JP2002512243A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2002512243A5 JP2002512243A5 JP2000544665A JP2000544665A JP2002512243A5 JP 2002512243 A5 JP2002512243 A5 JP 2002512243A5 JP 2000544665 A JP2000544665 A JP 2000544665A JP 2000544665 A JP2000544665 A JP 2000544665A JP 2002512243 A5 JP2002512243 A5 JP 2002512243A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- general formula
- substituted
- formula
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 description 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 8
- 125000004432 carbon atom Chemical group C* 0.000 description 7
- 229910052739 hydrogen Inorganic materials 0.000 description 7
- 239000001257 hydrogen Substances 0.000 description 7
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 description 6
- 229910052736 halogen Inorganic materials 0.000 description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 6
- -1 trifluoromethoxy, carboxyl Chemical group 0.000 description 6
- 150000002367 halogens Chemical group 0.000 description 5
- 125000001424 substituent group Chemical group 0.000 description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 4
- 125000004122 cyclic group Chemical group 0.000 description 4
- 150000002431 hydrogen Chemical class 0.000 description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 125000003118 aryl group Chemical group 0.000 description 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 3
- 125000004093 cyano group Chemical group *C#N 0.000 description 3
- 229910052760 oxygen Inorganic materials 0.000 description 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
- 125000004076 pyridyl group Chemical group 0.000 description 3
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 description 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 125000003710 aryl alkyl group Chemical group 0.000 description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
- 125000000753 cycloalkyl group Chemical group 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 229910052717 sulfur Inorganic materials 0.000 description 2
- 125000001425 triazolyl group Chemical group 0.000 description 2
- 206010059193 Acute hepatitis B Diseases 0.000 description 1
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 208000037628 acute hepatitis B virus infection Diseases 0.000 description 1
- 125000002252 acyl group Chemical group 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 150000001409 amidines Chemical class 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 125000004104 aryloxy group Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 150000001540 azides Chemical group 0.000 description 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 208000016350 chronic hepatitis B virus infection Diseases 0.000 description 1
- 125000004663 dialkyl amino group Chemical group 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 125000001072 heteroaryl group Chemical group 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
- 125000001183 hydrocarbyl group Chemical group 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 229930195734 saturated hydrocarbon Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 229930195735 unsaturated hydrocarbon Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19817264A DE19817264A1 (de) | 1998-04-18 | 1998-04-18 | Neue Dihydropyrimidine |
| DE19817264.8 | 1998-04-18 | ||
| PCT/EP1999/002344 WO1999054326A1 (de) | 1998-04-18 | 1999-04-07 | Dihydropyrimidine |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010165860A Division JP5237332B2 (ja) | 1998-04-18 | 2010-07-23 | ジヒドロピリミジン類 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002512243A JP2002512243A (ja) | 2002-04-23 |
| JP2002512243A5 true JP2002512243A5 (https=) | 2006-06-01 |
| JP4590097B2 JP4590097B2 (ja) | 2010-12-01 |
Family
ID=7864972
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000544665A Expired - Lifetime JP4590097B2 (ja) | 1998-04-18 | 1999-04-07 | ジヒドロピリミジン類 |
| JP2010165860A Expired - Lifetime JP5237332B2 (ja) | 1998-04-18 | 2010-07-23 | ジヒドロピリミジン類 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010165860A Expired - Lifetime JP5237332B2 (ja) | 1998-04-18 | 2010-07-23 | ジヒドロピリミジン類 |
Country Status (36)
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000058302A1 (de) * | 1999-03-25 | 2000-10-05 | Bayer Aktiengesellschaft | Dihydropyrimidine und ihre verwendung zur behandlung von hepatitis b |
| WO2000078730A1 (en) | 1999-06-23 | 2000-12-28 | Ajinomoto Co., Inc. | Novel dihydropyrimidine derivatives |
| AU3009801A (en) * | 1999-12-22 | 2001-07-03 | Bayer Aktiengesellschaft | Combinations of medicaments for treating viral diseases |
| DE10012823A1 (de) | 2000-03-16 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10013126A1 (de) * | 2000-03-17 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10013125A1 (de) * | 2000-03-17 | 2001-09-20 | Bayer Ag | Arzneimittel gegen virale Erkrankungen |
| DE10125131A1 (de) * | 2001-05-23 | 2002-12-05 | Bayer Ag | Verfahren zur Spaltung des Methyl 4-(2-chlor-4-fluorphenyl)-2-(3,5-difluor-2-pyridinyl)-6-methyl-1,4-dihydro-5-pyrmidincarboxylat-Racemats |
| US20040092735A1 (en) * | 2002-11-08 | 2004-05-13 | Orchid Chemicals & Pharmaceuticals Limited | Process for the preparation of cefuroxime sodium |
| 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 |
| RU2452733C2 (ru) * | 2007-04-27 | 2012-06-10 | Пэдью Фарма Л.П. | Антагонисты trpv1 и их применение |
| AU2008265397C1 (en) * | 2007-06-18 | 2013-08-29 | Sunshine Lake Pharma Co., Ltd. | Bromo-phenyl substituted thiazolyl dihydropyrimidines |
| NZ582443A (en) | 2007-07-12 | 2011-04-29 | Novartis Ag | Oral pharmaceutical solutions containing telbivudine |
| 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 |
| CN104926808B (zh) | 2012-08-24 | 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 |
| CA2881322A1 (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 |
| 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 |
| HK1215030A1 (zh) * | 2012-11-09 | 2016-08-12 | Indiana University Research And Technology Corporation | 用於hbv組裝效應劑的替代用途 |
| BR102014028162A2 (pt) * | 2013-11-12 | 2015-09-08 | Dow Agrosciences Llc | processo para fluoração de compostos |
| WO2015074546A1 (en) | 2013-11-19 | 2015-05-28 | Sunshine Lake Pharma Co., Ltd. | Dihydropyrimidine compounds and their application in pharmaceuticals |
| KR102284938B1 (ko) | 2013-11-27 | 2021-08-02 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 다이하이드로피리미딘 유도체 및 이의 중간산물의 제조 방법 |
| CN104945395B (zh) | 2014-03-28 | 2018-01-23 | 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 |
| CN106459061B (zh) * | 2014-05-30 | 2020-01-21 | 齐鲁制药有限公司 | 作为hbv抑制剂的二氢嘧啶并环衍生物 |
| 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 |
| US10098889B2 (en) | 2015-02-07 | 2018-10-16 | Sunshine Lake Pharma Co., Ltd. | Complexes and salts of dihydropyrimidine derivatives and their application in pharmaceuticals |
| AU2018291688B2 (en) * | 2017-06-27 | 2022-02-03 | Janssen Pharmaceutica Nv | Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis B infections |
| US10759774B2 (en) | 2017-09-28 | 2020-09-01 | The Curators Of The University Of Missouri | Inhibitors of hepatitis B virus targeting capsid assembly |
| KR20200083552A (ko) | 2017-11-02 | 2020-07-08 | 아이쿠리스 게엠베하 운트 코. 카게 | B형 간염 바이러스 (hbv)에 활성인 신규 고활성 피라졸로-피페리딘 치환된 인돌-2-카르복스아미드 |
| EA202091113A1 (ru) | 2017-11-02 | 2020-08-28 | Айкурис Гмбх Унд Ко. Кг | Новые высокоактивные аминотиазолзамещенные индол-2-карбоксамиды, активные в отношении вируса гепатита b (hbv) |
| KR20210006412A (ko) * | 2018-05-08 | 2021-01-18 | 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 | 디히드로피리미딘 유도체 및 hbv 감염 또는 hbv-유도성 질환의 치료에 있어서의 이의 용도 |
| 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 |
| 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) |
| 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) |
| 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) |
| PY1991603A (es) | 2018-11-02 | 2020-09-17 | Aicuris Gmbh & Co Kg | Nueva 6,7-dihidro-4h-pirazolo [1,5-a] pirazina indole -2-carboxamidas activas contra el virus de la hepatitis b (vhb) |
| WO2020089460A1 (en) * | 2018-11-02 | 2020-05-07 | Aicuris Gmbh & Co. Kg | Novel urea 6,7-dihydro-4h-thiazolo[5,4-c]pyridines active against the hepatitis b virus (hbv) |
| PY1991611A (es) | 2018-11-02 | 2022-03-14 | Aicuris Gmbh & Co Kg | Nueva urea 6,7-dihidro-4h-pirazolo [1,5-a] pirazinas activas contra el virus de la hepatitis b (vhb) |
| CN113227090A (zh) | 2018-12-20 | 2021-08-06 | 詹森药业有限公司 | 杂芳基二氢嘧啶衍生物和治疗乙型肝炎感染的方法 |
| WO2020221824A1 (en) | 2019-04-30 | 2020-11-05 | Aicuris Gmbh & Co. Kg | Novel indolizine-2-carboxamides active against the hepatitis 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) |
| JP2022533008A (ja) | 2019-04-30 | 2022-07-21 | 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）に対し活性な新規のオキサリルピペラジン |
| BR112021021564A2 (pt) | 2019-04-30 | 2022-01-04 | Aicuris Gmbh & Co Kg | Indol-2-carboxamidas inovadoras ativas contra o vírus da hepatite b (hbv) |
| WO2020255016A1 (en) | 2019-06-18 | 2020-12-24 | Janssen Sciences Ireland Unlimited Company | Combination of hepatitis b virus (hbv) vaccines and dihydropyrimidine derivatives as capsid assembly modulators |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL130304C (https=) * | 1964-02-12 | |||
| CH550189A (de) | 1971-01-08 | 1974-06-14 | Ciba Geigy Ag | Verfahren zur herstellung von neuen dibenzo (b,f) thiepincarbonsaeuren. |
| CH569043A5 (https=) | 1973-01-23 | 1975-11-14 | Ciba Geigy Ag | |
| US4371537A (en) * | 1981-08-13 | 1983-02-01 | The Dow Chemical Company | Sulfur-substituted phenoxypyridines having antiviral activity |
| DE3234684A1 (de) | 1982-09-18 | 1984-03-22 | Bayer Ag, 5090 Leverkusen | Neue dihydropyrimidine, verfahren zu ihrer herstellung sowie ihre verwendung in arzneimitteln |
| JPS60185764A (ja) | 1984-03-05 | 1985-09-21 | Wako Pure Chem Ind Ltd | ピリジン誘導体の新規な製造法 |
| US4698340A (en) * | 1984-07-19 | 1987-10-06 | Fujisawa Pharmaceutical Co., Ltd. | Pyrimidine derivatives, processes for preparation thereof and composition containing the same |
| US4727073A (en) | 1984-10-01 | 1988-02-23 | Fujisawa Pharmaceutical Co., Ltd. | Pyrimidine derivatives and composition of the same |
| GB8906168D0 (en) | 1989-03-17 | 1989-05-04 | Pfizer Ltd | Therapeutic agents |
| CN1237166A (zh) | 1996-11-12 | 1999-12-01 | 诺瓦提斯公司 | 可用作除草剂的吡唑衍生物 |
| SE9702564D0 (sv) * | 1997-07-02 | 1997-07-02 | Astra Ab | New compounds |
-
1998
- 1998-04-18 DE DE19817264A patent/DE19817264A1/de not_active Withdrawn
-
1999
- 1999-04-07 BR BRPI9917862A patent/BRPI9917862B8/pt not_active IP Right Cessation
- 1999-04-07 TR TR2000/03011T patent/TR200003011T2/xx unknown
- 1999-04-07 JP JP2000544665A patent/JP4590097B2/ja not_active Expired - Lifetime
- 1999-04-07 DK DK99920603T patent/DK1080086T3/da active
- 1999-04-07 ID IDW20002111A patent/ID27263A/id unknown
- 1999-04-07 NZ NZ507569A patent/NZ507569A/en not_active IP Right Cessation
- 1999-04-07 EP EP99920603A patent/EP1080086B1/de not_active Expired - Lifetime
- 1999-04-07 BR BRPI9909730-3A patent/BR9909730B1/pt not_active IP Right Cessation
- 1999-04-07 IL IL13858499A patent/IL138584A0/xx active IP Right Grant
- 1999-04-07 CA CA002328780A patent/CA2328780C/en not_active Expired - Lifetime
- 1999-04-07 PT PT99920603T patent/PT1080086E/pt unknown
- 1999-04-07 ES ES99920603T patent/ES2183548T3/es not_active Expired - Lifetime
- 1999-04-07 CU CU20000220A patent/CU23049A3/es unknown
- 1999-04-07 KR KR1020007011527A patent/KR100636771B1/ko not_active Expired - Lifetime
- 1999-04-07 PL PL99343481A patent/PL193898B1/pl unknown
- 1999-04-07 DE DE59902573T patent/DE59902573D1/de not_active Expired - Lifetime
- 1999-04-07 CN CNB998074950A patent/CN1159311C/zh not_active Expired - Lifetime
- 1999-04-07 CZ CZ20003871A patent/CZ293482B6/cs not_active IP Right Cessation
- 1999-04-07 HU HU0102372A patent/HUP0102372A3/hu unknown
- 1999-04-07 SK SK1565-2000A patent/SK286407B6/sk not_active IP Right Cessation
- 1999-04-07 RU RU2000129148/04A patent/RU2245881C9/ru active
- 1999-04-07 US US09/673,592 patent/US6696451B1/en not_active Expired - Lifetime
- 1999-04-07 AT AT99920603T patent/ATE223401T1/de active
- 1999-04-07 WO PCT/EP1999/002344 patent/WO1999054326A1/de not_active Ceased
- 1999-04-07 AU AU38133/99A patent/AU740318B2/en not_active Expired
- 1999-04-07 SI SI9930139T patent/SI1080086T1/xx unknown
- 1999-04-15 PE PE1999000309A patent/PE20000427A1/es not_active IP Right Cessation
- 1999-04-16 AR ARP990101779A patent/AR018187A1/es active IP Right Grant
- 1999-04-16 SV SV1999000047A patent/SV1999000047A/es active IP Right Grant
- 1999-04-16 TW TW088106067A patent/TW548274B/zh active
- 1999-04-16 CO CO99022937A patent/CO5021127A1/es unknown
- 1999-04-16 MY MYPI99001481A patent/MY126527A/en unknown
- 1999-04-16 GT GT199900056A patent/GT199900056A/es unknown
- 1999-07-04 UA UA2000116511A patent/UA63998C2/uk unknown
-
2000
- 2000-09-20 IL IL138584A patent/IL138584A/en not_active IP Right Cessation
- 2000-09-26 ZA ZA200005136A patent/ZA200005136B/xx unknown
- 2000-09-29 BG BG104812A patent/BG64649B1/bg unknown
- 2000-10-17 NO NO20005215A patent/NO321985B1/no not_active IP Right Cessation
-
2004
- 2004-02-17 US US10/781,075 patent/US20040167135A1/en not_active Abandoned
- 2004-12-01 NO NO20045259A patent/NO329020B1/no not_active IP Right Cessation
-
2006
- 2006-12-15 US US11/639,955 patent/US7514565B2/en not_active Expired - Fee Related
-
2010
- 2010-07-23 JP JP2010165860A patent/JP5237332B2/ja not_active Expired - Lifetime
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2002512243A5 (https=) | ||
| JP2005508967A5 (https=) | ||
| JP2007517044A5 (https=) | ||
| JP2010535722A5 (https=) | ||
| WO2002040486A3 (en) | METHODS OF TREATING p38 KINASE-ASSOCIATED CONDITIONS AND PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS | |
| JP2004533444A5 (https=) | ||
| JP2012528166A5 (https=) | ||
| JP2007534702A5 (https=) | ||
| JP2002502874A5 (https=) | ||
| JP2005535586A5 (https=) | ||
| JP2001526269A5 (https=) | ||
| JP2008525416A5 (https=) | ||
| JP2013507425A5 (https=) | ||
| JP2001525411A5 (https=) | ||
| JP2009533410A5 (https=) | ||
| NO20060220L (no) | Forbindelser med inhiberene aktivitet mot natriumavhengige transportorer | |
| JP2009536620A5 (https=) | ||
| AR049239A1 (es) | Compuestos heterociclicos inhibidores de la proteina kinasa (erk-2) y metodo de inhibicion | |
| JP2007534636A5 (https=) | ||
| JP2010530431A5 (https=) | ||
| JP2006514626A5 (https=) | ||
| JP2011505347A5 (https=) | ||
| JP2005502621A5 (https=) | ||
| JP2010501478A5 (https=) | ||
| JP2013542213A5 (https=) |