PE20020500A1 - Derivados de piperidina, tetrahidroquinolina, tetrahidroisoquinolina como inhibidores de caspasas - Google Patents
Derivados de piperidina, tetrahidroquinolina, tetrahidroisoquinolina como inhibidores de caspasasInfo
- Publication number
- PE20020500A1 PE20020500A1 PE2001000916A PE2001000916A PE20020500A1 PE 20020500 A1 PE20020500 A1 PE 20020500A1 PE 2001000916 A PE2001000916 A PE 2001000916A PE 2001000916 A PE2001000916 A PE 2001000916A PE 20020500 A1 PE20020500 A1 PE 20020500A1
- Authority
- PE
- Peru
- Prior art keywords
- piperidine
- carbonyl
- tetrahydroquinoline
- tetrahydroisoquinoline
- derivatives
- Prior art date
Links
- UWYZHKAOTLEWKK-UHFFFAOYSA-N 1,2,3,4-tetrahydroisoquinoline Chemical compound C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 title abstract 6
- LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 title abstract 6
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical class C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 208000001840 Dandruff Diseases 0.000 title 1
- -1 2-CHLOROPHENOTHIAZINE-10-CARBONYL Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 230000006907 apoptotic process Effects 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 208000035196 congenital hypomyelinating 2 neuropathy Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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Abstract
SE REFIERE A DERIVADOS DE PIPERIDINA, TETRAHIDROQUINOLINA, TETRAHIDROISOQUINOLINA DE FORMULA I DONDE A ES UN ANILLO DE PIPERIDINA, TETRAHIDROQUINOLINA O TETRAHIDROISOQUINOLINA; R1 ES H, CN, CHN2, R, CH2Y; R ES UN GRUPO ALIFATICO, ARILO, ARALQUILO; Y ES UN GRUPO SALIENTE ELECTRONEGATIVO; R2 ES CO2H, CH2CO2H, ESTERES, AMIDAS, ISOSTERES; R3 ES H, ARILO, ARALQUILO, UN GRUPO ALIFATICO C1-C6; R4 ES ARILO, HETEROCICLILO; R3 Y R4 JUNTO A N FORMAN UN ANILLO MONOCICLICLO, BICICLICO, TRICICLICO. SON COMPUESTOS PREFERIDOS [3S/R,(2S)]-3-{[1-(2-CLOROFENOTIAZINA-10-CARBONIL)PIPERIDINA-2-CARBONIL]AMINO}-4-FLUORO-4-OXO-ACIDO PENTANOICO, [3S/R,(2S)]-3-{[1-(3-CLOROFENOTIAZINA-10-CARBONIL)PIPERIDINA-2-CARBONIL]AMINO}-4-FLUORO-4-OXO-ACIDO PENTANOICO, [3S/R,(2S)]-3-{[1-(3,4-DICLOROFENOTIAZINA-10-CARBONIL)PIPERIDINA-2-CARBONIL]AMINO}-4-FLUORO-4-OXO-ACIDO PENTANOICO, ENTRE OTROS. LOS COMPUESTOS MENCIONADOS SON INHIBIDORES DE LA ACTIVIDAD DE LAS CASPASAS E INTERVIENEN EN LA APOPTOSIS CELULAR E INFLAMACION
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23257300P | 2000-09-13 | 2000-09-13 |
Publications (1)
| Publication Number | Publication Date |
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| PE20020500A1 true PE20020500A1 (es) | 2002-06-25 |
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| PE2001000916A PE20020500A1 (es) | 2000-09-13 | 2001-09-12 | Derivados de piperidina, tetrahidroquinolina, tetrahidroisoquinolina como inhibidores de caspasas |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US6800619B2 (es) |
| EP (1) | EP1317454B1 (es) |
| JP (2) | JP2004509120A (es) |
| AT (1) | ATE510837T1 (es) |
| AU (1) | AU2001290795A1 (es) |
| CA (1) | CA2418720A1 (es) |
| PE (1) | PE20020500A1 (es) |
| WO (1) | WO2002022611A2 (es) |
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| FR2815541B1 (fr) * | 2000-10-24 | 2008-02-29 | Lipha | Utilisation d'inhibiteurs de l'apoptose des pericytes pour le traitement et/ou la prevention de la retinopathie diabetique |
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| PT1470818E (pt) * | 2003-04-25 | 2006-11-30 | Neuro3D | Utilização de derivados de fenotiazina piperazina no fabrico de um medicamento com efeitos neuroprotectores e/ou neurotróficos no cns e/ou pns |
| AU2003902704A0 (en) * | 2003-05-29 | 2003-06-19 | Crc For Waste Management And Pollution Control Limited Of Unsw | Process for producing a nanoscale zero-valent metal |
| JP2007525503A (ja) * | 2004-02-27 | 2007-09-06 | バーテックス ファーマシューティカルズ インコーポレイテッド | カスパーゼインヒビターおよびそれらの使用 |
| SI2399915T1 (sl) * | 2004-03-12 | 2015-05-29 | Vertex Pharmaceuticals Incorporated | Postopek in intermediati za pripravo inhibitorjev asparagin-acetal-kaspaze |
| CN1980648A (zh) | 2004-05-15 | 2007-06-13 | 沃泰克斯药物股份有限公司 | 使用ice抑制剂治疗癫痫发作 |
| US7531570B2 (en) | 2004-05-27 | 2009-05-12 | Vertex Pharmaceuticals Incorporated | Treatment of diseases using ICE inhibitors |
| CN103059100A (zh) | 2004-11-24 | 2013-04-24 | 奇斯药制品公司 | 用作双重胱天蛋白酶-2/-6 抑制剂的新肽及其生物学应用 |
| US8012751B2 (en) * | 2005-03-31 | 2011-09-06 | Wisconsin Alumni Research Foundation | Differentiation of pluripotent embryonic stem cells |
| AU2006276096A1 (en) * | 2005-07-28 | 2007-02-08 | Vertex Pharmaceuticals Incorporated | Caspase inhibitor prodrugs |
| EP1956898A2 (en) | 2005-11-30 | 2008-08-20 | Massachusetts Institute of Technology | Pathogen-detecting cell preservation systems |
| AU2007273035A1 (en) * | 2006-07-07 | 2008-01-17 | The Board Of Trustees Of The Leland Stanford Junior University | Selective caspase inhibitors |
| WO2008137567A1 (en) * | 2007-05-01 | 2008-11-13 | Cedars-Sinai Medical Center | Caspase inhibitors in the treatment of infection-associated preterm delivery |
| ES2640814T3 (es) | 2008-05-21 | 2017-11-06 | Genesis Technologies Limited | Inhibidores selectivos de caspasa y usos de los mismos |
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| WO2011094426A1 (en) * | 2010-01-29 | 2011-08-04 | The United State Of America, As Represented By The Secretary, Department Of Health & Human Services | Caspase inhibitors |
| CN102241627B (zh) * | 2010-05-14 | 2014-07-02 | 中国人民解放军总医院 | 脲类化合物及其医药用途 |
| EP2635907A4 (en) | 2010-11-05 | 2014-04-16 | Univ Brandeis | ICE-COLDED ALPHA SYNNUCLEINE A BIOMARKERS |
| DK2697246T3 (en) | 2011-04-15 | 2018-05-28 | Genesis Tech Limited | SELECTIVE CYSTEIN PROTEASE INHIBITORS AND USES THEREOF |
| US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
| CN106470679A (zh) | 2014-05-12 | 2017-03-01 | 科内图斯医药公司 | 用半胱天冬酶抑制剂治疗慢性肝脏疾病并发症 |
| WO2017079566A1 (en) | 2015-11-05 | 2017-05-11 | Conatus Pharmaceuticals, Inc. | Caspase inhibitors for use in the treatment of liver cancer |
| WO2017117478A1 (en) | 2015-12-31 | 2017-07-06 | Conatus Pharmaceuticals Inc. | Methods of using caspase inhibitors in treatment of liver disease |
| AU2017311691B2 (en) | 2016-08-18 | 2021-12-02 | Vidac Pharma Ltd. | Piperazine derivatives, pharmaceutical compositions and methods of use thereof |
| JP2019530696A (ja) | 2016-10-05 | 2019-10-24 | ノバルティス アーゲー | 線維性、硬変性の疾患もしくは障害を治療または予防するためのfxrアゴニストを含む組合せ組成物 |
| WO2022123062A1 (en) | 2020-12-11 | 2022-06-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Blocking caspase and/or fasl for preventing fatal outcome in covid-19 patients |
| IT202300000834A1 (it) | 2023-01-20 | 2024-07-20 | Scylla Biotech Srl | Inibitori selettivi della caspasi-8 ed usi degli stessi per potenziare le difese innate |
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| JPH0789951A (ja) * | 1993-06-03 | 1995-04-04 | Sterling Winthrop Inc | インターロイキン−1β転換酵素阻害剤 |
| IL112759A0 (en) * | 1994-02-25 | 1995-05-26 | Khepri Pharmaceuticals Inc | Novel cysteine protease inhibitors |
| US5843904A (en) * | 1995-12-20 | 1998-12-01 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1βconverting enzyme |
| IL129091A0 (en) | 1996-10-11 | 2000-02-17 | Warner Lambert Co | Aspartate ester inhibitors of interleukin-1beta converting enzyme |
| CN1138472C (zh) * | 1997-10-10 | 2004-02-18 | 西托维亚公司 | 二肽型编程性细胞死亡抑制剂及其用途 |
| JP2002506829A (ja) * | 1998-03-16 | 2002-03-05 | サイトビア インコーポレイテッド | ジペプチドのアポトーシスインヒビターおよびそれらの使用 |
| EP2261235A3 (en) * | 1998-03-19 | 2011-04-20 | Vertex Pharmaceuticals Incorporated | Inhibitors of caspases |
| JP2002541237A (ja) * | 1999-04-09 | 2002-12-03 | サイトビア インコーポレイテッド | カスパーゼインヒビターおよびその使用 |
| EP1317454B1 (en) * | 2000-09-13 | 2011-05-25 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
-
2001
- 2001-09-12 EP EP01970836A patent/EP1317454B1/en not_active Expired - Lifetime
- 2001-09-12 WO PCT/US2001/028450 patent/WO2002022611A2/en not_active Ceased
- 2001-09-12 CA CA002418720A patent/CA2418720A1/en not_active Abandoned
- 2001-09-12 AU AU2001290795A patent/AU2001290795A1/en not_active Abandoned
- 2001-09-12 PE PE2001000916A patent/PE20020500A1/es not_active Application Discontinuation
- 2001-09-12 AT AT01970836T patent/ATE510837T1/de not_active IP Right Cessation
- 2001-09-12 US US09/951,006 patent/US6800619B2/en not_active Expired - Fee Related
- 2001-09-12 JP JP2002526864A patent/JP2004509120A/ja active Pending
-
2008
- 2008-07-31 JP JP2008198860A patent/JP2008297321A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| ATE510837T1 (de) | 2011-06-15 |
| WO2002022611A3 (en) | 2002-10-31 |
| WO2002022611A2 (en) | 2002-03-21 |
| EP1317454A2 (en) | 2003-06-11 |
| JP2008297321A (ja) | 2008-12-11 |
| EP1317454B1 (en) | 2011-05-25 |
| US6800619B2 (en) | 2004-10-05 |
| JP2004509120A (ja) | 2004-03-25 |
| AU2001290795A1 (en) | 2002-03-26 |
| US20020058630A1 (en) | 2002-05-16 |
| CA2418720A1 (en) | 2002-03-21 |
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