AR081377A1 - Compuestos de pirazolopiridina bifuncionales - Google Patents
Compuestos de pirazolopiridina bifuncionalesInfo
- Publication number
- AR081377A1 AR081377A1 ARP110101594A ARP110101594A AR081377A1 AR 081377 A1 AR081377 A1 AR 081377A1 AR P110101594 A ARP110101594 A AR P110101594A AR P110101594 A ARP110101594 A AR P110101594A AR 081377 A1 AR081377 A1 AR 081377A1
- Authority
- AR
- Argentina
- Prior art keywords
- arylene
- het
- alkyl
- cycloalkylene
- alkynylene
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 230000001588 bifunctional effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000002993 cycloalkylene group Chemical group 0.000 abstract 5
- 125000004450 alkenylene group Chemical group 0.000 abstract 4
- 125000002947 alkylene group Chemical group 0.000 abstract 4
- 125000004419 alkynylene group Chemical group 0.000 abstract 4
- 125000000732 arylene group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000006413 ring segment Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- 125000006585 (C6-C10) arylene group Chemical group 0.000 abstract 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 abstract 1
- 206010006482 Bronchospasm Diseases 0.000 abstract 1
- 206010035664 Pneumonia Diseases 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000007885 bronchoconstriction Effects 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical group O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- A61P11/10—Expectorants
-
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se proveen su uso en la terapia de la inflamacion pulmonar o la broncoconstriccion; y composiciones que comprenden dichos compuestos y procesos para su preparacion. Reivindicacion 1: Un compuesto de la formula (1) o una de sus sales farmacéuticamente aceptables, donde X se selecciona de los grupos de formulas (2) y (3); R1 es CH2OH, CH2CH2OH, N(H)C(O)H, N(H)S(O2)CH3, y R2 es H; o R1 y R2 junto con el fenilo al cual están unidos forman un anillo heterocíclico fusionado bicíclico, que tiene 9 o 10 átomos de anillo, donde 1 o 2 átomos de anillo se seleccionan de N, O y S, y los átomos de anillo restantes son C, donde dicho anillo heterocíclico fusionado bicíclico está opcionalmente sustituido con uno, dos o tres sustituyentes adicionales seleccionados de manera independiente de alquilo, oxo y OH; R3 se selecciona de alquileno C4-12, alquenileno C4-12, alquinileno C4-12, R4-O-R4, R4-N(R8)-R4, cicloalquileno C3-6, R4-cicloalquileno C3-6, cicloalquileno C3-6-R4, R4-cicloalquileno C3-6-R4, arileno C6-10, R4-arileno C6-10, arileno C6-10-R4, R4-arileno C6-10-R4, R4-arileno C6-10-O-R4, R4-arileno C6-10-N(R8)-R4, R4-arileno C6-10-arileno C6-10, Het, R4-Het, R4-Het-arileno C6-10, R4-arileno 6-C10-arileno C6-10, Het-R4, R4-Het-R4, R4-O-Het R4-arileno C6-10-O-Het, R4-arileno C6-10-C(O)-Het y R4-arileno C6-10-N(R8)-Het; donde dichos alquileno, alquenileno, alquinileno, cicloalquileno, o arileno están opcionalmente sustituidos con 1, 2 o 3 sustituyentes seleccionados de halo, oxo y OR8; Het es un heterocicleno de 5-6 miembros, saturado o insaturado, donde 1 o 2 átomos de anillo se seleccionan de N, O y S, y donde dicho heterocicleno está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de halo, alquilo, alcoxi, oxo y OH; R4 es alquileno C1-10, alquenileno C2-10 o alquinileno C2-10, donde cada R4 está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de halo, oxo y OR8; con la condicion de que el numero total de átomos de carbono en las cadenas de alquileno C1-10, alquenileno C2-10 o alquinileno C2-10 de dos grupos R4 en cualquier definicion de R3 no sea superior a 12; Y es C(O), C(O)N(R8)CH2, N(R8)C(O), O-C(O)N(R8)CH2, N(R8)C(O)N(R8)CH2, o SO2N(R8)CH2; R5 es alquilo; R6 es H o alquilo; R7 se selecciona de cicloalquilo C3-6 no sustituido, cicloalquilo C3-6 sustituido, y un grupo heterocíclico seleccionado de las formulas (4), (5) y (6); donde Z es O, S, S(O)2, NH o N-R7a, y R7a se selecciona de alquilo, C(O)alquilo, C(O)NH2, (O)N(H)alquilo y C(O)N(alquilo)2 y R8 es H o alquilo.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33303110P | 2010-05-10 | 2010-05-10 | |
| US40693310P | 2010-10-26 | 2010-10-26 | |
| US201161477264P | 2011-04-20 | 2011-04-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR081377A1 true AR081377A1 (es) | 2012-08-29 |
Family
ID=44453952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101594A AR081377A1 (es) | 2010-05-10 | 2011-05-09 | Compuestos de pirazolopiridina bifuncionales |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US8367829B2 (es) |
| AR (1) | AR081377A1 (es) |
| UY (1) | UY33373A (es) |
| WO (1) | WO2011143106A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011143106A1 (en) | 2010-05-10 | 2011-11-17 | Gilead Sciences, Inc. | Bi - functional pyrazolopyridine compounds |
| AU2011253203A1 (en) * | 2010-05-10 | 2012-11-22 | Gilead Sciences, Inc. | Bifunctional quinoline derivatives |
| EA201591360A1 (ru) | 2013-02-19 | 2016-03-31 | Пфайзер Инк. | Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств |
| EP3172210B1 (en) | 2014-07-24 | 2020-01-15 | Pfizer Inc | Pyrazolopyrimidine compounds |
| PT3177624T (pt) | 2014-08-06 | 2019-07-11 | Pfizer | Compostos de imidazopiridazina |
| SG11201705069YA (en) | 2014-12-26 | 2017-07-28 | Univ Emory | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| WO2017089347A1 (en) | 2015-11-25 | 2017-06-01 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of braf inhibitor resistant melanomas |
| PL3706762T3 (pl) | 2017-12-07 | 2025-02-10 | Emory University | N4-hydroksycytydyna i pochodne oraz związane z nimi zastosowania przeciwwirusowe |
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| UY31635A1 (es) | 2008-02-06 | 2009-08-31 | Farmacóforos duales-antagonistas muscarínicos de pde4 | |
| WO2009142589A1 (en) | 2008-05-20 | 2009-11-26 | Astrazeneca Ab | Combination of (a) glucocorticoid receptor modulator and (b) a muscarinic antagonist |
| US8263623B2 (en) | 2008-07-11 | 2012-09-11 | Pfizer Inc. | Triazol derivatives useful for the treatment of diseases |
| UY32521A (es) | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Combinación para emplear en el tratamiento de enfermedades respiratorias |
| WO2011143106A1 (en) | 2010-05-10 | 2011-11-17 | Gilead Sciences, Inc. | Bi - functional pyrazolopyridine compounds |
-
2011
- 2011-05-09 WO PCT/US2011/035741 patent/WO2011143106A1/en not_active Ceased
- 2011-05-09 UY UY0001033373A patent/UY33373A/es not_active Application Discontinuation
- 2011-05-09 AR ARP110101594A patent/AR081377A1/es unknown
- 2011-05-09 US US13/103,598 patent/US8367829B2/en not_active Expired - Fee Related
-
2012
- 2012-09-14 US US13/619,792 patent/US8450490B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US8450490B2 (en) | 2013-05-28 |
| US20110275623A1 (en) | 2011-11-10 |
| US20130018050A1 (en) | 2013-01-17 |
| WO2011143106A1 (en) | 2011-11-17 |
| UY33373A (es) | 2011-12-30 |
| US8367829B2 (en) | 2013-02-05 |
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