[go: up one dir, main page]

PE20091834A1 - Compuestos de 2-imino-3-metilpirrolopirimidinona tiofenilo-sustituida como inhibidores de bace-1 y composiciones que los contienen - Google Patents

Compuestos de 2-imino-3-metilpirrolopirimidinona tiofenilo-sustituida como inhibidores de bace-1 y composiciones que los contienen

Info

Publication number
PE20091834A1
PE20091834A1 PE2009000553A PE2009000553A PE20091834A1 PE 20091834 A1 PE20091834 A1 PE 20091834A1 PE 2009000553 A PE2009000553 A PE 2009000553A PE 2009000553 A PE2009000553 A PE 2009000553A PE 20091834 A1 PE20091834 A1 PE 20091834A1
Authority
PE
Peru
Prior art keywords
bace
inhibitors
methylpyrroloopyrimidinone
thiophenyl
imino
Prior art date
Application number
PE2009000553A
Other languages
English (en)
Inventor
Andrew W Stamford
Zhaoning Zhu
Mihirbaran Mandal
Xiaoxiang Lius
Original Assignee
Schering Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40806727&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20091834(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of PE20091834A1 publication Critical patent/PE20091834A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A UN DERIVADO DE PIRROLOPIRIMIDINONA DE FORMULA (III), DONDE R2 ES H, F, Cl, Br, CN; R3 Y R4 SON H, F, Cl, CN; R6 ES ALQUILO C1-C6, ALCOXI C1-C6, HALOALQUILO C1-C6, HALOALCOXI C1-C6; R7 ES F O Cl; R8 ES ALQUILO C1-C6, ALCOXI C1-C6, CICLOALQUILO C3-C10, ENTRE OTROS; R9 ES H O ALQUILO C1-C6. SON COMPUESTOS PREFERIDOS: (a), (b), ENTRE OTROS. TAMBIEN ESTA RELACIONADA A UN METODO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA DE DISOCIACION DE APP DE SITIO BETA (BACE-1) E INHIBEN LA PRODUCCION DE BETA-AMILOIDES Y SON UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, SINDROME DE DOWN, ENFERMEDAD DE PARKINSON, ENTRE OTRAS
PE2009000553A 2008-04-22 2009-04-21 Compuestos de 2-imino-3-metilpirrolopirimidinona tiofenilo-sustituida como inhibidores de bace-1 y composiciones que los contienen PE20091834A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4700608P 2008-04-22 2008-04-22

Publications (1)

Publication Number Publication Date
PE20091834A1 true PE20091834A1 (es) 2009-12-19

Family

ID=40806727

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2009000553A PE20091834A1 (es) 2008-04-22 2009-04-21 Compuestos de 2-imino-3-metilpirrolopirimidinona tiofenilo-sustituida como inhibidores de bace-1 y composiciones que los contienen
PE2009000554A PE20091734A1 (es) 2008-04-22 2009-04-21 Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2009000554A PE20091734A1 (es) 2008-04-22 2009-04-21 Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso

Country Status (23)

Country Link
US (2) US8450331B2 (es)
EP (2) EP2288613B1 (es)
JP (2) JP2011518225A (es)
KR (1) KR20110003347A (es)
CN (1) CN102066380A (es)
AR (2) AR071385A1 (es)
AU (2) AU2009239536C1 (es)
BR (1) BRPI0911356A2 (es)
CA (2) CA2723222C (es)
CL (2) CL2009000953A1 (es)
CO (1) CO6321265A2 (es)
CR (1) CR11738A (es)
DO (1) DOP2010000320A (es)
EA (1) EA201001532A1 (es)
EC (1) ECSP10010585A (es)
IL (1) IL208465A0 (es)
MA (1) MA32252B1 (es)
MX (1) MX2010011563A (es)
PE (2) PE20091834A1 (es)
SV (1) SV2010003714A (es)
TW (2) TW200948364A (es)
WO (2) WO2009131975A1 (es)
ZA (1) ZA201007433B (es)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP1896478B1 (en) 2005-06-14 2014-05-21 Merck Sharp & Dohme Corp. Aspartyl protease inhibitors
EP1896032B1 (en) 2005-06-14 2012-10-31 Merck Sharp & Dohme Corp. The preparation and use of compounds as protease inhibitors
ES2537898T3 (es) 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
CA2651519A1 (en) 2006-06-06 2007-12-13 Intra-Cellular Therapies, Inc. Organic compounds
AU2007258435A1 (en) 2006-06-12 2007-12-21 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
EP2689780A1 (en) 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group
US8846693B2 (en) 2007-12-06 2014-09-30 Intra-Cellular Therapies, Inc. Optionally substituted pyrazolo[3,4-d]pyrimidine-4,6-diones
AU2009239536C1 (en) 2008-04-22 2012-12-13 Merck Sharp & Dohme Corp. Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
BRPI0918449A2 (pt) 2008-09-11 2019-09-24 Amgen Inc compostos de anel espiro-tricíclico como moduladores de beta-secretas e métodos de uso
EP2360155A4 (en) 2008-10-22 2012-06-20 Shionogi & Co 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT
WO2010065152A1 (en) 2008-12-06 2010-06-10 Intra-Cellular Therapies, Inc. Organic compounds
CA2740398A1 (en) 2008-12-06 2010-06-10 Intra-Cellular Therapies, Inc. Organic compounds
CA2740385A1 (en) 2008-12-06 2010-06-10 Intra-Cellular Therapies, Inc. Organic compounds
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation 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
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US20120245155A1 (en) 2009-12-11 2012-09-27 Shionogi & Co., Ltd. Fused heterocyclic compound having amino group
CN102834384A (zh) 2009-12-11 2012-12-19 盐野义制药株式会社 *嗪衍生物
CA2791281A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators
WO2011115928A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as beta - secretase modulators and their medical use
WO2011153135A1 (en) * 2010-05-31 2011-12-08 Intra-Cellular Therapies, Inc. Organic compounds
US9434730B2 (en) 2010-05-31 2016-09-06 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
WO2012057247A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
JP5816630B2 (ja) 2010-10-29 2015-11-18 塩野義製薬株式会社 ナフチリジン誘導体
GB201100181D0 (en) * 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
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
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
WO2012138590A1 (en) * 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
JP2014514302A (ja) 2011-04-13 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション Bace阻害薬としての5−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用
CN103608345A (zh) 2011-04-26 2014-02-26 盐野义制药株式会社 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂
RU2014111055A (ru) 2011-08-22 2015-09-27 Мерк Шарп И Доум Корп. 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
JO3143B1 (ar) 2012-04-03 2017-09-20 Lilly Co Eli مركبات تتراهيدرو بيرولو ثيازين
GB201212871D0 (en) 2012-07-20 2012-09-05 Eisai Ltd Novel compounds
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
US8865723B2 (en) 2012-10-25 2014-10-21 Tetra Discovery Partners Llc Selective PDE4 B inhibition and improvement in cognition in subjects with brain injury
CA2886507C (en) 2012-10-26 2016-09-20 Eli Lilly And Company Bace inhibitors
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
WO2014099788A1 (en) * 2012-12-21 2014-06-26 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
TWI593692B (zh) * 2013-03-12 2017-08-01 美國禮來大藥廠 四氫吡咯并噻嗪化合物
CN103910781B (zh) * 2014-03-18 2016-02-17 重庆大学 一种Aβ聚集抑制剂
US9546175B2 (en) 2014-08-07 2017-01-17 Intra-Cellular Therapies, Inc. Organic compounds
CN104761557B (zh) * 2015-04-08 2017-02-22 河南师范大学 六氢‑1H‑吡咯并[3,4‑d]嘧啶类化合物及其制备方法
PT2017095250B (pt) 2015-11-30 2021-08-06 Univ De Coimbra Peptídeos inibidores da bace1 para o tratamento de doenças neurológicas
CA3088000A1 (en) * 2018-02-28 2019-09-06 Japan Tobacco Inc. Saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds and pharmaceutical use thereof
CN109503582A (zh) * 2018-12-17 2019-03-22 上海合全药物研发有限公司 顺式螺[哌啶并-4,1'-吡咯并[3,4-c]吡咯]-1-甲酸叔丁酯的合成方法
CN115043780B (zh) * 2022-07-11 2024-01-16 上海飞琰化工科技有限公司 一种4-羟基-5-氟-6-乙基嘧啶的合成方法及其应用
KR20240056140A (ko) 2022-10-21 2024-04-30 주식회사 포스코 수거박스 및 이를 이용한 배출방법

Family Cites Families (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7330279B2 (en) * 2002-07-25 2008-02-12 Timbre Technologies, Inc. Model and parameter selection for optical metrology
AR045219A1 (es) * 2003-08-08 2005-10-19 Pharmacopeia Inc Aminas ciclicas inhibidoras de base - 1 que poseen un sustiuyente heterociclico
ATE424383T1 (de) 2003-08-08 2009-03-15 Schering Corp Cyclische amine mit benzamidsubstituent als bace- 1-inhibitoren
CA2548388A1 (en) 2003-12-15 2005-06-30 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) * 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2006009655A1 (en) * 2004-06-16 2006-01-26 Wyeth Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase
MXPA06014793A (es) 2004-06-16 2007-02-16 Wyeth Corp Derivados de amino-5, 5-difenilimidazolona para la inhibicion de ??-secretasa.
AR049726A1 (es) 2004-07-22 2006-08-30 Schering Corp Amidas sustituidas inhibidoras de beta secretasa
CA2575340A1 (en) 2004-07-28 2006-02-09 Schering Corporation Macrocyclic beta-secretase inhibitors
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
JP5046932B2 (ja) 2004-08-06 2012-10-10 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ β−セクレターゼ(BACE)のインヒビターとして有用な新規の2−アミノ−キナゾリン誘導体
ES2349594T3 (es) 2004-08-06 2011-01-05 Janssen Pharmaceutica Nv Derivados de 2-amino-quinazolín usados como inhibidores de b-secretase (bace).
CN101084198A (zh) * 2004-10-15 2007-12-05 阿斯利康(瑞典)有限公司 取代的氨基-嘧啶酮及其用途
RU2007126570A (ru) 2005-01-14 2009-02-20 Вайет (Us) Аминоимидазолоны, применяемые для ингибирования бета-секретазы
US7759353B2 (en) 2005-06-14 2010-07-20 Schering Corporation Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment
AR054620A1 (es) 2005-06-14 2007-07-04 Schering Corp Inhibidores de aspartil proteasas
AR053902A1 (es) 2005-06-14 2007-05-23 Schering Corp Inhibidores de aspartil proteasa heterociclicos macrociclicos
EP1896478B1 (en) * 2005-06-14 2014-05-21 Merck Sharp & Dohme Corp. Aspartyl protease inhibitors
BRPI0613578A2 (pt) 2005-06-30 2012-01-17 Wyeth Corp composito da fórmula i; uso de um composto de fórmula i; e composição farmacêutica
TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
TW200730523A (en) * 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
CN101273018A (zh) 2005-09-26 2008-09-24 惠氏公司 用于β分泌酶(BACE)抑制剂的氨基-5-[4-(二氟甲氧基)苯基]-5-苯基咪唑酮化合物
ES2537898T3 (es) 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
EP1966198B1 (en) * 2005-10-25 2011-03-16 Janssen Pharmaceutica NV 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of beta-secretase (bace)
WO2007050721A2 (en) 2005-10-27 2007-05-03 Schering Corporation Heterocyclic aspartyl protease inhibitors
CA2628264A1 (en) * 2005-10-31 2007-05-10 Schering Corporation Aspartyl protease inhibitors
AR058381A1 (es) * 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
WO2007092846A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
WO2007092839A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. Macrocycle derivatives useful as inhibitors of beta-secretase (bace)
WO2007092854A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
WO2007100536A1 (en) * 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
US20090099217A1 (en) 2006-04-05 2009-04-16 Astex Therapeutics Ltd. 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies
AU2007258435A1 (en) 2006-06-12 2007-12-21 Schering Corporation Heterocyclic aspartyl protease inhibitors
TW200815447A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds IV
TW200808796A (en) * 2006-06-14 2008-02-16 Astrazeneca Ab New compounds III
US20080051420A1 (en) * 2006-06-14 2008-02-28 Astrazeneca Ab New Compounds 317
TW200815449A (en) * 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
TW200817406A (en) 2006-08-17 2008-04-16 Wyeth Corp Imidazole amines as inhibitors of β-secretase
TW200831484A (en) * 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
EP2689780A1 (en) 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group
TW200902499A (en) * 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
TW200902503A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
WO2009005470A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
WO2009005471A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
CA2687750C (en) 2007-07-06 2016-10-18 Boehringer Ingelheim International Gmbh Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture
WO2009038686A2 (en) 2007-09-14 2009-03-26 Tessera Technologies Hungary Kft. Hermetic wafer level cavity package
DE102007052733A1 (de) 2007-11-06 2009-05-07 Krones Ag Geländerführung
PT2233474E (pt) 2008-01-18 2015-10-26 Eisai R&D Man Co Ltd Derivado de aminodihidrotiazina condensado
TW200932218A (en) 2008-01-22 2009-08-01 Boehringer Ingelheim Int Substituted amino-benzimidazoles, medicaments comprising said compound, their use and their method of manufacture
MX2010008202A (es) 2008-01-28 2010-12-06 Janssen Pharmaceutica Nv Derivados de tio-2-aminoquinolina 6-sustituida utiles como inhibidores de beta-secretasa (bace).
RU2010136050A (ru) 2008-01-29 2012-03-10 Янссен Фармацевтика Нв (Be) 2-аминохинолиновые производные для использования в качестве ингибиторов секретазы (васе)
WO2009103626A1 (en) * 2008-02-18 2009-08-27 F. Hoffmann-La Roche Ag 4, 5-dihydro-oxazol-2-yl amine derivatives
US8492387B2 (en) 2008-02-28 2013-07-23 Merck, Sharp & Dohme, Corp. 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
AU2009239536C1 (en) 2008-04-22 2012-12-13 Merck Sharp & Dohme Corp. Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
ES2433223T3 (es) 2008-07-28 2013-12-10 Eisai R&D Management Co., Ltd. Derivados de espiroaminodihidrotiazina
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
US8198269B2 (en) 2008-09-30 2012-06-12 Eisai R&D Management Co., Ltd. Fused aminodihydrothiazine derivative
EP2360155A4 (en) 2008-10-22 2012-06-20 Shionogi & Co 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT
US20100125081A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
EP2376083A4 (en) 2008-11-20 2012-06-20 Purdue Research Foundation QUINAZOLIN-BASED BACE-1 INHIBITORS AND METHODS OF USE

Also Published As

Publication number Publication date
US20110110957A1 (en) 2011-05-12
US20110110927A1 (en) 2011-05-12
AR071385A1 (es) 2010-06-16
WO2009131974A8 (en) 2010-03-18
EP2283016B1 (en) 2014-09-24
WO2009131974A1 (en) 2009-10-29
JP2011518225A (ja) 2011-06-23
EP2288613A1 (en) 2011-03-02
AU2009239536C1 (en) 2012-12-13
CN102066380A (zh) 2011-05-18
EA201001532A1 (ru) 2011-06-30
PE20091734A1 (es) 2009-11-13
AU2009239536B2 (en) 2012-06-28
CO6321265A2 (es) 2011-09-20
DOP2010000320A (es) 2010-12-15
CA2721738A1 (en) 2009-10-29
MX2010011563A (es) 2010-11-12
AU2009239536A1 (en) 2009-10-29
SV2010003714A (es) 2011-02-08
TW200948364A (en) 2009-12-01
CA2723222A1 (en) 2009-10-29
CR11738A (es) 2011-01-10
AR072952A1 (es) 2010-10-06
CL2009000954A1 (es) 2010-12-31
EP2283016A1 (en) 2011-02-16
TW201004957A (en) 2010-02-01
JP2011518224A (ja) 2011-06-23
BRPI0911356A2 (pt) 2019-09-24
US8450331B2 (en) 2013-05-28
IL208465A0 (en) 2010-12-30
MA32252B1 (fr) 2011-04-01
ECSP10010585A (es) 2011-04-29
AU2009239535A1 (en) 2009-10-29
EP2288613B1 (en) 2016-07-13
ZA201007433B (en) 2011-06-29
WO2009131975A1 (en) 2009-10-29
CA2723222C (en) 2013-04-02
KR20110003347A (ko) 2011-01-11
CL2009000953A1 (es) 2010-12-31
US8541427B2 (en) 2013-09-24

Similar Documents

Publication Publication Date Title
PE20091834A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona tiofenilo-sustituida como inhibidores de bace-1 y composiciones que los contienen
PE20141726A1 (es) Heterociclilaminas como inhibidores de pi 3k
NI201100081A (es) Aminotetrahidropiranos como inhibidores de dipeptidil peptidasa - iv para el tratamiento o prevención de diabetes.
ECSP088765A (es) Aminotetrahidropiranos como inhibidores de dipeptidil peptidasa-iv para el tratamiento o prevención de diabetes
PE20120505A1 (es) Derivados de 1-heterociclil-1,5-dihidro-pirazolo[3,4-d]pirimidin-4-ona como moduladores de pde9a
PE20090362A1 (es) Derivados de piperidina/piperazina como moduladores de dgat
PE20091376A1 (es) Derivados de fenilamino como moduladores de beta-amiloide
CR11491A (es) Derivados de tiazol usados como inhibidores de pi 3-cinasa
CR10383A (es) Derivados triazolopirazina.
CO6341581A2 (es) Derivados de heteroarilo como inhibidores de dgat1
UY32543A (es) Análogos de isoxazol-3(2h)-ona como agentes terapéuticos
EA201101618A1 (ru) Арилпиридины в качестве ингибиторов альдостеронсинтазы
SV2011003855A (es) Heteroarilos sustituidos
CO6290658A2 (es) Derivados de azetidina y ciclobutano como inhibidores de jack
PE20070367A1 (es) Compuestos de espiropiperidina como inhibidores de la enzima beta secretasa
ECSP088103A (es) Nuevos derivados de 2-azetidinona como inhibidores de la absorción del colesterol para el tratamiento de condiciones de hiperlipidemia
PE20121182A1 (es) Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina
UY31870A (es) Receptor metabotrópico de glutamato potenciadores 286
ECSP15012804A (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
CR8246A (es) Forma cristalina gamma-d del clorhidrato de ivabradina, su procedimiento de preparacion y composiciones farmaceuticas que las contienen
AR082968A1 (es) Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto
CO6270285A2 (es) Derivados de 4-[(4-amino-1, 3, 5-triazin-2-il)amino]-n-arilmetilcicloalquilcarboxamida
ECSP088257A (es) Derivados de amida
CR9472A (es) Derivados de aminoacidos
UY30673A1 (es) Derivados 6, 7 y 8 sustituidos del acido (3r)-5-oxo-2,3-dihidro-5h-tiazolo[3,2a]piridin-3-carboxilico, composiciones farmacéuticas conteniéndolos y aplicaciones.

Legal Events

Date Code Title Description
FD Application declared void or lapsed