PE20150730A1 - Compuestos de pirazolopirimidina - Google Patents
Compuestos de pirazolopirimidinaInfo
- Publication number
- PE20150730A1 PE20150730A1 PE2015000238A PE2015000238A PE20150730A1 PE 20150730 A1 PE20150730 A1 PE 20150730A1 PE 2015000238 A PE2015000238 A PE 2015000238A PE 2015000238 A PE2015000238 A PE 2015000238A PE 20150730 A1 PE20150730 A1 PE 20150730A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrazolo
- pyrrolidin
- pyrimidin
- hexyl
- butyl
- Prior art date
Links
- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical class C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000014150 Interferons Human genes 0.000 abstract 2
- 108010050904 Interferons Proteins 0.000 abstract 2
- 229940079322 interferon Drugs 0.000 abstract 2
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 abstract 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- BBTFCXBNLOYHSA-SPIKMXEPSA-N (z)-but-2-enedioic acid;5-butyl-3-(6-pyrrolidin-1-ylhexyl)-2h-pyrazolo[4,3-d]pyrimidin-7-amine Chemical compound OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.C12=NC(CCCC)=NC(N)=C2NN=C1CCCCCCN1CCCC1 BBTFCXBNLOYHSA-SPIKMXEPSA-N 0.000 abstract 1
- HIAVOIORLCZTDY-BTJKTKAUSA-N (z)-but-2-enedioic acid;5-butyl-3-(6-pyrrolidin-1-ylhexyl)-2h-pyrazolo[4,3-d]pyrimidin-7-amine Chemical compound OC(=O)\C=C/C(O)=O.C12=NC(CCCC)=NC(N)=C2NN=C1CCCCCCN1CCCC1 HIAVOIORLCZTDY-BTJKTKAUSA-N 0.000 abstract 1
- FWOBFZXKEUOXAS-UHFFFAOYSA-N 5-butyl-3-(6-pyrrolidin-1-ylhexyl)-2h-pyrazolo[4,3-d]pyrimidin-7-amine Chemical compound C12=NC(CCCC)=NC(N)=C2NN=C1CCCCCCN1CCCC1 FWOBFZXKEUOXAS-UHFFFAOYSA-N 0.000 abstract 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 206010039085 Rhinitis allergic Diseases 0.000 abstract 1
- 201000009961 allergic asthma Diseases 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 201000010105 allergic rhinitis Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 239000000411 inducer Substances 0.000 abstract 1
- 230000004968 inflammatory condition Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012646 vaccine adjuvant Substances 0.000 abstract 1
- 229940124931 vaccine adjuvant Drugs 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/39—Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- 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
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/555—Medicinal preparations containing antigens or antibodies characterised by a specific combination antigen/adjuvant
- A61K2039/55511—Organic adjuvants
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Mycology (AREA)
- Microbiology (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La invencion se refiere a compuestos de formula (I) y sales de los mismos: en la que R1 es n-alquilo C1-6 o alcoxi C1-2-alquilo C1-2, R2 es halo, OH o alquilo C1-3, m es un numero entero que tiene un valor de 4, 5, 6 o 7, n es un numero entero que tiene un valor de 0, 1, 2 o 3, y p es un numero entero que tiene un valor de 0, 1 o 2, son inductores de interferon humano. Los compuestos que inducen interferon humano pueden ser utiles en el tratamiento de diversos trastornos, por ejemplo en el tratamiento de enfermedades alergicas y otras afecciones inflamatorias, por ejemplo rinitis alergica y asma, enfermedades infecciosas y cancer y tambien pueden ser utiles como coadyuvantes de vacuna. Son compuestos preferidos: maleato de 5-butil-3-(6-(pirrolidin-1-il)hexil)-1H-pirazolo[4,3-d]pirimidin-7- amina; dimaleato de 5-butil-3-(6-(pirrolidin-1-il)hexil)-1H-pirazolo[4,3-d]pirimidin-7-amina; hemi-succinato de 5-butil-3-(6-(pirrolidin-1-il)hexil)-1H-pirazolo[4,3-d]pirimidin-7-amina; entre otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261692853P | 2012-08-24 | 2012-08-24 | |
| US201361774094P | 2013-03-07 | 2013-03-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20150730A1 true PE20150730A1 (es) | 2015-06-02 |
Family
ID=49085221
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015000238A PE20150730A1 (es) | 2012-08-24 | 2013-08-22 | Compuestos de pirazolopirimidina |
Country Status (26)
| Country | Link |
|---|---|
| US (5) | US9173872B2 (es) |
| EP (1) | EP2888264B1 (es) |
| JP (1) | JP6196674B2 (es) |
| KR (1) | KR20150046267A (es) |
| CN (1) | CN104755480B (es) |
| AR (1) | AR092198A1 (es) |
| AU (1) | AU2013305790B2 (es) |
| BR (1) | BR112015003259A2 (es) |
| CA (1) | CA2880576A1 (es) |
| CL (1) | CL2015000408A1 (es) |
| CR (1) | CR20150061A (es) |
| DO (1) | DOP2015000027A (es) |
| EA (1) | EA026354B1 (es) |
| ES (1) | ES2653254T3 (es) |
| HK (1) | HK1211029A1 (es) |
| IL (1) | IL236983B (es) |
| MX (1) | MX359671B (es) |
| MY (1) | MY175676A (es) |
| NZ (1) | NZ704224A (es) |
| PE (1) | PE20150730A1 (es) |
| PH (1) | PH12015500401A1 (es) |
| SG (1) | SG11201500787YA (es) |
| TW (1) | TWI625331B (es) |
| UA (1) | UA114109C2 (es) |
| UY (1) | UY34987A (es) |
| WO (1) | WO2014031815A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA103195C2 (uk) | 2008-08-11 | 2013-09-25 | Глаксосмитклайн Ллк | Похідні пурину для застосування у лікуванні алергій, запальних та інфекційних захворювань |
| DK2734186T3 (en) | 2011-07-22 | 2019-01-07 | Glaxosmithkline Llc | COMPOSITION |
| UA114109C2 (xx) * | 2012-08-24 | 2017-04-25 | Піразолопіримідинові сполуки | |
| RU2640200C2 (ru) | 2012-11-20 | 2017-12-27 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | Новые соединения |
| US9550785B2 (en) | 2012-11-20 | 2017-01-24 | Glaxosmithkline Llc | Pyrrolopyrimidines as therapeutic agents for the treatment of diseases |
| LT2922549T (lt) | 2012-11-20 | 2017-09-11 | Glaxosmithkline Llc | Naujieji junginiai |
| US11485741B2 (en) | 2018-04-24 | 2022-11-01 | Bristol-Myers Squibb Company | Macrocyclic toll-like receptor 7 (TLR7) agonists |
| US11554120B2 (en) | 2018-08-03 | 2023-01-17 | Bristol-Myers Squibb Company | 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor |
| CN110772523B (zh) * | 2019-11-07 | 2020-06-26 | 黑龙江中医药大学 | 一种用于防治肾病的药物组合物 |
| KR20220132593A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| KR20220132594A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| WO2021154663A1 (en) | 2020-01-27 | 2021-08-05 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
| KR20220132601A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| EP4097102A1 (en) | 2020-01-27 | 2022-12-07 | Bristol-Myers Squibb Company | 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists |
| JP2023512204A (ja) | 2020-01-27 | 2023-03-24 | ブリストル－マイヤーズ スクイブ カンパニー | トール様受容体７（ＴＬＲ７）アゴニストとしての１Ｈ－ピラゾロ［４，３－ｄ］ピリミジン化合物 |
| US20230131192A1 (en) | 2020-01-27 | 2023-04-27 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
| KR20220132595A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 C3-치환된 1H-피라졸로[4,3-d]피리미딘 화합물 |
| WO2021154669A1 (en) | 2020-01-27 | 2021-08-05 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
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