CA2433879A1 - C-terminal modified oxamyl dipeptides as inhibitors of the ice/ced-3 family of cysteine proteases - Google Patents
C-terminal modified oxamyl dipeptides as inhibitors of the ice/ced-3 family of cysteine proteases Download PDFInfo
- Publication number
- CA2433879A1 CA2433879A1 CA002433879A CA2433879A CA2433879A1 CA 2433879 A1 CA2433879 A1 CA 2433879A1 CA 002433879 A CA002433879 A CA 002433879A CA 2433879 A CA2433879 A CA 2433879A CA 2433879 A1 CA2433879 A1 CA 2433879A1
- Authority
- CA
- Canada
- Prior art keywords
- phenyl
- substituted
- naphthyl
- cycloalkyl
- alkyl
- 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.)
- Abandoned
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- KZAUOCCYDRDERY-UHFFFAOYSA-N oxamyl Chemical group CNC(=O)ON=C(SC)C(=O)N(C)C KZAUOCCYDRDERY-UHFFFAOYSA-N 0.000 title abstract description 58
- 239000003112 inhibitor Substances 0.000 title abstract description 15
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- 125000000217 alkyl group Chemical group 0.000 claims description 171
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Classifications
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- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
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- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
- C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C317/50—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/32—Esters thereof
- C07F9/3258—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/3264—Esters with hydroxyalkyl compounds
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/56—Ring systems containing bridged rings
- C07C2603/58—Ring systems containing bridged rings containing three rings
- C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/765,105 | 2001-01-16 | ||
| US09/765,105 US7053056B2 (en) | 1998-07-02 | 2001-01-16 | C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| PCT/US2002/001538 WO2002057298A2 (en) | 2001-01-16 | 2002-01-16 | C-terminal modified oxamyl dipeptides as inhibitors of the ice/ced-3 family of cysteine proteases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2433879A1 true CA2433879A1 (en) | 2002-07-25 |
Family
ID=25072661
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002433879A Abandoned CA2433879A1 (en) | 2001-01-16 | 2002-01-16 | C-terminal modified oxamyl dipeptides as inhibitors of the ice/ced-3 family of cysteine proteases |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7053056B2 (https=) |
| EP (1) | EP1351975A2 (https=) |
| JP (1) | JP2004521107A (https=) |
| CN (1) | CN1283656C (https=) |
| CA (1) | CA2433879A1 (https=) |
| WO (1) | WO2002057298A2 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6184210B1 (en) * | 1997-10-10 | 2001-02-06 | Cytovia, Inc. | Dipeptide apoptosis inhibitors and the use thereof |
| EP1718639A2 (en) | 2004-02-27 | 2006-11-08 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| KR101125932B1 (ko) * | 2006-12-06 | 2012-03-22 | 아이디유엔 파마슈티칼즈, 인코포레이티드 | (3s)-3-[n-(n'-(2-tert-부틸페닐)옥사밀)알라니닐]아미노-5-(2',3',5',6'-테트라플루오로페녹시)-4-옥소펜탄산의 결정 형태 |
| CA2737774A1 (en) | 2008-09-19 | 2010-03-25 | Henry Ford Health System | Methods, systems, and compositions for calpain inhibition |
| WO2012021800A2 (en) * | 2010-08-13 | 2012-02-16 | Banyan Biomarkers | Caspase inhibitors as therapeutics for neural and organ injury and imaging |
| US9539050B2 (en) * | 2011-04-12 | 2017-01-10 | Covidien Lp | System and method for process monitoring and intelligent shut-off |
| ES2751652T3 (es) | 2014-05-12 | 2020-04-01 | Conatus Pharmaceuticals Inc | Tratamiento con inhibidor de caspasa emricasan de las complicaciones por las enfermedades hepáticas crónicas |
| MX378266B (es) | 2014-10-06 | 2025-03-10 | Lighthouse Pharmaceuticals Inc | Inhibidores de gingipaina de lisina. |
| EP3265440A1 (en) | 2015-03-06 | 2018-01-10 | Concert Pharmaceuticals Inc. | Deuterated emricasan |
| WO2017079566A1 (en) | 2015-11-05 | 2017-05-11 | Conatus Pharmaceuticals, Inc. | Caspase inhibitors for use in the treatment of liver cancer |
| CN108602787A (zh) | 2015-11-09 | 2018-09-28 | 库特克希米公司 | 精氨酸牙龈卟啉菌蛋白酶的抑制剂 |
| JP2019500397A (ja) | 2015-12-31 | 2019-01-10 | クオナトウス ファーマシューティカルズ,インコーポレイテッド | カスパーゼ阻害剤を肝疾患の治療に使用する方法 |
| CN109983012B (zh) | 2016-09-16 | 2023-12-01 | 莱特豪斯制药公司 | 赖氨酸牙龈蛋白酶的酮抑制剂 |
| RU2019113150A (ru) | 2016-10-05 | 2020-11-06 | Новартис Аг | Комбинация композиций, содержащих агонисты fxr, предназначенная для лечения или предупреждения фиброзирующего, цирротического заболевания или нарушения |
| 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 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6204261B1 (en) | 1995-12-20 | 2001-03-20 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β Converting enzyme inhibitors |
| EP0618223A3 (en) | 1993-03-08 | 1996-06-12 | Sandoz Ltd | Peptides, the release of Interleukin 1-Bêta, useful as anti-inflammatory agents. |
| TW494094B (en) | 1993-04-29 | 2002-07-11 | Vertex Pharma | Peptide analogs as irreversible interleukin-1β protease inhibitors and pharmaceutical compositions comprising the same |
| US5869519A (en) | 1996-12-16 | 1999-02-09 | Idun Pharmaceuticals, Inc. | C-terminal modified (n-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| EP0929311B8 (en) | 1996-09-12 | 2006-02-01 | Idun Pharmaceuticals, Inc. | INHIBITION OF APOPTOSIS USING INTERLEUKIN-1 beta-CONVERTING ENZYME (ICE)/CED-3 FAMILY INHIBITORS |
| US5968927A (en) | 1996-09-20 | 1999-10-19 | Idun Pharmaceuticals, Inc. | Tricyclic compounds for the inhibition of the ICE/ced-3 protease family of enzymes |
| US5877197A (en) | 1996-12-16 | 1999-03-02 | Karanewsky; Donald S. | C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| US6184244B1 (en) | 1996-12-16 | 2001-02-06 | Idun Pharmaceuticals, Inc. | C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| FR2766188B1 (fr) | 1997-07-15 | 2000-02-11 | Hoechst Marion Roussel Inc | Nouveau procede de preparation de derives amines d'alkyloxy furanone, composes issus de ce procede et utilisation de ces composes |
| US6544951B2 (en) | 1998-07-02 | 2003-04-08 | Idun Pharmaceuticals, Inc. | C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| US6197750B1 (en) | 1998-07-02 | 2001-03-06 | Idun Pharmaceuticals, Inc. | C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
| US6242422B1 (en) | 1998-10-22 | 2001-06-05 | Idun Pharmacueticals, Inc. | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
| US6515173B1 (en) | 2000-01-13 | 2003-02-04 | Idun Pharmaceuticals, Inc. | Inhibitors of the ICE/ced-3 family of cysteine proteases |
| CA2402128A1 (en) | 2000-04-24 | 2001-11-01 | Vertex Pharmaceuticals Incorporated | Process and intermediates for making substituted aspartic acid acetals |
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2002
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- 2002-01-16 CN CNB028052781A patent/CN1283656C/zh not_active Expired - Fee Related
- 2002-01-16 EP EP02705856A patent/EP1351975A2/en not_active Withdrawn
- 2002-01-16 WO PCT/US2002/001538 patent/WO2002057298A2/en not_active Ceased
- 2002-01-16 JP JP2002557974A patent/JP2004521107A/ja active Pending
-
2004
- 2004-08-25 US US10/926,800 patent/US7183260B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| US20020042376A1 (en) | 2002-04-11 |
| CN1525978A (zh) | 2004-09-01 |
| US7183260B2 (en) | 2007-02-27 |
| CN1283656C (zh) | 2006-11-08 |
| WO2002057298A3 (en) | 2003-05-15 |
| JP2004521107A (ja) | 2004-07-15 |
| US20050020504A1 (en) | 2005-01-27 |
| WO2002057298A2 (en) | 2002-07-25 |
| US7053056B2 (en) | 2006-05-30 |
| EP1351975A2 (en) | 2003-10-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |