CO2017010725A2 - N-[3-[(4as,5s,7as)-2-amino-5-(1,1-difluoroetil)-4,4a,5,7-tetrahidrofuro[3,4-d][1,3]tiazin-7a-il]-4-fluoro-fenil]-5-ciano-2-picolamida, su sal metanosulfonato y una forma cristalina hemihidrato de la sal 4-metilbencenosulfonato del mismo, composiciones que los contienen y procedimientos para su elaboración - Google Patents
N-[3-[(4as,5s,7as)-2-amino-5-(1,1-difluoroetil)-4,4a,5,7-tetrahidrofuro[3,4-d][1,3]tiazin-7a-il]-4-fluoro-fenil]-5-ciano-2-picolamida, su sal metanosulfonato y una forma cristalina hemihidrato de la sal 4-metilbencenosulfonato del mismo, composiciones que los contienen y procedimientos para su elaboraciónInfo
- Publication number
- CO2017010725A2 CO2017010725A2 CONC2017/0010725A CO2017010725A CO2017010725A2 CO 2017010725 A2 CO2017010725 A2 CO 2017010725A2 CO 2017010725 A CO2017010725 A CO 2017010725A CO 2017010725 A2 CO2017010725 A2 CO 2017010725A2
- Authority
- CO
- Colombia
- Prior art keywords
- salt
- picolamide
- tetrahydrofuro
- thiazin
- difluoroethyl
- Prior art date
Links
- JJADJMODPHLYCB-DAESXHAQSA-N N-[3-[(4aS,5S,7aS)-2-amino-5-(1,1-difluoroethyl)-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-cyanopyridine-2-carboxamide Chemical compound NC=1SC[C@H]2[C@@](N=1)(CO[C@@H]2C(C)(F)F)C=1C=C(C=CC=1F)NC(=O)C1=NC=C(C=C1)C#N JJADJMODPHLYCB-DAESXHAQSA-N 0.000 title 1
- YKGMKSIHIVVYKY-UHFFFAOYSA-N dabrafenib mesylate Chemical compound CS(O)(=O)=O.S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 YKGMKSIHIVVYKY-UHFFFAOYSA-N 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical class CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
- C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
- C07C309/31—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups by alkyl groups containing at least three carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562154242P | 2015-04-29 | 2015-04-29 | |
| PCT/US2016/028896 WO2016176118A1 (en) | 2015-04-29 | 2016-04-22 | Tetrahydrofurane-fused aminohydrothiazine derivatives which are useful in the treatment of alzheimer's disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2017010725A2 true CO2017010725A2 (es) | 2018-01-31 |
Family
ID=55861291
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2017/0010725A CO2017010725A2 (es) | 2015-04-29 | 2017-10-20 | N-[3-[(4as,5s,7as)-2-amino-5-(1,1-difluoroetil)-4,4a,5,7-tetrahidrofuro[3,4-d][1,3]tiazin-7a-il]-4-fluoro-fenil]-5-ciano-2-picolamida, su sal metanosulfonato y una forma cristalina hemihidrato de la sal 4-metilbencenosulfonato del mismo, composiciones que los contienen y procedimientos para su elaboración |
Country Status (40)
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR103680A1 (es) * | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
| TWI669119B (zh) * | 2016-10-21 | 2019-08-21 | 美國禮來大藥廠 | 組合療法 |
| US11559528B2 (en) * | 2019-09-05 | 2023-01-24 | The Cleveland Clinic Foundation | BACE1 inhibition for the treatment of cancer |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR054617A1 (es) | 2005-06-14 | 2007-07-04 | Schering Corp | Derivados de pirrol[3, 4 - d]pirimidina como inhibidores de aspartil proteasas y composiciones farmacéuticas que los comprenden |
| BRPI0906962B8 (pt) * | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| ES2738123T3 (es) | 2008-06-13 | 2020-01-20 | Shionogi & Co | Derivado heterocíclico que contiene azufre que tiene actividad inhibitoria de ß-secretasa |
| US20110207723A1 (en) | 2008-09-30 | 2011-08-25 | Eisai R&D Management Co., Ltd. | Novel fused aminodihydrothiazine derivative |
| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| WO2011071057A1 (ja) | 2009-12-09 | 2011-06-16 | 塩野義製薬株式会社 | 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物 |
| 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 |
| JPWO2012147762A1 (ja) * | 2011-04-26 | 2014-07-28 | 塩野義製薬株式会社 | ピリジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| WO2012162334A1 (en) | 2011-05-24 | 2012-11-29 | Bristol-Myers Squibb Company | Compounds for the reduction of beta-amyloid production |
| WO2014015125A1 (en) | 2012-07-19 | 2014-01-23 | Eisai R&D Management Co., Ltd. | Fused aminodihydrothiazine derivative salts and uses thereof |
| JP2014101354A (ja) | 2012-10-24 | 2014-06-05 | Shionogi & Co Ltd | Ｂａｃｅ１阻害作用を有するオキサジン誘導体 |
| 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 |
| AR103680A1 (es) | 2015-02-23 | 2017-05-24 | Lilly Co Eli | Inhibidores selectivos de bace1 |
| TWI675034B (zh) | 2016-05-20 | 2019-10-21 | 美商美國禮來大藥廠 | 四氫呋喃并<img align="absmiddle" height="18px" width="27px" file="d10999.TIF" alt="其他非圖式 ed10999.png" img-content="tif" orientation="portrait" inline="yes" giffile="ed10999.png"></img>化合物及其作為選擇性ＢＡＣＥ１抑制劑之用途 |
| JP2019524788A (ja) | 2016-08-11 | 2019-09-05 | イーライ リリー アンド カンパニー | アミノチアジンおよびｂａｃｅ１阻害剤としてのそれらの使用 |
-
2016
- 2016-04-13 AR ARP160100992A patent/AR104241A1/es unknown
- 2016-04-15 TW TW105111913A patent/TWI619719B/zh not_active IP Right Cessation
- 2016-04-22 JP JP2016567244A patent/JP2017515831A/ja not_active Withdrawn
- 2016-04-22 NZ NZ735249A patent/NZ735249A/en not_active IP Right Cessation
- 2016-04-22 CA CA2981091A patent/CA2981091A1/en active Pending
- 2016-04-22 HR HRP20192237TT patent/HRP20192237T1/hr unknown
- 2016-04-22 AU AU2016254980A patent/AU2016254980B2/en not_active Ceased
- 2016-04-22 KR KR1020177030721A patent/KR101979534B1/ko not_active Expired - Fee Related
- 2016-04-22 EA EA201792109A patent/EA032293B1/ru not_active IP Right Cessation
- 2016-04-22 SI SI201630511T patent/SI3288949T1/sl unknown
- 2016-04-22 HU HUE16719728A patent/HUE047160T2/hu unknown
- 2016-04-22 RS RS20191653A patent/RS59729B1/sr unknown
- 2016-04-22 EP EP16719728.4A patent/EP3288949B1/en active Active
- 2016-04-22 CN CN201680024772.6A patent/CN107531728B/zh active Active
- 2016-04-22 MA MA41975A patent/MA41975B1/fr unknown
- 2016-04-22 DK DK16719728.4T patent/DK3288949T3/da active
- 2016-04-22 HK HK18103304.5A patent/HK1243709A1/zh unknown
- 2016-04-22 ME MEP-2019-353A patent/ME03660B/me unknown
- 2016-04-22 CR CR20170433A patent/CR20170433A/es unknown
- 2016-04-22 ES ES16719728T patent/ES2765646T3/es active Active
- 2016-04-22 US US15/135,580 patent/US10011610B2/en active Active
- 2016-04-22 PT PT167197284T patent/PT3288949T/pt unknown
- 2016-04-22 TN TNP/2017/000448A patent/TN2017000448A1/en unknown
- 2016-04-22 BR BR112017020180-1A patent/BR112017020180A2/pt not_active Application Discontinuation
- 2016-04-22 WO PCT/US2016/028896 patent/WO2016176118A1/en not_active Ceased
- 2016-04-22 MD MDE20180225T patent/MD3288949T2/ro unknown
- 2016-04-22 MY MYPI2017704013A patent/MY180727A/en unknown
- 2016-04-22 SG SG11201708003WA patent/SG11201708003WA/en unknown
- 2016-04-22 PE PE2017001998A patent/PE20180048A1/es unknown
- 2016-04-22 MX MX2017013694A patent/MX2017013694A/es unknown
- 2016-04-22 PL PL16719728T patent/PL3288949T3/pl unknown
-
2017
- 2017-08-31 IL IL254252A patent/IL254252A0/en unknown
- 2017-10-17 DO DO2017000240A patent/DOP2017000240A/es unknown
- 2017-10-17 SV SV2017005547A patent/SV2017005547A/es unknown
- 2017-10-18 CL CL2017002651A patent/CL2017002651A1/es unknown
- 2017-10-20 CO CONC2017/0010725A patent/CO2017010725A2/es unknown
- 2017-10-26 PH PH12017501955A patent/PH12017501955A1/en unknown
- 2017-10-27 GT GT201700227A patent/GT201700227A/es unknown
- 2017-10-27 EC ECIEPI201771769A patent/ECSP17071769A/es unknown
-
2018
- 2018-03-13 JP JP2018045585A patent/JP6777668B2/ja active Active
-
2019
- 2019-12-04 CY CY20191101285T patent/CY1122375T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JOP20180113A1 (ar) | مركبات ,تركيبات وطرق | |
| PE20160862A1 (es) | Polimorfo de los inhibidores de la syk | |
| MX2018003432A (es) | Compuestos heterociclicos y usos de los mismos. | |
| MX375970B (es) | Compuestos de triazolopirimidina y usos de los mismos. | |
| MX2018003130A (es) | Compuestos de heteroarilo como inhibidores de cinasas asociadas a receptor de interleucina-1 (irak) y usos de los mismos. | |
| CO2018000589A2 (es) | Oxiesteroles y composiciones farmacéuticas que los contienen | |
| MA39866A (fr) | Amides 2-amino-6-méthyl-4,4a,5,6-tétrahydropyrano[3,4-d][1,3]thiazin-8a(8h)-yl-1,3-thiazol-4-yle | |
| EA201692521A1 (ru) | Пиразольные соединения и их применение в качестве блокаторов кальциевых каналов т-типа | |
| CL2018002089A1 (es) | Maleato de agonista de tlr7, sus formas cristalinas c, d y e, sus procesos de preparación y su uso | |
| EA201792425A1 (ru) | Трициклические соединения и их применение в качестве ингибиторов фосфодиэстераз | |
| EA201691670A1 (ru) | Тетразолонзамещенные дигидропиридиноновые ингибиторы mgat2 | |
| CO2018004581A2 (es) | Compuestos de criptoficina y productos conjugados, y sus métodos de preparación | |
| AR105821A1 (es) | COMPUESTOS ÚTILES PARA INHIBIR ROR-g-T | |
| EA201592268A1 (ru) | Дигидропиридиноновые ингибиторы mgat2 | |
| AR095097A1 (es) | Compuestos de fenoxietoxi | |
| DOP2019000021A (es) | Derivado de triazolopirazinona útil como un inhibidor de pde1 humana | |
| JO3742B1 (ar) | مركب بيرانو داي بيريدين | |
| JOP20200030A1 (ar) | مركب خماسي الحلقة | |
| CO2017010725A2 (es) | N-[3-[(4as,5s,7as)-2-amino-5-(1,1-difluoroetil)-4,4a,5,7-tetrahidrofuro[3,4-d][1,3]tiazin-7a-il]-4-fluoro-fenil]-5-ciano-2-picolamida, su sal metanosulfonato y una forma cristalina hemihidrato de la sal 4-metilbencenosulfonato del mismo, composiciones que los contienen y procedimientos para su elaboración | |
| AR100095A1 (es) | Formas sólidas del ácido {[(2r,3s,4r,5s)-4-(4-cloro-2-fluoro-fenil)-3-(3-cloro-2-fluoro-fenil)-4-ciano-5-(2,2-dimetil-propil)-pirrolidin-2-carbonil]-amino}-3-metoxi-benzoico | |
| SV2017005478A (es) | Sal de tosilato n-[3-[(4ar,7as)-2-amino-6-(5-fluoropirimidina-2-il)-4,4a,5,7-tetrahidropirrolo[3,4-d][1,3]tiazina-7a-il]-4-fluoro-fenil]-5-metoxi-pirazina-2-carboxamida | |
| AR117467A2 (es) | Procesos para preparar isoquinolinonas y formas sólidas de isoquinolinonas | |
| AR105924A1 (es) | Compuestos terapéuticos y síntesis | |
| MX2018011117A (es) | Forma cristalina. | |
| EA201691661A1 (ru) | Способ получения производных 21-метокси-11-бета- фенил-19-норпрегна-4,9-диен-3,20-диона |