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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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds

Landscapes

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

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)
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)
PH (1) PH12013501480A1 (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
ES2537898T3 (es) 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
EP2464232B1 (en) 2009-08-10 2015-10-07 Samumed, LLC Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
EP2515655B1 (en) 2009-12-21 2015-08-05 Samumed, LLC 1h-pyrazolo[3,4-beta]pyridines and therapeutic uses thereof
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
JP5766198B2 (ja) 2010-10-29 2015-08-19 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
AU2012206527A1 (en) * 2011-01-13 2013-08-01 Novartis Ag BACE-2 inhibitors for the treatment of metabolic disorders
ES2576182T3 (es) 2011-01-13 2016-07-06 Novartis Ag Derivados de heterocíclicos novedosos y su uso en el tratamiento de trastornos neurológicos
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
IN2014CN02646A (es) 2011-09-14 2015-08-07 Samumed Llc
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
NZ741907A (en) 2012-05-04 2020-02-28 Samumed Llc 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
US9908867B2 (en) 2013-01-08 2018-03-06 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the Wnt signaling pathway and therapeutic uses thereof
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
MX2015014083A (es) 2013-04-11 2016-07-26 Hoffmann La Roche Inhibidores de enzima de escision de proteina precursora beta-amiloide (app) en el sitio beta 1 (bace1).
AU2015220873A1 (en) 2014-02-19 2016-08-11 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as BACE1 inhibitors for treatment of Alzheimer's disease
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
WO2017023989A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]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
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
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
US10329309B2 (en) 2015-08-03 2019-06-25 Samumed, Llc 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017024003A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017024010A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles 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
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
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles 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
HK1253372A1 (zh) 2015-08-12 2019-06-14 H‧隆德贝克有限公司 作为bace1抑制剂的2-氨基-3-氟-3-(氟甲基)-6-甲基-6-苯基-3，4，5，6-四氢吡啶
WO2017051303A1 (en) 2015-09-24 2017-03-30 Pfizer Inc. Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors
WO2017079765A1 (en) 2015-11-06 2017-05-11 Samumed, Llc Treatment of osteoarthritis
JP6616525B2 (ja) 2016-03-01 2019-12-04 エフ．ホフマン−ラ ロシュ アーゲー Ｂａｃｅ１阻害剤
MD3464285T2 (ro) 2016-06-01 2023-01-31 Biosplice Therapeutics Inc Procedeu pentru prepararea N-(5-(3-(7-(3-fluorfenil)-3H-imidazo[4,5-c]piridin-2-il)-1H-indazol-5-il)piridin-3-il)-3-metilbutanamidei
SG11201900125PA (en) * 2016-07-07 2019-02-27 Ironwood Pharmaceuticals Inc Novel 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
CN110709082A (zh) 2016-10-21 2020-01-17 萨穆梅德有限公司 吲唑-3-甲酰胺的使用方法及其作为Wnt/β-连环蛋白信号传导途径抑制剂的用途
JP7630905B2 (ja) 2016-11-07 2025-02-18 バイオスプライス セラピューティクス インコーポレイテッド 単回用量の調整済み注射用製剤
CA3047290A1 (en) 2016-12-15 2018-06-21 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
WO2018112086A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
WO2018112084A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
MX388697B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso.
WO2018112081A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
JOP20190180A1 (ar) * 2017-01-20 2019-07-20 Novartis Ag مشتق أوكسازين حر القاعدة في صورة بلورية
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
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
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
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
AR044399A1 (es) 2003-05-20 2005-09-14 Novartis Ag Compuestos heterociclicos y su uso como activadores de receptores de ppar. composiciones farmaceuticas que los contienen
AU2005215379A1 (en) 2004-02-12 2005-09-01 Merck & Co., Inc. Bipyridyl amides as modulators of metabotropic glutamate receptor-5
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
ES2537898T3 (es) 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
AU2008221263B2 (en) 2007-03-01 2012-02-23 Novartis Ag Pim kinase inhibitors and methods of their use
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
SI2233474T1 (sl) 2008-01-18 2015-11-30 Eisai R&D Management Co., Ltd. Kondenziran derivat aminodihidrotiazina
CN101952260B (zh) * 2008-02-18 2013-02-13 弗·哈夫曼-拉罗切有限公司 4,5-二氢-*唑-2-基胺衍生物
US20100197688A1 (en) 2008-05-29 2010-08-05 Nantermet Philippe G Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
EP2305672B1 (en) 2008-06-13 2019-03-27 Shionogi & Co., Ltd. SULFUR-CONTAINING HETEROCYCLIC DERIVATIVE HAVING ß-SECRETASE-INHIBITING ACTIVITY
WO2010007756A1 (ja) 2008-07-14 2010-01-21 塩野義製薬株式会社 Ｔｔｋ阻害作用を有するピリジン誘導体
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
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
CN102686584A (zh) 2009-11-13 2012-09-19 盐野义制药株式会社 具有氨基连接基的氨基噻嗪或氨基噁嗪衍生物
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
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
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
WO2011077726A1 (ja) 2009-12-24 2011-06-30 塩野義製薬株式会社 ４－アミノ－１，３－チアジンまたはオキサジン誘導体
CN102712621B (zh) 2009-12-31 2015-03-11 诺华股份有限公司 吡嗪衍生物及其在治疗神经学障碍中的用途
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
CN102933564B (zh) * 2010-06-09 2015-07-22 詹森药业有限公司 用作β-分泌酶(BACE)抑制剂的5,6-二氢-2H-[1,4]噁嗪-3-基-胺衍生物
US20130079349A1 (en) 2010-06-09 2013-03-28 Janssen Pharmaceutica Nv 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace)
AU2011278825B2 (en) 2010-07-13 2012-09-20 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
MX2013008111A (es) 2011-01-12 2013-10-30 Novartis Ag Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos.
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
AU2012206527A1 (en) 2011-01-13 2013-08-01 Novartis Ag BACE-2 inhibitors for the treatment of metabolic disorders
ES2576182T3 (es) 2011-01-13 2016-07-06 Novartis Ag Derivados de heterocíclicos novedosos y su uso en el tratamiento de trastornos neurológicos
EP2688872A4 (en) 2011-03-22 2014-08-27 Merck Sharp & Dohme AMIDOPYRAZOLHEMMER OF INTERLEUKIN RECEPTOR-MEDIATED 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

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