WO1997030072B1 - Inhibiteurs peptidomimetiques de la cathepsine d et des plasmepsines i et ii - Google Patents
Inhibiteurs peptidomimetiques de la cathepsine d et des plasmepsines i et iiInfo
- Publication number
- WO1997030072B1 WO1997030072B1 PCT/US1997/002930 US9702930W WO9730072B1 WO 1997030072 B1 WO1997030072 B1 WO 1997030072B1 US 9702930 W US9702930 W US 9702930W WO 9730072 B1 WO9730072 B1 WO 9730072B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- ipr
- seq
- phch
- val
- mono
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 4
- 102000005600 Cathepsins Human genes 0.000 title 1
- 108010084457 Cathepsins Proteins 0.000 title 1
- 239000000816 peptidomimetic Substances 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 claims abstract 4
- 206010027476 Metastases Diseases 0.000 claims abstract 2
- 230000009545 invasion Effects 0.000 claims abstract 2
- 201000004792 malaria Diseases 0.000 claims abstract 2
- 230000009401 metastasis Effects 0.000 claims abstract 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000003710 aryl alkyl group Chemical group 0.000 claims 13
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- -1 heteroaroyl Chemical group 0.000 claims 10
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 125000003435 aroyl group Chemical group 0.000 claims 4
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 4
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 4
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 4
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 4
- 125000005326 heteroaryloxy alkyl group Chemical group 0.000 claims 4
- 125000005226 heteroaryloxycarbonyl group Chemical group 0.000 claims 4
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims 3
- 125000004659 aryl alkyl thio group Chemical group 0.000 claims 3
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 3
- 241000224016 Plasmodium Species 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 210000004881 tumor cell Anatomy 0.000 claims 2
- UUFQTNFCRMXOAE-UHFFFAOYSA-N 1-methylmethylene Chemical compound C[CH] UUFQTNFCRMXOAE-UHFFFAOYSA-N 0.000 claims 1
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 101150065749 Churc1 gene Proteins 0.000 claims 1
- 241000223960 Plasmodium falciparum Species 0.000 claims 1
- 102100038239 Protein Churchill Human genes 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 102000003908 Cathepsin D Human genes 0.000 abstract 2
- 108090000258 Cathepsin D Proteins 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 108090000568 Plasmepsin II Proteins 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 108010020708 plasmepsin Proteins 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Abstract
L'invention concerne la conception et la synthèse d'inhibiteurs linéaires et cycliques de cathépsine D et de plasmépsines I et II. L'invention porte également sur les utilisations de ces inhibiteurs pour la prévention de l'invasion et de la métastase des cellules cancéreuses. Elle porte en outre sur l'utilisation d'inhibiteurs de la cathépsine D et des plasmépsines I et II pour la prévention ou le traitement de la maladie d'Alzheimer et du paludisme.
Priority Applications (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP97906763A EP0912600A2 (fr) | 1996-02-20 | 1997-02-20 | Inhibiteurs peptidomimetiques de la cathepsine d et des plasmepsines i et ii |
| JP9529609A JPH11508604A (ja) | 1996-02-20 | 1997-02-20 | カテプシンｄならびにプラスメプシン▲ｉ▼および▲ｉｉ▼のペプチド模倣インヒビター |
| CA002246758A CA2246758C (fr) | 1996-02-20 | 1997-02-20 | Inhibiteurs peptidomimetiques de la cathepsine d et des plasmepsines i et ii |
| AU21368/97A AU726206B2 (en) | 1996-02-20 | 1997-02-20 | Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/603,737 | 1996-02-20 | ||
| US08/603,737 US5849691A (en) | 1996-02-20 | 1996-02-20 | Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO1997030072A1 WO1997030072A1 (fr) | 1997-08-21 |
| WO1997030072B1 true WO1997030072B1 (fr) | 1997-10-23 |
Family
ID=24416708
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1997/002930 WO1997030072A1 (fr) | 1996-02-20 | 1997-02-20 | Inhibiteurs peptidomimetiques de la cathepsine d et des plasmepsines i et ii |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US5849691A (fr) |
| EP (1) | EP0912600A2 (fr) |
| JP (1) | JPH11508604A (fr) |
| AU (1) | AU726206B2 (fr) |
| CA (1) | CA2246758C (fr) |
| WO (1) | WO1997030072A1 (fr) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1996039194A1 (fr) * | 1995-06-06 | 1996-12-12 | Athena Neurosciences, Inc. | Nouvelle cathepsine et procedes et compositions d'inhibition de cathepsine |
| US6211235B1 (en) | 1996-11-22 | 2001-04-03 | Elan Pharmaceuticals, Inc. | Compounds for inhibiting β-amyloid peptide release and/or its synthesis |
| US6207710B1 (en) | 1996-11-22 | 2001-03-27 | Elan Pharmaceuticals, Inc. | Compounds for inhibiting β-amyloid peptide release and/or its synthesis |
| US6191166B1 (en) | 1997-11-21 | 2001-02-20 | Elan Pharmaceuticals, Inc. | Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis |
| US6635632B1 (en) | 1996-12-23 | 2003-10-21 | Athena Neurosciences, Inc. | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds |
| WO1998028268A2 (fr) * | 1996-12-23 | 1998-07-02 | Elan Pharmaceuticals, Inc. | CYCLOALKYLE, LACTAME ET COMPOSES ASSOCIES, COMPOSITIONS PHARMACEUTIQUES CONTENANT CES COMPOSES, ET PROCEDES D'INHIBITION DE LA LIBERATION DU PEPTIDE β-AMYLOIDE ET/OU DE SA SYNTHESE AU MOYEN DE TELS COMPOSES |
| US6228986B1 (en) * | 1998-04-13 | 2001-05-08 | Ortho-Mcneil Pharmaceutical, Inc. | Solid-phase synthesis of novel 14-membered macroycles for high throughput screening |
| US6552013B1 (en) | 1998-06-22 | 2003-04-22 | Elan Pharmaceuticals, Inc. | Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds |
| US6569851B1 (en) | 1998-06-22 | 2003-05-27 | Elan Pharmaceutials, Inc. | Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds |
| US6958330B1 (en) | 1998-06-22 | 2005-10-25 | Elan Pharmaceuticals, Inc. | Polycyclic α-amino-ε-caprolactams and related compounds |
| US6774125B2 (en) | 1998-06-22 | 2004-08-10 | Elan Pharmaceuticals, Inc. | Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds |
| US6509331B1 (en) | 1998-06-22 | 2003-01-21 | Elan Pharmaceuticals, Inc. | Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds |
| US6528505B1 (en) | 1998-06-22 | 2003-03-04 | Elan Pharmaceuticals, Inc. | Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds |
| US7192713B1 (en) | 1999-05-18 | 2007-03-20 | President And Fellows Of Harvard College | Stabilized compounds having secondary structure motifs |
| US6864240B1 (en) | 1999-06-15 | 2005-03-08 | Elan Pharmaceuticals, Inc. | Dipeptide inhibitors of β-secretase |
| DE60124080T2 (de) | 2000-03-23 | 2007-03-01 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen und verfahren zur behandlung der alzheimerschen krankheit |
| PE20020276A1 (es) | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
| ATE314343T1 (de) | 2000-06-30 | 2006-01-15 | Elan Pharm Inc | Verbindungen zur behandlung der alzheimerischen krankheit |
| US6846813B2 (en) | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
| AU2001278084A1 (en) * | 2000-07-31 | 2002-02-13 | The Regents Of The University Of California | Model for alzheimer's disease and other neurodegenerative diseases |
| US7247704B2 (en) | 2000-12-18 | 2007-07-24 | Arriva Pharmaceuticals, Inc. | Multifunctional protease inhibitors and their use in treatment of disease |
| BR0210721A (pt) | 2001-06-27 | 2004-07-20 | Elan Pharm Inc | Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição |
| CA2528375C (fr) | 2003-06-18 | 2013-11-19 | Tranzyme Pharma, Inc. | Antagonistes macrocycliques du recepteur de motiline |
| US20060122266A1 (en) * | 2004-08-11 | 2006-06-08 | Photini Sinnis | Methods and compositions for malaria prophylaxis |
| US20090092619A1 (en) * | 2004-08-11 | 2009-04-09 | Photini Sinnis | Methods and compositions for malaria prophylaxis |
| WO2006102159A2 (fr) * | 2005-03-17 | 2006-09-28 | Yale University | Composes et procedes pour le traitement de la malaria et du cancer |
| US7981998B2 (en) | 2006-12-14 | 2011-07-19 | Aileron Therapeutics, Inc. | Bis-sulfhydryl macrocyclization systems |
| EP2094721B1 (fr) * | 2006-12-14 | 2018-02-14 | Aileron Therapeutics, Inc. | Systèmes de macrocyclisation bis-sulfhydryle |
| US8889632B2 (en) | 2007-01-31 | 2014-11-18 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| ES2648687T3 (es) | 2007-02-23 | 2018-01-05 | Aileron Therapeutics, Inc. | Péptidos macrocíclicos unidos a triazol |
| US8592377B2 (en) | 2007-03-28 | 2013-11-26 | President And Fellows Of Harvard College | Stitched polypeptides |
| JP2012515172A (ja) | 2009-01-14 | 2012-07-05 | エルロン・セラピューティクス・インコーポレイテッド | ペプチド模倣大環状分子 |
| JP2013505300A (ja) | 2009-09-22 | 2013-02-14 | エルロン・セラピューティクス・インコーポレイテッド | ペプチド模倣大環状分子 |
| WO2012021876A2 (fr) | 2010-08-13 | 2012-02-16 | Aileron Therapeutics, Inc. | Macrocycles peptidomimétiques |
| ES2649964T3 (es) | 2011-02-08 | 2018-01-16 | Merck Patent Gmbh | Derivados de aminoestatina para el tratamiento de la artrosis |
| CN108929375A (zh) | 2011-10-18 | 2018-12-04 | 爱勒让治疗公司 | 拟肽大环化合物 |
| WO2013123267A1 (fr) | 2012-02-15 | 2013-08-22 | Aileron Therapeutics, Inc. | Macrocycles peptidomimétiques réticulés par triazole et par thioéther |
| RU2642299C2 (ru) | 2012-02-15 | 2018-01-24 | Эйлерон Терапьютикс, Инк. | P53 пептидомиметические макроциклы |
| CA2879754C (fr) | 2012-07-24 | 2021-02-16 | Merck Patent Gmbh | Derives d'hydroxystatine pour le traitement de l'arthrose |
| US9604919B2 (en) | 2012-11-01 | 2017-03-28 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
| WO2014084430A1 (fr) * | 2012-11-30 | 2014-06-05 | 경상대학교 산학협력단 | Thérapie combinatoire anticancéreuse |
| US10202418B2 (en) * | 2013-06-12 | 2019-02-12 | Merck Patent Gmbh | Hydroxy-ethylene derivatives for the treatment of arthrosis |
| AU2015320545C1 (en) | 2014-09-24 | 2020-05-14 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and formulations thereof |
| KR20170058424A (ko) | 2014-09-24 | 2017-05-26 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방 거대고리 및 이의 용도 |
| MX2017011834A (es) | 2015-03-20 | 2018-04-11 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y usos de los mismos. |
| US10059741B2 (en) | 2015-07-01 | 2018-08-28 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| EP3347372A4 (fr) | 2015-09-10 | 2019-09-04 | Aileron Therapeutics, Inc. | Macrocycles peptidomimétiques en tant que modulateurs de mcl-1 |
| JP6868267B2 (ja) * | 2017-02-01 | 2021-05-12 | 国立研究開発法人産業技術総合研究所 | アミノ酸含有両親媒性分子および有機ナノチューブ |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4485099A (en) * | 1983-06-15 | 1984-11-27 | Merck & Co., Inc. | Renin inhibitors containing a C-terminal amide cycle |
| US4477441A (en) * | 1983-09-14 | 1984-10-16 | Merck & Co., Inc. | Renin inhibitors containing a C-terminal disulfide cycle |
| US5212157A (en) * | 1989-06-06 | 1993-05-18 | Bio-Mega, Inc. | Enzyme inhibitors |
| US5126326A (en) * | 1989-06-06 | 1992-06-30 | Bio-Mega, Inc. | Enzyme inhibiting peptide derivatives |
| CA2036398C (fr) * | 1990-02-23 | 2000-06-13 | Boehringer Ingelheim (Canada) Ltd./ Boehringer Ingelheim (Canada) Ltee | Agents d'inhibition de la protease du vih |
| CA2036397C (fr) * | 1990-02-23 | 2000-12-12 | Paul Cates Anderson | Inhibiteurs de la protease du vih, renfermant des unites d'amino-acides |
| CA2091151A1 (fr) * | 1992-03-13 | 1993-09-14 | Kwan Y. Hui | Inhibiteurs de la protease retrovirale |
| NZ264143A (en) * | 1993-08-09 | 1996-11-26 | Lilly Co Eli | Use of an aspartyl protease inhibitor to inhibit beta-amyloid peptide production |
-
1996
- 1996-02-20 US US08/603,737 patent/US5849691A/en not_active Expired - Fee Related
-
1997
- 1997-02-20 AU AU21368/97A patent/AU726206B2/en not_active Ceased
- 1997-02-20 CA CA002246758A patent/CA2246758C/fr not_active Expired - Fee Related
- 1997-02-20 EP EP97906763A patent/EP0912600A2/fr not_active Withdrawn
- 1997-02-20 JP JP9529609A patent/JPH11508604A/ja active Pending
- 1997-02-20 WO PCT/US1997/002930 patent/WO1997030072A1/fr not_active Application Discontinuation
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