JP2006528941A5 - - Google Patents
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- Publication number
- JP2006528941A5 JP2006528941A5 JP2006529741A JP2006529741A JP2006528941A5 JP 2006528941 A5 JP2006528941 A5 JP 2006528941A5 JP 2006529741 A JP2006529741 A JP 2006529741A JP 2006529741 A JP2006529741 A JP 2006529741A JP 2006528941 A5 JP2006528941 A5 JP 2006528941A5
- Authority
- JP
- Japan
- Prior art keywords
- oxadiazolyl
- triazolyl
- isoxazol
- thiophen
- ylmethyl
- 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 claims 2
- MUXSXTKRNCHFTL-UHFFFAOYSA-N 1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-5-phenyl-n-(1-propan-2-ylpiperidin-4-yl)-1,2,4-triazole-3-carboxamide Chemical compound C1CN(C(C)C)CCC1NC(=O)C1=NN(CC2=NOC(=C2)C=2SC(Cl)=CC=2)C(C=2C=CC=CC=2)=N1 MUXSXTKRNCHFTL-UHFFFAOYSA-N 0.000 claims 1
- YHVLHKDYUITXNE-UHFFFAOYSA-N 1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-n-(1-propan-2-ylpiperidin-4-yl)-5-pyridin-2-yl-1,2,4-triazole-3-carboxamide Chemical compound C1CN(C(C)C)CCC1NC(=O)C1=NN(CC2=NOC(=C2)C=2SC(Cl)=CC=2)C(C=2N=CC=CC=2)=N1 YHVLHKDYUITXNE-UHFFFAOYSA-N 0.000 claims 1
- XBTSMICULXRDAG-UHFFFAOYSA-N 1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-n-(1-propan-2-ylpiperidin-4-yl)-5-pyrrol-1-yl-1,2,4-triazole-3-carboxamide Chemical compound C1CN(C(C)C)CCC1NC(=O)C1=NN(CC2=NOC(=C2)C=2SC(Cl)=CC=2)C(N2C=CC=C2)=N1 XBTSMICULXRDAG-UHFFFAOYSA-N 0.000 claims 1
- KUICBYXMOLTTPZ-UHFFFAOYSA-N 2-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-n-(1-propan-2-ylpiperidin-4-yl)-5-pyridin-2-yl-1,2,4-triazole-3-carboxamide Chemical compound C1CN(C(C)C)CCC1NC(=O)C1=NC(C=2N=CC=CC=2)=NN1CC1=NOC(C=2SC(Cl)=CC=2)=C1 KUICBYXMOLTTPZ-UHFFFAOYSA-N 0.000 claims 1
- KGFWAMSYIURHEM-UHFFFAOYSA-N 2-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-n-(1-propan-2-ylpiperidin-4-yl)tetrazole-5-carboxamide Chemical compound C1CN(C(C)C)CCC1NC(=O)C1=NN(CC2=NOC(=C2)C=2SC(Cl)=CC=2)N=N1 KGFWAMSYIURHEM-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- -1 azaspirodecanyl Chemical group 0.000 description 86
- 125000001544 thienyl group Chemical group 0.000 description 6
- 125000002053 thietanyl group Chemical group 0.000 description 6
- 125000000623 heterocyclic group Chemical group 0.000 description 5
- 125000004628 isothiazolidinyl group Chemical group S1N(CCC1)* 0.000 description 5
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 5
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 4
- 125000000842 isoxazolyl group Chemical group 0.000 description 4
- 125000004076 pyridyl group Chemical group 0.000 description 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 4
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 4
- 125000004502 1,2,3-oxadiazolyl group Chemical group 0.000 description 3
- 125000004511 1,2,3-thiadiazolyl group Chemical group 0.000 description 3
- 125000004529 1,2,3-triazinyl group Chemical group N1=NN=C(C=C1)* 0.000 description 3
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 description 3
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 description 3
- 125000004514 1,2,4-thiadiazolyl group Chemical group 0.000 description 3
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 description 3
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 description 3
- 125000004517 1,2,5-thiadiazolyl group Chemical group 0.000 description 3
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 description 3
- 125000004520 1,3,4-thiadiazolyl group Chemical group 0.000 description 3
- JPRPJUMQRZTTED-UHFFFAOYSA-N 1,3-dioxolanyl Chemical group [CH]1OCCO1 JPRPJUMQRZTTED-UHFFFAOYSA-N 0.000 description 3
- 125000000164 1,3-thiazinyl group Chemical group S1C(N=CC=C1)* 0.000 description 3
- 125000005962 1,4-oxazepanyl group Chemical group 0.000 description 3
- 125000000183 1,4-thiazinyl group Chemical group S1C(C=NC=C1)* 0.000 description 3
- 125000005955 1H-indazolyl group Chemical group 0.000 description 3
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 description 3
- 125000005602 azabenzimidazolyl group Chemical group 0.000 description 3
- 125000002785 azepinyl group Chemical group 0.000 description 3
- 125000002393 azetidinyl group Chemical group 0.000 description 3
- 125000004069 aziridinyl group Chemical group 0.000 description 3
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 3
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 description 3
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 description 3
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 description 3
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 3
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 description 3
- 125000004623 carbolinyl group Chemical group 0.000 description 3
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 description 3
- 125000004230 chromenyl group Chemical group O1C(C=CC2=CC=CC=C12)* 0.000 description 3
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 description 3
- 125000004856 decahydroquinolinyl group Chemical group N1(CCCC2CCCCC12)* 0.000 description 3
- 125000003838 furazanyl group Chemical group 0.000 description 3
- 125000002632 imidazolidinyl group Chemical group 0.000 description 3
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 description 3
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 description 3
- 125000001041 indolyl group Chemical group 0.000 description 3
- 125000001977 isobenzofuranyl group Chemical group C=1(OC=C2C=CC=CC12)* 0.000 description 3
- 125000003384 isochromanyl group Chemical group C1(OCCC2=CC=CC=C12)* 0.000 description 3
- 125000005438 isoindazolyl group Chemical group 0.000 description 3
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 description 3
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 description 3
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 description 3
- 125000001786 isothiazolyl group Chemical group 0.000 description 3
- 125000002757 morpholinyl group Chemical group 0.000 description 3
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 description 3
- 125000004930 octahydroisoquinolinyl group Chemical group C1(NCCC2CCCC=C12)* 0.000 description 3
- 125000001715 oxadiazolyl group Chemical group 0.000 description 3
- 125000000160 oxazolidinyl group Chemical group 0.000 description 3
- 125000005968 oxazolinyl group Chemical group 0.000 description 3
- 125000002971 oxazolyl group Chemical group 0.000 description 3
- 125000004934 phenanthridinyl group Chemical group C1(=CC=CC2=NC=C3C=CC=CC3=C12)* 0.000 description 3
- 125000004625 phenanthrolinyl group Chemical group N1=C(C=CC2=CC=C3C=CC=NC3=C12)* 0.000 description 3
- 125000001791 phenazinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3N=C12)* 0.000 description 3
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 description 3
- 125000004932 phenoxathinyl group Chemical group 0.000 description 3
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 description 3
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 3
- 125000004193 piperazinyl group Chemical group 0.000 description 3
- 125000003386 piperidinyl group Chemical group 0.000 description 3
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 description 3
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 description 3
- 125000003373 pyrazinyl group Chemical group 0.000 description 3
- 125000003072 pyrazolidinyl group Chemical group 0.000 description 3
- 125000002755 pyrazolinyl group Chemical group 0.000 description 3
- 125000003226 pyrazolyl group Chemical group 0.000 description 3
- 125000002098 pyridazinyl group Chemical group 0.000 description 3
- 125000000714 pyrimidinyl group Chemical group 0.000 description 3
- 125000001422 pyrrolinyl group Chemical group 0.000 description 3
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 3
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 description 3
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 3
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 description 3
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 description 3
- 125000001984 thiazolidinyl group Chemical group 0.000 description 3
- 125000002769 thiazolinyl group Chemical group 0.000 description 3
- 125000000335 thiazolyl group Chemical group 0.000 description 3
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 3
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 3
- 125000004604 benzisothiazolyl group Chemical group S1N=C(C2=C1C=CC=C2)* 0.000 description 2
- 125000002541 furyl group Chemical group 0.000 description 2
- 125000002636 imidazolinyl group Chemical group 0.000 description 2
- 125000002883 imidazolyl group Chemical group 0.000 description 2
- 125000005969 isothiazolinyl group Chemical group 0.000 description 2
- 125000003965 isoxazolidinyl group Chemical group 0.000 description 2
- 125000003971 isoxazolinyl group Chemical group 0.000 description 2
- 125000000168 pyrrolyl group Chemical group 0.000 description 2
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 2
- 125000001425 triazolyl group Chemical group 0.000 description 2
- 125000004530 1,2,4-triazinyl group Chemical group N1=NC(=NC=C1)* 0.000 description 1
- 125000003363 1,3,5-triazinyl group Chemical group N1=C(N=CN=C1)* 0.000 description 1
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical compound C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 description 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 description 1
- XWIYUCRMWCHYJR-UHFFFAOYSA-N 1h-pyrrolo[3,2-b]pyridine Chemical compound C1=CC=C2NC=CC2=N1 XWIYUCRMWCHYJR-UHFFFAOYSA-N 0.000 description 1
- 125000005428 anthryl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C3C(*)=C([H])C([H])=C([H])C3=C([H])C2=C1[H] 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03011309A EP1479679A1 (en) | 2003-05-19 | 2003-05-19 | Triazole-derivatives as factor Xa inhibitors |
| PCT/EP2004/004752 WO2004101555A1 (en) | 2003-05-19 | 2004-05-05 | TRIAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006528941A JP2006528941A (ja) | 2006-12-28 |
| JP2006528941A5 true JP2006528941A5 (https=) | 2007-06-21 |
| JP4608495B2 JP4608495B2 (ja) | 2011-01-12 |
Family
ID=33040956
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006529741A Expired - Fee Related JP4608495B2 (ja) | 2003-05-19 | 2004-05-05 | 第Ｘａ因子阻害剤としてのトリアゾール誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| EP (2) | EP1479679A1 (https=) |
| JP (1) | JP4608495B2 (https=) |
| AT (1) | ATE394396T1 (https=) |
| AU (1) | AU2004238498B2 (https=) |
| BR (1) | BRPI0410763A (https=) |
| CA (1) | CA2526082C (https=) |
| DE (1) | DE602004013577D1 (https=) |
| IL (1) | IL171843A (https=) |
| MX (1) | MXPA05012058A (https=) |
| PE (1) | PE20050154A1 (https=) |
| TW (1) | TW200503694A (https=) |
| WO (1) | WO2004101555A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7453002B2 (en) | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered heterocycles useful as serine protease inhibitors |
| NZ571441A (en) * | 2006-03-24 | 2010-08-27 | Eisai R&D Man Co Ltd | Triazolone derivative |
| HRP20151052T1 (xx) * | 2007-07-19 | 2015-11-06 | H. Lundbeck A/S | Peteroäślani heterocikliäśki amidi i srodne tvari |
| JPWO2009038157A1 (ja) | 2007-09-21 | 2011-01-06 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ２，３−ジヒドロ−イミノイソインドール誘導体 |
| CN102918034B (zh) | 2010-03-30 | 2015-06-03 | 维颂公司 | 多取代芳族化合物作为凝血酶的抑制剂 |
| LT2968297T (lt) | 2013-03-15 | 2019-01-10 | Verseon Corporation | Multipakeistieji aromatiniai junginiai kaip serino proteazės inhibitoriai |
| ES2791749T3 (es) * | 2013-03-15 | 2020-11-05 | Verseon Corp | Halogenopirazoles como inhibidores de la trombina |
| EA033168B1 (ru) | 2013-03-15 | 2019-09-30 | Сайклерион Терапьютикс, Инк. | СТИМУЛЯТОРЫ sGC |
| CN106687445A (zh) | 2014-09-17 | 2017-05-17 | 维颂公司 | 作为丝氨酸蛋白酶抑制剂的吡唑基取代的吡啶酮化合物 |
| RU2017131562A (ru) | 2015-02-27 | 2019-03-27 | Версеон Корпорейшн | Замещенные пиразольные соединения как ингибиторы сериновых протеаз |
| US11724997B2 (en) | 2018-03-01 | 2023-08-15 | Annapurna Bio, Inc. | Compounds and compositions for treating conditions associated with APJ receptor activity |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6020357A (en) * | 1996-12-23 | 2000-02-01 | Dupont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
| US5998424A (en) * | 1997-06-19 | 1999-12-07 | Dupont Pharmaceuticals Company | Inhibitors of factor Xa with a neutral P1 specificity group |
| US6339099B1 (en) * | 1997-06-20 | 2002-01-15 | Dupont Pharmaceuticals Company | Guanidine mimics as factor Xa inhibitors |
| EP1042299A1 (en) * | 1997-12-22 | 2000-10-11 | Du Pont Pharmaceuticals Company | Nitrogen containing heteroaromatics with ortho-substituted p1's as factor xa inhibitors |
| US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| EP1226123A1 (en) * | 1999-11-03 | 2002-07-31 | Du Pont Pharmaceuticals Company | Cyano compounds as factor xa inhibitors |
| AU2001273040A1 (en) * | 2000-06-27 | 2002-01-08 | Du Pont Pharmaceuticals Company | Factor xa inhibitors |
-
2003
- 2003-05-19 EP EP03011309A patent/EP1479679A1/en not_active Withdrawn
-
2004
- 2004-05-05 BR BRPI0410763-2A patent/BRPI0410763A/pt not_active IP Right Cessation
- 2004-05-05 MX MXPA05012058A patent/MXPA05012058A/es active IP Right Grant
- 2004-05-05 WO PCT/EP2004/004752 patent/WO2004101555A1/en not_active Ceased
- 2004-05-05 CA CA2526082A patent/CA2526082C/en not_active Expired - Fee Related
- 2004-05-05 AU AU2004238498A patent/AU2004238498B2/en not_active Ceased
- 2004-05-05 DE DE602004013577T patent/DE602004013577D1/de not_active Expired - Lifetime
- 2004-05-05 AT AT04731152T patent/ATE394396T1/de not_active IP Right Cessation
- 2004-05-05 JP JP2006529741A patent/JP4608495B2/ja not_active Expired - Fee Related
- 2004-05-05 EP EP04731152A patent/EP1628971B1/en not_active Expired - Lifetime
- 2004-05-11 PE PE2004000482A patent/PE20050154A1/es not_active Application Discontinuation
- 2004-05-17 TW TW093113794A patent/TW200503694A/zh unknown
-
2005
- 2005-11-08 IL IL171843A patent/IL171843A/en not_active IP Right Cessation
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