JP2005502644A5 - - Google Patents
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- Publication number
- JP2005502644A5 JP2005502644A5 JP2003518554A JP2003518554A JP2005502644A5 JP 2005502644 A5 JP2005502644 A5 JP 2005502644A5 JP 2003518554 A JP2003518554 A JP 2003518554A JP 2003518554 A JP2003518554 A JP 2003518554A JP 2005502644 A5 JP2005502644 A5 JP 2005502644A5
- Authority
- JP
- Japan
- Prior art keywords
- lower alkyl
- phenyl
- oxo
- benzo
- yloxy
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 112
- -1 di-substituted phenyl Chemical group 0.000 claims 61
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 58
- 229910052739 hydrogen Inorganic materials 0.000 claims 26
- 239000001257 hydrogen Substances 0.000 claims 26
- 229910052736 halogen Inorganic materials 0.000 claims 23
- 150000002367 halogens Chemical class 0.000 claims 23
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 125000003282 alkyl amino group Chemical group 0.000 claims 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 21
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 21
- 125000004414 alkyl thio group Chemical group 0.000 claims 19
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000004217 4-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])* 0.000 claims 7
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical group C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims 6
- 125000005530 alkylenedioxy group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- ZLFGTKRXAZLBRB-UHFFFAOYSA-N 1,2,4-thiadiazolidin-5-one Chemical compound O=C1NCNS1 ZLFGTKRXAZLBRB-UHFFFAOYSA-N 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000006507 2,4-difluorobenzyl group Chemical group [H]C1=C(F)C([H])=C(F)C(=C1[H])C([H])([H])* 0.000 claims 1
- 125000006508 2,6-difluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C(F)=C1[H])C([H])([H])* 0.000 claims 1
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims 1
- 125000000173 4-trifluoromethoxy benzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC(F)(F)F)C([H])([H])* 0.000 claims 1
- 125000001318 4-trifluoromethylbenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])*)C(F)(F)F 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 241000894006 Bacteria Species 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 206010011878 Deafness Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 241000790917 Dioxys <bee> Species 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010020880 Hypertrophy Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000001647 Renal Insufficiency Diseases 0.000 claims 1
- 206010038419 Renal colic Diseases 0.000 claims 1
- 206010063897 Renal ischaemia Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- 208000032851 Subarachnoid Hemorrhage Diseases 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 238000002399 angioplasty Methods 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 238000007675 cardiac surgery Methods 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 208000018631 connective tissue disease Diseases 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 208000000718 duodenal ulcer Diseases 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
- 230000010370 hearing loss Effects 0.000 claims 1
- 231100000888 hearing loss Toxicity 0.000 claims 1
- 208000016354 hearing loss disease Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 208000007232 portal hypertension Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000035939 shock Effects 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 125000006510 trifluorobenzyl group Chemical group 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 238000007631 vascular surgery Methods 0.000 claims 1
- 0 **C(C1(*)c2c(*)c(*)c(*)c(*)c2**1)N Chemical compound **C(C1(*)c2c(*)c(*)c(*)c(*)c2**1)N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0109235 | 2001-08-09 | ||
| PCT/EP2002/008523 WO2003013545A1 (en) | 2001-08-09 | 2002-07-31 | Novel benzo-fused heterocycles as endothelin antagonisits |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005502644A JP2005502644A (ja) | 2005-01-27 |
| JP2005502644A5 true JP2005502644A5 (enExample) | 2006-01-12 |
| JP4364637B2 JP4364637B2 (ja) | 2009-11-18 |
Family
ID=8164539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003518554A Expired - Fee Related JP4364637B2 (ja) | 2001-08-09 | 2002-07-31 | 新規なベンゾ縮合へテロ環化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7238685B2 (enExample) |
| JP (1) | JP4364637B2 (enExample) |
| KR (1) | KR100909122B1 (enExample) |
| CN (1) | CN100418955C (enExample) |
| AR (1) | AR036386A1 (enExample) |
| AU (1) | AU2002328999B8 (enExample) |
| BR (1) | BR0211729A (enExample) |
| CA (1) | CA2454417A1 (enExample) |
| HU (1) | HUP0401107A3 (enExample) |
| IL (1) | IL159963A0 (enExample) |
| MX (1) | MXPA04001252A (enExample) |
| NO (1) | NO20040563L (enExample) |
| NZ (1) | NZ530741A (enExample) |
| WO (1) | WO2003013545A1 (enExample) |
| ZA (1) | ZA200400803B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602005003951T4 (de) | 2004-05-14 | 2012-10-11 | Millennium Pharmaceuticals, Inc. | Verbindungen und verfahren zur inhibierung der mitotischen progression durch hemmung von aurorakinase |
| WO2008021038A2 (en) | 2006-08-09 | 2008-02-21 | Millennium Pharmaceuticals, Inc. | Pyridobenzazepine compounds and methods for inhibiting mitotic progression |
| CL2007003244A1 (es) | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| WO2008108445A1 (ja) | 2007-03-07 | 2008-09-12 | Takeda Pharmaceutical Company Limited | ベンゾオキサゼピン誘導体およびその用途 |
| MX2009011923A (es) * | 2007-05-10 | 2009-11-18 | Amr Technology Inc | Tetrahidrobenzo-1,4-diazepinas aril- y heteroaril-sustituidas y uso de las mismas para bloquear reabsorcion de norepinefrina, dopamina y serotonina. |
| AU2008265655B2 (en) | 2007-06-21 | 2014-02-06 | Cara Therapeutics, Inc. | Substituted imidazoheterocycles |
| US8119629B2 (en) | 2007-10-03 | 2012-02-21 | Bristol-Meyers Squibb Company | Carboxamide GABAA α2 modulators |
| WO2010068520A2 (en) * | 2008-12-11 | 2010-06-17 | Cara Therapeutics, Inc. | Substituted imidazoheterocycle derivatives |
| RU2535032C2 (ru) | 2008-12-22 | 2014-12-10 | Милленниум Фармасьютикалз, Инк. | Сочетание ингибиторов аврора киназы и анти-cd 20 антител |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| CN104031049A (zh) | 2010-02-19 | 2014-09-10 | 米伦纽姆医药公司 | 极光激酶抑制剂的结晶形式 |
| CN101805283B (zh) * | 2010-03-23 | 2013-01-02 | 渤海大学 | 含薁类结构的1,4-二氢吡啶类化合物及其制备方法 |
| US20130303519A1 (en) | 2012-03-20 | 2013-11-14 | Millennium Pharmaceuticals, Inc. | Methods of treating cancer using aurora kinase inhibitors |
| JP6360881B2 (ja) | 2013-03-22 | 2018-07-18 | ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. | 触媒的mtorc1/2阻害薬及びオーロラaキナーゼの選択的阻害薬の組合せ |
| US20180207173A1 (en) | 2015-07-21 | 2018-07-26 | Millennium Pharmaceuticals, Inc. | Administration of aurora kinase inhibitor and chemotherapeutic agents |
| CN112939855B (zh) * | 2021-02-08 | 2024-03-26 | 马鞍山市泰博化工科技有限公司 | 一种制备含有薁环结构的1,4-二氢吡啶衍生物的方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5614498A (en) * | 1990-06-07 | 1997-03-25 | Banyu Pharmaceutical Co., Ltd. | Endothelin antagonistic substance |
| US5420123A (en) * | 1992-12-21 | 1995-05-30 | Bristol-Myers Squibb Company | Dibenzodiazepine endothelin antagonists |
| KR100340145B1 (ko) * | 1993-08-26 | 2002-10-18 | 야마노우치세이야쿠 가부시키가이샤 | 벤즈아제핀유도체및이의중간체화합물 |
| JP2000143636A (ja) * | 1998-09-02 | 2000-05-26 | Sumitomo Pharmaceut Co Ltd | アミノ誘導体 |
-
2002
- 2002-07-31 HU HU0401107A patent/HUP0401107A3/hu unknown
- 2002-07-31 JP JP2003518554A patent/JP4364637B2/ja not_active Expired - Fee Related
- 2002-07-31 IL IL15996302A patent/IL159963A0/xx unknown
- 2002-07-31 MX MXPA04001252A patent/MXPA04001252A/es active IP Right Grant
- 2002-07-31 CA CA002454417A patent/CA2454417A1/en not_active Abandoned
- 2002-07-31 BR BR0211729-0A patent/BR0211729A/pt not_active IP Right Cessation
- 2002-07-31 CN CNB028155394A patent/CN100418955C/zh not_active Expired - Fee Related
- 2002-07-31 KR KR1020047001815A patent/KR100909122B1/ko not_active Expired - Fee Related
- 2002-07-31 NZ NZ530741A patent/NZ530741A/en not_active IP Right Cessation
- 2002-07-31 AU AU2002328999A patent/AU2002328999B8/en not_active Ceased
- 2002-07-31 WO PCT/EP2002/008523 patent/WO2003013545A1/en not_active Ceased
- 2002-07-31 US US10/486,602 patent/US7238685B2/en not_active Expired - Fee Related
- 2002-08-06 AR ARP020102979A patent/AR036386A1/es unknown
-
2004
- 2004-01-30 ZA ZA200400803A patent/ZA200400803B/xx unknown
- 2004-02-06 NO NO20040563A patent/NO20040563L/no not_active Application Discontinuation
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