JP2002512243A5 - - Google Patents
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- 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
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- 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.)
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- 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 |
|---|---|---|---|
| DE19817264.8 | 1998-04-18 | ||
| DE19817264A DE19817264A1 (de) | 1998-04-18 | 1998-04-18 | Neue Dihydropyrimidine |
| 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 (enExample) | 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 |
| EP1193259A4 (en) | 1999-06-23 | 2003-01-29 | Ajinomoto Kk | dihydropyrimidine |
| WO2001045712A1 (de) * | 1999-12-22 | 2001-06-28 | Bayer Aktiengesellschaft | Arzneimittelkombinationen 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 |
| 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 |
| USRE45004E1 (en) * | 2007-06-18 | 2014-07-08 | Sunshine Lake Pharma Co., Ltd. | Bromo-phenyl substituted thiazolyl dihydropyrimidines |
| AR067630A1 (es) | 2007-07-12 | 2009-10-21 | Novartis Ag | Soluciones farmaceuticas de telbivudina y metodo de tratamiento |
| 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 |
| PL2888241T3 (pl) | 2012-08-24 | 2017-12-29 | Sunshine Lake Pharma Co., Ltd. | 2,4,5,6-Podstawione pochodne 3,6-dihydropirymidyny jako inhibitory polimerazy wirusa zapalenia wątroby typu B (HBV) do leczenia np. przewlekłego zapalenia wątroby |
| JP6113285B2 (ja) | 2012-09-10 | 2017-04-12 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｂ型肝炎ウイルス感染症の治療及び予防用の６−アミノ酸ヘテロアリールジヒドロピリミジン |
| 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 |
| EP2917184A4 (en) * | 2012-11-09 | 2016-06-29 | Univ Indiana Res & Tech Corp | ALTERNATIVE USES FOR HBV ARRANGEMENT EFFECTORS |
| TW201609652A (zh) * | 2013-11-12 | 2016-03-16 | 陶氏農業科學公司 | 用於氟化化合物之過程（三） |
| 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 |
| ES2688600T3 (es) | 2013-11-27 | 2018-11-05 | Sunshine Lake Pharma Co., Ltd. | Procesos para preparar derivados de dihidropirimidina e intermedios de los mismos |
| MY196243A (en) | 2014-03-28 | 2023-03-24 | Sunshine Lake Pharma Co Ltd | Dihydropyrimidine Compounds and Their Application In Pharmaceuticals |
| NZ727601A (en) | 2014-05-30 | 2022-01-28 | Qilu Pharmaceutical Co Ltd | Dihydropyrimido fused ring derivative as hbv inhibitor |
| 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 |
| AU2016214799A1 (en) | 2015-02-07 | 2017-06-15 | Sunshine Lake Pharma Co., Ltd. | Complexes and salts of dihydropyrimidine derivatives and their application in pharmaceuticals |
| WO2019001420A1 (en) * | 2017-06-27 | 2019-01-03 | Janssen Pharmaceutica Nv | HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING INFECTIONS WITH HEPATITIS B VIRUS |
| US10759774B2 (en) | 2017-09-28 | 2020-09-01 | The Curators Of The University Of Missouri | Inhibitors of hepatitis B virus targeting capsid assembly |
| GEP20227373B (en) | 2017-11-02 | 2022-04-25 | Aicuris Gmbh & Co Kg | Novel, highly active amino-thiazole substituted indole-2-carboxamides active against the hepatitis b virus (hbv) |
| CN111527087A (zh) | 2017-11-02 | 2020-08-11 | 艾库里斯有限及两合公司 | 具有抗乙型肝炎病毒(hbv)活性的新的高活性的吡唑并-哌啶取代的吲哚-2-甲酰胺 |
| EP3790866A4 (en) * | 2018-05-08 | 2022-03-02 | Janssen Sciences Ireland Unlimited Company | DIHYDROPYRIMIDINE DERIVATIVES AND THEIR USES IN THE TREATMENT OF HEPATITIS B VIRUS INFECTION OR HEPATITIS B VIRUS INDUCED DISEASES |
| 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) |
| UY38435A (es) | 2018-11-02 | 2020-05-29 | Aicuris Gmbh & Co Kg | Nuevas urea 6,7-dihidro-4h-pirazol[1,5-a] pirazinas activas contra el virus de la hepatitis b (vhb) |
| 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) |
| CA3118339A1 (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) |
| UY38434A (es) | 2018-11-02 | 2020-05-29 | Aicuris Gmbh & Co Kg | Nuevas 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activas contra el virus de la hepatitis b (hbv) |
| 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) |
| KR20210106421A (ko) | 2018-12-20 | 2021-08-30 | 얀센 파마슈티카 엔.브이. | 헤테로아릴디히드로피리미딘 유도체 및 b형 간염 감염의 치료 방법 |
| EP3962914A1 (en) | 2019-04-30 | 2022-03-09 | AiCuris GmbH & Co. KG | Novel indole-2-carboxamides active against the hepatitis b virus (hbv) |
| JP2022533007A (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インドリジン－２－カルボキサミド |
| BR112021021652A2 (pt) | 2019-04-30 | 2021-12-21 | Aicuris Gmbh & Co Kg | Oxalil piperazinas inovadoras ativas contra o vírus da hepatite b (hbv) |
| BR112021021580A2 (pt) | 2019-04-30 | 2022-01-04 | Aicuris Gmbh & Co Kg | Fenil e piridil ureias 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 (enExample) * | 1964-02-12 | |||
| CH550189A (de) | 1971-01-08 | 1974-06-14 | Ciba Geigy Ag | Verfahren zur herstellung von neuen dibenzo (b,f) thiepincarbonsaeuren. |
| CH569043A5 (enExample) | 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 |
| BR9713027A (pt) * | 1996-11-12 | 2000-01-25 | Novartis Ag | Derivados de pirazol úteis como herbicidas |
| 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 CA CA002328780A patent/CA2328780C/en not_active Expired - Lifetime
- 1999-04-07 ES ES99920603T patent/ES2183548T3/es not_active Expired - Lifetime
- 1999-04-07 BR BRPI9909730-3A patent/BR9909730B1/pt not_active IP Right Cessation
- 1999-04-07 SK SK1565-2000A patent/SK286407B6/sk not_active IP Right Cessation
- 1999-04-07 AU AU38133/99A patent/AU740318B2/en not_active Expired
- 1999-04-07 EP EP99920603A patent/EP1080086B1/de not_active Expired - Lifetime
- 1999-04-07 NZ NZ507569A patent/NZ507569A/en not_active IP Right Cessation
- 1999-04-07 HU HU0102372A patent/HUP0102372A3/hu unknown
- 1999-04-07 RU RU2000129148/04A patent/RU2245881C9/ru active
- 1999-04-07 DK DK99920603T patent/DK1080086T3/da active
- 1999-04-07 AT AT99920603T patent/ATE223401T1/de active
- 1999-04-07 BR BRPI9917862A patent/BRPI9917862B8/pt not_active IP Right Cessation
- 1999-04-07 JP JP2000544665A patent/JP4590097B2/ja not_active Expired - Lifetime
- 1999-04-07 CZ CZ20003871A patent/CZ293482B6/cs not_active IP Right Cessation
- 1999-04-07 PT PT99920603T patent/PT1080086E/pt unknown
- 1999-04-07 SI SI9930139T patent/SI1080086T1/xx unknown
- 1999-04-07 KR KR1020007011527A patent/KR100636771B1/ko not_active Expired - Lifetime
- 1999-04-07 US US09/673,592 patent/US6696451B1/en not_active Expired - Lifetime
- 1999-04-07 IL IL13858499A patent/IL138584A0/xx active IP Right Grant
- 1999-04-07 TR TR2000/03011T patent/TR200003011T2/xx unknown
- 1999-04-07 ID IDW20002111A patent/ID27263A/id unknown
- 1999-04-07 CU CU20000220A patent/CU23049A3/es unknown
- 1999-04-07 CN CNB998074950A patent/CN1159311C/zh not_active Expired - Lifetime
- 1999-04-07 DE DE59902573T patent/DE59902573D1/de not_active Expired - Lifetime
- 1999-04-07 WO PCT/EP1999/002344 patent/WO1999054326A1/de not_active Ceased
- 1999-04-07 PL PL99343481A patent/PL193898B1/pl unknown
- 1999-04-15 PE PE1999000309A patent/PE20000427A1/es not_active IP Right Cessation
- 1999-04-16 SV SV1999000047A patent/SV1999000047A/es active IP Right Grant
- 1999-04-16 CO CO99022937A patent/CO5021127A1/es unknown
- 1999-04-16 MY MYPI99001481A patent/MY126527A/en unknown
- 1999-04-16 TW TW088106067A patent/TW548274B/zh active
- 1999-04-16 AR ARP990101779A patent/AR018187A1/es active IP Right Grant
- 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