CR20230183A - Proceso para la preparación de compuestos de biheteroarilo y formas cristalinas de estos - Google Patents
Proceso para la preparación de compuestos de biheteroarilo y formas cristalinas de estosInfo
- Publication number
- CR20230183A CR20230183A CR20230183A CR20230183A CR20230183A CR 20230183 A CR20230183 A CR 20230183A CR 20230183 A CR20230183 A CR 20230183A CR 20230183 A CR20230183 A CR 20230183A CR 20230183 A CR20230183 A CR 20230183A
- Authority
- CR
- Costa Rica
- Prior art keywords
- certain
- steps
- biheteroaryl
- elimination
- need
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 4
- 150000001875 compounds Chemical group 0.000 title abstract 3
- 239000013078 crystal Chemical group 0.000 title 1
- 239000003054 catalyst Substances 0.000 abstract 2
- 230000008030 elimination Effects 0.000 abstract 2
- 238000003379 elimination reaction Methods 0.000 abstract 2
- 231100000252 nontoxic Toxicity 0.000 abstract 2
- 230000003000 nontoxic effect Effects 0.000 abstract 2
- 239000000376 reactant Substances 0.000 abstract 2
- SKMKJBYBPYBDMN-RYUDHWBXSA-N 3-(difluoromethoxy)-5-[2-(3,3-difluoropyrrolidin-1-yl)-6-[(1s,4s)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine Chemical compound C1=C(OC(F)F)C(N)=NC=C1C1=CC(N2[C@H]3C[C@H](OC3)C2)=NC(N2CC(F)(F)CC2)=N1 SKMKJBYBPYBDMN-RYUDHWBXSA-N 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 238000011097 chromatography purification Methods 0.000 abstract 1
- 238000000605 extraction Methods 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 230000003647 oxidation Effects 0.000 abstract 1
- 238000007254 oxidation reaction Methods 0.000 abstract 1
- 239000010970 precious metal Substances 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 229910052723 transition metal Inorganic materials 0.000 abstract 1
- 150000003624 transition metals Chemical class 0.000 abstract 1
- 239000002699 waste material Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/61—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged 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
- A61K31/535—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
- A61K31/537—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 spiro-condensed or forming part of bridged 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/38—One sulfur atom
-
- 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
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Liquid Crystal Substances (AREA)
- Steroid Compounds (AREA)
- Catalysts (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063087109P | 2020-10-02 | 2020-10-02 | |
| PCT/US2021/053005 WO2022072721A1 (en) | 2020-10-02 | 2021-09-30 | Process for the preparation of biheteroaryl compounds and crystal forms thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20230183A true CR20230183A (es) | 2023-06-14 |
Family
ID=78599176
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20230183A CR20230183A (es) | 2020-10-02 | 2021-09-30 | Proceso para la preparación de compuestos de biheteroarilo y formas cristalinas de estos |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20230312473A1 (enExample) |
| EP (1) | EP4222154A1 (enExample) |
| JP (1) | JP7805356B2 (enExample) |
| KR (1) | KR20230079123A (enExample) |
| CN (1) | CN116744933A (enExample) |
| AU (1) | AU2021353532A1 (enExample) |
| BR (1) | BR112023005853A2 (enExample) |
| CA (1) | CA3200566A1 (enExample) |
| CL (3) | CL2023000945A1 (enExample) |
| CR (1) | CR20230183A (enExample) |
| IL (1) | IL301266A (enExample) |
| MX (1) | MX2023003759A (enExample) |
| PE (1) | PE20230781A1 (enExample) |
| SA (1) | SA523440027B1 (enExample) |
| WO (1) | WO2022072721A1 (enExample) |
| ZA (1) | ZA202303449B (enExample) |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
| US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
| US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
| US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
| EP0652775B1 (en) | 1992-07-27 | 2000-04-19 | THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by the SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES | Targeting of liposomes to the blood-brain barrier |
| US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
| WO2002017930A2 (en) | 2000-08-30 | 2002-03-07 | The Board Of Trustees Of The Leland Stanford Junior University | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| US7034036B2 (en) | 2000-10-30 | 2006-04-25 | Pain Therapeutics, Inc. | Inhibitors of ABC drug transporters at the blood-brain barrier |
| DE10121982B4 (de) | 2001-05-05 | 2008-01-24 | Lts Lohmann Therapie-Systeme Ag | Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung |
| AU2002322720B2 (en) | 2001-07-25 | 2008-11-13 | Raptor Pharmaceutical Inc. | Compositions and methods for modulating blood-brain barrier transport |
| US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| AU2003302676A1 (en) | 2002-12-03 | 2004-06-23 | Blanchette Rockefeller Neurosciences Institute | Artificial low-density lipoprotein carriers for transport of substances across the blood-brain barrier |
| EP1663239A4 (en) | 2003-09-10 | 2008-07-23 | Cedars Sinai Medical Center | KALIUM CHANNEL-MEDIATED FEEDING OF MEDICINES BY THE BLOOD BRAIN BARRIER |
| CN104043126A (zh) | 2009-10-22 | 2014-09-17 | 霍夫曼-拉罗奇有限公司 | 轴突变性的调节 |
| PE20161063A1 (es) * | 2013-05-01 | 2016-10-22 | Hoffmann La Roche | Compuestos de biheteroarilo y usos de los mismos |
-
2021
- 2021-09-30 JP JP2023520162A patent/JP7805356B2/ja active Active
- 2021-09-30 EP EP21806494.7A patent/EP4222154A1/en active Pending
- 2021-09-30 CR CR20230183A patent/CR20230183A/es unknown
- 2021-09-30 MX MX2023003759A patent/MX2023003759A/es unknown
- 2021-09-30 KR KR1020237013971A patent/KR20230079123A/ko not_active Ceased
- 2021-09-30 WO PCT/US2021/053005 patent/WO2022072721A1/en not_active Ceased
- 2021-09-30 AU AU2021353532A patent/AU2021353532A1/en active Pending
- 2021-09-30 CA CA3200566A patent/CA3200566A1/en active Pending
- 2021-09-30 CN CN202180067829.1A patent/CN116744933A/zh active Pending
- 2021-09-30 BR BR112023005853A patent/BR112023005853A2/pt unknown
- 2021-09-30 PE PE2023001333A patent/PE20230781A1/es unknown
- 2021-09-30 IL IL301266A patent/IL301266A/en unknown
-
2023
- 2023-03-09 ZA ZA2023/03449A patent/ZA202303449B/en unknown
- 2023-03-30 CL CL2023000945A patent/CL2023000945A1/es unknown
- 2023-03-31 US US18/194,423 patent/US20230312473A1/en active Pending
- 2023-04-02 SA SA523440027A patent/SA523440027B1/ar unknown
-
2024
- 2024-10-07 CL CL2024003034A patent/CL2024003034A1/es unknown
- 2024-10-07 CL CL2024003032A patent/CL2024003032A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023544037A (ja) | 2023-10-19 |
| US20230312473A1 (en) | 2023-10-05 |
| BR112023005853A2 (pt) | 2023-05-02 |
| ZA202303449B (en) | 2025-04-30 |
| WO2022072721A1 (en) | 2022-04-07 |
| AU2021353532A8 (en) | 2023-05-04 |
| CL2024003034A1 (es) | 2025-02-21 |
| IL301266A (en) | 2023-05-01 |
| JP7805356B2 (ja) | 2026-01-23 |
| CL2024003032A1 (es) | 2025-02-21 |
| CL2023000945A1 (es) | 2023-09-29 |
| PE20230781A1 (es) | 2023-05-09 |
| AU2021353532A1 (en) | 2023-04-13 |
| CA3200566A1 (en) | 2022-04-07 |
| SA523440027B1 (ar) | 2024-07-31 |
| EP4222154A1 (en) | 2023-08-09 |
| MX2023003759A (es) | 2023-04-24 |
| CN116744933A (zh) | 2023-09-12 |
| KR20230079123A (ko) | 2023-06-05 |
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