PE20070018A1 - Compuestos heterociclicos como inhibidores de aspartil proteasas - Google Patents
Compuestos heterociclicos como inhibidores de aspartil proteasasInfo
- Publication number
- PE20070018A1 PE20070018A1 PE2006000661A PE2006000661A PE20070018A1 PE 20070018 A1 PE20070018 A1 PE 20070018A1 PE 2006000661 A PE2006000661 A PE 2006000661A PE 2006000661 A PE2006000661 A PE 2006000661A PE 20070018 A1 PE20070018 A1 PE 20070018A1
- Authority
- PE
- Peru
- Prior art keywords
- aspartile
- proteases
- inhibitors
- compounds
- heterocyclic compounds
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
SE REIFERE A COMPUESTOS DE FORMULA (I) DONDE W ES UN ENLACE, -S(O)-, -S(O)2-, -C(=O)-, -O-, ENTRE OTROS; U ES UN ENLACE, -S(O)-, -S(O)2-, -C(O)-, ENTRE OTROS; R ES H, ALQUILO(C1-C20), ARILALQUILO, NO2, ENTRE OTROS; R1 Y R2 SON ALQUILENO, ARILALQUILENO, ENTRE OTROS, O JUNTOS SON UNA CADENA DE (C2-C6) OPCIONALMENTE SUSTITUIDO CON O, C(O), C(S), S(O), ENTRE OTROS; R3 Y R4 SON H, ALQUILO(C1-C20), ARILALQUILO(C6-C14), ARILO(C6-C14), HALO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 3'-(4,4-DIFLUORO-8-METIL-2,7-DIOXO-2,4,5,7,8,9-HEXAHIDROIMIDAZO-[2,1-d]-[1,3,5]OXADIAZEPIN-8-IL)-1,1'-BIFENIL-3-CARBONITRILO, 3'-[8-METIL-3-(METILSULFONIL)-2,7-DIOXO-2,4,5,7,8,9-HEXAHIDROIMIDAZO-[1,2-a][1,3,5]TRIAZEPIN-8-IL)-1,1'-BIFENIL-3-CARBONITRILO, 2,2-DIFENIL-1,5,6,7-TETRAHIDROIMIDAZOL[1,2-a]PIRIMIDIN-3-ONA, ENTRE OTROS SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE ASPARTIL PROTEASAS SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDADES CARDIOVASCULARES TAL COMO HIPERTENSION, INSUFICIENCIA CARDIACA CONGESTIVA, ENFERMEDADES COGNITIVAS Y NEURODEGENERATIVAS TAL COMO ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US69032605P | 2005-06-14 | 2005-06-14 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20070018A1 true PE20070018A1 (es) | 2007-03-08 |
Family
ID=37074234
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2006000661A PE20070018A1 (es) | 2005-06-14 | 2006-06-13 | Compuestos heterociclicos como inhibidores de aspartil proteasas |
Country Status (18)
Country | Link |
---|---|
US (1) | US7759354B2 (es) |
EP (1) | EP1896477B1 (es) |
JP (1) | JP2008543840A (es) |
KR (1) | KR20080031189A (es) |
CN (1) | CN101198609A (es) |
AR (1) | AR054620A1 (es) |
AT (1) | ATE482214T1 (es) |
AU (1) | AU2006259675A1 (es) |
CA (1) | CA2610812A1 (es) |
DE (1) | DE602006017073D1 (es) |
ES (1) | ES2350854T3 (es) |
HK (1) | HK1109151A1 (es) |
IL (1) | IL187623A0 (es) |
MX (1) | MX2007016175A (es) |
PE (1) | PE20070018A1 (es) |
TW (1) | TW200716644A (es) |
WO (1) | WO2006138192A1 (es) |
ZA (1) | ZA200710337B (es) |
Families Citing this family (47)
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US7763609B2 (en) * | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
MX2007016175A (es) | 2005-06-14 | 2008-03-07 | Schering Corp | Inhibidor de aspartil proteasas. |
TW201004961A (en) | 2005-06-14 | 2010-02-01 | Schering Corp | Aspartyl protease inhibitors |
CN101346357B (zh) | 2005-10-25 | 2014-04-02 | 盐野义制药株式会社 | 氨基二氢噻嗪衍生物 |
CN101484429A (zh) | 2006-06-12 | 2009-07-15 | 先灵公司 | 杂环的天冬氨酰基蛋白酶抑制剂 |
CA2672295A1 (en) * | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors containing a tricyclic ring system |
MX2009006228A (es) | 2006-12-12 | 2009-06-22 | Schering Corp | Inhibidores de aspartil proteasa. |
EP2689780A1 (en) | 2007-04-24 | 2014-01-29 | Shionogi & Co., Ltd. | Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group |
EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
JP2010538068A (ja) | 2007-09-06 | 2010-12-09 | シェーリング コーポレイション | ガンマセクレターゼモジュレーター |
CA2704698A1 (en) | 2007-11-05 | 2009-05-14 | Schering Corporation | Gamma secretase modulators |
EP2227471A1 (en) | 2007-12-11 | 2010-09-15 | Schering Corporation | Gamma secretase modulators |
EP2288613B1 (en) | 2008-04-22 | 2016-07-13 | Merck Sharp & Dohme Corp. | Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use |
AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
WO2010021680A2 (en) * | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
CN102186841A (zh) | 2008-10-22 | 2011-09-14 | 盐野义制药株式会社 | 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物 |
WO2010056849A1 (en) | 2008-11-13 | 2010-05-20 | Schering Corporation | Gamma secretase modulators |
WO2010075204A2 (en) | 2008-12-22 | 2010-07-01 | Schering Corporation | Gamma secretase modulators |
CA2747744A1 (en) | 2008-12-22 | 2010-07-01 | Theodros Asberom | Gamma secretase modulators |
KR20120001756A (ko) | 2009-03-13 | 2012-01-04 | 비타이 파마슈티컬즈, 인코포레이티드 | 베타세크리타아제 저해제 |
EP2443118A1 (en) | 2009-06-16 | 2012-04-25 | Schering Corporation | Gamma secretase modulators |
US20120238546A1 (en) | 2009-06-16 | 2012-09-20 | Zhaoning Zhu | Gamma secretase modulators |
US20120245158A1 (en) | 2009-06-16 | 2012-09-27 | Xianhai Huang | Gamma secretase modulators |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
US8563543B2 (en) | 2009-10-08 | 2013-10-22 | Merck Sharp & Dohme Corp. | Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2485590B1 (en) | 2009-10-08 | 2015-01-07 | Merck Sharp & Dohme Corp. | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
WO2011044185A2 (en) | 2009-10-08 | 2011-04-14 | Schering Corporation | Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use |
UA110467C2 (uk) | 2009-12-11 | 2016-01-12 | Шионогі Енд Ко., Лтд. | Похідні оксазину |
JP5828848B2 (ja) | 2010-02-24 | 2015-12-09 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | ベータセクレターゼインヒビター |
CN103261199A (zh) | 2010-10-29 | 2013-08-21 | 盐野义制药株式会社 | 萘啶衍生物 |
US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
WO2012138734A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2694521B1 (en) | 2011-04-07 | 2015-11-25 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
US9181236B2 (en) | 2011-08-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use |
TWI557112B (zh) | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β-分泌酶抑制劑 |
JP6482458B2 (ja) | 2012-03-19 | 2019-03-13 | バック・インスティテュート・フォー・リサーチ・オン・エイジング | App特異性のbace(asbi)およびその使用 |
TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β-分泌酶抑制劑 |
EP2900650A1 (en) | 2012-09-28 | 2015-08-05 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
EP2908825B1 (en) | 2012-10-17 | 2018-04-18 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
EP2908824B1 (en) | 2012-10-17 | 2018-05-02 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity |
DK2956443T3 (da) | 2013-02-12 | 2020-01-20 | Buck Inst Res Aging | Hydantoiner som modulatorer af BACE-medieret APP-forarbejdning |
JP6321685B2 (ja) | 2013-02-25 | 2018-05-09 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | 2−アミノ−3,4−ジヒドロ−キナゾリン誘導体、およびそのカテプシンd阻害剤としての使用 |
US11766435B2 (en) | 2016-02-18 | 2023-09-26 | Merck Sharp & Dohme Llc | N3-substituted iminopyrimidinones as antimalarial agents |
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CA2637565A1 (en) | 2006-01-18 | 2007-07-26 | Schering Corporation | Cannibinoid receptor modulators |
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CA2669982A1 (en) | 2006-11-17 | 2008-05-29 | Schering Corporation | Combination therapy for proliferative disorders |
CA2672295A1 (en) | 2006-12-12 | 2008-06-19 | Schering Corporation | Aspartyl protease inhibitors containing a tricyclic ring system |
MX2009006228A (es) | 2006-12-12 | 2009-06-22 | Schering Corp | Inhibidores de aspartil proteasa. |
-
2006
- 2006-06-12 MX MX2007016175A patent/MX2007016175A/es unknown
- 2006-06-12 AT AT06784753T patent/ATE482214T1/de not_active IP Right Cessation
- 2006-06-12 US US11/451,074 patent/US7759354B2/en active Active
- 2006-06-12 EP EP06784753A patent/EP1896477B1/en active Active
- 2006-06-12 ES ES06784753T patent/ES2350854T3/es active Active
- 2006-06-12 KR KR1020077029729A patent/KR20080031189A/ko not_active Withdrawn
- 2006-06-12 CA CA002610812A patent/CA2610812A1/en not_active Abandoned
- 2006-06-12 CN CNA2006800212013A patent/CN101198609A/zh active Pending
- 2006-06-12 AR ARP060102466A patent/AR054620A1/es not_active Application Discontinuation
- 2006-06-12 AU AU2006259675A patent/AU2006259675A1/en not_active Abandoned
- 2006-06-12 WO PCT/US2006/022698 patent/WO2006138192A1/en active Application Filing
- 2006-06-12 DE DE602006017073T patent/DE602006017073D1/de active Active
- 2006-06-12 JP JP2008516963A patent/JP2008543840A/ja active Pending
- 2006-06-13 TW TW095121028A patent/TW200716644A/zh unknown
- 2006-06-13 PE PE2006000661A patent/PE20070018A1/es not_active Application Discontinuation
-
2007
- 2007-11-25 IL IL187623A patent/IL187623A0/en unknown
- 2007-11-28 ZA ZA200710337A patent/ZA200710337B/xx unknown
-
2008
- 2008-03-18 HK HK08103079.0A patent/HK1109151A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
EP1896477A1 (en) | 2008-03-12 |
US20060281730A1 (en) | 2006-12-14 |
TW200716644A (en) | 2007-05-01 |
US7759354B2 (en) | 2010-07-20 |
EP1896477B1 (en) | 2010-09-22 |
WO2006138192A1 (en) | 2006-12-28 |
DE602006017073D1 (en) | 2010-11-04 |
KR20080031189A (ko) | 2008-04-08 |
CN101198609A (zh) | 2008-06-11 |
HK1109151A1 (en) | 2008-05-30 |
ATE482214T1 (de) | 2010-10-15 |
AR054620A1 (es) | 2007-07-04 |
IL187623A0 (en) | 2008-03-20 |
CA2610812A1 (en) | 2006-12-28 |
JP2008543840A (ja) | 2008-12-04 |
ES2350854T3 (es) | 2011-01-27 |
ZA200710337B (en) | 2008-12-31 |
MX2007016175A (es) | 2008-03-07 |
AU2006259675A1 (en) | 2006-12-28 |
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