AR105575A1 - COMPUESTOS DE QUINOLINA COMO MODULADORES DE TNFa - Google Patents
COMPUESTOS DE QUINOLINA COMO MODULADORES DE TNFaInfo
- Publication number
- AR105575A1 AR105575A1 ARP160102357A ARP160102357A AR105575A1 AR 105575 A1 AR105575 A1 AR 105575A1 AR P160102357 A ARP160102357 A AR P160102357A AR P160102357 A ARP160102357 A AR P160102357A AR 105575 A1 AR105575 A1 AR 105575A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- aryl
- heterocyclyl
- independently
- Prior art date
Links
Classifications
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- 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
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
- C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Quinoline Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
También métodos para usar tales compuestos como moduladores de TNFa, y composiciones farmacéuticas que comprenden tales compuestos. Estos compuestos son útiles para tratar enfermedades inflamatorias y autoinmunitarias. Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o una sal de aquel, en donde: A es CR¹ o N; B es CR³ o N; D es CR⁴ o N; X es un enlace, -O-, -S- o -NR⁸-; L¹ es (CR⁷R⁷)ₘ; L² es -(CR⁷R⁷)ₙ-; Z es un grupo cíclico seleccionado de carbociclilo, heterociclilo, arilo y heteroarilo, en donde el grupo cíclico se sustituye con 0 a 3 Rᵃ; R¹ es H, halo, -CN, C₁₋₄ alquilo, C₁₋₆ haloalquilo o C₁₋₃ alcoxi; R² es H, R¹ᵃ, C₁₋₆ haloalquilo, C₂₋₆ alquenilo sustituido con 0 a 6 R¹ᵃ, C₂₋₆ alquinilo sustituido con 0 a 4 R¹ᵃ, -(CRᵍRᵍ)ʳ(carbociclilo de 3 a 14 miembros sustituido con 0 a 3 R¹ᵃ), -(CRᵍRᵍ)ʳ(arilo sustituido con 0 a 3 R¹ᵃ), -(CRᵍRᵍ)ʳ(heterociclilo de 5 a 7 miembros sustituido con 0 a 3 R¹ᵃ) o -(CRᵍRᵍ)ʳ(heteroarilo mono- o bicíclico sustituido con 0 a 3 R¹ᵃ); R³ es H, halo, -CN, -CF₃, -OCF₃, -NO₂, C₁₋₆ alquilo sustituido con 0 a 6 R¹ᵃ, -(CRᵍRᵍ)ʳORᵉ, (CRᵍRᵍ)ʳNRᶜRᶜ, -(CRᵍRᵍ)ʳS(O)ₚRᵇ, -(CRᵍRᵍ)ʳ(carbociclilo de 3 a 14 miembros sustituido con 0 a 3 R¹ᵃ), -(CRᵍRᵍ)ʳ(arilo sustituido con 0 a 3 R¹ᵃ), -(CRᵍRᵍ)ʳ(heterociclilo de 5 a 7 miembros sustituido con 0 a 3 R¹ᵃ) o -(CRᵍRᵍ)ʳ(heteroarilo monocíclico sustituido con 0 a 3 R¹ᵃ); R⁴ es H, halo, -CN, C₁₋₄ alquilo, C₁₋₆ haloalquilo o C₁₋₃ alcoxi; R⁵ y R⁶ son independientemente H, halo, -OH, -CN, C₁₋₅ alquilo sustituido con 0 a 6 Rᵃ, C₃₋₆ cicloalquilo sustituido con 0 a 6 Rᵃ, C₁₋₅ alquiltio sustituido con 0 a 6 Rᵃ, ariltio sustituido con 0 a 6 Rᵃ, C₁₋₅ alcoxi sustituido con 0 a 6 Rᵃ, ariloxi sustituido con 0 a 6 Rᵃ, -C(O)ORʰ, -C(O)NRʰRʰ, -NRʰRʰ, -NRᵇC(O)NRᶜRᶜ, -NRʰC(O)Rʸ, -NRᵇC(O)ORᵇ, -NRᵇS(O)₂NRᶜRᶜ o -NRʰS(O)₂Rʸ; o R⁵ y R⁶, junto con los carbonos a los que están unidos, forman un anillo carbocíclico o heterocíclico de 5 a 7 miembros; cada R⁷ es independientemente H, -OH, C₁₋₃ alquilo, C₁₋₃ fluoroalquilo, C₁₋₃ hidroxialquilo, C₁₋₂ aminoalquilo, -CH₂CH=CH₂, C₃₋₆ cicloalquilo, fenilo o -NRʰRʰ; o dos R⁷, junto con el átomo de carbono al que están unidos, forman un grupo espirocarbociclilo o espiroheterociclilo de 3 a 7 miembros; R⁸ es H o C₁₋₃ alquilo; cada R¹ᵃ es independientemente F, Cl, Br, -CN, C₁₋₆ alquilo sustituido con 0 a 6 Rᵃ, C₃₋₆ cicloalquilo sustituido con 0 a 6 Rᵃ, C₁₋₃ alcoxi sustituido con 0 a 7 Rᵃ, heterociclilo sustituido con 0 a 6 Rᵃ, arilo sustituido con 0 a 6 Rᵃ, heteroarilo mono- o bicíclico sustituido con 0 a 6 Rᵃ, -C(O)Rᵇ, -C(O)ORᵇ, -C(O)NRᶜRᶜ, -OC(O)Rᵇ, -OC(O)NRᶜRᶜ, -OC(O)ORᵈ, -NRᶜRᶜ, -NRᵇC(O)Rᵈ, -NRᵇC(O)ORᵈ, NRᵇS(O)ₚRᵈ, -NRᵇC(O)NRᶜRᶜ, -NRᵇS(O)ₚNRᶜRᶜ, S(O)ₚRᵇ, -S(O)ₚNRᶜRᶜ o -C(O)NRᵇ(CH₂)₁₋₃NRᶜRᶜ; cada Rᵃ es independientemente halo, -CN, -OH, -NO₂, -NH₂, -N₃, C₁₋₇ alquilo sustituido con 0 a 6 Rʷ; C₂₋₄ alquenilo, C₂₋₄ alquinilo, C₁₋₃ alcoxi, C₁₋₃ fluoroalcoxi, C₁₋₃ hidroxialcoxi, -O(CH=CH₂), -(CH₂)ʳC(O)OH, -O(CH₂)ʳC(O)OH, -(CH₂)ʳC(O)(C₁₋₆ alquilo), -C(O)O(C₁₋₄ alquilo), -OC(O)(C₁₋₃ alquilo), -NH(C₁₋₆ alquilo), -N(C₁₋₃ alquilo)₂, -(CH₂)₀₋₂C₍O₎NH₂, -(CH₂)₀₋₂C₍O₎NH₍C₁₋₃ alquilo), -(CH₂)₀₋₂C₍O₎N₍C₁₋₃ alquilo)₂, -OC(O)NH(C₁₋₃ alquilo), -C(O)CH(NH₂)(CH₂)₁₋₂C₍O₎OH, ₋C₍O₎CH₍NH₂)(CH₂)₁₋₂OH, -C(O)(CH₂)₁₋₂C(O)OH, -C(O)(C₂₋₄ alquenilo), -C(O)(C₂₋₄ alquinilo), -CºCH, -CºC(fenilo), -NHC(O)NH₂, -NHC(O)NH(C₁₋₃ alquilo), -CH=NOH, -C(=NH)(NH₂), C₃₋₇ carbociclilo, arilo, heterociclilo de 5 a 7 miembros, heteroarilo monocíclico o bicíclico, -(CH₂)ʳ(arilo), -(CH₂)ʳ(heteroarilo), -O(arilo), -O(bencilo), -O(heterociclilo), -O(heteroarilo), -S(O)₂NH₂, -S(O)₂CH₂CH₂C(O)O(C₁₋₃ alquilo), -S(O)ₚ(C₁₋₃ alquilo), -S(O)ₚ(arilo), -S(O)ₚ(heterociclilo), -NHS(O)₂(arilo), -NHS(O)₂(heterociclilo), -NHS(O)₂NH(arilo), -NHS(O)₂NH(heterociclilo), -NH(arilo sustituido con 0 a 3 Rˣ), -NH(heterociclilo), -NHC(O)(arilo), -NHC(O)(C₁₋₃ alquilo), -NHC(O)(heterociclilo), -OC(O)(arilo), -OC(O)(heterociclilo), -NHC(O)NH(arilo), -NHC(O)NH(heterociclilo), -OC(O)O(C₁₋₃ alquilo), -OC(O)O(arilo), -OC(O)O(heterociclilo), -OC(O)NH(arilo), -OC(O)NH(heterociclilo), -NHC(O)O(arilo), -NHC(O)O(heterociclilo), -NHC(O)O(C₁₋₄ alquilo), -C(O)NH(arilo), -C(O)NH(heterociclilo), -C(O)O(arilo), C(O)O(heterociclilo), -N(C₁₋₃ alquil)S(O)₂(arilo), -N(C₁₋₃ alquil)S(O)₂(heterociclilo), -N(C₁₋₃ alquil)S(O)₂NH(arilo), -N(C₁₋₃ alquil)S(O)₂NH(heterociclilo), -N(C₁₋₃ alquil)(arilo), -N(C₁₋₃ alquil)(heterociclilo), -N(C₁₋₃ alquil)C(O)(arilo), -N(C₁₋₃ alquil)C(O)(heterociclilo), -N(C₁₋₃ alquil)C(O)NH(arilo), -(CH₂)₀₋₃C₍O₎NH₍ₕₑₜₑʳₒᶜⁱᶜₗⁱₗₒ₎, ₋OC₍O₎N₍C₁₋₃ alquil)(arilo), -OC(O)N(C₁₋₃ alquil)(heterociclilo), -N(C₁₋₃ alquil)C(O)O(arilo), -N(C₁₋₃ alquil)C(O)O(heterociclilo), -C(O)N(C₁₋₃ alquil)(arilo), -C(O)N(C₁₋₃ alquil)(heterociclilo), -NHS(O)₂N(C₁₋₃ alquil)(arilo), -NHS(O)₂N(C₁₋₃ alquil)(heterociclilo), -NHP(O)₂N(C₁₋₃ alquil)(arilo), -NHC(O)N(C₁₋₃ alquil)(arilo), -NHC(O)N(C₁₋₃ alquil)(heterociclilo), -N(C₁₋₃ alquil)S(O)₂N(C₁₋₃ alquil)(arilo), -(CH₂)₀₋₂C₍O₎NHS₍O₎₂(C₁₋₃ alquilo), -N(C₁₋₃ alquil)S(O)₂N(C₁₋₃ alquil)(heterociclilo), -N(C₁₋₃ alquil)C(O)N(C₁₋₃ alquil)(arilo), -N(C₁₋₃ alquil)C(O)N(C₁₋₃ alquil)(heterociclilo) o -Si(C₁₋₃ alquilo)₃, en donde cada uno de carbociclilo, arilo, heterociclilo y heteroarilo se sustituye con 0 a 4 Rᶻ; o dos Rᵃ, unidos al mismo átomo de carbono, forman =O; cada Rᵇ es independientemente H, C₁₋₆ alquilo sustituido con 0 a 6 Rᶠ, C₃₋₇ cicloalquilo sustituido con 0 a 6 Rᶠ, heterociclilo sustituido con 0 a 6 Rᶠ, arilo sustituido con 0 a 3 Rᶠ o heteroarilo mono- o bicíclico sustituido con o a 3 Rᶠ; cada Rᶜ es independientemente H, C₁₋₆ alquilo sustituido con 0 a 6 Rᶠ, C₃₋₇ cicloalquilo sustituido con 0 a 6 Rᶠ, heterociclilo sustituido con 0 a 6 Rᶠ, arilo sustituido con 0 a 3 Rᶠ o heteroarilo mono- o bicíclico sustituido con 0 a 3 Rᶠ; o dos Rᶜ, unidos al mismo átomo de nitrógeno, forman un anillo heterocíclico de 4 a 8 miembros sustituido con 0 a 3 Rᵍ; cada Rᵈ es independientemente H, C₁₋₆ alquilo sustituido con 0 a 6 Rᶠ, C₃₋₇ cicloalquilo sustituido con 0 a 6 Rᶠ, heterociclilo sustituido con 0 a 6 Rᶠ, arilo sustituido con 0 a 3 Rᶠ o heteroarilo mono- o bicíclico sustituido con 0 a 3 Rᶠ; cada Rᵉ es independientemente H, C₁₋₆ alquilo sustituido con 0 a 7 Rᶠ, C₃₋₇ cicloalquilo sustituido con 0 a 6 Rᶠ, heterociclilo sustituido con 0 a 6 Rᶠ, arilo sustituido con 0 a 3 Rᶠ o heteroarilo mono- o bicíclico sustituido con 0 a 3 Rᶠ; cada Rᶠ es independientemente H, halo, -OH, -CN, -NH₂, C₁₋₆ alquilo sustituido con 0 a 6 Rᵃ, C₁₋₃ alcoxi sustituido con 0 a 7 Rᵃ, C₃₋₇ cicloalquilo sustituido con 0 a 6 Rᵃ, heterociclilo sustituido con 0 a 6 Rᵃ, arilo sustituido con 0 a 3 Rᵃ o heteroarilo mono- o bicíclico sustituido con 0 a 3 Rᵃ; cada Rᵍ es independientemente H, F, -OH, -CN, C₁₋₃ alquilo, -CF₃ o fenilo; cada Rʰ es independientemente H, C₁₋₅ alquilo sustituido con 0 a 2 Rˣ, C₃₋₇ cicloalquilo sustituido con 0 a 2 Rˣ, heterociclilo mono- o bicíclico sustituido con o a 2 Rˣ, arilo sustituido con 0 a 2 Rˣ o heteroarilo mono- o bicíclico sustituido con 0 a 2 Rˣ; cada Rʷ es independientemente F, -OH, -CN, -NH₂, -C(O)OH, -C(O)(C₁₋₃ alquilo), -C(O)NH₂, -C(O)NH(C₁₋₃ alquilo), -NHC(O)(C₁₋₃ alquilo) o -C(O)NHS(O)₂(C₁₋₃ alquilo); cada Rˣ es independientemente H, halo, -CN, C₁₋₄ alquilo, C₁₋₆ haloalquilo o C₁₋₃ alcoxi; cada Rʸ es independientemente C₁₋₅ alquilo; cada Rᶻ es independientemente H, halo, -CN, C₁₋₄ alquilo, C₁₋₄ hidroxialquilo, C₁₋₆ haloalquilo, C₁₋₃ alcoxi, -NH₂, -NH(C₁₋₃ alquilo), -N(C₁₋₃ alquilo)₂, -OC(O)(C₁₋₄ alquilo), -C(O)OH, -CH₂C(O)OH, -CH₂(fenilo), -CH₂CH₂(morfolinilo), C(O)(morfolinilo), C₃₋₆ cicloalquilo y morfolinilo; o dos Rᶻ, unidos al mismo átomo de carbono, forman =O; m es 0, 1, 2, 3 ó 4; n es 0, 1, 2, 3 ó 4; cada p es independientemente 0, 1 ó 2; y cada r es independientemente 0, 1, 2, 3 ó 4; siempre que cuando al menos uno de R⁵ y R⁶ es H, entonces X sea -O-, -S- o -NR⁸-, uno de m y n sea 1, 2, 3 ó 4, y el otro de m y n sea 0, 1, 2, 3 ó 4.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562200424P | 2015-08-03 | 2015-08-03 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR105575A1 true AR105575A1 (es) | 2017-10-18 |
Family
ID=56618285
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160102357A AR105575A1 (es) | 2015-08-03 | 2016-08-02 | COMPUESTOS DE QUINOLINA COMO MODULADORES DE TNFa |
Country Status (22)
Country | Link |
---|---|
US (1) | US10865191B2 (es) |
EP (1) | EP3331871A1 (es) |
JP (1) | JP6955482B2 (es) |
KR (1) | KR20180031772A (es) |
CN (1) | CN108137547B (es) |
AR (1) | AR105575A1 (es) |
AU (1) | AU2016302144B2 (es) |
BR (1) | BR112018001960A2 (es) |
CA (1) | CA2994717A1 (es) |
CL (1) | CL2018000293A1 (es) |
CO (1) | CO2018002061A2 (es) |
EA (1) | EA033686B1 (es) |
HK (1) | HK1252623A1 (es) |
IL (1) | IL257154A (es) |
MA (1) | MA43512A (es) |
MX (1) | MX2018001054A (es) |
PE (1) | PE20181366A1 (es) |
SG (1) | SG10201911831RA (es) |
TW (1) | TW201718536A (es) |
UY (1) | UY36838A (es) |
WO (1) | WO2017023905A1 (es) |
ZA (1) | ZA201800716B (es) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2016168633A1 (en) | 2015-04-17 | 2016-10-20 | Abbvie Inc. | Indazolones as modulators of tnf signaling |
TW201710257A (zh) | 2015-04-17 | 2017-03-16 | 艾伯維有限公司 | Tnf信號傳遞之三環調節劑 |
TW201702247A (zh) | 2015-04-17 | 2017-01-16 | 艾伯維有限公司 | 作為tnf信號傳遞調節劑之吲唑酮 |
GB201510758D0 (en) | 2015-06-18 | 2015-08-05 | Ucb Biopharma Sprl | Novel TNFa structure for use in therapy |
US9975887B2 (en) | 2015-08-03 | 2018-05-22 | Glenmark Pharmaceuticals S.A. | Compounds as ROR gamma modulators |
GB201513742D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
GB201621907D0 (en) | 2016-12-21 | 2017-02-01 | Ucb Biopharma Sprl And Sanofi | Antibody epitope |
JOP20190257A1 (ar) | 2017-04-28 | 2019-10-28 | Novartis Ag | مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats |
CN111868036A (zh) * | 2018-02-09 | 2020-10-30 | 美国政府健康与人类服务部 | 杂环p2y14受体拮抗剂 |
CN108658977A (zh) * | 2018-04-12 | 2018-10-16 | 苏州康润医药有限公司 | 一种7-溴-1,5-萘啶-3-甲酸的合成方法 |
US20230192617A1 (en) | 2020-05-19 | 2023-06-22 | Bayer Cropscience Aktiengesellschaft | Azabicyclic(thio)amides as fungicidal compounds |
WO2021249995A1 (en) | 2020-06-10 | 2021-12-16 | Bayer Aktiengesellschaft | Azabicyclyl-substituted heterocycles as fungicides |
US11926632B2 (en) | 2020-06-22 | 2024-03-12 | Pmv Pharmaceuticals, Inc. | Methods and compounds for restoring mutant p53 function |
EP4267554A1 (en) | 2020-12-22 | 2023-11-01 | Mekanistic Therapeutics LLC | Substituted aminobenzyl heteroaryl compounds as egfr and/or pi3k inhibitors |
WO2023067546A1 (en) * | 2021-10-21 | 2023-04-27 | Satyarx Pharma Innovations Pvt Ltd | Novel bicyclic heteroaryl derivatives as sos1:kras proteinprotein interaction inhibitors |
CN114605409B (zh) * | 2022-04-01 | 2024-04-02 | 苏州睿尔思科技有限公司 | 一种4-羟基-1,5-萘啶类配体的生产制备方法 |
CN114751858B (zh) * | 2022-04-20 | 2023-09-12 | 沈阳药科大学 | 含有喹啉基的氨甲环酸衍生物及其制备与应用 |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US856095A (en) * | 1906-09-01 | 1907-06-04 | Railway Safety Signal Company | Electric semaphore. |
NZ223875A (en) * | 1987-03-17 | 1991-01-29 | Hoechst Roussel Pharma | 9-aminotetrahydroacridines and related homologues and pharmaceutical compositions |
DE3917232A1 (de) * | 1989-05-26 | 1990-11-29 | Basf Ag | 4-arylmethamino-2,3-dialkyl-chinoline, ihre verwendung und daraus hergestellte arzneimittel |
SK14142003A3 (sk) | 2001-05-31 | 2005-03-04 | Sanofi-Aventis | Aminochinolínové a aminopyridínové deriváty a ich použitie ako adenozínových A3 ligandov |
WO2003024899A2 (en) * | 2001-09-17 | 2003-03-27 | Bristol-Myers Squibb Company | CYCLIC HYDROXAMIC ACIDS AS INHIBITORS OF MATRIX METALLOPROTEINASES AND/OR TNF-α CONVERTING ENZYME (TACE) |
AU2002357312A1 (en) * | 2001-12-20 | 2003-07-09 | Bristol-Myers Squibb Company | Barbituric acid derivatives as inhibitors of tnf-alpha converting enzyme (tace) and/or matrix metalloproteinases |
HUP0105406A3 (en) * | 2001-12-21 | 2003-12-29 | Sanofi Aventis | Imidazo[1,2-a]quinolin derivatives, process for their preparation, pharmaceutical compositions thereof and intermediates |
JP2007500689A (ja) | 2003-07-31 | 2007-01-18 | サノフイ−アベンテイス | アミノキノリン誘導体およびアデノシンa3リガンドとしてのそれらの使用 |
TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
CA2725014C (en) * | 2008-05-30 | 2014-06-17 | Amgen Inc. | Inhibitors of pi3 kinase |
CA2806332C (en) * | 2010-07-30 | 2017-11-14 | Oncotherapy Science, Inc. | Quinoline derivatives and melk inhibitors containing the same |
EP2858983B1 (en) | 2012-06-11 | 2018-04-18 | UCB Biopharma SPRL | Tnf-alpha modulating benzimidazoles |
GB201212513D0 (en) | 2012-07-13 | 2012-08-29 | Ucb Pharma Sa | Therapeutic agents |
US9309243B2 (en) | 2012-07-13 | 2016-04-12 | Ucb Biopharma Sprl | Imidazopyridine derivatives as modulators of TNF activity |
TR201812261T4 (tr) * | 2012-11-01 | 2018-11-21 | Infinity Pharmaceuticals Inc | Pi3 ki̇naz i̇zoform modülatörleri̇ i̇le kanser tedavi̇si̇ |
US9695179B2 (en) | 2013-03-14 | 2017-07-04 | Convergene Llc | Methods and compositions for inhibition of bromodomain-containing proteins |
AR105556A1 (es) | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
GB201513742D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
US9975887B2 (en) | 2015-08-03 | 2018-05-22 | Glenmark Pharmaceuticals S.A. | Compounds as ROR gamma modulators |
EP3436459B1 (en) | 2016-04-01 | 2021-08-25 | UCB Biopharma SRL | Fused pentacyclic imidazole derivatives as modulators of tnf activity |
-
2016
- 2016-08-02 MA MA043512A patent/MA43512A/fr unknown
- 2016-08-02 EP EP16750343.2A patent/EP3331871A1/en not_active Withdrawn
- 2016-08-02 AU AU2016302144A patent/AU2016302144B2/en not_active Ceased
- 2016-08-02 TW TW105124501A patent/TW201718536A/zh unknown
- 2016-08-02 BR BR112018001960A patent/BR112018001960A2/pt not_active IP Right Cessation
- 2016-08-02 KR KR1020187005707A patent/KR20180031772A/ko active IP Right Grant
- 2016-08-02 PE PE2018000172A patent/PE20181366A1/es unknown
- 2016-08-02 MX MX2018001054A patent/MX2018001054A/es active IP Right Grant
- 2016-08-02 CA CA2994717A patent/CA2994717A1/en not_active Abandoned
- 2016-08-02 US US15/887,214 patent/US10865191B2/en active Active
- 2016-08-02 UY UY0001036838A patent/UY36838A/es unknown
- 2016-08-02 SG SG10201911831RA patent/SG10201911831RA/en unknown
- 2016-08-02 AR ARP160102357A patent/AR105575A1/es unknown
- 2016-08-02 CN CN201680057509.7A patent/CN108137547B/zh active Active
- 2016-08-02 JP JP2018506144A patent/JP6955482B2/ja active Active
- 2016-08-02 EA EA201890165A patent/EA033686B1/ru not_active IP Right Cessation
- 2016-08-02 WO PCT/US2016/045110 patent/WO2017023905A1/en active Application Filing
-
2018
- 2018-01-25 IL IL257154A patent/IL257154A/en unknown
- 2018-02-01 CL CL2018000293A patent/CL2018000293A1/es unknown
- 2018-02-02 ZA ZA2018/00716A patent/ZA201800716B/en unknown
- 2018-02-26 CO CONC2018/0002061A patent/CO2018002061A2/es unknown
- 2018-09-17 HK HK18111924.8A patent/HK1252623A1/zh unknown
Also Published As
Publication number | Publication date |
---|---|
IL257154A (en) | 2018-03-29 |
MA43512A (fr) | 2018-11-07 |
EA201890165A1 (ru) | 2018-07-31 |
EP3331871A1 (en) | 2018-06-13 |
JP6955482B2 (ja) | 2021-10-27 |
UY36838A (es) | 2017-01-31 |
CL2018000293A1 (es) | 2018-07-13 |
BR112018001960A2 (pt) | 2018-09-18 |
US10865191B2 (en) | 2020-12-15 |
MX2018001054A (es) | 2018-07-06 |
AU2016302144B2 (en) | 2020-10-08 |
AU2016302144A1 (en) | 2018-03-22 |
US20180222883A1 (en) | 2018-08-09 |
ZA201800716B (en) | 2019-07-31 |
JP2018525379A (ja) | 2018-09-06 |
CN108137547B (zh) | 2021-11-12 |
CA2994717A1 (en) | 2017-02-09 |
EA033686B1 (ru) | 2019-11-15 |
TW201718536A (zh) | 2017-06-01 |
WO2017023905A1 (en) | 2017-02-09 |
KR20180031772A (ko) | 2018-03-28 |
CO2018002061A2 (es) | 2018-06-20 |
SG10201911831RA (en) | 2020-02-27 |
PE20181366A1 (es) | 2018-08-27 |
CN108137547A (zh) | 2018-06-08 |
HK1252623A1 (zh) | 2019-05-31 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR105575A1 (es) | COMPUESTOS DE QUINOLINA COMO MODULADORES DE TNFa | |
AR105845A1 (es) | Compuestos de heteroarilo bicíclicos fusionados como moduladores de la función irak4 | |
AR099177A1 (es) | Determinadas (2s)-n-[(1s)-1-ciano-2-feniletil]-1,4-oxazepan-2-carboxamidas como inhibidores de dipeptidil peptidasa 1 | |
AR108838A1 (es) | Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa | |
AR100809A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
AR104176A1 (es) | Inhibidores de ido (indolamina-2,3-dioxigenasa) | |
AR095359A1 (es) | Compuestos heteroaromáticos y su uso como ligandos d1 de dopamina | |
AR106798A1 (es) | Inhibidores pirazol de acc y usos de los mismos | |
AR103833A1 (es) | Compuestos bicíclicos de sulfonamida cetona | |
AR094452A1 (es) | COMPUESTOS HETEROCÍCLICOS SUSTITUIDOS CON AMIDA ÚTILES COMO MODULADORES DE LAS RESPUESTAS DE IL-12, IL-23 Y/O INFa | |
AR093505A1 (es) | Derivados de 5-fluoro-n-(piridin-2-il)piridin-2-amina que contienen un grupo sulfoximina | |
AR094537A1 (es) | COMPUESTOS DE PIRIDILO SUSTITUIDOS CON ALQUILAMIDA ÚTILES COMO MODULADORES DE LAS RESPUESTAS DE IL-12, IL-23 Y/O IFNa | |
AR104884A1 (es) | Compuestos de 4-hidroxi-3-(heteroaril)piridin-2-ona como agonistas de apj | |
AR091193A1 (es) | HETEROCICLOS DE 5 MIEMBROS QUE CONTIENEN NITROGENO SUSTITUIDO POR CARBOXAMIDA O SULFONAMIDA COMO MODULADORES PARA EL RECEPTOR NUCLEAR HUERFANO RORg | |
AR111407A1 (es) | Compuestos inhibidores de ask1 y usos de los mismos | |
AR106297A1 (es) | Compuestos macrocíclicos modificados como inhibidores selectivos de la quinasa cdk9 | |
AR092869A1 (es) | Alcoxipirazoles como activadores de guanilato ciclasa soluble | |
AR095430A1 (es) | Compuestos de pirimidina y piridina y su uso como inhibidores de la actividad de fgfr | |
AR100808A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
AR093503A1 (es) | Derivados de n-(piridin-2-il)pirimidin-4-amina que contienen un grupo sulfoximina | |
AR093504A1 (es) | 4-(orto)-fluorofenil-5-fluoropirimidin-2-ilaminas que contienen un grupo sulfoximina como inhibidores de cdk9, un intermediario para su sintesis y metodos de obtencion de ambos compuestos | |
AR106604A1 (es) | Compuestos de criptoficina y productos conjugados, su preparación y su uso terapéutico | |
AR099890A1 (es) | Inhibidores de histona demetilasas | |
AR106185A1 (es) | Compuestos macrocíclicos de sulfondiimina | |
AR108010A1 (es) | Derivados de indolina y su uso como inhibidores de ews-fli1 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |