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 |
| AR110470A1 (es) * | 2016-10-21 | 2019-04-03 | Lilly Co Eli | Terapia de combinación para tratar la enfermedad de alzheimer |
| 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 |
|---|---|---|---|---|
| WO2006138264A2 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Aspartyl protease inhibitors |
| BRPI0906962B8 (pt) * | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| US8637504B2 (en) | 2008-06-13 | 2014-01-28 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity |
| KR20110076965A (ko) | 2008-09-30 | 2011-07-06 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 신규한 축합 아미노 디하이드로티아진 유도체 |
| 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 |
| GB201101140D0 (en) * | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| WO2012147762A1 (ja) * | 2011-04-26 | 2012-11-01 | 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 |
| TW201302763A (zh) | 2011-05-24 | 2013-01-16 | 必治妥美雅史谷比公司 | 用於減少β－類澱粉產生之化合物 |
| 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 |
| JOP20170106A1 (ar) | 2016-05-20 | 2017-11-20 | Lilly Co Eli | مركبات تترا هيدرو فوروكسازين واستخداماتها كمثبطات bace1 انتقائية |
| 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 |
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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 CN CN201680024772.6A patent/CN107531728B/zh active Active
- 2016-04-22 WO PCT/US2016/028896 patent/WO2016176118A1/en not_active Ceased
- 2016-04-22 TN TNP/2017/000448A patent/TN2017000448A1/en unknown
- 2016-04-22 SI SI201630511T patent/SI3288949T1/sl unknown
- 2016-04-22 RS RS20191653A patent/RS59729B1/sr unknown
- 2016-04-22 CR CR20170433A patent/CR20170433A/es unknown
- 2016-04-22 ES ES16719728T patent/ES2765646T3/es active Active
- 2016-04-22 JP JP2016567244A patent/JP2017515831A/ja not_active Withdrawn
- 2016-04-22 MY MYPI2017704013A patent/MY180727A/en unknown
- 2016-04-22 MD MDE20180225T patent/MD3288949T2/ro unknown
- 2016-04-22 MX MX2017013694A patent/MX2017013694A/es unknown
- 2016-04-22 CA CA2981091A patent/CA2981091A1/en active Pending
- 2016-04-22 PT PT167197284T patent/PT3288949T/pt unknown
- 2016-04-22 PL PL16719728T patent/PL3288949T3/pl unknown
- 2016-04-22 ME MEP-2019-353A patent/ME03660B/me unknown
- 2016-04-22 EP EP16719728.4A patent/EP3288949B1/en active Active
- 2016-04-22 KR KR1020177030721A patent/KR101979534B1/ko not_active Expired - Fee Related
- 2016-04-22 BR BR112017020180-1A patent/BR112017020180A2/pt not_active Application Discontinuation
- 2016-04-22 PE PE2017001998A patent/PE20180048A1/es unknown
- 2016-04-22 DK DK16719728.4T patent/DK3288949T3/da active
- 2016-04-22 SG SG11201708003WA patent/SG11201708003WA/en unknown
- 2016-04-22 HU HUE16719728A patent/HUE047160T2/hu unknown
- 2016-04-22 HR HRP20192237TT patent/HRP20192237T1/hr unknown
- 2016-04-22 EA EA201792109A patent/EA032293B1/ru not_active IP Right Cessation
- 2016-04-22 HK HK18103304.5A patent/HK1243709A1/zh unknown
- 2016-04-22 US US15/135,580 patent/US10011610B2/en active Active
- 2016-04-22 MA MA41975A patent/MA41975B1/fr unknown
- 2016-04-22 AU AU2016254980A patent/AU2016254980B2/en not_active Ceased
- 2016-04-22 NZ NZ735249A patent/NZ735249A/en not_active IP Right Cessation
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2017
- 2017-08-31 IL IL254252A patent/IL254252A0/en unknown
- 2017-10-17 SV SV2017005547A patent/SV2017005547A/es unknown
- 2017-10-17 DO DO2017000240A patent/DOP2017000240A/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 EC ECIEPI201771769A patent/ECSP17071769A/es unknown
- 2017-10-27 GT GT201700227A patent/GT201700227A/es unknown
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2018
- 2018-03-13 JP JP2018045585A patent/JP6777668B2/ja active Active
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2019
- 2019-12-04 CY CY20191101285T patent/CY1122375T1/el unknown
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