JP2017512789A - ジヒドロピリミジン化合物及び医薬におけるその適用 - Google Patents
ジヒドロピリミジン化合物及び医薬におけるその適用 Download PDFInfo
- Publication number
- JP2017512789A JP2017512789A JP2016558407A JP2016558407A JP2017512789A JP 2017512789 A JP2017512789 A JP 2017512789A JP 2016558407 A JP2016558407 A JP 2016558407A JP 2016558407 A JP2016558407 A JP 2016558407A JP 2017512789 A JP2017512789 A JP 2017512789A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- mmol
- methyl
- thiazol
- title compound
- 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.)
- Pending
Links
- QXIAGKWWKMKVLE-VIFPVBQESA-N CC(C)(C)OC(N1C[C@H](CCC(O)=O)OCC1)=O Chemical compound CC(C)(C)OC(N1C[C@H](CCC(O)=O)OCC1)=O QXIAGKWWKMKVLE-VIFPVBQESA-N 0.000 description 1
- DYGCSUICELQJIO-COBSHVIPSA-N CC(C[C@H]1OCCNC1)C(O)=O Chemical compound CC(C[C@H]1OCCNC1)C(O)=O DYGCSUICELQJIO-COBSHVIPSA-N 0.000 description 1
- 0 CC(C[C@]1OCC[Zn]C1)C(*)=O Chemical compound CC(C[C@]1OCC[Zn]C1)C(*)=O 0.000 description 1
- OGUVUOIKRVWUDL-ZDUSSCGKSA-N CC(NC(c1ncc[s]1)=N[C@H]1c(c(Cl)c2)ccc2Cl)=C1C(OC)=O Chemical compound CC(NC(c1ncc[s]1)=N[C@H]1c(c(Cl)c2)ccc2Cl)=C1C(OC)=O OGUVUOIKRVWUDL-ZDUSSCGKSA-N 0.000 description 1
- ZRKFCDVMSWDCFX-UHFFFAOYSA-N CCC(C)CCCC(C(C)I)[ClH]CC Chemical compound CCC(C)CCCC(C(C)I)[ClH]CC ZRKFCDVMSWDCFX-UHFFFAOYSA-N 0.000 description 1
- ILFIXUVIBJYIDE-VFNWGFHPSA-N CCOC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@H]1c(ccc(F)c1)c1Br)=O Chemical compound CCOC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@H]1c(ccc(F)c1)c1Br)=O ILFIXUVIBJYIDE-VFNWGFHPSA-N 0.000 description 1
- XOYWJUFEMRHPBF-VFNWGFHPSA-N CCOC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@H]1c1ccccc1Cl)=O Chemical compound CCOC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@H]1c1ccccc1Cl)=O XOYWJUFEMRHPBF-VFNWGFHPSA-N 0.000 description 1
- GTVGTNQWQJLDEG-BTYIYWSLSA-N CCOC(C1=C(CN2[C@@H](CCC(O)=O)COCC2)NC(c2ncc[s]2)=N[C@H]1c(ccc(F)c1)c1Br)=O Chemical compound CCOC(C1=C(CN2[C@@H](CCC(O)=O)COCC2)NC(c2ncc[s]2)=N[C@H]1c(ccc(F)c1)c1Br)=O GTVGTNQWQJLDEG-BTYIYWSLSA-N 0.000 description 1
- KJKXMYQMOZCMRZ-VXGBXAGGSA-N CCOC(CC[C@H]([C@@H](C)OCC1)N1C(OC(C)(C)C)=O)=O Chemical compound CCOC(CC[C@H]([C@@H](C)OCC1)N1C(OC(C)(C)C)=O)=O KJKXMYQMOZCMRZ-VXGBXAGGSA-N 0.000 description 1
- ONELXRQCJBCEOV-ZDUSSCGKSA-N COC(C1=C(CBr)NC(c2ncc[s]2)=N[C@H]1c(ccc(F)c1)c1Cl)=O Chemical compound COC(C1=C(CBr)NC(c2ncc[s]2)=N[C@H]1c(ccc(F)c1)c1Cl)=O ONELXRQCJBCEOV-ZDUSSCGKSA-N 0.000 description 1
- CCVSZMHYKHZCJN-JLTOFOAXSA-N COC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@@H]1c(c(Cl)c1)ccc1F)=O Chemical compound COC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@@H]1c(c(Cl)c1)ccc1F)=O CCVSZMHYKHZCJN-JLTOFOAXSA-N 0.000 description 1
- SKHFPNFIHFVECE-VLIAUNLRSA-N COC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@H]1c(c(Br)c1)ccc1F)=O Chemical compound COC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@H]1c(c(Br)c1)ccc1F)=O SKHFPNFIHFVECE-VLIAUNLRSA-N 0.000 description 1
- BWVKMHFWCULXRS-VLIAUNLRSA-N COC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@H]1c1ccccc1Cl)=O Chemical compound COC(C1=C(CN2C[C@@H](CCC(O)=O)OCC2)NC(c2ncc[s]2)=N[C@H]1c1ccccc1Cl)=O BWVKMHFWCULXRS-VLIAUNLRSA-N 0.000 description 1
- HJLJZZITBHJBPM-FPSMJMQUSA-N C[C@@H]1OCCN(CC(NC(c2ncc[s]2)=N[C@H]2c(c(Cl)c3)ccc3F)=C2C(OC)=O)[C@H]1CCC(O)=O Chemical compound C[C@@H]1OCCN(CC(NC(c2ncc[s]2)=N[C@H]2c(c(Cl)c3)ccc3F)=C2C(OC)=O)[C@H]1CCC(O)=O HJLJZZITBHJBPM-FPSMJMQUSA-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
- 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
- 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
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- 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
- A61P31/14—Antivirals for RNA viruses
-
- 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
-
- 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
- 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
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 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
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Biotechnology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410126202 | 2014-03-28 | ||
| CN201410126202.0 | 2014-03-28 | ||
| CN201410596489 | 2014-10-29 | ||
| CN201410596489.3 | 2014-10-29 | ||
| PCT/CN2015/075299 WO2015144093A1 (en) | 2014-03-28 | 2015-03-27 | Dihydropyrimidine compounds and their application in pharmaceuticals |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017512789A true JP2017512789A (ja) | 2017-05-25 |
| JP2017512789A5 JP2017512789A5 (OSRAM) | 2018-04-19 |
Family
ID=54160517
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016558407A Pending JP2017512789A (ja) | 2014-03-28 | 2015-03-27 | ジヒドロピリミジン化合物及び医薬におけるその適用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9771358B2 (OSRAM) |
| EP (1) | EP3122747B1 (OSRAM) |
| JP (1) | JP2017512789A (OSRAM) |
| KR (1) | KR20160133563A (OSRAM) |
| CN (1) | CN104945395B (OSRAM) |
| AU (1) | AU2015236982B2 (OSRAM) |
| CA (1) | CA2938050A1 (OSRAM) |
| MX (1) | MX2016012573A (OSRAM) |
| MY (1) | MY196243A (OSRAM) |
| RU (1) | RU2682672C2 (OSRAM) |
| SG (1) | SG11201605896WA (OSRAM) |
| WO (1) | WO2015144093A1 (OSRAM) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20200032098A (ko) * | 2017-06-26 | 2020-03-25 | 노스 앤드 사우스 브라더 파마시 인베스트먼트 컴파니 리미티드 | 디하이드로피리미딘 화합물 및 약제에서의 이의 용도 |
| JP2021523880A (ja) * | 2018-05-16 | 2021-09-09 | シチュアン ケルン−バイオテック バイオファーマシューティカル カンパニー リミテッド | ジヒドロピリミジン化合物の固体形態及びその調製方法及びその使用 |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA026368B1 (ru) | 2011-12-21 | 2017-03-31 | Новира Терапьютикс, Инк. | Противовирусные агенты против гепатита в |
| AU2013307337B2 (en) | 2012-08-28 | 2018-07-19 | Janssen Sciences Ireland Uc | Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of Hepatitis B |
| CN105189453B (zh) | 2013-02-28 | 2018-04-10 | 爱尔兰詹森科学公司 | 氨磺酰基‑芳基酰胺及其作为用于乙型肝炎治疗的药物的用途 |
| WO2014161888A1 (en) | 2013-04-03 | 2014-10-09 | Janssen R&D Ireland | N-phenyl-carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis b |
| BR112015028538A2 (pt) | 2013-05-17 | 2017-07-25 | Janssen Sciences Ireland Uc | derivados de sulfamoiltiofenamida e o uso dos mesmos como medicamentos para o tratamento da hepatite b |
| JO3603B1 (ar) | 2013-05-17 | 2020-07-05 | Janssen Sciences Ireland Uc | مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي |
| CA2935719C (en) | 2013-07-25 | 2021-11-02 | Janssen Sciences Ireland Uc | Glyoxamide substituted pyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis b |
| AU2014338947B2 (en) | 2013-10-23 | 2018-02-22 | Janssen Sciences Ireland Uc | Carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis B |
| AU2014356986B2 (en) | 2013-11-27 | 2018-01-04 | Sunshine Lake Pharma Co., Ltd. | Processes for preparing dihydropyrimidine derivatives and intermediates thereof |
| US10392349B2 (en) | 2014-01-16 | 2019-08-27 | Novira Therapeutics, Inc. | Azepane derivatives and methods of treating hepatitis B infections |
| US9169212B2 (en) | 2014-01-16 | 2015-10-27 | Novira Therapeutics, Inc. | Azepane derivatives and methods of treating hepatitis B infections |
| KR20160128305A (ko) | 2014-02-05 | 2016-11-07 | 노비라 테라퓨틱스, 인코포레이티드 | Hbv 감염의 치료를 위한 병용 요법 |
| JP6495929B2 (ja) | 2014-02-06 | 2019-04-03 | ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー | スルファモイルピロールアミド誘導体およびｂ型肝炎の治療のための医薬としてのその使用 |
| AU2016232801A1 (en) | 2015-03-19 | 2017-10-12 | Novira Therapeutics, Inc. | Azocane and azonane derivatives and methods of treating hepatitis B infections |
| 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 |
| US10875876B2 (en) | 2015-07-02 | 2020-12-29 | Janssen Sciences Ireland Uc | Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B |
| 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 |
| TW201718496A (zh) | 2015-09-29 | 2017-06-01 | 諾維拉治療公司 | B型肝炎抗病毒劑之晶型 |
| WO2017136403A1 (en) | 2016-02-02 | 2017-08-10 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| MX384836B (es) | 2016-03-07 | 2025-03-14 | Enanta Pharm Inc | Agentes antivirales contra la hepatitis b |
| BR112018071048A2 (pt) | 2016-04-15 | 2019-05-07 | Janssen Sciences Ireland Uc | combinações e métodos que compreendem um inibidor da montagem de capsídeos |
| 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 |
| EP3508483B1 (en) | 2016-11-18 | 2021-10-06 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Dihydropyrimidine compound and preparation method and use thereof |
| US11166954B2 (en) | 2016-11-18 | 2021-11-09 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Dihydropyrimidine compound and preparation method and use thereof |
| EP3645516A4 (en) | 2017-06-27 | 2021-07-07 | Janssen Pharmaceutica NV | HETEROARYLDIHYDROPYRIMIDE DERIVATIVES AND METHODS OF TREATMENT OF HEPATITIS B INFECTIONS |
| NZ762994A (en) | 2017-08-28 | 2025-11-28 | Enanta Pharm Inc | Hepatitis b antiviral agents |
| JP2021501768A (ja) | 2017-11-02 | 2021-01-21 | アイクリス ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Ｂ型肝炎ウイルス（ｈｂｖ）に対し活性を有する新規の高活性なピラゾロ−ピペリジン置換インドール−２−カルボキサミド |
| MA50524A (fr) | 2017-11-02 | 2020-09-09 | Aicuris Gmbh & Co Kg | Nouveaux indole-2-carboxamides à substitution amino-thiazole hautement actifs agissant contre le virus de l'hépatite b (vhb) |
| US10723733B2 (en) | 2017-12-06 | 2020-07-28 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| WO2019113173A1 (en) | 2017-12-06 | 2019-06-13 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| US11058678B2 (en) | 2018-01-22 | 2021-07-13 | Enanta Pharmaceuticals, Inc. | Substituted heterocycles as antiviral agents |
| MA52019A (fr) | 2018-03-14 | 2021-01-20 | Janssen Sciences Ireland Unlimited Co | Schéma posologique de modulateur d'assemblage de capside |
| WO2019191166A1 (en) | 2018-03-29 | 2019-10-03 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| CN109021015B (zh) * | 2018-07-12 | 2019-12-03 | 山东大学 | 二氢嘧啶-磷酰胺类衍生物及其制备方法与应用 |
| US11053235B2 (en) | 2018-08-09 | 2021-07-06 | Janssen Sciences Ireland Unlimited Company | Substituted 1,4-dihydropyrimidines for the treatment of HBV infection or HBV-induced diseases |
| AR116474A1 (es) | 2018-09-21 | 2021-05-12 | Enanta Pharm Inc | DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV |
| AR116946A1 (es) | 2018-11-02 | 2021-06-30 | Aicuris Gmbh & Co Kg | Derivados de urea 6,7-dihidro-4h-pirazolo[4,3-c]piridinas activas contra el virus de la hepatitis b (vhb) |
| UY38437A (es) | 2018-11-02 | 2020-05-29 | Aicuris Gmbh & Co Kg | Nuevas urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (hbv) |
| AR116947A1 (es) | 2018-11-02 | 2021-06-30 | Aicuris Gmbh & Co Kg | Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas-indol-2-carboxamidas activas contra el virus de la hepatitis b (vhb) |
| JP2022506351A (ja) | 2018-11-02 | 2022-01-17 | アイクリス ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Ｂ型肝炎ウイルス（ｈｂｖ）に対して活性を有する新規ウレア６，７－ジヒドロ－４ｈ－チアゾロ［５，４－ｃ］ピリジン |
| AR116948A1 (es) | 2018-11-02 | 2021-06-30 | Aicuris Gmbh & Co Kg | Derivados de urea 6,7-dihidro-4h-pirazolo[1,5-a]pirazinas activas contra el virus de la hepatitis b (vhb) |
| AR117189A1 (es) | 2018-11-02 | 2021-07-21 | Aicuris Gmbh & Co Kg | Derivados de 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activos contra el virus de la hepatitis b (vhb) |
| SG11202105007TA (en) | 2018-11-21 | 2021-06-29 | Enanta Pharm Inc | Functionalized heterocycles as antiviral agents |
| TW202035412A (zh) * | 2018-12-20 | 2020-10-01 | 比利時商健生藥品公司 | 雜芳基二氫嘧啶衍生物和治療ｂ型肝炎感染之方法 |
| CA3127152A1 (en) | 2019-02-22 | 2020-08-27 | Janssen Sciences Ireland Unlimited Company | Amide derivatives useful in the treatment of hbv infection or hbv-induced diseases |
| US20220306647A1 (en) | 2019-04-30 | 2022-09-29 | Aicuris Gmbh & Co. Kg | Novel indole-2-carboxamides active against the hepatitus b virus (hbv) |
| US20220227785A1 (en) | 2019-04-30 | 2022-07-21 | Aicuris Gmbh & Co. Kg | Novel phenyl and pyridyl ureas active against the hepatitis b virus (hbv) |
| WO2020221824A1 (en) | 2019-04-30 | 2020-11-05 | Aicuris Gmbh & Co. Kg | Novel indolizine-2-carboxamides active against the hepatitis b virus (hbv) |
| WO2020221811A1 (en) | 2019-04-30 | 2020-11-05 | Aicuris Gmbh & Co. Kg | Novel oxalyl piperazines active against the hepatitis b virus (hbv) |
| US11491148B2 (en) | 2019-05-06 | 2022-11-08 | Janssen Sciences Ireland Unlimited Company | Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases |
| US11236111B2 (en) | 2019-06-03 | 2022-02-01 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| US11760755B2 (en) | 2019-06-04 | 2023-09-19 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| WO2020247575A1 (en) | 2019-06-04 | 2020-12-10 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| US20220249647A1 (en) * | 2019-06-18 | 2022-08-11 | Janssen Sciences Ireland Unlimited Company | Combination of hepatitis b virus (hbv) vaccines and dihydropyrimidine derivatives as capsid assembly modulators |
| WO2021007488A1 (en) | 2019-07-11 | 2021-01-14 | Enanta Pharmaceuticals, Inc. | Substituted heterocycles as antiviral agents |
| WO2021055425A2 (en) | 2019-09-17 | 2021-03-25 | Enanta Pharmaceuticals, Inc. | Functionalized heterocycles as antiviral agents |
| CN110615797A (zh) * | 2019-10-11 | 2019-12-27 | 李丽丽 | 用于治疗乙型肝炎的化合物及其用途 |
| WO2021188414A1 (en) | 2020-03-16 | 2021-09-23 | Enanta Pharmaceuticals, Inc. | Functionalized heterocyclic compounds as antiviral agents |
| EP4263535A1 (en) | 2020-12-17 | 2023-10-25 | Astrazeneca AB | N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)- quinoline-4-carboxamides |
| JP2024505709A (ja) | 2021-02-05 | 2024-02-07 | ヘパジーン セラピューティクス（エイチケー）リミティド | フェニルジヒドロピリミジン系化合物及びその使用 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014029193A1 (en) * | 2012-08-24 | 2014-02-27 | Sunshine Lake Pharma Co., Ltd. | Dihydropyrimidine compounds and their application in pharmaceuticals |
| WO2014037480A1 (en) * | 2012-09-10 | 2014-03-13 | F. Hoffmann-La Roche Ag | 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0202654A3 (en) | 1985-05-20 | 1987-12-16 | E.R. Squibb & Sons, Inc. | 5-carboxy-1,4-dihydropyrimidine derivatives |
| GB8906168D0 (en) | 1989-03-17 | 1989-05-04 | Pfizer Ltd | Therapeutic agents |
| SE9702563D0 (sv) | 1997-07-02 | 1997-07-02 | Astra Ab | Compounds |
| SE9702564D0 (sv) | 1997-07-02 | 1997-07-02 | Astra Ab | New compounds |
| DE19817262A1 (de) | 1998-04-18 | 1999-10-21 | Bayer Ag | Neue 2-heterocyclisch substituierte Dihydropyrimidine |
| DE19817264A1 (de) | 1998-04-18 | 1999-10-21 | Bayer Ag | Neue Dihydropyrimidine |
| DE19817265A1 (de) | 1998-04-18 | 1999-10-21 | Bayer Ag | Verwendung von Dihydropyrimidinen als Arzneimittel und neue Stoffe |
| WO2000058302A1 (de) | 1999-03-25 | 2000-10-05 | Bayer Aktiengesellschaft | Dihydropyrimidine und ihre verwendung zur behandlung von hepatitis b |
| DE10012549A1 (de) | 2000-03-15 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10012824A1 (de) | 2000-03-16 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10012823A1 (de) | 2000-03-16 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10013125A1 (de) | 2000-03-17 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10013126A1 (de) | 2000-03-17 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| US7157461B2 (en) | 2003-07-23 | 2007-01-02 | Bristol-Myers Squibb Co. | Substituted dihydropyrimidine inhibitors of calcium channel function |
| CN101104617B (zh) | 2006-07-10 | 2010-06-23 | 北京摩力克科技有限公司 | 二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途 |
| CN101104604B (zh) | 2006-07-10 | 2011-03-02 | 北京摩力克科技有限公司 | 光学纯二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途 |
| CN101225084A (zh) | 2007-01-16 | 2008-07-23 | 北京摩力克科技有限公司 | 二氢嘧啶类化合物及其用于制备治疗和预防病毒性疾病的药物的用途 |
| WO2008154819A1 (fr) | 2007-06-18 | 2008-12-24 | Zhang, Zhongneng | Thiazolyl-dihydropyrimidines à substitution carbéthoxy |
| BRPI0813237B8 (pt) | 2007-06-18 | 2021-05-25 | Sunshine Lake Pharma Co Ltd | composto, método para preparar o composto, medicamento, e, uso do composto |
| CN101328168B (zh) | 2007-06-18 | 2011-09-07 | 张中能 | 一种乙氧碳酰基-取代噻唑二氢嘧啶 |
| CN101328170B (zh) | 2007-06-18 | 2011-09-14 | 张中能 | 一种氟苯基-取代噻唑二氢嘧啶 |
| WO2010069147A1 (zh) | 2008-12-17 | 2010-06-24 | 张中能 | 二氢嘧啶类化合物、其组合物及其应用 |
| CN101744823B (zh) | 2008-12-17 | 2013-06-19 | 广东东阳光药业有限公司 | 一种二氢嘧啶类化合物的固体分散体及其药用制剂 |
| CN101575318B (zh) | 2009-06-25 | 2012-02-08 | 中国人民解放军军事医学科学院毒物药物研究所 | 二氢嘧啶类化合物及其用于制备治疗和/或预防病毒性疾病的药物的用途 |
| WO2013019967A1 (en) | 2011-08-02 | 2013-02-07 | Scripps Research Institute, A Not-For-Profit Public Benefit Corporation Of California | Modulators of virus assembly as antiviral agents |
| EA026977B1 (ru) | 2012-01-06 | 2017-06-30 | Янссен Сайенсиз Айрлэнд Юси | 4,4-дизамещенные 1,4-дигидропиримидины и их применение в качестве лекарственных препаратов для лечения гепатита b |
| 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 |
| CN103664897B (zh) | 2012-09-01 | 2018-04-03 | 广东东阳光药业有限公司 | 二氢嘧啶类化合物及其在药物中的应用 |
| CN103664925B (zh) | 2012-09-07 | 2018-01-23 | 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 |
| 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 |
| US20150292045A1 (en) | 2012-11-09 | 2015-10-15 | Indiana University Research And Technology Corporation | Alternative uses for hbv assembly effectors |
| CA2907490A1 (en) | 2013-03-20 | 2014-09-25 | Indiana University Research And Technology Corporation | Fluorescent-hap: a diagnostic stain for hbv cores in cells |
| WO2014184328A1 (en) | 2013-05-17 | 2014-11-20 | F. Hoffmann-La Roche Ag | 6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
| 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 |
| RU2678990C1 (ru) | 2013-11-19 | 2019-02-05 | Саншайн Лейк Фарма Ко., Лтд. | Соединения дигидропиримидина и их применение в фармацевтических препаратах |
| CN104650070B (zh) | 2013-11-25 | 2018-09-14 | 广东东阳光药业有限公司 | 二氢嘧啶类化合物及其在药物中的应用 |
| AU2014356986B2 (en) * | 2013-11-27 | 2018-01-04 | Sunshine Lake Pharma Co., Ltd. | Processes for preparing dihydropyrimidine derivatives and intermediates thereof |
| EP3114128B1 (en) | 2014-03-07 | 2019-01-02 | F. Hoffmann-La Roche AG | Novel 6-fused heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
| WO2015180631A1 (zh) | 2014-05-30 | 2015-12-03 | 南京明德新药研发股份有限公司 | 作为hbv抑制剂的二氢嘧啶并环衍生物 |
-
2015
- 2015-03-27 WO PCT/CN2015/075299 patent/WO2015144093A1/en not_active Ceased
- 2015-03-27 US US15/116,226 patent/US9771358B2/en active Active
- 2015-03-27 JP JP2016558407A patent/JP2017512789A/ja active Pending
- 2015-03-27 RU RU2016138735A patent/RU2682672C2/ru active
- 2015-03-27 EP EP15769748.3A patent/EP3122747B1/en active Active
- 2015-03-27 MX MX2016012573A patent/MX2016012573A/es unknown
- 2015-03-27 CN CN201510141969.5A patent/CN104945395B/zh active Active
- 2015-03-27 MY MYPI2016702906A patent/MY196243A/en unknown
- 2015-03-27 KR KR1020167029448A patent/KR20160133563A/ko not_active Withdrawn
- 2015-03-27 SG SG11201605896WA patent/SG11201605896WA/en unknown
- 2015-03-27 AU AU2015236982A patent/AU2015236982B2/en active Active
- 2015-03-27 CA CA2938050A patent/CA2938050A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014029193A1 (en) * | 2012-08-24 | 2014-02-27 | Sunshine Lake Pharma Co., Ltd. | Dihydropyrimidine compounds and their application in pharmaceuticals |
| WO2014037480A1 (en) * | 2012-09-10 | 2014-03-13 | F. Hoffmann-La Roche Ag | 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
Non-Patent Citations (3)
| Title |
|---|
| 光学異性体の分離（季刊 化学総説 NO.6）, JPN6011000511, 1989, pages 2 - 5, ISSN: 0003988203 * |
| 加藤隆一: "光学異性薬物の研究の流れ", 薬事, vol. 第２９巻、第１０号, JPN3011000611, 1 October 1987 (1987-10-01), JP, pages 2039 - 2042, ISSN: 0003988202 * |
| 山中 宏、宮崎 浩、村上尚道: "光学活性体のプレパレーション・生理活性・利用", 季刊 化学総説 光学異性体の分離, JPN3011000610, 10 June 1999 (1999-06-10), JP, pages 8 - 9, ISSN: 0003988201 * |
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|---|---|---|---|---|
| KR20200032098A (ko) * | 2017-06-26 | 2020-03-25 | 노스 앤드 사우스 브라더 파마시 인베스트먼트 컴파니 리미티드 | 디하이드로피리미딘 화합물 및 약제에서의 이의 용도 |
| JP2020525453A (ja) * | 2017-06-26 | 2020-08-27 | ノース・アンド・サウス・ブラザー・ファーマシー・インベストメント・カンパニー・リミテッド | ジヒドロピリミジン化合物、及び医薬におけるその使用 |
| JP7260488B2 (ja) | 2017-06-26 | 2023-04-18 | サンシャイン・レイク・ファーマ・カンパニー・リミテッド | ジヒドロピリミジン化合物、及び医薬におけるその使用 |
| KR102665544B1 (ko) | 2017-06-26 | 2024-05-14 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 디하이드로피리미딘 화합물 및 약제에서의 이의 용도 |
| JP2021523880A (ja) * | 2018-05-16 | 2021-09-09 | シチュアン ケルン−バイオテック バイオファーマシューティカル カンパニー リミテッド | ジヒドロピリミジン化合物の固体形態及びその調製方法及びその使用 |
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| WO2015144093A1 (en) | 2015-10-01 |
| MY196243A (en) | 2023-03-24 |
| RU2016138735A (ru) | 2018-05-03 |
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| RU2016138735A3 (OSRAM) | 2018-05-03 |
| RU2682672C2 (ru) | 2019-03-20 |
| AU2015236982A1 (en) | 2016-08-11 |
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| US20160347746A1 (en) | 2016-12-01 |
| EP3122747A1 (en) | 2017-02-01 |
| US9771358B2 (en) | 2017-09-26 |
| SG11201605896WA (en) | 2016-08-30 |
| CN104945395A (zh) | 2015-09-30 |
| CA2938050A1 (en) | 2015-10-01 |
| MX2016012573A (es) | 2018-02-19 |
| CN104945395B (zh) | 2018-01-23 |
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