PE20141110A1 - Derivados heterociclicos novedosos para el tratamiento de trastornos neurologicos - Google Patents

Derivados heterociclicos novedosos para el tratamiento de trastornos neurologicos

Info

Publication number
PE20141110A1
PE20141110A1 PE2013001546A PE2013001546A PE20141110A1 PE 20141110 A1 PE20141110 A1 PE 20141110A1 PE 2013001546 A PE2013001546 A PE 2013001546A PE 2013001546 A PE2013001546 A PE 2013001546A PE 20141110 A1 PE20141110 A1 PE 20141110A1
Authority
PE
Peru
Prior art keywords
novelty
treatment
neurological disorders
heterocyclic derivatives
halogen
Prior art date
Application number
PE2013001546A
Other languages
English (en)
Inventor
Sangamesh Badiger
Murali Chebrolu
Konstanze Hurth
Sebastien Jacquier
Rainer Martin Lueoend
Rainer Machauer
Heinrich Rueeger
Marina Tintelnot-Blomley
Siem Jacob Veenstra
Markus Voegtle
Original Assignee
Novartis Ag
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=46491227&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20141110(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20141110A1 publication Critical patent/PE20141110A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P25/28Drugs 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds

Abstract

REFERIDO A COMPUESTOS DE FORMULA (I) DONDE: X ES CR1 O N; X3 ES CR3 O N; X4 ES CR4 O N; X5 ES CR5 O N; EN DONDE AL MENOS UNO DE X1,X3,X4 Y X5 ES N Y NO MAS DE 2 ENTRE X1, X3, X4, Y X5 SON N; O X1 ES CR1 O N; X3 ES CR3, N O S; X4 ES UN ENLACE; X5 ES CR5, N O S; EN DONDE AL MENOS UNO DE X1, X3 Y X5 ES N O S, NO MAS DE 2 ENTRE X1, X3 Y X5 SON N Y NO MAS DE 1 ENTRE X3 Y X5 SON S; R1, R3, R4 Y R5 SON INDEPENDIENTEMENTE H, CIANO, HALOGENO, (C2-8)ALQUINILO, ENTRE OTROS; R6 ES (C1-8)ALQUILO, HALOGENO-(C1-8)ALQUILO, (C2-8)ALQUINILO, ENTRE OTROS; R2 ES HETEROARILO O HETEROCICLICO NO AROMATICO, ENTRE OTROS; E1 ES -C(R7)(R8)-, ENTRE OTROS; E2 ES -C(R11)(R12)-, ENTRE OTROS; R7, R8, R11 Y R12 SON INDEPENDIENTEMENTE H, CIANO, HALOGENO, ENTRE OTROS. ES UN COMPUESTO PREFERIDO: [6-(5-AMINO-3-METIL-3,6-DIHIDRO-2H-[1,4]-OXAZIN-3-IL)-PIRIDIN-2-IL]-AMIDA DEL ACIDO 5-BROMO-PIRIDINA-2-CARBOXILICO, ENTRE OTROS. REFERIDO ADEMAS A UNA COMPOSICION Y A UNA COMBINACION FARMACEUTICA
PE2013001546A 2011-01-13 2012-01-11 Derivados heterociclicos novedosos para el tratamiento de trastornos neurologicos PE20141110A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN77DE2011 2011-01-13
US201161534591P 2011-09-14 2011-09-14

Publications (1)

Publication Number Publication Date
PE20141110A1 true PE20141110A1 (es) 2014-09-05

Family

ID=46491227

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013001546A PE20141110A1 (es) 2011-01-13 2012-01-11 Derivados heterociclicos novedosos para el tratamiento de trastornos neurologicos

Country Status (40)

Country Link
US (6) US8637508B2 (es)
EP (1) EP2663561B1 (es)
JP (1) JP5715710B2 (es)
KR (1) KR101569260B1 (es)
CN (2) CN103403001B (es)
AP (1) AP3807A (es)
AR (1) AR084849A1 (es)
AU (1) AU2012206561B2 (es)
CA (1) CA2824220C (es)
CL (2) CL2013001964A1 (es)
CO (1) CO6751293A2 (es)
CR (1) CR20130339A (es)
CU (1) CU20130101A7 (es)
CY (1) CY1117580T1 (es)
DK (1) DK2663561T3 (es)
EA (1) EA024059B1 (es)
ES (1) ES2576182T3 (es)
GT (1) GT201300179A (es)
HK (1) HK1188453A1 (es)
HR (1) HRP20160647T1 (es)
HU (1) HUE029226T2 (es)
IL (1) IL227294A (es)
JO (1) JO3146B1 (es)
MA (1) MA34898B1 (es)
ME (1) ME02409B (es)
MX (1) MX336966B (es)
MY (1) MY162413A (es)
PE (1) PE20141110A1 (es)
PL (1) PL2663561T3 (es)
PT (1) PT2663561E (es)
RS (1) RS54782B1 (es)
SG (1) SG191812A1 (es)
SI (1) SI2663561T1 (es)
SM (1) SMT201600144B (es)
TN (1) TN2013000285A1 (es)
TW (1) TWI531570B (es)
UA (1) UA113051C2 (es)
UY (1) UY33865A (es)
WO (1) WO2012095469A1 (es)
ZA (1) ZA201304921B (es)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103936690B (zh) 2005-10-25 2016-06-08 盐野义制药株式会社 氨基二氢噻嗪衍生物
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
MX2009011498A (es) 2007-04-24 2009-11-10 Shionogi & Co Derivados de aminodihidrotiazina sustituida con un grupo ciclico.
KR20130018370A (ko) 2008-06-13 2013-02-20 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
DK2987487T3 (da) 2009-08-10 2020-12-07 Samumed Llc Indazolinhibitorer af wnt-signalvejen og terapeutiske anvendelser deraf
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011071135A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
DK3001903T3 (en) 2009-12-21 2017-12-18 Samumed Llc 1H-PYRAZOLO [3,4 -?] PYRIDINES AND THERAPEUTIC APPLICATIONS THEREOF
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
US8927721B2 (en) 2010-10-29 2015-01-06 Shionogi & Co., Ltd. Naphthyridine derivative
CA2824220C (en) 2011-01-13 2020-09-01 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
US20140128385A1 (en) * 2011-01-13 2014-05-08 Novartis Ag Bace-2 inhibitors for the treatment of metabolic disorders
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するbace1阻害剤
AU2012308570B2 (en) 2011-09-14 2016-11-10 Samumed, Llc Indazole-3-carboxamides and their use as Wnt/b-catenin signaling pathway inhibitors
AU2012322329A1 (en) 2011-10-13 2014-05-01 Novartis Ag Novel oxazine derivatives and their use in the treatment of disease
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
WO2013161929A1 (ja) * 2012-04-26 2013-10-31 塩野義製薬株式会社 ピリジニルモルホリノン誘導体およびそれらを含有する医薬組成物
DK2770994T3 (da) 2012-05-04 2019-11-11 Samumed Llc 1h-pyrazolo[3,4-b]pyridiner og terapeutiske anvendelser deraf
WO2014065434A1 (en) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
CN105120862A (zh) 2013-01-08 2015-12-02 萨穆梅德有限公司 Wnt信号途径的3-(苯并咪唑-2-基)-吲唑抑制剂及其治疗应用
WO2014134341A1 (en) 2013-03-01 2014-09-04 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
WO2014166906A1 (en) 2013-04-11 2014-10-16 F. Hoffmann-La Roche Ag Bace1 inhibitors
UA117695C2 (uk) * 2014-02-19 2018-09-10 Х. Луннбек А/С 2-аміно-3,5,5-трифтор-3,4,5,6-тетрагідропіридини як інгібітори bace1 для лікування хвороби альцгеймера
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040188A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040182A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
US10226448B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-yl)-1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
US10206908B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017023980A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10604512B2 (en) 2015-08-03 2020-03-31 Samumed, Llc 3-(1H-indol-2-yl)-1H-indazoles and therapeutic uses thereof
WO2017024026A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10226453B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017024015A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10231956B2 (en) 2015-08-03 2019-03-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023972A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10188634B2 (en) 2015-08-03 2019-01-29 Samumed, Llc 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
WO2017024004A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
US10392383B2 (en) 2015-08-03 2019-08-27 Samumed, Llc 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, LLC 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10519169B2 (en) 2015-08-03 2019-12-31 Samumed, Llc 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017024021A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
TW201717948A (zh) 2015-08-10 2017-06-01 H 朗德貝克公司 包括給予2-胺基-3,5,5-三氟-3,4,5,6-四氫吡啶的聯合治療
EP3334720A1 (en) 2015-08-12 2018-06-20 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors
JP2018531924A (ja) 2015-09-24 2018-11-01 ファイザー・インク テトラヒドロピラノ[3,4−d][1,3]オキサジン誘導体、およびbace阻害剤としてのその使用
CA3004297A1 (en) 2015-11-06 2017-05-11 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-c]pyridines and their anti-inflammatory uses thereof
CN108699051B (zh) 2016-03-01 2021-12-24 豪夫迈·罗氏有限公司 Bace1抑制剂
PL3464285T3 (pl) 2016-06-01 2023-02-06 Biosplice Therapeutics, Inc. Sposób wytwarzania n-(5-(3-(7-(3-fluorofenylo)-3h-imidazo[4,5-c]pirydyn-2-ylo)-1h-indazol-5-ilo)pirydyn-3-ylo)-3-metylobutanoamidu
US11834444B2 (en) 2016-07-07 2023-12-05 Cyclerion Therapeutics, Inc. Processes for preparation of soluble guanylate cyclase stimulators
JOP20190003A1 (ar) * 2016-07-19 2019-01-10 Novartis Ag مشتق أوكسازين للاستخدام في الوقاية من مرض ألزهايمر في مرضى عُرضه للخطر
JOP20190081A1 (ar) * 2016-10-13 2019-04-11 Novartis Ag مشتق أوكسازين للاستخدام في علاج أو الوقاية من اعتلال وعائي دماغي نشواني
JP2019535672A (ja) 2016-10-21 2019-12-12 サミュメッド リミテッド ライアビリティ カンパニー インダゾール−3−カルボキサミドの使用方法およびwnt/β−カテニンシグナル伝達経路阻害剤としてのそれらの使用
MA46696A (fr) 2016-11-07 2019-09-11 Samumed Llc Formulations injectables à dose unique prêtes à l'emploi
MX2019007103A (es) 2016-12-15 2019-11-05 Amgen Inc Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.
MX2019007104A (es) 2016-12-15 2019-11-05 Amgen Inc Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso.
CA3047285A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
AU2017376441B2 (en) 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
JOP20190178A1 (ar) * 2017-01-20 2019-07-16 Novartis Ag تركيبة صيدلانية تتضمن مشتق أوكسازين واستخدامها في علاج أو الوقاية من مرض الزهايمر
WO2019142111A1 (en) 2018-01-18 2019-07-25 Novartis Ag Salt forms of an oxazine derivative bace inhibitor
CN108997202A (zh) * 2018-07-10 2018-12-14 湖南华腾制药有限公司 一种(5-三氟甲基-吡啶-2-基)-乙酸盐的制备方法

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL6911868A (es) 1968-08-31 1970-03-03
IL112778A0 (en) 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
DE19725802A1 (de) 1996-07-10 1998-01-15 Lonza Ag Verfahren zur Herstellung von (S)- oder (R)-3,3,3-trifluor-2-hydroxy-2-methylpropionsäure
GB9900416D0 (en) * 1999-01-08 1999-02-24 Alizyme Therapeutics Ltd Inhibitors
TW200303742A (en) 2001-11-21 2003-09-16 Novartis Ag Organic compounds
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
CA2525764C (en) 2003-05-20 2012-07-17 Novartis Ag N-acyl nitrogen heterocycles as ligands of peroxisome proliferator-activated receptors
JP2007524682A (ja) 2004-02-12 2007-08-30 メルク エンド カムパニー インコーポレーテッド 代謝調節型グルタミン酸受容体−5の調節物質としてのビピリジルアミド
PE20060692A1 (es) 2004-09-21 2006-07-19 Lilly Co Eli Inhibidores bace
US7888374B2 (en) 2005-01-28 2011-02-15 Abbott Laboratories Inhibitors of c-jun N-terminal kinases
TW200730523A (en) * 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
CN103936690B (zh) * 2005-10-25 2016-06-08 盐野义制药株式会社 氨基二氢噻嗪衍生物
BRPI0808523A2 (pt) 2007-03-01 2014-08-19 Novartis Vaccines & Diagnostic Inibidores de pim cinase e métodos de seu uso
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
MX2009011498A (es) 2007-04-24 2009-11-10 Shionogi & Co Derivados de aminodihidrotiazina sustituida con un grupo ciclico.
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
RU2476431C2 (ru) 2008-01-18 2013-02-27 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Конденсированное производное аминодигидротиазина
BRPI0907563A2 (pt) * 2008-02-18 2015-08-04 Hoffmann La Roche Derivados de 4,5-di-hidro-xazol-2-il amina
US20100197688A1 (en) 2008-05-29 2010-08-05 Nantermet Philippe G Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
KR20130018370A (ko) 2008-06-13 2013-02-20 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
TW201028381A (en) 2008-07-14 2010-08-01 Shionogi & Co Pyridine derivative having ttk inhibition activity
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体
WO2010063718A1 (en) 2008-12-02 2010-06-10 ETH Zürich Screening assay for metabolic disease therapeuticals
US9237972B2 (en) 2008-12-16 2016-01-19 Kimberly-Clark Worldwide, Inc. Liquid surfactant compositions that adhere to surfaces and solidify and swell in the presence of water and articles using the same
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
JP2012180281A (ja) * 2009-06-29 2012-09-20 Dainippon Sumitomo Pharma Co Ltd 新規オキサジアゾール誘導体
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US8188079B2 (en) * 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20120238557A1 (en) 2009-11-13 2012-09-20 Shionogi & Co., Ltd. Aminothiazine or aminooxazine derivative having amino linker
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
WO2011071135A1 (ja) 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
UA103272C2 (uk) 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
EP2518059A4 (en) 2009-12-24 2013-05-29 Shionogi & Co 4-AMINO-1,3-THIAZINE OR OXAZINE DERIVATIVE
PE20121640A1 (es) 2009-12-31 2012-12-17 Novartis Ag Derivados de pirazina como inhibidores de bace
US8673894B2 (en) 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
BR112012031337A2 (pt) 2010-06-09 2016-10-25 Janssen Pharmaceutica Nv derivados de 5-amino-3,6-di-hidro-1h-pirazin-2-ona úteis como inibidores de beta-secretase (bace)
KR101730937B1 (ko) * 2010-06-09 2017-04-27 얀센 파마슈티카 엔.브이. 베타-세크레타아제(bace) 저해제로 유용한 5,6-디하이드로-2h-[1,4]옥사진-3-일-아민 유도체
WO2012006953A1 (en) 2010-07-13 2012-01-19 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
CN103429589A (zh) 2011-01-12 2013-12-04 诺瓦提斯公司 噁嗪衍生物及其在治疗神经障碍中的用途
US20140128385A1 (en) 2011-01-13 2014-05-08 Novartis Ag Bace-2 inhibitors for the treatment of metabolic disorders
CA2824220C (en) * 2011-01-13 2020-09-01 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
US9169260B2 (en) 2011-03-22 2015-10-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
UY34278A (es) 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
AU2012322329A1 (en) 2011-10-13 2014-05-01 Novartis Ag Novel oxazine derivatives and their use in the treatment of disease
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders

Also Published As

Publication number Publication date
ME02409B (me) 2016-09-20
EA201391032A1 (ru) 2013-12-30
MX336966B (es) 2016-02-08
US20200048236A1 (en) 2020-02-13
US8637508B2 (en) 2014-01-28
EA024059B1 (ru) 2016-08-31
SMT201600144B (it) 2016-07-01
MX2013008108A (es) 2013-10-30
MY162413A (en) 2017-06-15
NZ612990A (en) 2014-11-28
CA2824220C (en) 2020-09-01
MA34898B1 (fr) 2014-02-01
EP2663561B1 (en) 2016-03-16
CL2013001964A1 (es) 2013-11-29
WO2012095469A1 (en) 2012-07-19
CR20130339A (es) 2013-09-04
HRP20160647T1 (hr) 2016-07-01
US20150203481A1 (en) 2015-07-23
AP3807A (en) 2016-09-30
US20190062319A1 (en) 2019-02-28
GT201300179A (es) 2014-06-06
CN106117193B (zh) 2019-09-13
UY33865A (es) 2012-08-31
IL227294A (en) 2017-03-30
CN103403001A (zh) 2013-11-20
JP2014502626A (ja) 2014-02-03
US10301296B2 (en) 2019-05-28
US20140107118A1 (en) 2014-04-17
CY1117580T1 (el) 2017-04-26
AU2012206561B2 (en) 2015-12-17
ES2576182T3 (es) 2016-07-06
CA2824220A1 (en) 2012-07-19
CU20130101A7 (es) 2014-01-29
US8865712B2 (en) 2014-10-21
KR20130119970A (ko) 2013-11-01
AR084849A1 (es) 2013-06-26
SG191812A1 (en) 2013-08-30
DK2663561T3 (en) 2016-06-06
UA113051C2 (xx) 2016-12-12
US20170320864A1 (en) 2017-11-09
TW201309688A (zh) 2013-03-01
PT2663561E (pt) 2016-06-07
RS54782B1 (sr) 2016-10-31
AP2013006990A0 (en) 2013-07-31
ZA201304921B (en) 2016-01-27
PL2663561T3 (pl) 2016-10-31
CL2014002518A1 (es) 2014-12-05
US20120184539A1 (en) 2012-07-19
HUE029226T2 (en) 2017-02-28
HK1188453A1 (zh) 2014-05-02
EP2663561A1 (en) 2013-11-20
US10035794B2 (en) 2018-07-31
CN106117193A (zh) 2016-11-16
TN2013000285A1 (en) 2015-01-20
JO3146B1 (ar) 2017-09-20
KR101569260B1 (ko) 2015-11-13
US10683287B2 (en) 2020-06-16
CO6751293A2 (es) 2013-09-16
US9550758B2 (en) 2017-01-24
JP5715710B2 (ja) 2015-05-13
AU2012206561A1 (en) 2013-08-01
SI2663561T1 (sl) 2016-07-29
IL227294A0 (en) 2013-09-30
CN103403001B (zh) 2016-08-17
TWI531570B (zh) 2016-05-01

Similar Documents

Publication Publication Date Title
PE20141110A1 (es) Derivados heterociclicos novedosos para el tratamiento de trastornos neurologicos
PE20171341A1 (es) Compuestos de pirazina para el tratamiento de enfermedades infecciosas
PE20170666A1 (es) 2-(morfolin-4-il)-1,7-naftiridinas
PH12019500432A1 (en) 7-substituted sulfonimidoylpurinone compounds for the treatment and prophylaxis of virus infection
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
AR077975A1 (es) Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
PE20142339A1 (es) Derivados macrociclicos para el tratamiento de enfermedades
PE20151951A1 (es) Heteroarildihidropirimidinas unidas por puentes en 6 para el tratamiento y la profilaxis de infeccion por el virus de la hepatitis b
AR073622A1 (es) Compuestos de benzo[d]isoxazol moduladores de receptores de dopamina d3 y de la serotonina 5-ht2a, proceso para prepararlos, composiciones farmaceuticas que los comprenden y uso de los mismos para el tratamiento de trastornos psicoticos
ES2564010T3 (es) Composición farmacéutica para tratar o prevenir el glaucoma
PE20191528A1 (es) Nuevos derivados de triazolo[4,5-d]pirimidina
AR055563A1 (es) Compuestos de piridil acido acetico, agente farmaceutico y utilizacion del compuesto para preparar dicho agente
PE20130281A1 (es) Derivados de acido 5-alquinil-3-amida-2-tiofeno-carboxilico como inhibidores del virus flaviviridae
AR054035A1 (es) Derivados benzodioxano y benzodioxolano y uso de los mismos
AR077935A1 (es) Derivados de 3-amino-5 fenil-5,6-dihidro-2h-(1,4)oxazina
PE20110835A1 (es) Piridiloxi-indoles inhibidores del vegf-r2 y uso de los mismos para el tratamiento de enfermedades
TW200718692A (en) Dihydrobenzofuran derivatives and uses thereof
AR056979A1 (es) Derivados de dihidrobenzofuranos y usos de los mismos
AR062409A1 (es) Compuesto y composicion farmaceutica, utiles como agentes terapeuticos en el tratamiento, prevencion o mejoramiento de enfermedad o trastorno caracterizado por depositos o niveles de b-amiloide elevados o para inhibir o elucidar la enzima b-secretasa, y proceso para la preparacion del compuesto
AR075583A1 (es) Derivados de isoxazol/o-piridina con eslabon etilo o etenilo
PE20141556A1 (es) Derivados de etinilo como moduladores alostericos de mglur5
ECSP15035530A (es) Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas
ECSP15012804A (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
AR087915A1 (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 bace1
PE20161407A1 (es) Piridina 5,6 disustituida -2-carboxamidas como agonistas del receptor canabinoide

Legal Events

Date Code Title Description
FG Grant, registration