ES2282685T3 - Derivados de hidroxietilamina para el tratamiento de la enfermedad de alzheimer. - Google Patents

Derivados de hidroxietilamina para el tratamiento de la enfermedad de alzheimer. Download PDF

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Publication number
ES2282685T3
ES2282685T3 ES03767756T ES03767756T ES2282685T3 ES 2282685 T3 ES2282685 T3 ES 2282685T3 ES 03767756 T ES03767756 T ES 03767756T ES 03767756 T ES03767756 T ES 03767756T ES 2282685 T3 ES2282685 T3 ES 2282685T3
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Spain
Prior art keywords
disease
treatment
alzheimer
beta
hydroxyethylamine
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Expired - Lifetime
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ES03767756T
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English (en)
Inventor
Emmanuel GlaxoSmithKline Demont
Andrew c/o GlaxoSmithKline Faller
David Timothy GlaxoSmithKline MacPherson
Peter Henry GlaxoSmithKline Milner
Alan GlaxoSmithKline NAYLOR
Sally GlaxoSmithKline REDSHAW
Steven James GlaxoSmithKline Stanway
David R. GlaxoSmithKline Vesey
Daryl S. GlaxoSmithKline Walter
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Glaxo Group Ltd
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Glaxo Group Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/267—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
    • C07D275/03—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/02—1,2-Thiazines; Hydrogenated 1,2-thiazines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Un compuesto de fórmula, en la que R1 representa alquilo C1-6, alquenilo C2-6, halógeno, alcoxi C1-6, amino, ciano, hidroxi, arilo, heteroarilo o heterociclilo; R2a representa hidrógeno, alquilo C1-3, alcoxi C1-3 o halógeno; m y n representan independientemente 0, 1 ó 2; X representa CO, SO o SO2; p representa un número entero de 1 a 3; R2b representa hidrógeno, alquilo C1-6, alquenilo C2-6, halógeno, alcoxi C1-6, amino, ciano, hidroxi, arilo, heteroarilo o heterociclilo; o su sal o solvato farmacéuticamente aceptable.
ES03767756T 2002-12-05 2003-12-03 Derivados de hidroxietilamina para el tratamiento de la enfermedad de alzheimer. Expired - Lifetime ES2282685T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0228410 2002-12-05
GBGB0228410.7A GB0228410D0 (en) 2002-12-05 2002-12-05 Novel Compounds

Publications (1)

Publication Number Publication Date
ES2282685T3 true ES2282685T3 (es) 2007-10-16

Family

ID=9949141

Family Applications (1)

Application Number Title Priority Date Filing Date
ES03767756T Expired - Lifetime ES2282685T3 (es) 2002-12-05 2003-12-03 Derivados de hidroxietilamina para el tratamiento de la enfermedad de alzheimer.

Country Status (24)

Country Link
US (1) US7253198B2 (es)
EP (1) EP1567488B1 (es)
JP (1) JP2006514634A (es)
KR (1) KR20050084143A (es)
CN (1) CN1735592A (es)
AT (1) ATE354565T1 (es)
AU (1) AU2003292198B2 (es)
BR (1) BR0317020A (es)
CA (1) CA2508325A1 (es)
DE (1) DE60312031T2 (es)
DK (1) DK1567488T3 (es)
ES (1) ES2282685T3 (es)
GB (1) GB0228410D0 (es)
IS (1) IS7925A (es)
MA (1) MA27608A1 (es)
MX (1) MXPA05006088A (es)
NO (1) NO20053263L (es)
NZ (1) NZ539841A (es)
PL (1) PL377587A1 (es)
PT (1) PT1567488E (es)
RU (1) RU2005121146A (es)
SI (1) SI1567488T1 (es)
WO (1) WO2004050619A1 (es)
ZA (1) ZA200503693B (es)

Families Citing this family (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0314302D0 (en) * 2003-06-19 2003-07-23 Glaxo Group Ltd Novel compounds
GB0328900D0 (en) * 2003-12-12 2004-01-14 Glaxo Group Ltd Novel compounds
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
JP2007517781A (ja) * 2003-12-19 2007-07-05 メルク　エンド　カムパニー　インコーポレーテッド アルツハイマー病治療用のフェニルアミドおよびピリジルアミド系β−セクレターゼ阻害薬
EP1734961A2 (en) * 2004-03-09 2006-12-27 Elan Pharmaceuticals, Inc. Methods of treatment of amyloidosis using bi-cyclic aspartyl protease inhibitors
US20050239790A1 (en) * 2004-03-09 2005-10-27 Varghese John Substituted hydroxyethylamine aspartyl protease inhibitors
CA2558034A1 (en) 2004-03-09 2005-09-22 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamine aspartyl protease inhibitors
JP2007528404A (ja) * 2004-03-09 2007-10-11 エラン ファーマシューティカルズ，インコーポレイテッド 置換された尿素およびカルバメート、フェナシル−２−ヒドロキシ−３−ジアミノアルカン、ならびにベンズアミド−２−ヒドロキシ−３−ジアミノアルカン系のアスパラギン酸プロテアーゼ阻害薬
AU2005236063A1 (en) 2004-04-20 2005-11-03 Merck & Co., Inc. 2, 4, 6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
US7847100B2 (en) 2004-04-20 2010-12-07 Merck, Sharp & Dohme, Inc. 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
GB0411404D0 (en) * 2004-05-21 2004-06-23 Glaxo Group Ltd Novel compounds
CA2572775A1 (en) * 2004-07-09 2006-01-26 Elan Pharmaceuticals, Inc. Oxime derivative hydroxyethylamine aspartyl-protease inhibitors
EP1773756A2 (en) * 2004-07-09 2007-04-18 Elan Pharmaceuticals, Inc. Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors
JP2008513495A (ja) * 2004-09-17 2008-05-01 コメンティス，インコーポレーテッド ベータ−セクレターゼ活性を阻害する二環式化合物およびその使用方法
BRPI0515383A (pt) * 2004-09-21 2008-07-22 Pfizer Prod Inc n-etil hidroxietilamina útil no tratamento de condições do snc
MX2007002459A (es) 2004-09-21 2007-05-04 Pfizer Prod Inc N-metilhidroxietilamina util en el tratamiento de afecciones del snc.
WO2006043710A1 (ja) * 2004-10-19 2006-04-27 Reverse Proteomics Research Institute Co., Ltd. 創薬標的タンパク質及び標的遺伝子、並びにスクリーニング方法
AU2005309760A1 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
EP1828130A2 (en) * 2004-12-14 2007-09-05 Pfizer Products Incorporated Heterocycloalkyl-benzyl substituted hydroxyethlamines
WO2006101937A1 (en) 2005-03-18 2006-09-28 Janssen Pharmaceutica N.V. Acylhydrazones as kinase modulators
MX2007012341A (es) 2005-04-08 2008-02-12 Comentis Inc Compuestos que inhiben actividad beta-secretasa y metodos de uso de los mismos.
US7476764B2 (en) 2005-08-04 2009-01-13 Bristol-Myers Squibb Company Phenylcarboxyamides as beta-secretase inhibitors
WO2007047305A1 (en) 2005-10-12 2007-04-26 Elan Pharmaceuticals, Inc. Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors
US7745484B2 (en) * 2005-11-21 2010-06-29 Amgen Inc. Beta-secretase modulators and methods of use
US7838676B2 (en) * 2005-11-21 2010-11-23 Amgen Inc. Beta-secretase modulators and methods of use
US7872009B2 (en) 2005-11-21 2011-01-18 Amgen Inc. Beta-Secretase modulators and methods of use
EP1971598A1 (en) 2005-11-21 2008-09-24 Amgen Inc. Beta-secretase modulators and methods of use
US8835426B2 (en) * 2007-02-26 2014-09-16 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11β-hydroxysteroid dehydrogenase 1
US20080277393A1 (en) * 2007-05-07 2008-11-13 True Charles W Collapsible, stackable, semi-rigid universal cotainer for hazardous and non-hazardous goods
CA2687608C (en) 2007-05-25 2013-07-02 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
CL2008001500A1 (es) 2007-05-25 2008-12-26 Amgen Inc Compuestos derivados de hidroxietil amina sustituidas, moduladores de betasecretasa; proceso de preparacion de dichos c ompuestos; composicion farmaceutica que los comprende; y su uso para tratar un trastorno neurologico, tal como alzheimer, sindrome de down, demencia degenerativa, entre otros.
JP5451611B2 (ja) * 2007-07-26 2014-03-26 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 １１β−ヒドロキシステロイドデヒドロゲナーゼ１のサイクリックインヒビター
EP2178837A2 (en) * 2007-07-26 2010-04-28 Comentis, Inc. Isophthalamide derivatives inhibiting beta-secretase activity
FR2919285B1 (fr) * 2007-07-27 2012-08-31 Sanofi Aventis Derives de 1-oxo-isoindoline-4-carboxamides et de 1-oxo- 1,2,3,4-tetrahydroisoquinoleine-5-carboxamides, leur preparation et leur application en therapeutique.
CN101868457B (zh) * 2007-09-24 2013-02-13 科门蒂斯公司 作为β-分泌酶抑制剂用于治疗的(3-羟基-4-氨基-丁-2-基)-3-(2-噻唑-2-基-吡咯烷-1-羰基)苯甲酰胺衍生物和相关化合物
AR069207A1 (es) * 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
US7803809B2 (en) 2008-11-12 2010-09-28 Amgen Inc. Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use
CA2708303A1 (en) 2007-12-11 2009-06-18 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
TW200934490A (en) * 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
WO2009094169A1 (en) 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2714532A1 (en) * 2008-02-11 2009-08-20 Vitae Pharmaceuticals, Inc. 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
US8598160B2 (en) * 2008-02-15 2013-12-03 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
CA2718264A1 (en) * 2008-03-18 2009-09-24 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
CA2723032A1 (en) * 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
KR20110002492A (ko) 2008-05-01 2011-01-07 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
EP2291370B1 (en) 2008-05-01 2013-11-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
TW201004945A (en) 2008-05-01 2010-02-01 Vitae Pharmaceuticals Inc Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2010011314A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1
US8846668B2 (en) 2008-07-25 2014-09-30 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
MX2011002705A (es) * 2008-09-11 2011-09-09 Amgen Inc Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso.
JP5679997B2 (ja) 2009-02-04 2015-03-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
EP2411000A4 (en) * 2009-03-25 2012-09-19 Comentis Inc PYRROLIDIN COMPOUNDS FOR INHIBITING THE BETA-SECRETASE EFFECT AND METHOD FOR THE APPLICATION THEREOF
TW201039034A (en) * 2009-04-27 2010-11-01 Chunghwa Picture Tubes Ltd Pixel structure and the method of forming the same
KR20120061771A (ko) * 2009-04-30 2012-06-13 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
UA109255C2 (ru) 2009-04-30 2015-08-10 Берінгер Інгельхайм Інтернешнл Гмбх Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1
WO2011011123A1 (en) 2009-06-11 2011-01-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
CN102803212A (zh) * 2009-06-24 2012-11-28 弗·哈夫曼-拉罗切有限公司 抗病毒的杂环化合物
WO2011002910A1 (en) 2009-07-01 2011-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP2013506713A (ja) * 2009-10-05 2013-02-28 コメンティス，インコーポレーテッド β−セクレターゼ活性を阻害するスルホンアミドピロリジン化合物及びその使用方法
WO2011063233A1 (en) 2009-11-23 2011-05-26 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
US8822485B2 (en) 2009-11-23 2014-09-02 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
ES2546063T3 (es) * 2009-12-10 2015-09-18 The Regents Of The University Of California Agentes de enlace a amiloides
WO2011090911A1 (en) 2010-01-19 2011-07-28 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
MX2012010658A (es) 2010-03-15 2012-12-05 Amgen Inc Compuestos de anillo espiro tetraciclico como moduladores de beta-secretasa.
US8497264B2 (en) 2010-03-15 2013-07-30 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
EP2582698B1 (en) 2010-06-16 2016-09-14 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
WO2011161128A1 (en) 2010-06-25 2011-12-29 Boehringer Ingelheim International Gmbh Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders
CA2813671A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
US9346827B2 (en) 2011-02-07 2016-05-24 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
DE102011000683A1 (de) 2011-02-11 2012-08-16 Huf Hülsbeck & Fürst Gmbh & Co. Kg Montagebaugruppe zur vereinfachten Montage am Fahrzeug
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
CN102336672B (zh) * 2011-09-21 2014-06-18 浙江建业化工股份有限公司 生产异戊胺的方法
AU2012321345B2 (en) 2011-10-03 2016-03-17 The University Of Utah Research Foundation Application of 5-HT6 receptor antagonists for the alleviation of cognitive deficits of down syndrome
CN103508957B (zh) * 2012-06-25 2017-02-08 中国科学院上海药物研究所 羟乙基吡唑类化合物或氨乙基吡唑类化合物及其制备方法和用途
AR091731A1 (es) * 2012-07-19 2015-02-25 Merck Sharp & Dohme Antagonistas del receptor de mineralocorticoides
BR112015003824B1 (pt) * 2012-08-24 2022-10-04 Treventis Corporation Composto, composição farmacêutica e uso do composto
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
CN109485638B (zh) * 2017-09-12 2020-07-17 新发药业有限公司 一种奥希替尼中间体的制备方法
CN109053445A (zh) * 2018-06-13 2018-12-21 燕山大学 一种酯的交换方法
CN110372628B (zh) * 2019-07-09 2021-04-02 武汉大学 内磺酰胺类化合物及其制备方法
CN114591192B (zh) * 2020-12-04 2024-06-21 江西仰立新材料有限公司 一种n-环丙甲基苯胺类化合物的制备方法
AR129265A1 (es) 2022-05-12 2024-08-07 Syngenta Crop Protection Ag Compuestos de alcoxi-heteroaril-carboxamida o tioamida
WO2024033374A1 (en) 2022-08-11 2024-02-15 Syngenta Crop Protection Ag Novel arylcarboxamide or arylthioamide compounds
CN116082181B (zh) * 2022-12-12 2025-03-04 爱斯特（成都）生物制药股份有限公司 一种制备3-氨基-5-乙氧基-苯甲酸的方法
JP2026500298A (ja) 2022-12-15 2026-01-06 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺有害生物剤として有用である新規な二環式カルボキサミド化合物
WO2025196119A1 (en) 2024-03-22 2025-09-25 Lonza Ltd Continuous deoxyfluorination of ketones using in situ formed dast

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992006691A1 (en) 1990-10-19 1992-04-30 Biota Scientific Management Pty. Ltd. Anti-viral compounds that bind the active site of influenza neuramidase and display in vivo activity against orthomyxovirus and paramyxovirus
DE4109169A1 (de) 1991-03-20 1992-09-24 Koehler Chemie Dr Franz Wasserloesliche nicht ionische roentgenkontrastmittel sowie mittel und verfahren zu ihrer herstellung
DE122007000045I2 (de) 1992-08-25 2011-07-21 Gd Searle Llc Gd Searle Llc Darunavir oder pharmazeutisch vertragliche Salze, Hydroxyethylaminosulfonamide verwendbar als InhibiEster oder Prodrugs davon. toren retroviraler Proteasen.
US5968942A (en) * 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
IT1256248B (it) 1992-12-24 1995-11-29 Bracco Spa Formulazioni iniettabili acquose per radiodiagnostica comprendenti miscele di composti aromatici iodurati utili come agenti opacizzanti ai raggi x
ES2127938T3 (es) 1993-08-24 1999-05-01 Searle & Co Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas.
TW308598B (es) 1994-01-14 1997-06-21 Hoffmann La Roche
US5811581A (en) * 1994-08-04 1998-09-22 Dibra S.P.A. Process for the purification of opacifying contrast agents
US5728718A (en) 1994-12-20 1998-03-17 The United States Of America As Represented By The Department Of Health And Human Services 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane isosteres comprising benzamide, sulfonamide and anthranilamide subunits and methods of using same
US5545640A (en) * 1995-04-04 1996-08-13 Bio-Mega/Boehringer Ingeleheim Research Inc. Protease inhibiting succinic acid derivatives
JP4104656B2 (ja) * 1995-12-19 2008-06-18 ブラッコ・リサーチ・ソシエテ・アノニム トリヨードベンゼンポリマーからなる胃腸管の画像形成用組成物
IT1282653B1 (it) 1996-02-20 1998-03-31 Bracco Spa Dispositivo e metodo per la rigenerazione di letti misti di resine a scambio ionico
EP0944582B1 (de) 1996-12-11 2003-07-02 Abbott GmbH & Co. KG Ketobenzamide als calpain-inhibitoren
WO1998033795A1 (en) * 1997-02-04 1998-08-06 The Regents Of The University Of California Nanomolar, non-peptide inhibitors of cathepsin d
HUP0004200A3 (en) 1997-11-18 2001-04-28 Dupont Pharmaceuticals Res Lab Cyclic amine derivatives and their use as drugs
DE19818614A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Amide, deren Herstellung und Anwendung
DE19817461A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Benzamide, deren Herstellung und Anwendung
ES2325140T3 (es) 1998-04-20 2009-08-26 ABBOTT GMBH & CO. KG Amidas sustituidas con heterociclos como inhibidores de la calpaina.
SE9801901L (sv) 1998-05-29 1999-08-02 Bone Support Ab Förfarande för framställning av pulverkomponent till cement för medicinskt bruk, användning av sådan pulverkomponent samt sådan pulverkomponent
SE9904652D0 (sv) 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
AU2001252958A1 (en) 2000-03-23 2001-10-03 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
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
CA2410680A1 (en) 2000-06-30 2002-01-10 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
AR035960A1 (es) * 2001-04-23 2004-07-28 Elan Pharm Inc Epoxidos sustituidos y procesos para prepararlos
AR039555A1 (es) 2001-11-08 2005-02-23 Upjohn Co Derivados n,n'-sustituidos de 1,3-diamino-2-hidroxipropano

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