MX2013002398A - Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes. - Google Patents

Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes.

Info

Publication number
MX2013002398A
MX2013002398A MX2013002398A MX2013002398A MX2013002398A MX 2013002398 A MX2013002398 A MX 2013002398A MX 2013002398 A MX2013002398 A MX 2013002398A MX 2013002398 A MX2013002398 A MX 2013002398A MX 2013002398 A MX2013002398 A MX 2013002398A
Authority
MX
Mexico
Prior art keywords
diabetes
treatment
bace inhibitors
present
isophthalamides
Prior art date
Application number
MX2013002398A
Other languages
English (en)
Inventor
Harald Mauser
Mathias Nettekoven
Sebastien Schmitt
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2013002398A publication Critical patent/MX2013002398A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28Radicals substituted by nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/547Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/06Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms

Abstract

La presente invención está relacionada con las N-1-bencil-2-hidroxi-3-(hetero) arilamino-propil) isoftalamidas de la fórmula (I) que tiene actividad inhibidora de BACE2 y a su uso como substancias terapéuticamente activas, a su manufactura y a las composiciones farmacéuticas. Los compuestos activos de la presente invención son útiles en el tratamiento terapéutico y/o profiláctico por ejemplo de la diabetes del tipo 2.
MX2013002398A 2010-09-01 2011-08-29 Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes. MX2013002398A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10174819 2010-09-01
PCT/EP2011/064778 WO2012028563A1 (en) 2010-09-01 2011-08-29 Bace inhibitors for use in the treatment of diabetes

Publications (1)

Publication Number Publication Date
MX2013002398A true MX2013002398A (es) 2013-04-03

Family

ID=44511021

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013002398A MX2013002398A (es) 2010-09-01 2011-08-29 Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes.

Country Status (10)

Country Link
US (1) US20120053200A1 (es)
EP (1) EP2611441A1 (es)
JP (1) JP2013540709A (es)
KR (1) KR20130099077A (es)
CN (1) CN103079562A (es)
BR (1) BR112013004386A2 (es)
CA (1) CA2809222A1 (es)
MX (1) MX2013002398A (es)
RU (1) RU2013112560A (es)
WO (1) WO2012028563A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9096541B2 (en) 2012-03-29 2015-08-04 Oklahoma Medical Research Foundation Inhibition of memapsin 1 cleavage in the treatment of diabetes
CN104910097A (zh) * 2015-02-10 2015-09-16 佛山市赛维斯医药科技有限公司 一类含苯基脒结构的卤代苯基噻唑羧酸酰胺类化合物、其制备方法及用途
PE20171349A1 (es) 2015-03-20 2017-09-13 Hoffmann La Roche Inhibidores de bace1
WO2017066742A1 (en) * 2015-10-16 2017-04-20 Jortan Pharmaceuticals Inc. Bace-2 inhibitory compounds and related methods of use

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20080015079A (ko) * 2005-04-08 2008-02-18 코멘티스, 인코포레이티드 베타 세크레타제 활성을 억제하는 화합물 및 이것의 사용방법
ZA200709236B (en) * 2005-04-08 2009-06-24 Comentis Inc Compounds which inhibit beta-secretase activity and methods of use thereof
JP2009504614A (ja) * 2005-08-11 2009-02-05 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 アルツハイマー病の治療用化合物
EP1915339A1 (de) * 2005-08-11 2008-04-30 Boehringer Ingelheim International GmbH Inhibitoren der beta-sekretase zur behandlung der alzheimer- erkrankung
WO2009015369A2 (en) 2007-07-26 2009-01-29 Comentis, Inc. Compounds which inhibit beta-secretase activity and methods of use thereof
WO2009042694A1 (en) * 2007-09-24 2009-04-02 Comentis, Inc. (3-hydroxy-4-amino-butan-2-yl) -3- (2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating
WO2009042964A1 (en) * 2007-09-28 2009-04-02 Schweitzer Engineering Laboratories, Inc. Amplitude and phase comparators for line protection
CA2739875A1 (en) * 2008-10-10 2010-04-15 Comentis, Inc. Pyrrolidine compounds which inhibit beta-secretase activity and methods of use thereof
WO2010063718A1 (en) * 2008-12-02 2010-06-10 ETH Zürich Screening assay for metabolic disease therapeuticals

Also Published As

Publication number Publication date
KR20130099077A (ko) 2013-09-05
CN103079562A (zh) 2013-05-01
EP2611441A1 (en) 2013-07-10
WO2012028563A1 (en) 2012-03-08
RU2013112560A (ru) 2014-10-10
BR112013004386A2 (pt) 2016-05-17
JP2013540709A (ja) 2013-11-07
US20120053200A1 (en) 2012-03-01
CA2809222A1 (en) 2012-03-08

Similar Documents

Publication Publication Date Title
MX2013007558A (es) 1,4-oxazinas como inhibidores de los genes enzima de segmentacion de la proteina precursora del sitio 1 y/o 2 (bace1 y/o bace2).
MX2013007957A (es) 1,4-oxazinas como inhibidores de los genes de enzima de segmentacion de la proteina precursora amiloide del sitio beta 1 y/o (bace1 y/o bace2).
MX2013013692A (es) Halogenoalquil-1,3-oxazinas como inhibidores de beta secretasa 1 (bace1) y/o beta secretasa 2 (bace2).
MX2013010795A (es) 1,3 oxazinas como inhibidores de beta-secretasa 1 (bace 1) y/o la beta-secretasa 2 (beta 2).
EA201391752A1 (ru) Спиро-[1,3]-оксазины и спиро-[1,4]-оксазепины в качестве ингибиторов bace1 и/или bace2
MY169962A (en) 2-amino-5,5-difluoro-5,6-dihydro-oxazines as bace 1 and/or bace 2 inhibitors
MX2013014007A (es) [1,3] oxazinas.
MX2013008478A (es) 1, 4 riazepinas/sulfonas como inhibidores de beta secretasa 1 (base1) y/o beta secretasa 2 (bace2).
MX2012001985A (es) Derivados de 3-amino-5-fenil-5,6-dihidro-2h-[1,4]oxazina.
EA201391670A1 (ru) 1,3-оксазины в качестве ингибиторов bace1 и/или bace2
MX2013014194A (es) 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).
MX336381B (es) Boronatos como inhibidores de arginasa.
MX2015003653A (es) Derivados de amida del acido benzoimidazol-carboxilico como moduladores del receptor apj.
MX2013008213A (es) N-[3-(5-amino-3,3a,7,7a-tetrahidro-1h-2,4-dioxa-6-aza-inden-7-il) -fenil]-amidas como inhibidores de beta-secretasa 1 (bace1) y/o beta-secretasa 2 (bace2).
MX2015008957A (es) Fluoro-[1,3]oxazinas como inhibidores de beta-secretasa 1 (bace1).
EP2571876A4 (en) SUBSTITUTED SEVEN-HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL-PEPTIDASE IV INHIBITORS FOR THE TREATMENT OF DIABETES
MX2011011854A (es) Dihidropirimidinonas para uso como inhibidores de la bace2.
IN2012DN01233A (es)
PH12014501334A1 (en) Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
MX2014003408A (es) N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][ 1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la beta-secretasa 1 (bace1).
PH12015502365A1 (en) Bace1 inhibitors
PH12014502541A1 (en) 5-amino [1,4] thiazines as bace 1 inhibitors
PH12014502623B1 (en) Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors
WO2011006935A3 (en) Tetrazole derivatives
MX2013002398A (es) Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal