JP2006522824A5 - - Google Patents
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- Publication number
- JP2006522824A5 JP2006522824A5 JP2006509889A JP2006509889A JP2006522824A5 JP 2006522824 A5 JP2006522824 A5 JP 2006522824A5 JP 2006509889 A JP2006509889 A JP 2006509889A JP 2006509889 A JP2006509889 A JP 2006509889A JP 2006522824 A5 JP2006522824 A5 JP 2006522824A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- hydrogen
- aliphatic
- ring
- halo
- 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
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- 125000001931 aliphatic group Chemical group 0.000 claims 72
- 229910052739 hydrogen Inorganic materials 0.000 claims 61
- 239000001257 hydrogen Substances 0.000 claims 61
- 125000005843 halogen group Chemical group 0.000 claims 34
- 150000002431 hydrogen Chemical class 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 30
- 125000000623 heterocyclic group Chemical group 0.000 claims 30
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 14
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 13
- 125000003277 amino group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 125000004043 oxo group Chemical group O=* 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- 125000002947 alkylene group Chemical group 0.000 claims 6
- -1 —OR 7 Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000003275 alpha amino acid group Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 125000006244 carboxylic acid protecting group Chemical group 0.000 claims 1
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 208000026037 malignant tumor of neck Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000000010 osteolytic effect Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 CC(CC1OC1NC(CC(Cl)=C1)c2c1c1ccncc1[n]2)COC(C)(C)CNC=*NC(c1c(C)ncnc1)=O Chemical compound CC(CC1OC1NC(CC(Cl)=C1)c2c1c1ccncc1[n]2)COC(C)(C)CNC=*NC(c1c(C)ncnc1)=O 0.000 description 10
- UUUSROHBEMVRKP-UHFFFAOYSA-N C(C1NCCC1)N1CCOCC1 Chemical compound C(C1NCCC1)N1CCOCC1 UUUSROHBEMVRKP-UHFFFAOYSA-N 0.000 description 1
- FYEGYIJPAZUCQZ-UHFFFAOYSA-N CC1(C)OCC(C(Nc2cc(Cl)cc3c2[nH]c2cnccc32)=O)N(CCNC(c2c(C)nccc2)=O)C1 Chemical compound CC1(C)OCC(C(Nc2cc(Cl)cc3c2[nH]c2cnccc32)=O)N(CCNC(c2c(C)nccc2)=O)C1 FYEGYIJPAZUCQZ-UHFFFAOYSA-N 0.000 description 1
- KUBIRPSTEODLSB-UHFFFAOYSA-N CCSc(c(Cl)cc1c2[nH]c3cnccc13)c2NC(c1cccnc1C)=O Chemical compound CCSc(c(Cl)cc1c2[nH]c3cnccc13)c2NC(c1cccnc1C)=O KUBIRPSTEODLSB-UHFFFAOYSA-N 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- SHCAWLTYOZRESG-UHFFFAOYSA-N CNCCN(CC(C1)C(Nc(c2c(cc3Cl)c4ccncc4[nH]2)c3OC)=O)C1=O Chemical compound CNCCN(CC(C1)C(Nc(c2c(cc3Cl)c4ccncc4[nH]2)c3OC)=O)C1=O SHCAWLTYOZRESG-UHFFFAOYSA-N 0.000 description 1
- RIGIDEOYCAEKHN-UHFFFAOYSA-N CNCCN(CC(C1)C(Nc2cc(Cl)cc3c2[nH]c2cnccc32)=O)C1=O Chemical compound CNCCN(CC(C1)C(Nc2cc(Cl)cc3c2[nH]c2cnccc32)=O)C1=O RIGIDEOYCAEKHN-UHFFFAOYSA-N 0.000 description 1
- ILCVYWBYVFZKLQ-UHFFFAOYSA-N Cc(nccc1)c1C(Nc(c1c(cc2Cl)c3ccncc3[nH]1)c2F)=O Chemical compound Cc(nccc1)c1C(Nc(c1c(cc2Cl)c3ccncc3[nH]1)c2F)=O ILCVYWBYVFZKLQ-UHFFFAOYSA-N 0.000 description 1
- ATXHUFABJPSLOJ-UHFFFAOYSA-N Cc1ncccc1C(Nc(c1c(cc2Cl)c3ccncc3[nH]1)c2SC)=O Chemical compound Cc1ncccc1C(Nc(c1c(cc2Cl)c3ccncc3[nH]1)c2SC)=O ATXHUFABJPSLOJ-UHFFFAOYSA-N 0.000 description 1
- AHXUFMIHZXMEGF-JTDNENJMSA-N NC(CCC1)[C@@H]1C(Nc1cc(Cl)cc2c1[nH]c1cnccc21)=O Chemical compound NC(CCC1)[C@@H]1C(Nc1cc(Cl)cc2c1[nH]c1cnccc21)=O AHXUFMIHZXMEGF-JTDNENJMSA-N 0.000 description 1
- HHZQETZZACUFHE-UHFFFAOYSA-N Nc1cc(Cl)cc2c1[nH]c1cnccc21 Chemical compound Nc1cc(Cl)cc2c1[nH]c1cnccc21 HHZQETZZACUFHE-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46146803P | 2003-04-09 | 2003-04-09 | |
| PCT/US2004/011080 WO2004092167A1 (en) | 2003-04-09 | 2004-04-09 | Beta-carbolines useful for treating inflammatory disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006522824A JP2006522824A (ja) | 2006-10-05 |
| JP2006522824A5 true JP2006522824A5 (https=) | 2007-05-31 |
Family
ID=33299818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006509889A Pending JP2006522824A (ja) | 2003-04-09 | 2004-04-09 | 炎症性疾患を処置するために有用なβ−カルボリン |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US7727985B2 (https=) |
| EP (1) | EP1611134A1 (https=) |
| JP (1) | JP2006522824A (https=) |
| KR (1) | KR20060006031A (https=) |
| CN (1) | CN1802375A (https=) |
| AU (1) | AU2004230952A1 (https=) |
| BR (1) | BRPI0409263A (https=) |
| CA (1) | CA2521300A1 (https=) |
| CO (1) | CO5700746A2 (https=) |
| CR (1) | CR8042A (https=) |
| EA (1) | EA009121B1 (https=) |
| EC (1) | ECSP056145A (https=) |
| HR (1) | HRP20050926A2 (https=) |
| MA (1) | MA27837A1 (https=) |
| MX (1) | MXPA05010793A (https=) |
| NI (1) | NI200500174A (https=) |
| NO (1) | NO20054598L (https=) |
| OA (1) | OA13115A (https=) |
| RS (1) | RS20050832A (https=) |
| TN (1) | TNSN05257A1 (https=) |
| WO (1) | WO2004092167A1 (https=) |
| ZA (1) | ZA200508198B (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0409263A (pt) | 2003-04-09 | 2006-03-28 | Millennium Pharm Inc | composto; composição farmacêutica; método para tratar uma doença mediada por ikk e método para inibir ikk em um paciente que dele necessita |
| BRPI0509660A (pt) * | 2004-04-09 | 2007-10-09 | Millennium Pharm Inc | compostos de beta-carbolina de utilidade no tratamento de doenças inflamatórias |
| US8119655B2 (en) * | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| JP5249772B2 (ja) * | 2005-11-22 | 2013-07-31 | メルク・シャープ・アンド・ドーム・コーポレーション | キナーゼの阻害剤として有用な三環式化合物 |
| EP2001455A2 (en) | 2006-03-15 | 2008-12-17 | Theralogics, Inc. | Methods of treating muscular wasting diseases using nf-kb activation inhibitors |
| WO2008002246A1 (en) * | 2006-06-28 | 2008-01-03 | Astrazeneca Ab | A pharmaceutical composition comprising an ikk2 inhibitor and a second active ingrdient. |
| EP2125841A1 (en) * | 2006-12-13 | 2009-12-02 | Gilead Sciences, Inc. | Monophosphates as mutual prodrugs of anti-inflammatory signal transduction modulators (aistm's) and beta-agonists for the treatment of pulmonary inflammation and bronchoconstriction |
| US20090131422A1 (en) * | 2007-10-23 | 2009-05-21 | Millennium Pharmaceuticals, Inc. | Salts of an IKK inhibitor |
| US20090137579A1 (en) * | 2007-10-23 | 2009-05-28 | Millennium Pharmaceuticals, Inc. | Mesylate salt of an IKK inhibitor |
| US20110111417A1 (en) | 2008-05-14 | 2011-05-12 | Millennium Pharmaceuticals, Inc. | Methods and kits for monitoring the effects of immunomodulators on adaptive immunity |
| EP2366699B1 (en) | 2008-10-02 | 2013-08-07 | Asahi Kasei Pharma Corporation | 8-substituted isoquinoline derivative and use thereof |
| KR101461767B1 (ko) | 2010-03-30 | 2014-11-13 | 노파르티스 아게 | 만성 활성 ｂ-세포-수용체 신호전달이 있는 ｂ-세포 림프종의 치료를 위한 ｐｋｃ 억제제 |
| CN103596949A (zh) * | 2011-03-28 | 2014-02-19 | Sjt分子研究有限公司 | 用于代谢综合征的治疗的化合物 |
| CN102416014B (zh) * | 2011-09-13 | 2012-11-21 | 河南中医学院 | 一种生物碱类成分组合物在制备抗甲型h1n1流感病毒药物中的应用 |
| CN102391323B (zh) * | 2011-10-18 | 2013-09-25 | 首都医科大学 | 四氢-β-咔啉衍生物、其制备方法及其用途 |
| KR101646916B1 (ko) | 2015-07-13 | 2016-08-09 | 강원대학교산학협력단 | 베타-카르볼린 알칼로이드 화합물을 함유하는 염증성 질환의 예방 또는 치료용 조성물 |
| WO2017067670A1 (en) | 2015-10-23 | 2017-04-27 | Pharmathen S.A. | A novel process for the preparation of tryptamines and derivatives thereof |
| CN109593089B (zh) * | 2019-01-24 | 2022-01-28 | 西南大学 | 二氮杂螺癸烷哌啶甲酰胺类化合物制备和应用 |
| CN112824387B (zh) * | 2019-11-21 | 2023-03-21 | 济南尚博生物科技有限公司 | 一种2-甲基烟酸酯及其制备方法和应用 |
| CN117510494B (zh) * | 2023-11-07 | 2024-04-19 | 桂林医学院附属医院 | β-咔啉-沙利度胺偶联物及其在制备逆转ABT-199耐药的药物中的应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2242402T3 (es) * | 1998-08-12 | 2005-11-01 | Pfizer Products Inc. | Inhibidores de tace. |
| DE19951360A1 (de) * | 1999-10-26 | 2001-05-03 | Aventis Pharma Gmbh | Substituierte Indole |
| HK1054039B (zh) * | 2000-03-15 | 2010-04-16 | 萨诺费－阿文蒂斯德国有限公司 | 取代的β-咔啉 |
| EP1268477B1 (en) * | 2000-03-15 | 2010-04-21 | Sanofi-Aventis Deutschland GmbH | Substituted beta-carbolines with ikb-kinase inhibiting activity |
| ATE363473T1 (de) * | 2001-09-19 | 2007-06-15 | Pharmacia Corp | Substituierte pyrazoloverbindungen zur behandlung von entzündungen |
| US9248124B2 (en) * | 2001-11-07 | 2016-02-02 | Millennium Pharmaceuticals, Inc. | Use of inhibitors of IκB kinase for the treatment of cancer |
| US7396943B2 (en) * | 2003-03-07 | 2008-07-08 | Eli Lilly And Company | Opioid receptor antagonists |
| BRPI0409263A (pt) | 2003-04-09 | 2006-03-28 | Millennium Pharm Inc | composto; composição farmacêutica; método para tratar uma doença mediada por ikk e método para inibir ikk em um paciente que dele necessita |
-
2004
- 2004-04-09 BR BRPI0409263-5A patent/BRPI0409263A/pt not_active IP Right Cessation
- 2004-04-09 WO PCT/US2004/011080 patent/WO2004092167A1/en not_active Ceased
- 2004-04-09 CA CA002521300A patent/CA2521300A1/en not_active Abandoned
- 2004-04-09 MX MXPA05010793A patent/MXPA05010793A/es active IP Right Grant
- 2004-04-09 EA EA200501584A patent/EA009121B1/ru not_active IP Right Cessation
- 2004-04-09 JP JP2006509889A patent/JP2006522824A/ja active Pending
- 2004-04-09 OA OA1200500279A patent/OA13115A/en unknown
- 2004-04-09 CN CNA2004800160170A patent/CN1802375A/zh active Pending
- 2004-04-09 RS YUP-2005/0832A patent/RS20050832A/sr unknown
- 2004-04-09 HR HR20050926A patent/HRP20050926A2/hr not_active Application Discontinuation
- 2004-04-09 US US10/821,545 patent/US7727985B2/en not_active Expired - Lifetime
- 2004-04-09 AU AU2004230952A patent/AU2004230952A1/en not_active Abandoned
- 2004-04-09 EP EP04759390A patent/EP1611134A1/en not_active Withdrawn
- 2004-04-09 KR KR1020057019268A patent/KR20060006031A/ko not_active Ceased
-
2005
- 2005-10-06 NO NO20054598A patent/NO20054598L/no not_active Application Discontinuation
- 2005-10-07 NI NI200500174A patent/NI200500174A/es unknown
- 2005-10-07 TN TNP2005000257A patent/TNSN05257A1/en unknown
- 2005-10-11 ZA ZA200508198A patent/ZA200508198B/xx unknown
- 2005-10-12 CR CR8042A patent/CR8042A/es not_active Application Discontinuation
- 2005-11-04 CO CO05113041A patent/CO5700746A2/es not_active Application Discontinuation
- 2005-11-07 EC EC2005006145A patent/ECSP056145A/es unknown
- 2005-11-09 MA MA28592A patent/MA27837A1/fr unknown
-
2009
- 2009-12-17 US US12/640,335 patent/US20100093713A1/en not_active Abandoned
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