[go: up one dir, main page]

AR118082A1 - Inhibidores de enzimas - Google Patents

Inhibidores de enzimas

Info

Publication number
AR118082A1
AR118082A1 ARP200100396A ARP200100396A AR118082A1 AR 118082 A1 AR118082 A1 AR 118082A1 AR P200100396 A ARP200100396 A AR P200100396A AR P200100396 A ARP200100396 A AR P200100396A AR 118082 A1 AR118082 A1 AR 118082A1
Authority
AR
Argentina
Prior art keywords
ring
optionally
independently selected
membered
halo
Prior art date
Application number
ARP200100396A
Other languages
English (en)
Inventor
Xuezheng Yang
Joseph William Wrigglesworth
Alun John Smith
Smith Colin Peter Sambrook
Rachael Pittaway
Iain Robert Miller
Matthew Robert Conroy
Thomas Matthew Baker
Terence Aaron Panchal
Stefano Levanto
Karamjit Singh Jandu
Paul Stuart Hinchliffe
Julie Nicole Hamblin
Erica Lee Goldsmith
Emanuela Gancia
Andrew Peter Cridland
David Edward Clark
Michael John Stocks
David Philip Rooker
Alicja Stela Obara
Alessandro Mazzacani
Sally Louise Marsh
Simon Teanby Hodgson
David Michael Evans
Hannah Joy Edwards
Rebecca Louise Davie
Mitchell Lewis Childs
Original Assignee
Kalvista Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kalvista Pharmaceuticals Ltd filed Critical Kalvista Pharmaceuticals Ltd
Publication of AR118082A1 publication Critical patent/AR118082A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • 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
    • A61P25/06—Antimigraine 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/37—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a saturated carbon skeleton containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/58—Radicals substituted by 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
    • C07D401/14—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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente proporciona compuestos de la fórmula (1), composiciones que comprenden dichos compuestos; el uso terapéutico de cada uno de dichos compuestos y métodos de tratamiento en pacientes con cada uno de dichos compuestos; en donde A, Y, n, R¹, R²A, R²B, R³ y *1 son definidos anteriormente en el presente documento. Reivindicación 1: Un compuesto de fórmula (1), en donde *1 denota un centro quiral; n = 0, 1 ó 2; A se selecciona de H, -(C=O)R⁴, -SO₂R⁶, y -(CH₂)-R¹³; Y es un enlace o -[CHR⁵]-; R¹ es H o alquiloᵇ; R²A se selecciona de H, alquilo, -(CH₂)₀₋₃arilo, -(CH₂)₀₋₃heteroarilo, -(CH₂)₀₋₃cicloalquilo, -(CH₂)₀₋₃-[benzotiofeno], -(CH₂)₀₋₃-[indol], y un resto de fórmula (3); o, cuando Y es un enlace, R¹ y R²A, junto con el átomo de nitrógeno al que está unido R¹ y el átomo de carbono al que está unido R²A, pueden estar unidos mediante alquileno para formar un heterociclo saturado de 4, 5 ó 6 miembros, en donde opcionalmente el heterociclo saturado de 4, 5 ó 6 miembros puede ser sustituido con arilo o en donde dos átomos de carbono adyacentes en el heterociclo saturado de 4, 5 ó 6 miembros pueden estar unidos para formar un anillo aromático de 6 miembros, o en donde dos átomos de carbono adyacentes en el heterociclo saturado de 4, 5 ó 6 miembros pueden estar unidos para formar un anillo de hidrocarburo saturado de 3, 4 ó 5 miembros el cual puede ser opcionalmente mono o disustituido por alquiloᵇ; cuando Y es -[CHR⁵]-, R⁵ es H; o, cuando Y es -[CHR⁵]-, junto con los átomos de carbono a los que cada uno de R⁵ y R²A están unidos, R⁵ y R²A pueden estar unidos mediante alquileno para formar un anillo saturado de 4, 5 y 6 miembros; o, cuando Y es -[CHR⁵]-, junto con el átomo de nitrógeno al que está unido R¹, el átomo de carbono al que está unido R⁵, y el átomo de carbono al que tanto R²A como R²B están unidos, R⁵ y R¹ pueden estar unidos mediante alquileno para formar un heterociclo saturado de 4, 5 y 6 miembros, en donde opcionalmente un átomo en el heterociclo saturado de 4, 5 ó 6 miembros puede estar unido mediante alquileno para unirse a R²A; R²B es H o alquiloᵇ; o, R²A y R²B, junto con el carbono al que tanto R²A como R²B están unidos, pueden estar unidos mediante alquileno o heteroalquileno para formar un anillo saturado de 3, 4, 5 y 6 miembros, en donde opcionalmente el anillo saturado de 3, 4, 5 ó 6 miembros contiene uno o dos miembros de anillo seleccionados entre N y O; R³ es: (i) un anillo bicíclico fusionado de 6,5 ó 6,6, que contiene un heteroátomo seleccionado de S y N, en donde al menos uno de los anillos es aromático y, opcionalmente, el anillo bicíclico contiene un heteroátomo adicional seleccionado independientemente de N, O y S; en donde opcionalmente el anillo bicíclico 6,5 ó 6,6 fusionado puede ser sustituido con 1, 2 ó 3 sustituyentes seleccionados de alquiloᵇ, alcoxi, OH, NH₂, halo, CN, y CF₃; en donde el anillo bicíclico 6,5 fusionado se puede unir a través del anillo de 6 ó 5 miembros; o (ii) fenilo, piridilo o tiofenilo, que pueden estar opcionalmente sustituidos con 1, 2 ó 3 sustituyentes seleccionados independientemente entre alquiloᵇ, alcoxi, OH, NH₂, halo, CN, CF₃, -C(=NH)NH₂, y heteroariloᵇ; en donde cuando n = 1, y R³ es sustituido con fenilo con como mínimo -(CH₂NH₂), R²A es alquilo y R²B es H; o (iii) un compuesto de fórmula (4); R⁴ es uno de: (i) un grupo de fórmula (2), en donde -[L]- es un enlace, -[(CH₂)₁₋₄]-, -[(CH₂)-O-(CH₂)]-, o -[O-(CH₂)]-; y P es alcoxi, OH o NR¹¹R¹²; en donde *2 denota un centro quiral, y en donde cuando -[L]- es un enlace, B es un hidrocarburo C₁₋₄ de cadena lineal o ramificada, y en donde cuando -[L]- es -[(CH₂)₁₋₄]-, -[(CH₂)-O-(CH₂)]-, o -[O-(CH₂)]-, B es OH, arilo heteroarilo heterociclilo, cicloalquilo o un resto de fórmula (5); o, (ii) -(CH₂)ₘ-[anillo bicíclico heteroaromático 6,5 ó 6,6 fusionado], en donde como mínimo un átomo de anillo es un heteroátomo seleccionado de O, N o S, y opcionalmente, 1, 2 ó 3 átomos de anillo adicionales pueden ser seleccionados de N o NH; en donde el anillo bicíclico heteroaromático 6,5 ó 6,6 fusionado puede ser sustituido opcionalmente con 1, 2 ó 3 sustituyentes seleccionados independientemente entre alquiloᵇ; en donde el anillo bicíclico heteroaromático 6,5 puede estar unido a -(CH₂)ₘ- a través del anillo de 6 ó 5 miembros; o, (iii) metilo, -C(CH₃)₂(OH), -C(CH₃)₂(NHMe), -(CH₂)ₘ-(arilo), -(CH₂)ₘ-(cicloalquilo), -(CH₂)ₘ-(heteroarilo), -(CH₂)ₘ-(heterociclilo), -(CH₂)-(alquilo), -(CH(halo)₂), -(CH₂)ₘ-(NR⁸R⁹), -(CH₂)ₘ-(NR¹⁰R⁷), -(CH₂)ₘ-O-(CH₂)ₖ-(arilo), -(CH₂)ₘ-(SO₂)-(CH₂)ₖ-(arilo), -(CH₂)ₘ-(alcoxi), -(CH₂)ₘ-O-(CH₂)ₖ-(heteroarilo), o -(CH₂)ₘ-[piridona, el cual puede ser opcionalmente sustituido por alquiloᵇ, o CF₃]; en donde k = 0, 1, 2 ó 3; en donde m = 0, 1, 2 ó 3; en donde: cuando Y es -[CHR⁵]- y R⁵ es H, R²A es CH₂arilo o H; y cuando Y es -[CHR⁵]-, R³ es un resto de fórmula (6); cuando A es H, R³ es el resto de fórmula (6); y cuando R³ es un compuesto de fórmula (7), R²A no es H; en donde: R⁶ es alquilo o -(CH₂)₀₋₃-(arilo); R⁷ se selecciona independientemente de H, -SO₂CH₃, metilo, etilo, propilo, isopropilo y cicloalquilo; R⁸ y R⁹ se selecciona independientemente de H, -SO₂CH₃, alquiloᵇ, heteroariloᵇ, y cicloalquilo; o R⁸ y R⁹ junto con el átomo de nitrógeno al cual están unidos forman un anillo heterocíclico de 4, 5, 6 ó 7 miembros que contiene carbono, que contiene opcionalmente un heteroátomo adicional seleccionado de N, NR¹⁰, S, y O, el cual puede ser saturado o insaturado con 1 ó 2 enlaces dobles y el cual puede ser opcionalmente mono o disustituido con sustituyentes seleccionados independientemente entre oxo, alquiloᵇ, alcoxi, OH, halo, -SO₂CH₃, y CF₃; o R⁸ y R⁹ junto con el átomo de nitrógeno al cual están unidos forman un anillo heterocíclico de 5 ó 6 miembros que contiene carbono, el cual se fusiona a un ariloᵇ o un heteroariloᵇ; R¹⁰ se selecciona independientemente de H, -SO₂R⁶, alquiloᵇ, -(CH₂)₀₋₃ariloᵇ, -(CH₂)₀₋₃heteroariloᵇ, cicloalquilo-(C=O)-(arilo), y -(CH₂)₀₋₃heterocicliloᵇ; o R¹⁰ es un anillo heterocíclico de 4, 5, 6 ó 7 miembros que contiene carbono, que contiene opcionalmente un heteroátomo adicional seleccionado de N, NR⁷, S, SO, SO₂, y O, el cual puede ser saturado o insaturado con 1 ó 2 enlaces dobles y el cual puede ser opcionalmente mono o disustituido con sustituyentes seleccionados independientemente entre oxo, alquiloᵇ, alcoxi, OH, halo, -SO₂CH₃, y CF₃; R¹¹ y R¹² se seleccionan independientemente de H, alquiloᵇ, -SO₂R⁶, cicloalquilo -(C=O)O-(alquiloᵇ), -(C=O)-fenilo, -CH₂-fenilo, y CH₂-COOH; o R¹¹ y R¹² junto con el átomo de nitrógeno al cual están unidos forman un anillo heterocíclico de 4, 5, 6 ó 7 miembros que contiene carbono que contiene opcionalmente un heteroátomo adicional seleccionado de N, O, y NR¹⁰, en donde el anillo heterocíclico puede ser opcionalmente mono o disustituido con sustituyentes seleccionados independientemente entre alquiloᵇ, OH, halo y CF₃; R¹³ se selecciona de heteroarilo cicloalquilo heterociclilo y ariloᵇ; en donde: alcoxi es un hidrocarburo lineal ligado a O de entre 1 y 6 átomos de carbono (C₁₋₆) o un hidrocarburo ramificado vinculado a O de entre 3 y 6 átomos de carbono (C₃₋₆); alcoxi puede sustituirse opcionalmente con 1 ó 2 sustituyentes seleccionados independientemente entre OH, CN, CF₃, -N(R⁷)₂ y fluoro; alquilo es un hidrocarburo saturado lineal que tiene hasta 6 átomos de carbono (C₁₋₆) o un hidrocarburo saturado ramificado de entre 3 y 6 átomos de carbono (C₃₋₆); el alquilo puede sustituirse opcionalmente con 1 ó 2 sustituyentes seleccionados independientemente entre C₁₋₆alcoxi, OH, -NR⁸R⁹, -NHCOCH₃, -CO(heterocicliloᵇ), -COOR⁸, -CONR⁸R⁹, CN, CF₃, halo, oxo y heterocicliloᵇ; alquiloᵇ es un hidrocarburo saturado lineal que tiene hasta 6 átomos de carbono (C₁₋₆) o un hidrocarburo saturado ramificado de entre 3 y 6 átomos de carbono (C₃₋₆); el alquilo puede sustituirse opcionalmente con 1 ó 2 sustituyentes seleccionados independientemente entre C₁₋₆alcoxi, OH, -N(R⁷)₂, -NHCOCH₃, CF₃, halo, oxo y ciclopropano; alquileno es un hidrocarburo saturado lineal bivalente que tiene 1 a 5 átomos de carbono (C₁₋₅); el alquileno puede sustituirse opcionalmente con 1 ó 2 sustituyentes seleccionados independientemente entre alquilo, C₁₋₆alcoxi, OH, CN, CF; y halo; arilo es fenilo, bifenilo o naftilo; el arilo puede ser sustituido opcionalmente con 1, 2 ó 3 sustituyentes seleccionados independientemente entre alquilo, alcoxi, OH, -SO₂CH₃, halo, -SO₂NR⁸R⁹, CN, -(CH₂)₀₋₃-O-heteroariloᵇ, ariloᵇ, -O-ariloᵇ, -(CH₂)₀₋₃-heterocicliloᵇ, -(CH₂)₁₋₃-ariloᵇ, -(CH₂)₀₋₃-heteroariloᵇ, -COOR⁸, -CONR⁸R⁹, -(CH₂)₀₋₃-NR⁸R⁹, OCF₃ y CF₃; o dos átomos de anillo de carbono adyacentes en él pueden estar unidos opcionalmente por un heteroalquileno para formar un anillo no aromático que contiene 5, 6 ó 7 miembros de anillo el cual puede ser sustituido opcionalmente con OH; o en donde opcionalmente dos átomos de anillo adyacentes en el arilo están unidos para formar un anillo aromático de 5 ó 6 miembros que contiene 1 ó 2 heteroátomos que se seleccionan entre N, NR¹⁰, S, y O; ariloᵇ es fenilo, bifenilo o naftilo, que puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados independientemente entre metilo, etilo, propilo, isopropilo, alcoxi, OH, -SO₂CH₃, N(R⁷)₂, halo, CN, y CF₃; o dos átomos de carbono adyacentes en el anillo en el arilo pueden estar opcionalmente unidos por un heteroalquileno para formar un anillo no aromático que contiene 5, 6 ó 7 miembros del anillo; cicloalquilo es un anillo de hidrocarburo saturado monocíclico de entre 3 y 6 átomos de carbono (C₃₋₆); el cicloalquilo puede sustituirse opcionalmente con 1 ó 2 sustituyentes seleccionados independientemente entre metilo, etilo, propilo, isopropilo, metoxi, etoxi, propoxi, isopropoxi, OH, CN, CF₃ y halo; en donde opcionalmente dos átomos de anillo adyacentes en el cicloalquilo están unidos para formar un anillo de hidrocarburo saturado de 5 ó 6 miembros; halo es F, Cl, Br, o I; heteroalquileno es un hidrocarburo saturado lineal bivalente que tiene 2 a 5 átomos de carbono (C₂₋₅), en donde 1 ó 2 de los 2 a 5 átomos de carbono son reemplazados con NR¹⁰, S u O; el heteroalquileno puede sustituirse opcionalmente con 1 ó 2 sustituyentes seleccionados independientemente entre alquilo, C₁₋₆alcoxi, OH, CN, CF₃ y halo; heteroarilo es un anillo aromático que contiene carbono de 5 ó 6 miembros que contiene uno, dos o tres miembros de anillo que se seleccionan entre N, NR¹⁰, S, y O; el heteroarilo puede ser sustituido opcionalmente con 1, 2 ó 3 sustituyentes seleccionados independientemente entre alquilo, alcoxi, heteroariloᵇ, fenilo, cicloalquilo, OH, OCF₃, halo, heterocicliloᵇ, CN, y CF₃; heteroariloᵇ es un anillo aromático que contiene carbono de 5 ó 6 miembros que contiene uno, dos o tres miembros de anillo que se seleccionan entre N, NR¹⁰, S, y O; heteroariloᵇ puede ser sustituido opcionalmente con 1, 2 ó 3 sustituyentes seleccionados independientemente entre metilo, etilo, propilo, isopropilo, alcoxi, OH, OCF₃, COOCH₃, COOCH₂CH₃, COO-(CH₂)₂-CH₃, COO-(iPr), halo, CN, y CF₃; heterociclilo es un anillo no aromático que contiene carbono de 4, 5, 6 ó 7 miembros que contiene uno, dos, tres o cuatro miembros de anillo que se seleccionan entre N, NR¹⁰, S, SO, SO₂ y O; el heterociclilo puede ser sustituido opcionalmente con 1, 2, 3, o 4 sustituyentes seleccionados independientemente entre alquilo, alcoxi, ariloᵇ, OH, OCF₃, halo, oxo, CN, NR⁸R⁹, -O(ariloᵇ), -O(heteroariloᵇ) y CF₃; o en donde opcionalmente dos átomos de anillo en el heterociclilo están enlazados con un alquileno para formar un anillo no aromático que contiene 5, 6 ó 7 miembros de anillo; o en donde opcionalmente dos átomos de anillo en el heterociclilo están enlazados con un heteroalquileno para formar un anillo no aromático que contiene 5, 6 ó 7 miembros de anillo; o en donde opcionalmente dos átomos de anillo adyacentes en el heterociclilo están unidos para formar un anillo aromático de 5 ó 6 miembros los cuales pueden contener opcionalmente 1 ó 2 heteroátomos que se seleccionan entre N, NR¹⁰, S, y O; heterocicliloᵇ es un anillo no aromático que contiene carbono de 4, 5, 6 ó 7 miembros que contiene uno, dos o tres miembros de anillo que se seleccionan entre N, NR⁷, S, SO, SO₂ y O; heterocicliloᵇ puede ser sustituido opcionalmente con 1, 2, 3 ó 4 sustituyentes seleccionados independientemente entre metilo, etilo, propilo, isopropilo, alcoxi, OH, OCF₃, halo, oxo, CN, y CF₃; y tautómeros, isómeros, estereoisómeros (que incluye enantiómeros, diastereoisómeros y mezclas racémicas y no racémicas de los mismos), isótopos deuterados y ventas y/o solvatos de los mismos aceptables farmacéuticamente.
ARP200100396A 2019-08-21 2020-02-13 Inhibidores de enzimas AR118082A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/GB2019/052356 WO2021032933A1 (en) 2019-08-21 2019-08-21 Enzyme inhibitors

Publications (1)

Publication Number Publication Date
AR118082A1 true AR118082A1 (es) 2021-09-15

Family

ID=67777356

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP200100396A AR118082A1 (es) 2019-08-21 2020-02-13 Inhibidores de enzimas

Country Status (15)

Country Link
US (1) US20220298138A1 (es)
EP (1) EP4017586A1 (es)
JP (1) JP2022552048A (es)
KR (1) KR20220050942A (es)
CN (1) CN114269431A (es)
AR (1) AR118082A1 (es)
AU (1) AU2019462669A1 (es)
BR (1) BR112022001054A2 (es)
CA (1) CA3147564A1 (es)
CO (1) CO2022000422A2 (es)
IL (1) IL289863A (es)
MX (1) MX2022001933A (es)
PH (1) PH12022550124A1 (es)
TW (1) TW202115007A (es)
WO (1) WO2021032933A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
WO2019231935A1 (en) 2018-05-29 2019-12-05 Omeros Corporation Masp-2 inhibitors and methods of use
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
CA3159159A1 (en) * 2019-12-04 2021-06-10 Neil S. Cutshall Masp-2 inhibitors and methods of use
WO2021113682A1 (en) * 2019-12-04 2021-06-10 Omeros Corporation Masp-2 inhibitors and methods of use
WO2022255399A1 (ja) * 2021-06-01 2022-12-08 国立研究開発法人理化学研究所 Ｇ９ａ阻害剤
CN121079081A (zh) * 2023-04-21 2025-12-05 图宾根埃伯哈德卡尔斯大学 转录因子HilD抑制剂

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0442878A4 (en) * 1988-04-05 1991-10-23 Abbott Laboratories Derivatives of tryptophan as cck antagonists
AU698911B2 (en) * 1995-04-04 1998-11-12 Merck & Co., Inc. Thrombin inhibitors
IL123986A (en) * 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
AU747776B2 (en) 1998-10-30 2002-05-23 Merck & Co., Inc. Thrombin inhibitors
IL146245A0 (en) 1999-05-19 2002-07-25 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
ATE303988T1 (de) * 1999-06-14 2005-09-15 Lilly Co Eli Inhibitoren von serin proteasen
US7217722B2 (en) * 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
GB0030305D0 (en) * 2000-12-13 2001-01-24 Lilly Co Eli Compounds
JP2004506648A (ja) * 2000-08-11 2004-03-04 コーバス　インターナショナル，　インコーポレイテッド ウロキナーゼおよび血管形成の非共有結合性インヒビター
ATE517910T1 (de) * 2000-08-11 2011-08-15 Wilex Ag NICHT-KOVALENTE INHIBITOREN VON UROKINASE UND BLUTGEFÄßBILDUNG
US20020091090A1 (en) * 2000-12-28 2002-07-11 Cole Bridget M. Somatostatin antagonists and agonists
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
DE10301300B4 (de) * 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
EP3168304A1 (en) 2003-08-27 2017-05-17 Ophthotech Corporation Combination therapy for the treatment of ocular neovascular disorders
EP1768955A1 (en) * 2004-07-12 2007-04-04 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Amide derivatives as inhibitors of histone deacetylase
WO2008141010A2 (en) * 2007-05-11 2008-11-20 Mpex Pharmaceuticals, Inc. Polybasic bacterial efflux pump inhibitors and therapeutic uses thereof
MX2009012847A (es) * 2007-06-13 2009-12-08 Bristol Myers Squibb Co Analogos dipeptidicos como inhibidores de factores de coagulacion.
GB0807828D0 (en) * 2008-04-29 2008-06-04 Vantia Ltd Aminopyridine derivatives
GB0918924D0 (en) * 2009-10-28 2009-12-16 Vantia Ltd Azaindole derivatives
JP5709902B2 (ja) * 2010-01-28 2015-04-30 ザ メディシンズ カンパニー （ライプツィヒ） ゲーエムベーハー トリプシン様セリンプロテアーゼ阻害剤、ならびにその調製および使用
WO2012041986A1 (en) * 2010-10-01 2012-04-05 Ucb Pharma Gmbh Process for the preparation of amino acid derivatives
CN103415301A (zh) 2011-03-09 2013-11-27 德国杰特贝林生物制品有限公司 用于与包括与人造表面接触的医疗操作一起施用的fxii抑制剂
EP2714684B1 (en) * 2011-05-27 2018-09-05 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
GB2494851A (en) * 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
EP3049435A4 (en) * 2013-09-27 2017-03-29 Merck Sharp & Dohme Corp. Factor xia inhibitors
GB201421088D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
PL3337791T3 (pl) * 2015-08-17 2023-01-23 University Health Network Inhibitory enzymów deiminaz peptydyloargininowych (pad) i ich zastosowania
WO2017123518A1 (en) 2016-01-11 2017-07-20 The Rockefeller University Aminotriazole immunomodulators for treating autoimmune diseases
US10538512B2 (en) 2016-05-23 2020-01-21 The Rockefeller University Aminoacylindazole immunomodulators for treatment of autoimmune diseases
WO2018093695A1 (en) 2016-11-18 2018-05-24 Merck Sharp & Dohme Corp. FACTOR XIIa INHIBITORS
US11014920B2 (en) 2016-11-18 2021-05-25 Merck Sharp & Dohme Corp. Factor XIIa inhibitors
CN108239081B (zh) * 2016-12-26 2020-07-28 成都先导药物开发股份有限公司 一种抑制rock的化合物及其应用
AU2018375308A1 (en) 2017-11-29 2020-06-25 The Rockefeller University Pyranopyrazole and pyrazolopyridine immunomodulators for treatment of autoimmune diseases
GB201805174D0 (en) * 2018-03-29 2018-05-16 Univ Leeds Innovations Ltd Compounds

Also Published As

Publication number Publication date
CO2022000422A2 (es) 2022-01-28
CA3147564A1 (en) 2021-02-25
CN114269431A (zh) 2022-04-01
TW202115007A (zh) 2021-04-16
US20220298138A1 (en) 2022-09-22
MX2022001933A (es) 2022-03-11
JP2022552048A (ja) 2022-12-15
AU2019462669A1 (en) 2022-02-24
KR20220050942A (ko) 2022-04-25
WO2021032933A1 (en) 2021-02-25
PH12022550124A1 (en) 2022-11-14
EP4017586A1 (en) 2022-06-29
BR112022001054A2 (pt) 2022-03-15
IL289863A (en) 2022-03-01

Similar Documents

Publication Publication Date Title
AR118082A1 (es) Inhibidores de enzimas
AR105820A1 (es) Análogos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5
AR119698A2 (es) Compuesto amida n-urea sustituida derivado de aminoácido
AR092108A1 (es) Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn
AR089865A1 (es) Derivados de bencimidazol e imidazopiridinas como moduladores de canales de sodio
AR112804A1 (es) Compuestos de bisamida que activan el sarcómero y sus usos
PE20060570A1 (es) Compuestos de quinazolina e isoquinolina piperidilo sustituidos como inhibidores de fosfodiesterasa pde-10
AR088061A1 (es) Compuestos de pirazol-4-il-heterociclil-carboxamida y metodos de uso
AR096979A1 (es) Derivados de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen
AR118081A1 (es) Inhibidores de enzimas
AR059428A1 (es) Pirazoles para el tratamiento de enfermedades mediadas por la modulacion de los receptores de histamina h3 y una composicion farmaceutica que los comprende.
AR092288A1 (es) Ligandos del receptor ep1
AR123848A1 (es) Compuestos espiro heterocíclicos y métodos de uso
AR110298A1 (es) Compuestos de heterociclo tetracíclicos útiles como inhibidores de la integrasa del vih
AR082696A1 (es) Derivados heterociclicos nitrogenados de 1,2,4-oxadiazol, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares e inflamatorias, entre otras
AR052903A1 (es) Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno.
AR121744A1 (es) MODULADORES DE a 1-ANTITRIPSINA
AR116114A1 (es) Amidas heterocíclicas de entre 5 y 7 miembros como inhibidores de jak
AR046603A1 (es) Alcanaminas dihidrobenzofuranilo y metodos para su uso como farmacos en el snc
AR121275A1 (es) Compuesto de sulfonamida o sulfinamida que tiene acción inhibidora de la proteína brd4 y su uso como medicamento
AR115464A1 (es) Compuestos para el tratamiento, alivio o prevención de trastornos asociados con los agregados de tau
AR108387A1 (es) Compuestos de tipo tetrahidropirimidodiazepina y dihidropiridodiazepina para tratar el dolor y afecciones relacionadas con el dolor
AR118085A1 (es) Inhibidores de enzimas
AR114430A1 (es) Compuestos herbicidas
AR118119A1 (es) Compuestos de pirido-pirimidinilo y métodos de uso

Legal Events

Date Code Title Description
FA Abandonment or withdrawal