AR114464A1 - PROFÁRMACOS DE ANTAGONISTAS DE C5aR BICÍCLICOS FUSIONADOS - Google Patents
PROFÁRMACOS DE ANTAGONISTAS DE C5aR BICÍCLICOS FUSIONADOSInfo
- Publication number
- AR114464A1 AR114464A1 ARP190100863A ARP190100863A AR114464A1 AR 114464 A1 AR114464 A1 AR 114464A1 AR P190100863 A ARP190100863 A AR P190100863A AR P190100863 A ARP190100863 A AR P190100863A AR 114464 A1 AR114464 A1 AR 114464A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- haloalkyl
- independently selected
- hydrogen
- Prior art date
Links
- 102100032957 C5a anaphylatoxin chemotactic receptor 1 Human genes 0.000 title 1
- 101710098483 C5a anaphylatoxin chemotactic receptor 1 Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 abstract 10
- 239000001257 hydrogen Substances 0.000 abstract 7
- 150000002431 hydrogen Chemical class 0.000 abstract 6
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 150000003839 salts Chemical class 0.000 abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 3
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 abstract 3
- 150000001413 amino acids Chemical class 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 2
- 108010016626 Dipeptides Proteins 0.000 abstract 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 abstract 2
- 101100133350 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) nhp-1 gene Proteins 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 229940024606 amino acid Drugs 0.000 abstract 2
- 235000001014 amino acid Nutrition 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 1
- 239000004471 Glycine Substances 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 abstract 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 abstract 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 abstract 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 abstract 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 abstract 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 abstract 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 abstract 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 abstract 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 abstract 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 abstract 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 abstract 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 abstract 1
- 239000004472 Lysine Substances 0.000 abstract 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 abstract 1
- 229960003767 alanine Drugs 0.000 abstract 1
- 235000004279 alanine Nutrition 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 229940009098 aspartate Drugs 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229960002433 cysteine Drugs 0.000 abstract 1
- 235000018417 cysteine Nutrition 0.000 abstract 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 abstract 1
- 229940049906 glutamate Drugs 0.000 abstract 1
- 229930195712 glutamate Natural products 0.000 abstract 1
- 229960002449 glycine Drugs 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 229960002885 histidine Drugs 0.000 abstract 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 229960000310 isoleucine Drugs 0.000 abstract 1
- 235000014705 isoleucine Nutrition 0.000 abstract 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 abstract 1
- 229960003136 leucine Drugs 0.000 abstract 1
- 235000005772 leucine Nutrition 0.000 abstract 1
- 235000018977 lysine Nutrition 0.000 abstract 1
- 229960003646 lysine Drugs 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229960005190 phenylalanine Drugs 0.000 abstract 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229960004295 valine Drugs 0.000 abstract 1
- 235000014393 valine Nutrition 0.000 abstract 1
- 239000004474 valine Substances 0.000 abstract 1
Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- 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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- 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
- A61P37/06—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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- 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
-
- 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
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Biochemistry (AREA)
- Pulmonology (AREA)
- Molecular Biology (AREA)
- Ophthalmology & Optometry (AREA)
- Transplantation (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Reivindicación 1: Un compuesto de una cualquiera de las fórmulas (1), (2), (3), (4), (5) ó (6), o una sal farmacéuticamente aceptable de los mismos, caracterizado porque: el vértice del anillo a es N o C(R²ᶜ), el vértice del anillo b es N o C(R²ᵈ), y el vértice del anillo e es N o C(R²ᵉ), en donde no más de uno de a, b y e es N; X¹ se selecciona entre el grupo que consiste en un enlace, alquileno C₁₋₈, C(O), C(O)-alquileno C₁₋₄, y S(O)₂; R¹ se selecciona entre el grupo que consiste en: a) heteroarilo de 5 a 10 miembros que tiene desde 1 hasta 4 heteroátomos como vértices del anillo seleccionados entre N, O y S; b) arilo C₆₋₁₀; c) cicloalquilo C₃₋₈; d) heterocicloalquilo de 4 a 8 miembros que tiene desde 1 hasta 2 heteroátomos como vértices del anillo seleccionados entre N, O y S; y e) alquilo C₁₋₈, alcoxi C₁₋₈, haloalquilo C₁₋₈, -C(O)NR¹ᵃR¹ᵇ, y -CO₂R¹ᵃ; en donde R¹ᵃ y R¹ᵇ se seleccionan, cada uno independientemente, entre el grupo que consiste en hidrógeno, alquilo C₁₋₈, arilo C₆₋₁₀, y -alquileno C₁₋₆-arilo C₆₋₁₀; en donde el grupo -X¹-R¹ no está sustituido o está sustituido con 1 a 5 sustituyentes Rˣ; R²ᵃ y R²ᵉ se seleccionan, cada uno independientemente, entre el grupo que consiste en hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, -O-haloalquilo C₁₋₆, -S-alquilo C₁₋₆, -alquilo C₁₋₆-O-alquilo C₁₋₆, -alquilo C₁₋₆-S-alquilo C₁₋₆, CN, y halógeno, y al menos uno de R²ᵃ y R²ᵉ es distinto de hidrógeno; R²ᵇ, R²ᶜ, y R²ᵈ se seleccionan, cada uno independientemente, entre el grupo que consiste en hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, -O-haloalquilo C₁₋₆, -S-alquilo C₁₋₆, -alquilo C₁₋₆-O-alquilo C₁₋₆, -alquilo C₁₋₆-S-alquilo C₁₋₆, ciano, y halógeno; cada R³ se selecciona independientemente entre el grupo que consiste en hidroxilo, alquilo C₁₋₄, haloalquilo C₁₋₄ e hidroxialquilo C₁₋₄, y opcionalmente dos grupos R³ sobre el mismo átomo de carbono se combinan para formar oxo (=O), y opcionalmente dos grupos R³ y los átomos de carbono a los que están unidos para formar un anillo de 3 - 6 miembros con 0 - 2 heteroátomos como miembros del anillo seleccionados entre O, N, y S; R⁴ es un miembro seleccionado entre el grupo que consiste en: -NHP¹, -NHC(O)NHP¹, -CH₂NHP¹ y -CH₂NHC(O)NHP¹; cada R⁵ se selecciona independientemente entre el grupo que consiste en alquilo C₁₋₈, alcoxi C₁₋₈, haloalquilo C₁₋₈, haloalcoxi C₁₋₈, hidroxialquilo C₁₋₈, halógeno, OH, CN, C(O)R⁵ᵃ y CO₂R⁵ᵃ; R⁵ es un miembro seleccionado entre el grupo que consiste en hidrógeno, alquilo C₁₋₈, haloalquilo C₁₋₈, hidroxialquilo C₁₋₈, C(O)R⁵ᵃ y CO₂R⁵ᵃ; en donde cada R⁵ᵃ se selecciona independientemente entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, y haloalquilo C₁₋₄; R⁶ es un miembro seleccionado entre el grupo que consiste en hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, -O-haloalquilo C₁₋₆, -S-alquilo C₁₋₆, -alquilo C₁₋₆-O-alquilo C₁₋₆, -alquilo C₁₋₆-S-alquilo C₁₋₆, ciano, y halógeno; R⁷ es P¹; y R⁸ es -CH₂OP¹; cada P¹ es un componente profármaco; cada Rˣ se selecciona independientemente entre el grupo que consiste en halógeno, CN, alquilo C₁₋₄, alcoxi C₁₋₄, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, hidroxialquilo C₁₋₄, alquenilo C₂₋₄, cicloalquilo C₃₋₆, CO₂-alquilo C₁₋₄, y CONH₂; el subíndice m es 0, 1, 2, 3 ó 4; y el subíndice n es 0, 1, 2 ó 3. Reivindicación 8: El compuesto de una cualquiera de las reivindicaciones 1 a 7, o una sal farmacéuticamente aceptable del mismo, caracterizado porque P¹ se selecciona entre el grupo que consiste en: el grupo de fórmulas (7), en donde cada R⁹ se selecciona independientemente entre el grupo que consiste en H y alquilo C₁₋₃; y cada R¹⁰ se selecciona independientemente entre el grupo que consiste en H, alquilo C₁₋₃, fenilo, y bencilo. Reivindicación 10: El compuesto de una cualquiera de las reivindicaciones 1 a 7, o una sal farmacéuticamente aceptable del mismo, caracterizado porque P¹ se selecciona entre el grupo que consiste en -CH₂OH, -P(O)(OR¹⁰)₂, y -CH₂-O-P(O)(OR¹⁰)₂, en donde cada R¹⁰ se selecciona independientemente entre el grupo que consiste en H, alquilo C₁₋₃, fenilo, y bencilo. Reivindicación 11: El compuesto de una cualquiera de las reivindicaciones 1 a 7, o una sal farmacéuticamente aceptable del mismo, caracterizado porque P¹ se selecciona entre el grupo que consiste en un aminoácido, un dipéptido, y un tripéptido. Reivindicación 12: El compuesto de la reivindicación 12, caracterizado porque dicho aminoácido, dipéptido o tripéptido se selecciona independientemente entre el grupo que consiste en glicina, alanina, valina, leucina, isoleucina, lisina, cisteína, aspartato, glutamato, histidina y fenilalanina, en donde el átomo de N de cada unidad de aminoácido puede ser metilado o acilado.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862651512P | 2018-04-02 | 2018-04-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR114464A1 true AR114464A1 (es) | 2020-09-09 |
Family
ID=68054774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190100863A AR114464A1 (es) | 2018-04-02 | 2019-04-01 | PROFÁRMACOS DE ANTAGONISTAS DE C5aR BICÍCLICOS FUSIONADOS |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US11608336B2 (es) |
| EP (1) | EP3773563B1 (es) |
| JP (1) | JP7337833B2 (es) |
| KR (1) | KR20200139751A (es) |
| CN (1) | CN111954525B (es) |
| AR (1) | AR114464A1 (es) |
| BR (1) | BR112020019822A2 (es) |
| CA (1) | CA3095184A1 (es) |
| IL (1) | IL277608B2 (es) |
| MA (1) | MA52245A (es) |
| MX (1) | MX2020010390A (es) |
| SG (1) | SG11202009588PA (es) |
| TW (1) | TWI827590B (es) |
| WO (1) | WO2019195159A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110997674B (zh) | 2017-05-31 | 2022-12-20 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的6-5稠合环类 |
| CN111032658B (zh) | 2017-05-31 | 2022-12-20 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的5-5稠合环类 |
| CA3073956A1 (en) | 2017-09-03 | 2019-03-07 | Angion Biomedica Corp. | Vinylheterocycles as rho-associated coiled-coil kinase (rock) inhibitors |
| IL275516B2 (en) | 2017-12-22 | 2023-12-01 | Chemocentryx Inc | Ring compounds fused at the 5- and 6-position are diaryl-converted as C5AR inhibitors |
| CA3085946A1 (en) * | 2017-12-22 | 2019-06-27 | Chemocentryx, Inc. | Diaryl substituted 6,5-fused ring compounds as c5ar inhibitors |
| SG11202009588PA (en) | 2018-04-02 | 2020-10-29 | Chemocentryx Inc | PRODRUGS OF FUSED-BICYCLIC C5aR ANTAGONISTS |
| BR112021022682A2 (pt) | 2019-05-14 | 2022-02-22 | Provention Bio Inc | Métodos e composições para prevenir diabetes do tipo 1 |
| EP3886858B1 (en) | 2019-12-19 | 2022-05-11 | Active Biotech AB | Compounds for treatment of eye diseases associated with excessive vascularisation |
| CR20220371A (es) | 2020-02-07 | 2022-10-27 | Gasherbrum Bio Inc | Agonistas heterocíclicos de glp-1 |
| CA3182445A1 (en) | 2020-06-11 | 2021-12-16 | Francisco Leon | Methods and compositions for preventing type 1 diabetes |
| US20220047592A1 (en) * | 2020-08-13 | 2022-02-17 | Chemocentryx, Inc. | METHODS OF TREATING RESPIRATORY DISEASES USING C5a INHIBITORS |
| US20230303562A1 (en) * | 2020-09-28 | 2023-09-28 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Pyrazole compound and preparation method therefor and use thereof |
| CN113666985A (zh) * | 2021-10-22 | 2021-11-19 | 山东谷雨春生物科技有限公司 | 一种曲安奈德的制备方法 |
| CA3234517A1 (en) | 2021-10-22 | 2023-04-27 | Xin Li | Nitrogen-containing tetracyclic compound, preparation method therefor, and medical use thereof |
| CN116023321A (zh) * | 2022-12-30 | 2023-04-28 | 中国药科大学 | Sting抑制剂前药及其医药用途 |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1268002A (en) | 1917-09-12 | 1918-05-28 | William M Goodwin | Measuring instrument. |
| US4166452A (en) | 1976-05-03 | 1979-09-04 | Generales Constantine D J Jr | Apparatus for testing human responses to stimuli |
| US4256108A (en) | 1977-04-07 | 1981-03-17 | Alza Corporation | Microporous-semipermeable laminated osmotic system |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| GB8613591D0 (en) * | 1986-06-04 | 1986-07-09 | Roussel Lab Ltd | Chemical compounds |
| FR2761266B1 (fr) | 1997-03-28 | 1999-07-02 | Sanofi Sa | Composition pharmaceutique formee par granulation humide pour l'administration orale d'un derive du n-piperidino-3- pyrazolecarboxamide, de ses sels et de leurs solvates |
| PT1320531E (pt) | 2000-08-10 | 2010-10-27 | Pfizer Italia Srl | Biciclo-pirazoles activos como inibidores da cinase, processo para a sua preparação e composições farmacêuticas compreendendo estes |
| MXPA03002788A (es) | 2000-09-29 | 2004-12-13 | Neurogen Corp | Moduladores de receptor c5a de molecula pequena de alta afinidad. |
| SE524438C2 (sv) | 2000-10-05 | 2004-08-10 | Magnus Georg Goertz | Fjärrstyrt dörrelaterat låsarrangemang, första och andra datorpogramprodukt, bärande medium och ett datorlösbart medium |
| EP1396493A4 (en) | 2001-04-26 | 2005-08-03 | Ajinomoto Kk | HETEROCYCLIC COMPOUNDS |
| DE10293174D2 (de) | 2001-07-19 | 2004-07-01 | Luk Lamellen & Kupplungsbau | Übertragungsstrecke zum Ansteuern einer Kupplung |
| ITMI20012025A1 (it) | 2001-09-28 | 2003-03-28 | Dompe Spa | Sali di ammonio quaternari di omega-amminoalchilammidi di acidi r 2-aril-propionici e composizioni farmaceutiche che li contengono |
| EP1487796A4 (en) | 2002-03-28 | 2005-11-16 | Neurogen Corp | SUBSTITUTED BIARYLAMIDES AS MODULATORS OF THE C5A RECEPTOR |
| WO2003082828A1 (en) | 2002-03-28 | 2003-10-09 | Neurogen Corporation | Substituted tetrahydroisoquinolines as c5a receptor modulators |
| EP1490044A4 (en) | 2002-03-29 | 2008-04-16 | Neurogen Corp | COMBINATION THERAPY FOR THE TREATMENT OF CONDITIONS WITH PATHOGENIC INFLAMMABLE COMPONENTS |
| EP1534680B1 (en) | 2002-08-14 | 2012-02-22 | Pharmaco Investments, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| AU2003265625A1 (en) | 2002-08-21 | 2004-03-11 | Neurogen Corporation | Amino methyl imidazoles as c5a receptor modulators |
| ATE552253T1 (de) | 2002-11-08 | 2012-04-15 | Novartis Int Pharm Ltd | 3-substituierte-6-aryl- pyridin derivate als liganden für c5a-rezeptoren |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US20040214856A1 (en) | 2003-04-23 | 2004-10-28 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| AU2003902354A0 (en) | 2003-05-15 | 2003-05-29 | Harkin, Denis W. | Treatment of haemorrhagic shock |
| WO2005007087A2 (en) | 2003-07-03 | 2005-01-27 | Neurogen Corporation | Substituted (heterocycloalkyl)methyl azole derivatives as c5a receptor modulators |
| US7906528B2 (en) | 2004-10-05 | 2011-03-15 | Novartis International Pharmaceutical Ltd. | Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds |
| US7598255B2 (en) | 2005-08-04 | 2009-10-06 | Janssen Pharmaceutica Nv | Pyrimidine compounds as serotonin receptor modulators |
| US20070112015A1 (en) | 2005-10-28 | 2007-05-17 | Chemocentryx, Inc. | Substituted dihydropyridines and methods of use |
| AU2009259867A1 (en) | 2008-06-20 | 2009-12-23 | Genentech, Inc. | Triazolopyridine JAK inhibitor compounds and methods |
| NZ594140A (en) | 2008-12-22 | 2013-09-27 | Chemocentryx Inc | C5ar antagonists |
| US20110275639A1 (en) | 2008-12-22 | 2011-11-10 | Chemocentryx, Inc. | C5aR ANTAGONISTS |
| CN102595897A (zh) | 2009-09-02 | 2012-07-18 | 默沙东公司 | 作为用于糖尿病的治疗或预防的二肽基肽酶-iv抑制剂的氨基四氢吡喃 |
| SI2585064T1 (sl) | 2010-06-24 | 2017-08-31 | Chemocentryx, Inc. | Antagonisti C5AR |
| US8846656B2 (en) | 2011-07-22 | 2014-09-30 | Novartis Ag | Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators |
| KR20150042271A (ko) | 2012-08-16 | 2015-04-20 | 얀센 파마슈티카 엔.브이. | N형 칼슘 채널 차단제로서의 치환된 피롤로피라졸 |
| CN103421006B (zh) | 2013-08-18 | 2016-06-22 | 上海师范大学 | 2,3,5,7-四取代二氢吡唑并六氢吡啶衍生物及其制备方法和应用 |
| GB201321746D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| RU2748260C2 (ru) * | 2016-04-04 | 2021-05-21 | Кемосентрикс, Инк. | РАСТВОРИМЫЕ С5аR АНТАГОНИСТЫ |
| CN110997674B (zh) * | 2017-05-31 | 2022-12-20 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的6-5稠合环类 |
| CN111032658B (zh) * | 2017-05-31 | 2022-12-20 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的5-5稠合环类 |
| CA3085946A1 (en) | 2017-12-22 | 2019-06-27 | Chemocentryx, Inc. | Diaryl substituted 6,5-fused ring compounds as c5ar inhibitors |
| IL275516B2 (en) | 2017-12-22 | 2023-12-01 | Chemocentryx Inc | Ring compounds fused at the 5- and 6-position are diaryl-converted as C5AR inhibitors |
| SG11202009588PA (en) | 2018-04-02 | 2020-10-29 | Chemocentryx Inc | PRODRUGS OF FUSED-BICYCLIC C5aR ANTAGONISTS |
-
2019
- 2019-04-01 SG SG11202009588PA patent/SG11202009588PA/en unknown
- 2019-04-01 EP EP19782402.2A patent/EP3773563B1/en active Active
- 2019-04-01 CA CA3095184A patent/CA3095184A1/en active Pending
- 2019-04-01 JP JP2020553520A patent/JP7337833B2/ja active Active
- 2019-04-01 IL IL277608A patent/IL277608B2/en unknown
- 2019-04-01 MA MA052245A patent/MA52245A/fr unknown
- 2019-04-01 US US16/982,817 patent/US11608336B2/en active Active
- 2019-04-01 AR ARP190100863A patent/AR114464A1/es unknown
- 2019-04-01 BR BR112020019822-6A patent/BR112020019822A2/pt unknown
- 2019-04-01 KR KR1020207031483A patent/KR20200139751A/ko active Search and Examination
- 2019-04-01 US US16/371,627 patent/US20190300526A1/en not_active Abandoned
- 2019-04-01 WO PCT/US2019/025165 patent/WO2019195159A1/en unknown
- 2019-04-01 CN CN201980024914.2A patent/CN111954525B/zh active Active
- 2019-04-01 MX MX2020010390A patent/MX2020010390A/es unknown
- 2019-04-02 TW TW108111647A patent/TWI827590B/zh active
Also Published As
| Publication number | Publication date |
|---|---|
| JP7337833B2 (ja) | 2023-09-04 |
| TWI827590B (zh) | 2024-01-01 |
| EP3773563B1 (en) | 2024-10-16 |
| IL277608A (en) | 2020-11-30 |
| CN111954525A (zh) | 2020-11-17 |
| IL277608B2 (en) | 2023-09-01 |
| AU2019246969A1 (en) | 2020-10-15 |
| MX2020010390A (es) | 2021-01-15 |
| MA52245A (fr) | 2021-04-28 |
| EP3773563A1 (en) | 2021-02-17 |
| IL277608B1 (en) | 2023-05-01 |
| US11608336B2 (en) | 2023-03-21 |
| US20210052612A1 (en) | 2021-02-25 |
| KR20200139751A (ko) | 2020-12-14 |
| RU2020135500A (ru) | 2022-05-05 |
| US20190300526A1 (en) | 2019-10-03 |
| NZ768284A (en) | 2024-04-26 |
| WO2019195159A1 (en) | 2019-10-10 |
| BR112020019822A2 (pt) | 2021-03-16 |
| CA3095184A1 (en) | 2019-10-10 |
| EP3773563A4 (en) | 2021-12-29 |
| SG11202009588PA (en) | 2020-10-29 |
| TW202002966A (zh) | 2020-01-16 |
| JP2021519794A (ja) | 2021-08-12 |
| CN111954525B (zh) | 2023-12-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR114464A1 (es) | PROFÁRMACOS DE ANTAGONISTAS DE C5aR BICÍCLICOS FUSIONADOS | |
| AR120338A1 (es) | Piridazinonas como inhibidores de parp7 | |
| AR100438A1 (es) | Pirazolopiridinas y pirazolopirimidinas | |
| AR119454A2 (es) | COMPUESTOS ÚTILES COMO MODULADORES DE RORg, SALES FARMACÉUTICAMENTE ACEPTABLES DE LOS MISMOS, COMPOSICIONES FARMACÉUTICAS Y DICHOS COMPUESTOS PARA USO COMO MEDICAMENTO | |
| AR121669A1 (es) | Compuesto de piridazina sustituida | |
| AR113964A1 (es) | Carbamoíl ciclohexil ácidos ligados a n de triazol como antagonistas de lpa | |
| AR074499A1 (es) | Carboxamidas heterobiciclicas como inhibidoras de cinasas | |
| AR091981A1 (es) | Dihidropiridona p1 como inhibidores del factor xia | |
| AR117139A1 (es) | Derivados de piridooxazinona como inhibidores de monoacilglicerol ligasa (magl) | |
| AR104020A1 (es) | Métodos y composiciones para inhibir la interacción de menina con proteínas mill | |
| AR118123A2 (es) | Derivados de isoxazolidina, proceso para preparar dichos compuestos, composición farmacéutica y combinación | |
| AR073829A1 (es) | Variantes de inmunoglobulinas y sus usos. | |
| AR093579A1 (es) | Inhibidores de bmi-1 de pirimidina inversa sustituida | |
| AR090548A1 (es) | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k | |
| AR053120A1 (es) | Aminopiridinas como inhibidores de beta secretasa | |
| AR112216A1 (es) | Derivados de azaquinolina | |
| AR120684A1 (es) | INHIBIDORES DE HIF-2a | |
| ES2577382T3 (es) | Nuevos derivados de tienopirimidina, procedimientos para su preparación, y sus usos terapéuticos | |
| PE20190503A1 (es) | Moduladores del receptor nmda espiro-lactam y uso de los mismos | |
| AR096332A1 (es) | Compuestos heterocíclicos tricíclicos condensados como inhibidores de la integrasa del vih | |
| PE20190504A1 (es) | Moduladores del receptor nmda espiro-lactam y uso de los mismos | |
| AR100328A1 (es) | Moduladores pirrolidina de gpr40 | |
| AR094496A1 (es) | Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas | |
| AR094550A1 (es) | Inhibidores de btk | |
| AR093758A1 (es) | Inhibidores de aril lactama quinasa |