AR095436A1 - Procedimiento para preparar inhibidores de la glucosilceramida sintasa - Google Patents
Procedimiento para preparar inhibidores de la glucosilceramida sintasaInfo
- Publication number
- AR095436A1 AR095436A1 ARP140100982A ARP140100982A AR095436A1 AR 095436 A1 AR095436 A1 AR 095436A1 AR P140100982 A ARP140100982 A AR P140100982A AR P140100982 A ARP140100982 A AR P140100982A AR 095436 A1 AR095436 A1 AR 095436A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- halo
- heteroaryl
- aryl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic 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
- C07D277/22—Heterocyclic 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
- C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Epidemiology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Procedimiento para preparar inhibidores de la glucosilceramida sintasa (GCS) útiles para el tratamiento de enfermedades metabólicas, tales como las tesaurismosis en el lisosoma, solas o en combinación con tratamiento enzimático de sustitución, y para el tratamiento del cáncer. Se proveen además, intermediarios de síntesis. Reivindicación 1: Procedimiento para preparar un compuesto de la fórmula (1) en la que: n es 1, 2 ó 3; m es 1; t es 0, 1 ó 2; y es 1 ó 2; z es 0, 1 ó 2; E es O; X¹ es CR¹; X² es O; X³ es -NH; X⁴ es CR⁴R⁵, CH₂CR⁴R⁵ o CH₂-alquil C₁₋₆-CR⁴R⁵; X⁵ es un enlace directo, O, S, SO₂, CR⁴R⁵; alquilo C₁₋₆, alquiloxi C₁₋₆, alquenilo C₁₋₆, alqueniloxi C₁₋₆; R es arilo C₆₋₁₂, heteroarilo C₂₋₉, alquilo C₁₋₆, heteroaril C₂₋₉alquilo C₁₋₆; R¹ es H, CN, alquil C₁₋₆carbonilo, o alquilo C₁₋₆; R² y R³ son cada uno independientemente -H, alquilo C₁₋₆ opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en halógeno, alquilo C₁₋₆, arilo C₆₋₁₂, heteroarilo C₂₋₉, alquil C₁₋₆arilo C₆₋₁₂, haloarilo C₆₋₁₂, y haloheteroarilo C₂₋₉, u opcionalmente cuando X² es -NR² y X³ es -NR³, R² y R³ se pueden tomar junto con los átomos de nitrógeno a los cuales están unidos para formar un anillo heterocíclico no aromático opcionalmente sustituido con uno o más sustituyentes seleccionados de halógeno, alquilo C₁₋₆, arilo C₆₋₁₂, heteroarilo C₂₋₉, alquil C₁₋₆arilo C₆₋₁₂, haloarilo C₆₋₁₂ y haloheteroarilo C₂₋₉; R⁴ y R⁵ se seleccionan independientemente de H, alquilo C₁₋₆, o se toman junto con el carbono al cual están unidos para formar un anillo espirocicloalquilo C₃₋₁₀ o un anillo espirocicloalcoxi C₃₋₁₀; R⁶ es -H, halógeno, -CN, arilo C₆₋₁₂, ariloxi C₆₋₁₂, alquiloxi C₁₋₆; alquilo C₁₋₆ opcionalmente sustituido con uno a cuatro halo o alquilo C₁₋₆; A¹ es alquinilo C₂₋₆; cicloalquilo C₃₋₁₀, arilo C₆₋₁₂, heteroarilo C₂₋₉, heterocicloalquilo C₂₋₉ o benzoheterocicloalquilo C₂₋₉ opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en halo, alquilo C₁₋₆ opcionalmente sustituido con uno a tres halo; alquenilo C₁₋₆, amino, alquil C₁₋₆amino, dialquil C₁₋₆amino, alcoxi C₁₋₆, nitro, CN, -OH, alquiloxi C₁₋₆ opcionalmente sustituido con uno a tres halo; alcoxi C₁₋₆carbonilo y alquil C₁₋₆carbonilo; A² es H, cicloalquilo C₃₋₁₀, arilo C₆₋₁₂, heteroarilo C₂₋₉, heterocicloalquilo C₂₋₉ o benzoheterocicloalquilo C₂₋₉ opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en halo, alquilo C₁₋₆ opcionalmente sustituido con uno a tres halo; alquilenilo C₁₋₆, amino, alquil C₁₋₆amino, dialquil C₁₋₆amino, alcoxi C₁₋₆, O-cicloalquilo C₃₋₆, cicloalcoxi C₃₋₆, nitro, CN, OH, alquiloxi C₁₋₆ opcionalmente sustituido con uno a tres halo; cicloalquilo C₃₋₆, alcoxi C₁₋₆carbonilo, alquil C₁₋₆carbonilo, haloalquilo C₁₋₆; siempre y cuando la suma de n + t + y + z no sea mayor de 6; que comprende hacer reaccionar el compuesto de la fórmula (2), con el compuesto de la fórmula (3) en donde n, t, y, z, X⁴, A¹, X⁵ y A² son según se define anteriormente. Reivindicación 31: Compuesto de la fórmula (4). Reivindicación 32: Compuesto de la fórmula (5). Reivindicación 33: Compuesto de la fórmula (6).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361791913P | 2013-03-15 | 2013-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR095436A1 true AR095436A1 (es) | 2015-10-14 |
Family
ID=50543333
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140100982A AR095436A1 (es) | 2013-03-15 | 2014-03-13 | Procedimiento para preparar inhibidores de la glucosilceramida sintasa |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US9682975B2 (es) |
| EP (2) | EP2970251B1 (es) |
| JP (2) | JP6543242B2 (es) |
| KR (1) | KR20150130386A (es) |
| CN (2) | CN108658970A (es) |
| AR (1) | AR095436A1 (es) |
| AU (2) | AU2014235132B2 (es) |
| BR (1) | BR112015020667A2 (es) |
| CA (2) | CA3092901C (es) |
| CY (1) | CY1121859T1 (es) |
| DK (1) | DK3514157T3 (es) |
| ES (2) | ES2968073T3 (es) |
| HK (1) | HK1220689A1 (es) |
| HU (2) | HUE043394T2 (es) |
| IL (2) | IL240617B (es) |
| MX (1) | MX365464B (es) |
| RU (1) | RU2015144035A (es) |
| SG (2) | SG10201706575UA (es) |
| TW (2) | TW201900625A (es) |
| UY (1) | UY35438A (es) |
| WO (1) | WO2014151291A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20130273B1 (ar) | 2012-09-11 | 2021-08-17 | Genzyme Corp | مثبطات انزيم (سينثاز) غلوكوسيل سيراميد |
| KR20150130386A (ko) | 2013-03-15 | 2015-11-23 | 젠자임 코포레이션 | 글루코실세라마이드 신타아제 저해제의 제조 방법 |
| EP3583653B1 (de) * | 2017-02-17 | 2020-12-16 | Westfälische Wilhelms-Universität Münster | Elektrolyt-zusatz für lithium-ionen-batterien |
| JP2021506920A (ja) | 2017-12-21 | 2021-02-22 | リソソーマル・セラピューティクス・インコーポレイテッドＬｙｓｏｓｏｍａｌ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | 結晶性の置換シクロヘキシルピラゾロ［１，５−ａ］ピリミジニルカルボキサミド化合物およびその治療的使用 |
| US10519157B2 (en) * | 2018-02-09 | 2019-12-31 | X-Cutag Therapeutics, Inc. | Deuterated compounds for treating Fabry, Gaucher, Parkinson's and related diseases and conditions, and compositions and methods thereof |
| IL295255A (en) | 2020-02-03 | 2022-10-01 | Genzyme Corp | Methods for treating neurological symptoms associated with lysosomal storage diseases |
| WO2021221953A1 (en) | 2020-04-28 | 2021-11-04 | The Regents Of The University Of Michigan | Pyridine inhibitors of glucosylceramide synthase and therapeutic methods using the same |
| CA3186766A1 (en) | 2020-07-24 | 2022-01-27 | Danielle Combessis | Pharmaceutical compositions comprising venglustat |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB725226A (en) * | 1952-06-03 | 1955-03-02 | Berger Brothers Co | Improvements in or relating to an inflatable surgical pad |
| GB725228A (en) * | 1952-06-19 | 1955-03-02 | Roche Products Ltd | Substituted carbamic acid esters and process for the manufacture thereof |
| NL130759C (es) * | 1965-10-07 | |||
| DE4326510A1 (de) * | 1993-08-06 | 1995-02-09 | Bayer Ag | Verfahren zur Herstellung von Cyclohexen-Derivaten |
| KR970701174A (ko) * | 1994-02-10 | 1997-03-17 | 오노다 마사요시 | 신규한 카바메이트 유도체 및 이의 의약 조성물(Novel carbamate derivative and medicinal composition containing the same) |
| JPH08198751A (ja) * | 1995-01-19 | 1996-08-06 | Yamanouchi Pharmaceut Co Ltd | カルバメート誘導体 |
| SE9600683D0 (sv) * | 1996-02-23 | 1996-02-23 | Astra Ab | Azabicyclic esters of carbamic acids useful in therapy |
| GB0400812D0 (en) | 2004-01-14 | 2004-02-18 | Celltech R&D Ltd | Novel compounds |
| US8003617B2 (en) | 2004-11-10 | 2011-08-23 | Genzyme Corporation | Methods of treating diabetes mellitus |
| JP5285643B2 (ja) * | 2010-03-15 | 2013-09-11 | シャープ株式会社 | 半導体集積回路および電子情報機器 |
| PL2639234T3 (pl) | 2010-11-12 | 2019-12-31 | Shionogi & Co., Ltd. | Krystaliczna pochodna morfinanu 6,7-nienasyconego-7-karbamoilu i sposób jej wytwarzania |
| RU2645675C2 (ru) * | 2011-03-18 | 2018-02-27 | Джензим Корпорейшн | Ингибиторы глюкозилцерамид-синтазы |
| EP2723734A1 (en) | 2011-06-22 | 2014-04-30 | Isochem | Process for the preparation of solifenacin and salts thereof |
| JP2013053228A (ja) * | 2011-09-02 | 2013-03-21 | Asahi Kasei E-Materials Corp | エポキシ樹脂用硬化剤及びマイクロカプセル型エポキシ樹脂用硬化剤 |
| JOP20130273B1 (ar) | 2012-09-11 | 2021-08-17 | Genzyme Corp | مثبطات انزيم (سينثاز) غلوكوسيل سيراميد |
| KR20150130386A (ko) * | 2013-03-15 | 2015-11-23 | 젠자임 코포레이션 | 글루코실세라마이드 신타아제 저해제의 제조 방법 |
-
2014
- 2014-03-13 KR KR1020157027836A patent/KR20150130386A/ko not_active Application Discontinuation
- 2014-03-13 SG SG10201706575UA patent/SG10201706575UA/en unknown
- 2014-03-13 AR ARP140100982A patent/AR095436A1/es unknown
- 2014-03-13 CA CA3092901A patent/CA3092901C/en active Active
- 2014-03-13 WO PCT/US2014/025384 patent/WO2014151291A1/en active Application Filing
- 2014-03-13 TW TW107132577A patent/TW201900625A/zh unknown
- 2014-03-13 HU HUE14718835A patent/HUE043394T2/hu unknown
- 2014-03-13 CN CN201810630738.4A patent/CN108658970A/zh active Pending
- 2014-03-13 US US14/776,443 patent/US9682975B2/en active Active
- 2014-03-13 BR BR112015020667A patent/BR112015020667A2/pt not_active Application Discontinuation
- 2014-03-13 MX MX2015012842A patent/MX365464B/es active IP Right Grant
- 2014-03-13 ES ES19153389T patent/ES2968073T3/es active Active
- 2014-03-13 ES ES14718835T patent/ES2727869T3/es active Active
- 2014-03-13 EP EP14718835.3A patent/EP2970251B1/en active Active
- 2014-03-13 JP JP2016501840A patent/JP6543242B2/ja active Active
- 2014-03-13 DK DK19153389.2T patent/DK3514157T3/da active
- 2014-03-13 RU RU2015144035A patent/RU2015144035A/ru not_active Application Discontinuation
- 2014-03-13 HU HUE19153389A patent/HUE064200T2/hu unknown
- 2014-03-13 CA CA2906581A patent/CA2906581C/en active Active
- 2014-03-13 TW TW103108899A patent/TWI649317B/zh not_active IP Right Cessation
- 2014-03-13 CN CN201480026302.4A patent/CN105189491B/zh active Active
- 2014-03-13 SG SG11201506415XA patent/SG11201506415XA/en unknown
- 2014-03-13 AU AU2014235132A patent/AU2014235132B2/en not_active Ceased
- 2014-03-13 EP EP19153389.2A patent/EP3514157B1/en active Active
- 2014-03-14 UY UY0001035438A patent/UY35438A/es not_active Application Discontinuation
-
2015
- 2015-08-17 IL IL240617A patent/IL240617B/en active IP Right Grant
-
2016
- 2016-07-20 HK HK16108676.6A patent/HK1220689A1/zh not_active IP Right Cessation
-
2017
- 2017-05-12 US US15/593,440 patent/US10065949B2/en active Active
-
2018
- 2018-06-03 IL IL259770A patent/IL259770B/en active IP Right Grant
- 2018-08-01 US US16/051,892 patent/US10604518B2/en active Active
-
2019
- 2019-01-18 AU AU2019200350A patent/AU2019200350A1/en not_active Abandoned
- 2019-05-27 CY CY20191100562T patent/CY1121859T1/el unknown
- 2019-06-13 JP JP2019109986A patent/JP6813626B2/ja active Active
-
2020
- 2020-02-14 US US16/791,854 patent/US10954230B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR095436A1 (es) | Procedimiento para preparar inhibidores de la glucosilceramida sintasa | |
| AR092522A1 (es) | Inhibidores de glucosilceramida sintasa | |
| AR095311A1 (es) | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante | |
| AR096979A1 (es) | Derivados de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen | |
| CU20170094A7 (es) | Derivados de 4h-pirrol[3,2-c]piridin-4-0na | |
| AR094299A1 (es) | Derivados de ftalazin-1(2h)-ona sustituidos | |
| AR099138A1 (es) | Piridinas fusionadas como inhibidores del complejo p97 | |
| ES2753816T3 (es) | Moduladores del receptor de glucocorticoides de azadecalina condensada con heteroaril-cetona | |
| AR091424A1 (es) | Compuestos triciclicos sustituidos como inhibidores de receptores del factor de crecimiento del fibroplasto (fgfr) | |
| AR106472A1 (es) | Inhibidores de acc y usos de los mismos | |
| AR100137A1 (es) | Compuestos 4-amino-imidazoquinolina | |
| ES2684517T3 (es) | Compuestos de heterociclilo como inhibidores de MEK | |
| EA201691272A1 (ru) | Тетрагидропиридопиразины в качестве модуляторов gpr6 | |
| AR077695A1 (es) | Derivados de pirimidina como inhibidores del factor ixa | |
| EA201401054A1 (ru) | N-циклиламиды в качестве нематоцидов | |
| AR085425A1 (es) | Inhibidores de la glucosilceramida sintasa | |
| AR085958A1 (es) | 8-etil-6-(aril)pirido[2,3-d]pirimidin-7(8h)-onas para el tratamiento de trastornos del cns y cancer | |
| AR092170A1 (es) | Proceso para la fabricacion de benzoxazinonas | |
| CO2017008600A2 (es) | Análogos de desacetoxitubulisina h, composiciones y método de producción de los mismos | |
| AR100418A1 (es) | Compuestos y composiciones para inducir condrogénesis | |
| AR097435A1 (es) | 6-alquinilpiridinas | |
| AR103742A1 (es) | Derivados de trifluorometilpropanamida | |
| DOP2015000002A (es) | Derivados de azaindol que actuan como inhibidores de p13k | |
| AR095351A1 (es) | Inhibidores de histona desacetilasa (hdac) | |
| AR109735A1 (es) | Método para la síntesis de derivado de 3-fenil-2,3,4,8,9,10-hexahidropirano[2,3-f]cromeno e isómero óptico del mismo |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |