O)NC([n]2ncnc2)=NC1c(c(Br)c1)ccc1F)=O Chemical compound CCOC(C1=C(CN(CCOC2)C2C(O)=O)NC([n]2ncnc2)=NC1c(c(Br)c1)ccc1F)=O XJYONJZVZMKDAC-UHFFFAOYSA-N 0.000 description 1
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- BRWAYHHCHJZPCL-UHFFFAOYSA-N CCOC(C1=C(CN2CC(C(NCC(O)=O)=O)OCC2)NC(c2ncc[s]2)=NC1c(c(Br)c1)ccc1F)=O Chemical compound CCOC(C1=C(CN2CC(C(NCC(O)=O)=O)OCC2)NC(c2ncc[s]2)=NC1c(c(Br)c1)ccc1F)=O BRWAYHHCHJZPCL-UHFFFAOYSA-N 0.000 description 1
- PBAXUOXKRRYXPP-UHFFFAOYSA-N CCOC(C1=C(CN2CC(CCCO)OCC2)NC(c2ncc[s]2)=NC1c(c(Br)c1)ccc1F)=O Chemical compound CCOC(C1=C(CN2CC(CCCO)OCC2)NC(c2ncc[s]2)=NC1c(c(Br)c1)ccc1F)=O PBAXUOXKRRYXPP-UHFFFAOYSA-N 0.000 description 1
- JEEQPNUWNKXYTE-UHFFFAOYSA-N CCOC(C1=C(CN2CC(CO)OCC2)NC(c2ncc[s]2)=NC1c(c(Cl)c1)ccc1F)=O Chemical compound CCOC(C1=C(CN2CC(CO)OCC2)NC(c2ncc[s]2)=NC1c(c(Cl)c1)ccc1F)=O JEEQPNUWNKXYTE-UHFFFAOYSA-N 0.000 description 1
- XBOYSNFVLIWDKG-KKFHFHRHSA-N CCOC(C1=C(CN2C[C@@H](C(C)(C)O)OCC2)NC(c2n[nH]cn2)=NC1c(c(Br)c1)ccc1F)=O Chemical compound CCOC(C1=C(CN2C[C@@H](C(C)(C)O)OCC2)NC(c2n[nH]cn2)=NC1c(c(Br)c1)ccc1F)=O XBOYSNFVLIWDKG-KKFHFHRHSA-N 0.000 description 1
- YIMSZROSRJOSQO-YJJYDOSJSA-N CCOC(C1=C(CN2C[C@H](CO)OCC2)NC(c2n[nH]cn2)=NC1c(c(Br)c1)ccc1F)=O Chemical compound CCOC(C1=C(CN2C[C@H](CO)OCC2)NC(c2n[nH]cn2)=NC1c(c(Br)c1)ccc1F)=O YIMSZROSRJOSQO-YJJYDOSJSA-N 0.000 description 1
- CJSQUDWTGGSTOR-IDKMENSTSA-N CC[C@@H](C(OC[C@@H]1N(CC(NC(c2ncc[s]2)=NC2c(c(Br)c3)ccc3F)=C2C(OCC)=O)CCOC1)=O)N Chemical compound CC[C@@H](C(OC[C@@H]1N(CC(NC(c2ncc[s]2)=NC2c(c(Br)c3)ccc3F)=C2C(OCC)=O)CCOC1)=O)N CJSQUDWTGGSTOR-IDKMENSTSA-N 0.000 description 1
- IJLHBRUCOZPNLF-MYJWUSKBSA-N COC(C1=C(CN(CCOC2)[C@@H]2C(O)=O)NC(c2ncc[s]2)=NC1c(ccc(F)c1)c1Br)=O Chemical compound COC(C1=C(CN(CCOC2)[C@@H]2C(O)=O)NC(c2ncc[s]2)=NC1c(ccc(F)c1)c1Br)=O IJLHBRUCOZPNLF-MYJWUSKBSA-N 0.000 description 1
- RYXRCGIYXJMBJQ-UHFFFAOYSA-N COC(CCC1OCCNC1)=O Chemical compound COC(CCC1OCCNC1)=O RYXRCGIYXJMBJQ-UHFFFAOYSA-N 0.000 description 1
- XDELKSRGBLWMBA-UHFFFAOYSA-N Ic1cnccc1 Chemical compound Ic1cnccc1 XDELKSRGBLWMBA-UHFFFAOYSA-N 0.000 description 1
- OPZDXMCOWFPQPE-UHFFFAOYSA-N O=Cc(ccc(F)c1)c1Br Chemical compound O=Cc(ccc(F)c1)c1Br OPZDXMCOWFPQPE-UHFFFAOYSA-N 0.000 description 1
- VYNVYTZERYFTHX-UHFFFAOYSA-N OCCCC1OCCNC1 Chemical compound OCCCC1OCCNC1 VYNVYTZERYFTHX-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510324031.7A CN104926808B (zh) | 2012-08-24 | 2013-08-23 | 二氢嘧啶类化合物及其在药物中的应用 |
| CN201310373003.5A CN103626752B (zh) | 2012-08-24 | 2013-08-23 | 二氢嘧啶类化合物及其在药物中的应用 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012103030334 | 2012-08-24 | ||
| CN201210303033 | 2012-08-24 | ||
| CN201210303033.4 | 2012-08-24 | ||
| CN201310116949.3 | 2013-04-03 | ||
| CN2013101169493 | 2013-04-03 | ||
| CN201310116949 | 2013-04-03 | ||
| CN201310373003.5A CN103626752B (zh) | 2012-08-24 | 2013-08-23 | 二氢嘧啶类化合物及其在药物中的应用 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510324031.7A Division CN104926808B (zh) | 2012-08-24 | 2013-08-23 | 二氢嘧啶类化合物及其在药物中的应用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103626752A CN103626752A (zh) | 2014-03-12 |
| CN103626752B true CN103626752B (zh) | 2015-08-12 |
Family
ID=50149385
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310373003.5A Active CN103626752B (zh) | 2012-08-24 | 2013-08-23 | 二氢嘧啶类化合物及其在药物中的应用 |
| CN201510324031.7A Active CN104926808B (zh) | 2012-08-24 | 2013-08-23 | 二氢嘧啶类化合物及其在药物中的应用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510324031.7A Active CN104926808B (zh) | 2012-08-24 | 2013-08-23 | 二氢嘧啶类化合物及其在药物中的应用 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9340538B2 (enExample) |
| EP (1) | EP2888241B1 (enExample) |
| JP (1) | JP6263533B2 (enExample) |
| KR (1) | KR102148678B1 (enExample) |
| CN (2) | CN103626752B (enExample) |
| AU (1) | AU2013305390C1 (enExample) |
| BR (1) | BR112015002858A2 (enExample) |
| CA (1) | CA2876690C (enExample) |
| DK (1) | DK2888241T3 (enExample) |
| ES (1) | ES2640049T3 (enExample) |
| HU (1) | HUE034919T2 (enExample) |
| MX (1) | MX2015002511A (enExample) |
| MY (1) | MY182403A (enExample) |
| PL (1) | PL2888241T3 (enExample) |
| PT (1) | PT2888241T (enExample) |
| RU (1) | RU2655914C9 (enExample) |
| SG (1) | SG11201408791TA (enExample) |
| TW (1) | TWI668217B (enExample) |
| WO (1) | WO2014029193A1 (enExample) |
| ZA (1) | ZA201500451B (enExample) |
Families Citing this family (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130267517A1 (en) | 2012-03-31 | 2013-10-10 | Hoffmann-La Roche Inc. | Novel 4-methyl-dihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
| KR20150054795A (ko) * | 2012-09-10 | 2015-05-20 | 에프. 호프만-라 로슈 아게 | B형 간염 바이러스 감염의 치료 및 예방을 위한 6-아미노산 헤테로아릴다이하이드로피리미딘 |
| CN103664899B (zh) * | 2012-09-11 | 2017-06-16 | 广东东阳光药业有限公司 | 杂芳基取代的二氢嘧啶类化合物及其在药物中的应用 |
| JP6524081B2 (ja) * | 2013-11-19 | 2019-06-05 | サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． | ジヒドロピリミジン化合物及び医薬におけるその適用 |
| CN104650069B (zh) * | 2013-11-19 | 2019-04-19 | 广东东阳光药业有限公司 | 4-甲基二氢嘧啶类化合物及其在药物中的应用 |
| AU2014356984B2 (en) * | 2013-11-27 | 2018-01-04 | Sunshine Lake Pharma Co., Ltd. | Processes for preparing dihydropyrimidine derivatives and intermediates thereof |
| RS58384B1 (sr) | 2014-03-07 | 2019-04-30 | Hoffmann La Roche | Novi 6-fuzionisani heteroarildihidropirimidini za lečenje i profilaksu infekcije virusom hepatitisa b |
| KR20160133563A (ko) * | 2014-03-28 | 2016-11-22 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 다이하이드로피리미딘 화합물 및 이의 약제학적 용도 |
| CN105153164B (zh) * | 2014-05-30 | 2018-10-30 | 齐鲁制药有限公司 | 作为hbv抑制剂的二氢嘧啶并环衍生物 |
| ES2687606T3 (es) * | 2014-05-30 | 2018-10-26 | Qilu Pharmaceutical Co., Ltd. | Derivado de bucle de dihidropirimido como inhibidor de HBV |
| WO2016012470A1 (en) * | 2014-07-25 | 2016-01-28 | F. Hoffmann-La Roche Ag | New amorphous and crystalline forms of (3s)-4-[[(4r)-4-(2-chloro-4-fluoro-phenyl)-5-methoxycarbonyl-2-thiazol-2-yl-1, 4-dihydropyrimidin-6-yl]methyl]morpholine-3-carboxylic acid |
| CN105859708B (zh) * | 2015-02-07 | 2020-01-21 | 广东东阳光药业有限公司 | 二氢嘧啶衍生物的盐及其在药物中的应用 |
| DK3270915T3 (da) * | 2015-03-16 | 2020-06-15 | Hoffmann La Roche | Kombineret behandling med en TLR7-agonist og en HBV-kapsidsamlingsinhibitor |
| WO2016161268A1 (en) | 2015-04-01 | 2016-10-06 | Enanta Pharmaceuticals, Inc. | Hepatitis b antviral agents |
| US10738035B2 (en) | 2015-05-13 | 2020-08-11 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| WO2017011552A1 (en) | 2015-07-13 | 2017-01-19 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| US10301255B2 (en) | 2015-07-22 | 2019-05-28 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| HK1255463A1 (zh) * | 2015-11-03 | 2019-08-16 | F. Hoffmann-La Roche Ag | Hbv衣壳组装抑制剂和干扰素的组合疗法 |
| WO2017136403A1 (en) | 2016-02-02 | 2017-08-10 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| AR107633A1 (es) | 2016-02-19 | 2018-05-16 | Hoffmann La Roche | Procedimiento para la preparación del ácido 4-fenil-5-alcoxicarbonil-2-tiazol-2-il-1,4-dihidropirimidin-6-il-[metil]-3-oxo-5,6,8,8a-tetrahidro-1h-imidazo[1,5a]pirazin-2-il-carboxílico |
| CN109069488B (zh) | 2016-03-07 | 2021-09-07 | 英安塔制药有限公司 | 乙型肝炎抗病毒剂 |
| WO2017198201A1 (en) * | 2016-05-19 | 2017-11-23 | Sunshine Lake Pharma Co., Ltd. | Crystalline form, salt and complex of dihydropyrimidine derivative, and uses thereof in medicine |
| KR20190027814A (ko) * | 2016-06-10 | 2019-03-15 | 이난타 파마슈티칼스, 인코포레이티드 | B형 간염 항바이러스제 |
| CN107674072B (zh) * | 2016-08-01 | 2020-11-24 | 广东东阳光药业有限公司 | 二氢嘧啶衍生物及其酸加成物的制备方法 |
| WO2018036941A1 (en) | 2016-08-24 | 2018-03-01 | F. Hoffmann-La Roche Ag | Combination therapy of an hbv capsid assembly inhibitor and a nucleos(t)ide analogue |
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