PE20130399A1 - COMPUESTOS DE NUCLEO IMIDAZO[1,2-a]PIRAZINA O 5,6,7,8-TETRAHIDROIMIDAZO[1,2-a]PIRAZINA SUSTITUIDOS Y COMPOSICIONES DE LOS MISMOS, UTILES EN EL TRATAMIENTO DE ENFERMEDADES PARASITICAS - Google Patents
COMPUESTOS DE NUCLEO IMIDAZO[1,2-a]PIRAZINA O 5,6,7,8-TETRAHIDROIMIDAZO[1,2-a]PIRAZINA SUSTITUIDOS Y COMPOSICIONES DE LOS MISMOS, UTILES EN EL TRATAMIENTO DE ENFERMEDADES PARASITICASInfo
- Publication number
- PE20130399A1 PE20130399A1 PE2012000026A PE2012000026A PE20130399A1 PE 20130399 A1 PE20130399 A1 PE 20130399A1 PE 2012000026 A PE2012000026 A PE 2012000026A PE 2012000026 A PE2012000026 A PE 2012000026A PE 20130399 A1 PE20130399 A1 PE 20130399A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- compositions
- pirazine
- useful
- treatment
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title 2
- GXWNSJYVSIJRLS-UHFFFAOYSA-N 6-bromo-8-methylimidazo[1,2-a]pyrazine Chemical compound CC1=NC(Br)=CN2C=CN=C12 GXWNSJYVSIJRLS-UHFFFAOYSA-N 0.000 title 1
- 208000030852 Parasitic disease Diseases 0.000 title 1
- -1 AMINO Chemical class 0.000 abstract 4
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- AXNUZKSSQHTNPZ-UHFFFAOYSA-N 3,4-difluoroaniline Chemical compound NC1=CC=C(F)C(F)=C1 AXNUZKSSQHTNPZ-UHFFFAOYSA-N 0.000 abstract 1
- QSNSCYSYFYORTR-UHFFFAOYSA-N 4-chloroaniline Chemical compound NC1=CC=C(Cl)C=C1 QSNSCYSYFYORTR-UHFFFAOYSA-N 0.000 abstract 1
- KRZCOLNOCZKSDF-UHFFFAOYSA-N 4-fluoroaniline Chemical compound NC1=CC=C(F)C=C1 KRZCOLNOCZKSDF-UHFFFAOYSA-N 0.000 abstract 1
- 241000222722 Leishmania <genus> Species 0.000 abstract 1
- 241000224016 Plasmodium Species 0.000 abstract 1
- 241000223960 Plasmodium falciparum Species 0.000 abstract 1
- 241001505293 Plasmodium ovale Species 0.000 abstract 1
- 241000223810 Plasmodium vivax Species 0.000 abstract 1
- 241000223109 Trypanosoma cruzi Species 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 201000004792 malaria Diseases 0.000 abstract 1
- 244000045947 parasite Species 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- 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
- A61K31/541—Non-condensed thiazines containing further heterocyclic 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
- A61K31/69—Boron compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/022—Boron compounds without C-boron linkages
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
REFERIDA A UN DERIVADO DE PIRAZINA DE FORMULA (Ia), (Ib) Y (Ic), DONDE n Y m SON UN ENTERO DE 0 A 4; Ra ES H, X3NR7R8, X3OR8, ENTRE OTROS; Rb ES H Y ALQUILO C1-C4; R1 ES OR13, C(O)OR13, ENTRE OTROS; R13 ES H, ALQUILO C1-C6, HALO ALQUILO C1-C6, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, AMINO, ENTRE OTROS; R4 ES H Y ALQUILO C1-C6; R5 ES H, ALQUILO C1-C6, ENTRE OTROS; R6 ES CICLOALQUILO C3-C8, ARILO C6-C10, ENTRE OTROS; R7 ES H O ALQUILO C1-C3; R8 ES ALQUILO C1-C10, CICLOALQUILO C3-C8, ENTRE OTROS; R9 ES H Y ALQUILO C1-C6; R10 ES H Y ALQUILO C1-C6; R11 ES H Y ALQUILO C1-C6; R12 ES H, ALQUILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-AMINO-1-(2-(4-FLUOROFENIL)-3-(4-FLUOROFENILAMINO)-8,8-DIMETIL-5,6-DIHIDROIMIDAZO[1,2-a]PIRAZIN-7(8H)-IL)ETANONA, 2-AMINO-1-(3-(3,4-DIFLUOROFENILAMINO)-2-(4-FLUOROFENIL)-5,6-DIHIDROIMIDAZO[1,2-a]PIRAZIN-7(8H)-IL)-2-METILPROPAN-1-ONA, 2-AMINO-1-(3-(4-CLOROFENILAMINO)-2-(4-FLUOROFENIL)-8,8-DIMETIL-5,6-DIHIDROIMIDAZO[1,2-a]PIRAZIN-7(8H)-IL)ETANONA, ENTRE OTROS. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO Y/O PREVENCION DE INFECCIONES CAUSADAS POR PLASMODIUM FALCIPARUM, PLASMODIUM VIVAX, PLASMODIUM OVALE, PLASMODIUM MALARIA, TRYPANOSOMA CRUZI Y PARASITOS DEL GENERO LEISHMANIA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22443309P | 2009-07-09 | 2009-07-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20130399A1 true PE20130399A1 (es) | 2013-04-06 |
Family
ID=42727573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012000026A PE20130399A1 (es) | 2009-07-09 | 2010-07-09 | COMPUESTOS DE NUCLEO IMIDAZO[1,2-a]PIRAZINA O 5,6,7,8-TETRAHIDROIMIDAZO[1,2-a]PIRAZINA SUSTITUIDOS Y COMPOSICIONES DE LOS MISMOS, UTILES EN EL TRATAMIENTO DE ENFERMEDADES PARASITICAS |
Country Status (38)
| Country | Link |
|---|---|
| US (3) | US8557801B2 (es) |
| EP (2) | EP2451814B1 (es) |
| JP (1) | JP5432376B2 (es) |
| KR (1) | KR101378666B1 (es) |
| CN (1) | CN102471341B (es) |
| AR (1) | AR077463A1 (es) |
| AU (1) | AU2010271247B2 (es) |
| BR (1) | BR112012000413B1 (es) |
| CA (1) | CA2767664C (es) |
| CL (1) | CL2012000042A1 (es) |
| CO (1) | CO6491060A2 (es) |
| CR (1) | CR20120008A (es) |
| CU (1) | CU24155B1 (es) |
| DK (1) | DK2451814T3 (es) |
| EA (1) | EA019655B1 (es) |
| EC (1) | ECSP12011585A (es) |
| ES (2) | ES2574529T3 (es) |
| GT (1) | GT201200004A (es) |
| HK (1) | HK1164304A1 (es) |
| HN (1) | HN2012000023A (es) |
| HR (1) | HRP20140641T1 (es) |
| IL (1) | IL217384A (es) |
| JO (1) | JO3156B1 (es) |
| MA (1) | MA33419B1 (es) |
| MX (1) | MX2012000389A (es) |
| MY (1) | MY157238A (es) |
| NZ (1) | NZ597275A (es) |
| PE (1) | PE20130399A1 (es) |
| PL (1) | PL2451814T3 (es) |
| PT (1) | PT2451814E (es) |
| SG (1) | SG176938A1 (es) |
| SI (1) | SI2451814T1 (es) |
| SM (1) | SMT201400096B (es) |
| TN (1) | TN2011000647A1 (es) |
| TW (1) | TWI421252B (es) |
| UA (1) | UA103930C2 (es) |
| UY (1) | UY32776A (es) |
| WO (1) | WO2011006143A2 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP2920169A1 (en) * | 2012-11-14 | 2015-09-23 | F. Hoffmann-La Roche AG | Imidazopyridine derivatives |
| PT2925757T (pt) | 2012-11-19 | 2018-01-09 | Novartis Ag | Compostos e composições para o tratamento de doenças parasitárias |
| US8871754B2 (en) | 2012-11-19 | 2014-10-28 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| CN105189506A (zh) * | 2012-11-19 | 2015-12-23 | 诺华股份有限公司 | 用于治疗寄生虫疾病的化合物和组合物 |
| CN103126782B (zh) * | 2013-02-26 | 2016-06-29 | 内蒙古农牧业科学院 | 一种寄生病的治疗方法 |
| AP2016009329A0 (en) * | 2013-12-19 | 2016-07-31 | Novartis Ag | [1,2,4]triazolo[1,5-a]pyrimidine derivatives as protozoan proteasome inhibitors for the treatment of parasitic diseases such as leishmaniasis |
| EP3328857B1 (en) * | 2015-07-31 | 2019-08-14 | Merck Patent GmbH | Bicyclic heterocyclic derivatives |
| RU2019107162A (ru) | 2016-08-15 | 2020-09-15 | Байер Кропсайенс Акциенгезельшафт | Конденсированные бициклические гетероциклические производные в качестве средств для борьбы с вредителями |
| WO2018198021A1 (en) * | 2017-04-24 | 2018-11-01 | Novartis Ag | Therapeutic regimen of 2-amino-l-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8h)-yl)ethanone and combinations thereof |
| FI3652178T3 (fi) | 2017-07-14 | 2024-03-19 | Hoffmann La Roche | Bisyklisiä ketoniyhdisteitä ja niiden käyttömenetelmiä |
| WO2019070943A1 (en) * | 2017-10-04 | 2019-04-11 | Dana-Farber Cancer Institute, Inc. | SMALL MOLECULE INHIBITION OF SALL4 TRANSCRIPTION FACTOR AND USES THEREOF |
| WO2022049548A1 (en) | 2020-09-04 | 2022-03-10 | Novartis Ag | Kaf156 combinations and methods for the treatment of malaria |
| WO2023168107A2 (en) * | 2022-03-04 | 2023-09-07 | University Of Central Florida Research Foundation, Inc. | Compounds and compositions for anitmalarial therapeutic and prophylactic use |
| CN114569711B (zh) * | 2022-03-24 | 2024-04-19 | 安徽医科大学 | 一种预防弓形虫病的ME49Δcdpk3减毒活疫苗及其制备方法和应用 |
| WO2024006974A2 (en) * | 2022-07-01 | 2024-01-04 | The Scripps Research Institute | Antimalarial compounds |
| WO2024006970A2 (en) * | 2022-07-01 | 2024-01-04 | The Scripps Research Institute | Antimalarial compounds |
| WO2024006971A2 (en) * | 2022-07-01 | 2024-01-04 | The Scripps Research Institute | Antimalarial compounds |
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| DK476885D0 (da) | 1985-10-17 | 1985-10-17 | Ferrosan As | Heterocycliske forbindelser og fremgangsmaader til fremstilling heraf |
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| FR2803525B1 (fr) | 2000-01-06 | 2002-05-03 | Sod Conseils Rech Applic | Inhibiteur de la transduction des signaux des proteines g heterotrimeriques associe a un agent anti-hypertenseur dans le traitement de l'hypertension arterielle |
| KR20030020960A (ko) | 2000-08-01 | 2003-03-10 | 소시에떼 더 콘세이유 더 레세르세 에 다플리까띠옹 시엔띠피끄, 에스.아.에스. | 이미다졸일 유도체 |
| BR0116662A (pt) * | 2001-01-02 | 2003-09-23 | Hoffmann La Roche | Derivados de quinazolona como antagonistas receptores alfa 1a/b adrenérgicos |
| FR2825278A1 (fr) | 2001-05-30 | 2002-12-06 | Sod Conseils Rech Applic | Produit comprenant du mikanolide, du dihydromikanolide ou un analogue de ceux-ci en association avec un autre agent anti-cancereux pour une utilisation therapeutique dans le traitement du cancer |
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