GEP20186880B - 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease - Google Patents

2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Info

Publication number
GEP20186880B
GEP20186880B GEAP201213485A GEAP2012013485A GEP20186880B GE P20186880 B GEP20186880 B GE P20186880B GE AP201213485 A GEAP201213485 A GE AP201213485A GE AP2012013485 A GEAP2012013485 A GE AP2012013485A GE P20186880 B GEP20186880 B GE P20186880B
Authority
GE
Georgia
Prior art keywords
alzheimer
treatment
tetrahydropyridines
trifluoro
disease
Prior art date
Application number
GEAP201213485A
Other languages
English (en)
Inventor
Ingelheim International Gmbh Boehringer
Original Assignee
Ingelheim International Gmbh Boehringer
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
Application filed by Ingelheim International Gmbh Boehringer filed Critical Ingelheim International Gmbh Boehringer
Publication of GEP20186880B publication Critical patent/GEP20186880B/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Immunology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Infusion, Injection, And Reservoir Apparatuses (AREA)
GEAP201213485A 2011-11-02 2012-10-29 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease GEP20186880B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11187553 2011-11-02

Publications (1)

Publication Number Publication Date
GEP20186880B true GEP20186880B (en) 2018-07-25

Family

ID=47073464

Family Applications (1)

Application Number Title Priority Date Filing Date
GEAP201213485A GEP20186880B (en) 2011-11-02 2012-10-29 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Country Status (34)

Country Link
US (4) US8759349B2 (enExample)
EP (1) EP2773633B1 (enExample)
JP (1) JP6091513B2 (enExample)
KR (1) KR102006612B1 (enExample)
CN (2) CN104024244B (enExample)
AP (1) AP2014007670A0 (enExample)
AU (1) AU2012331274B2 (enExample)
BR (1) BR112014010583A2 (enExample)
CA (1) CA2854217C (enExample)
CL (1) CL2014001047A1 (enExample)
CO (1) CO6940429A2 (enExample)
CY (1) CY1120974T1 (enExample)
DK (1) DK2773633T3 (enExample)
EA (1) EA025158B9 (enExample)
EC (1) ECSP14001929A (enExample)
ES (1) ES2645744T3 (enExample)
GE (1) GEP20186880B (enExample)
HR (1) HRP20171614T1 (enExample)
HU (1) HUE034929T2 (enExample)
IL (1) IL232035A (enExample)
LT (1) LT2773633T (enExample)
ME (1) ME02905B (enExample)
MX (1) MX348522B (enExample)
NO (1) NO2773633T3 (enExample)
PE (1) PE20141607A1 (enExample)
PH (1) PH12014500970B1 (enExample)
PL (1) PL2773633T3 (enExample)
PT (1) PT2773633T (enExample)
RS (1) RS56498B1 (enExample)
SG (1) SG11201401907TA (enExample)
SI (1) SI2773633T1 (enExample)
TN (1) TN2014000180A1 (enExample)
UA (1) UA115868C2 (enExample)
WO (1) WO2013064450A1 (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2006332726B2 (en) 2005-12-28 2012-12-13 Vertex Pharmaceuticals Incorporated. Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
JP6091513B2 (ja) 2011-11-02 2017-03-08 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 複素環化合物、前記化合物を含む薬物、これらの使用及びこれらの調製方法
CN105518000B (zh) * 2013-07-02 2018-09-14 加州生物医学研究所 用于治疗囊性纤维化的化合物
WO2015003958A1 (en) * 2013-07-08 2015-01-15 Boehringer Ingelheim International Gmbh Amiloride-type compounds as inhibitors in epithelial sodium channels for the treatment of diseases of the lungs and airways
CN107250113B (zh) 2014-10-07 2019-03-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调节蛋白的调节剂的共晶
BR112017008178A2 (pt) * 2014-10-24 2017-12-19 Ono Pharmaceutical Co ativador do canal de kcnq2-5
WO2016112120A1 (en) * 2015-01-07 2016-07-14 The California Institute For Biomedical Research Compounds for treatment of cystic fibrosis
GB201610854D0 (en) 2016-06-21 2016-08-03 Entpr Therapeutics Ltd Compounds
GB201619694D0 (en) 2016-11-22 2017-01-04 Entpr Therapeutics Ltd Compounds
GB201717051D0 (en) 2017-10-17 2017-11-29 Enterprise Therapeutics Ltd Compounds
GB201808093D0 (en) 2018-05-18 2018-07-04 Enterprise Therapeutics Ltd Compounds
AU2021341508A1 (en) 2020-09-10 2023-05-25 Precirix N.V. Antibody fragment against fap
CN112107580A (zh) * 2020-09-29 2020-12-22 北京鑫开元医药科技有限公司 一种脾酪氨酸激酶抑制剂的制剂组合物及其制备方法
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
CN119584994A (zh) 2022-05-02 2025-03-07 普雷西里克斯公司 预靶向
WO2024243025A1 (en) * 2023-05-19 2024-11-28 Ikena Oncology, Inc. Naphthyl-substituted pyrido[4,3-d]pyrimidines and related compounds and their use in treating medical conditions

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL6812003A (enExample) 1967-09-07 1969-03-11
US3953476A (en) 1971-12-27 1976-04-27 Merck & Co., Inc. 3-Amino-5-sulfonylbenzoic acids
CA2378181A1 (en) 1999-07-19 2001-01-25 Richard C. Boucher, Jr. Conjugates of sodium channel blockers and methods of using the same
AU2001229501A1 (en) 2000-01-24 2001-07-31 Isis Pharmaceuticals, Inc. Antisense modulation of inducible nitric oxide synthase expression
CA2575670A1 (en) 2004-08-18 2006-03-02 Michael R. Johnson Aliphatic amide & ester pyrazinoylguanidine sodium channel blockers
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
US20080124276A1 (en) * 2006-07-24 2008-05-29 Lifeline Cell Technology Synthetic cornea from retinal stem cells
CN101687851B (zh) * 2007-05-07 2013-02-27 诺瓦提斯公司 有机化合物
EA017919B1 (ru) 2007-12-10 2013-04-30 Новартис Аг Производные пиразин-2-карбоксамида для лечения заболеваний, которые поддаются лечению путем блокирования эпителиальных натриевых каналов
BRPI0912542A2 (pt) * 2008-05-13 2015-10-13 Novartis Ag derivados de ácido 3,5-diamino-cloro-pirazina-2-carboxílico e seu uso como bloqueadores do canal de sódio epitelial para o tratamento de vias aéreas.
EA201001848A1 (ru) 2008-06-10 2011-08-30 Новартис Аг Производные пиразина в качестве блокаторов эпителиальных натриевых каналов
US9050339B2 (en) 2010-09-17 2015-06-09 Novartis Ag Pyrazine derivatives as ENaC blockers
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
EP2723176B1 (en) 2011-06-27 2017-04-12 Parion Sciences, Inc. A chemically and metabolically stable dipeptide possessing potent sodium channel blocker activity
AR086745A1 (es) 2011-06-27 2014-01-22 Parion Sciences Inc 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida
JP2015501324A (ja) 2011-11-02 2015-01-15 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 アシルグアニジン及びアシルチオ尿素の新規調製方法
JP6091513B2 (ja) 2011-11-02 2017-03-08 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 複素環化合物、前記化合物を含む薬物、これらの使用及びこれらの調製方法

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Publication number Publication date
CN106279110B (zh) 2019-12-10
TN2014000180A1 (en) 2015-09-30
RS56498B1 (sr) 2018-01-31
CA2854217C (en) 2019-12-31
EP2773633B1 (en) 2017-08-02
PT2773633T (pt) 2017-11-14
CN104024244A (zh) 2014-09-03
CA2854217A1 (en) 2013-05-10
EA201400521A1 (ru) 2014-09-30
LT2773633T (lt) 2017-11-10
AU2012331274B2 (en) 2017-06-08
US20130109697A1 (en) 2013-05-02
CN106279110A (zh) 2017-01-04
KR102006612B1 (ko) 2019-08-02
JP2014534222A (ja) 2014-12-18
WO2013064450A1 (en) 2013-05-10
MX2014005166A (es) 2014-05-28
CO6940429A2 (es) 2014-05-09
IL232035A (en) 2017-05-29
PH12014500970B1 (en) 2017-10-06
CY1120974T1 (el) 2019-12-11
UA115868C2 (uk) 2018-01-10
PH12014500970A1 (en) 2014-06-09
EP2773633A1 (en) 2014-09-10
BR112014010583A2 (pt) 2020-04-22
AU2012331274A1 (en) 2014-04-03
AP2014007670A0 (en) 2014-05-31
HRP20171614T1 (hr) 2017-12-01
MX348522B (es) 2017-06-16
NO2773633T3 (enExample) 2017-12-30
US20140228374A1 (en) 2014-08-14
DK2773633T3 (da) 2017-11-13
HUE034929T2 (en) 2018-03-28
US9920035B2 (en) 2018-03-20
ME02905B (me) 2018-10-20
JP6091513B2 (ja) 2017-03-08
HK1196819A1 (zh) 2014-12-24
PE20141607A1 (es) 2014-11-23
IL232035A0 (en) 2014-05-28
US8759349B2 (en) 2014-06-24
US20180194747A1 (en) 2018-07-12
NZ622469A (en) 2016-08-26
PL2773633T3 (pl) 2018-01-31
KR20140085498A (ko) 2014-07-07
EA025158B1 (ru) 2016-11-30
CL2014001047A1 (es) 2014-11-07
SI2773633T1 (sl) 2017-11-30
CN104024244B (zh) 2016-09-14
US20150336933A1 (en) 2015-11-26
ES2645744T3 (es) 2017-12-07
ECSP14001929A (es) 2015-11-30
SG11201401907TA (en) 2014-05-29
EA025158B9 (ru) 2018-03-30

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