SG11201507382QA - Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c - Google Patents

Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c

Info

Publication number
SG11201507382QA
SG11201507382QA SG11201507382QA SG11201507382QA SG11201507382QA SG 11201507382Q A SG11201507382Q A SG 11201507382QA SG 11201507382Q A SG11201507382Q A SG 11201507382QA SG 11201507382Q A SG11201507382Q A SG 11201507382QA SG 11201507382Q A SG11201507382Q A SG 11201507382QA
Authority
SG
Singapore
Prior art keywords
cathepsin
aza
bicyclo
heptane
cyano
Prior art date
Application number
SG11201507382QA
Other languages
English (en)
Inventor
Ralf Anderskewitz
Matthias Grauert
Marc Grundl
Peter Wilhelm Haebel
Thorsten Oost
Alexander Pautsch
Stefan Peters
Florian Binder
Viktor Vintonyak
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of SG11201507382QA publication Critical patent/SG11201507382QA/en

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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/33—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
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or 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
    • A61K31/435—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
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • C07D209/52—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 condensed with a ring other than six-membered
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • 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
    • C07D413/14—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
    • C07D471/08—Bridged 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • AIDS & HIV (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
SG11201507382QA 2013-03-14 2014-03-12 Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c SG11201507382QA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13159240 2013-03-14
EP13170005 2013-05-31
PCT/EP2014/054794 WO2014140075A1 (en) 2013-03-14 2014-03-12 Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c

Publications (1)

Publication Number Publication Date
SG11201507382QA true SG11201507382QA (en) 2015-10-29

Family

ID=50272622

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201507382QA SG11201507382QA (en) 2013-03-14 2014-03-12 Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c

Country Status (27)

Country Link
US (8) US8987249B2 (enrdf_load_stackoverflow)
EP (1) EP2970283B1 (enrdf_load_stackoverflow)
JP (2) JP6218860B2 (enrdf_load_stackoverflow)
KR (1) KR102295740B1 (enrdf_load_stackoverflow)
CN (2) CN108707140B (enrdf_load_stackoverflow)
AP (1) AP2015008601A0 (enrdf_load_stackoverflow)
AU (1) AU2014230814B2 (enrdf_load_stackoverflow)
BR (1) BR112015019720B8 (enrdf_load_stackoverflow)
CA (1) CA2903569C (enrdf_load_stackoverflow)
CL (1) CL2015002301A1 (enrdf_load_stackoverflow)
DK (1) DK2970283T3 (enrdf_load_stackoverflow)
EA (1) EA029052B1 (enrdf_load_stackoverflow)
ES (1) ES2845473T3 (enrdf_load_stackoverflow)
GE (1) GEP201706780B (enrdf_load_stackoverflow)
HK (1) HK1211579A1 (enrdf_load_stackoverflow)
HU (1) HUE053431T2 (enrdf_load_stackoverflow)
IL (1) IL240030B (enrdf_load_stackoverflow)
MX (1) MX363936B (enrdf_load_stackoverflow)
NZ (1) NZ710034A (enrdf_load_stackoverflow)
PE (1) PE20151727A1 (enrdf_load_stackoverflow)
PH (1) PH12015501964B1 (enrdf_load_stackoverflow)
PL (1) PL2970283T3 (enrdf_load_stackoverflow)
SG (1) SG11201507382QA (enrdf_load_stackoverflow)
TN (1) TN2015000381A1 (enrdf_load_stackoverflow)
TW (1) TW201522307A (enrdf_load_stackoverflow)
UY (1) UY35391A (enrdf_load_stackoverflow)
WO (1) WO2014140075A1 (enrdf_load_stackoverflow)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 Ｐ２ｘ７調節劑
ES2666155T3 (es) 2013-03-14 2018-05-03 Janssen Pharmaceutica Nv Moduladores de P2X7
US9040534B2 (en) 2013-03-14 2015-05-26 Janssen Pharmaceutica Nv [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 Ｐ２ｘ７調控劑
AU2014230814B2 (en) 2013-03-14 2017-12-21 Boehringer Ingelheim International Gmbh Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C
NO2699580T3 (enrdf_load_stackoverflow) 2014-01-24 2018-02-24
CA2942761A1 (en) 2014-03-18 2015-09-24 Iteos Therapeutics Novel 3-indol substituted derivatives, pharmaceutical compositions and methods for use
WO2016016242A1 (en) 2014-08-01 2016-02-04 Boehringer Ingelheim International Gmbh Substituted oxetanes and their use as inhibitors of cathepsin c
JP6625616B2 (ja) 2014-09-12 2019-12-25 ヤンセン ファーマシューティカ エヌ．ベー． Ｐ２ｘ７調節ｎ−アシル−トリアゾロピラジン
EA034015B1 (ru) 2014-09-12 2019-12-19 Янссен Фармацевтика Нв Модуляторы р2х7
AU2015314355B2 (en) 2014-09-12 2019-06-20 Boehringer Ingelheim International Gmbh Spirocyclic inhibitors of Cathepsin C
UY36547A (es) 2015-02-05 2016-06-01 Bayer Cropscience Ag Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas
WO2016139355A1 (en) 2015-03-05 2016-09-09 Prozymex A/S N-substituted 3,3'-(biphenyl-4,4'-diyl)bis-2-aminopropanenitriles as dppi inhibitors
EP3265452B1 (en) 2015-03-05 2020-03-04 Neuprozyme Therapeutics ApS Peptidyl nitril compounds as dipeptidyl peptidase i inhibitors
RU2018108149A (ru) 2015-08-07 2019-09-09 Байер Кропсайенс Акциенгезельшафт 2-(гет)арил-замещенные конденсированные гетероциклические производные в качестве средства для борьбы с вредителями
UY37137A (es) * 2016-02-24 2017-09-29 Merial Inc Compuestos antiparasitarios de isoxazolina, formulaciones inyectables de acción prolongada que los comprenden, métodos y usos de los mismos
KR20190092374A (ko) * 2016-10-03 2019-08-07 시질론 테라퓨틱스, 인크. 화합물, 장치, 및 이의 용도
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
JP2020525448A (ja) * 2017-06-23 2020-08-27 ニューヨーク ソサエティ フォー ザ ラプチャード アンド クリップルド メインティニング ザ ホスピタル フォー スペシャル サージェリー ソニックヘッジホッグシグナル伝達経路を介する脊椎円板変性を治療する組成物、使用及び方法
CN107266373A (zh) * 2017-08-01 2017-10-20 安徽拜善晟制药有限公司 一种原料药达沙布韦的制备方法
WO2019121143A1 (en) 2017-12-20 2019-06-27 Basf Se Substituted cyclopropyl derivatives
SMT202500062T1 (it) 2018-03-01 2025-03-12 Astrazeneca Ab Composizioni farmaceutiche comprendenti (2s)-{(1s)-1-ciano-2-[4-(3-metil-2-osso-2,3-diidro-1,3-benzossazol-5-il)fenil]etil}-1,4-ossazepan-2-carbossammide
WO2019169245A1 (en) 2018-03-02 2019-09-06 Sigilon Therapeutics, Inc. Biocompatible hydrogel capsules and process for preparing same
EP3762379A1 (en) 2018-03-07 2021-01-13 Bayer Aktiengesellschaft Identification and use of erk5 inhibitors
CN112203646A (zh) 2018-04-04 2021-01-08 西吉隆医疗股份有限公司 可植入颗粒和相关方法
AU2019306532A1 (en) 2018-07-17 2021-03-04 Insmed Incorporated Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating Lupus Nephritis
MA53722A (fr) 2018-09-28 2022-03-30 Janssen Pharmaceutica Nv Modulateurs de la monoacylglycérol lipase
CA3111380A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
US11633399B2 (en) 2018-12-25 2023-04-25 Sol-Gel Technologies Ltd. Treatment of skin disorders with compositions comprising an EGFR inhibitor
CN110006871A (zh) * 2019-02-20 2019-07-12 常州大学 一个基于外源性组胺检测的细胞模型以及应用
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CA3156100A1 (en) 2019-09-30 2021-04-08 Janssen Pharmaceutica Nv Radiolabelled mgl pet ligands
CN115335378B (zh) 2020-03-26 2025-03-04 詹森药业有限公司 单酰基甘油脂肪酶调节剂
CN114106005B (zh) * 2020-08-26 2025-08-01 西藏海思科制药有限公司 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途
CN114159446A (zh) * 2020-09-11 2022-03-11 中国科学院上海营养与健康研究所 组织蛋白酶c抑制剂在治疗肿瘤转移中的应用
CN116157405A (zh) * 2020-12-04 2023-05-23 瑞石生物医药有限公司 组织蛋白酶c小分子抑制剂及其医药用途
US20240150335A1 (en) * 2021-02-05 2024-05-09 Medshine Discovery Inc. Fused ring derivatives containing 1,4-oxazepane
EP4329767A4 (en) * 2021-04-29 2025-03-12 Insmed Incorporated CERTAIN (1-CYANO-2-PHENYLETHYL)-1,4-OXAZEPAN-2-CARBOXAMIDES FOR THE TREATMENT OF CYSTIC FIBROSIS
CN113831360A (zh) * 2021-09-10 2021-12-24 中钢集团南京新材料研究院有限公司 酰胺邻位导向硼化合成1-咔唑-硼酸频哪醇酯的方法
CN116462677A (zh) * 2022-01-20 2023-07-21 上海和誉生物医药科技有限公司 一种多稠环prmt5抑制剂及其制备方法和应用
US20230234973A1 (en) * 2022-01-27 2023-07-27 Heron Neutron Medical Corp. Intermediate, preparing method thereof, and method of preparing drug
CN114773345B (zh) * 2022-03-22 2024-01-02 盐城工业职业技术学院 一种哌嗪二酮衍生物及其制备方法
WO2023208081A1 (en) * 2022-04-28 2023-11-02 Shenzhen Bay Laboratory Substituted fluorosulfate and use thereof
TW202413352A (zh) 2022-06-13 2024-04-01 日商模數探索股份有限公司 氮雜環烷基羰基環狀胺化合物
KR20250120411A (ko) 2022-12-16 2025-08-08 신젠타 크롭 프로텍션 아게 벤즈이미다졸 유도체
CN115974824B (zh) * 2022-12-27 2024-09-24 瑞石生物医药有限公司 一种组织蛋白酶c小分子抑制剂
WO2025167969A1 (en) * 2024-02-07 2025-08-14 Insmed Incorporated Dipeptidyl peptidase 1 inhibitors and uses thereof

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4125727A (en) 1976-10-18 1978-11-14 American Cyanamid Company Method of preparing imidazoisoindolediones
GB8922355D0 (en) 1989-10-04 1989-11-22 British Telecomm Sealing gland
US6960597B2 (en) 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
DE20012487U1 (de) 2000-07-19 2001-04-05 Wenger, Lukas, 85521 Ottobrunn Beheizbare Scheibenwischer an Kraftfahrzeugen
AU2002254099B2 (en) 2001-03-02 2006-07-06 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
TW200306189A (en) 2002-03-21 2003-11-16 Merz Pharma Gmbh & Co Kgaa Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT3, and neuronal nicotinic receptor antagonists
EP1638925A1 (en) 2003-06-18 2006-03-29 Prozymex A/S Protease inhibitors
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
JP2007517811A (ja) * 2004-01-08 2007-07-05 メルク フロスト カナダ リミテツド カテプシンシステインプロテアーゼ阻害剤
WO2006096807A1 (en) 2005-03-08 2006-09-14 Janssen Pharmaceutica N.V. Aza-bridged-bicyclic amino acid derivatives as alpha 4 integrin antagonists
WO2008038692A1 (fr) 2006-09-28 2008-04-03 Banyu Pharmaceutical Co., Ltd. dÉrivÉ de diarylcÉtimine
WO2009047829A1 (ja) 2007-10-12 2009-04-16 Fujitsu Limited Ｉｐ電話自動試験システム及び方法
WO2009074829A1 (en) 2007-12-12 2009-06-18 Astrazeneca Ab Peptidyl nitriles and use thereof as dipeptidyl peptidase i inhibitors
BRPI1015540A2 (pt) 2009-05-07 2019-09-24 Astrazeneca Ab ''composto de 1-cianoetil-heterociclilcarboxamida substituídos 750''
WO2010142985A1 (en) 2009-06-10 2010-12-16 Astrazeneca Ab Substituted n-[1-cyano-2-(phenyl)ethyl]piperidin-2-ylcarboxmide compounds 761
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2012119941A1 (en) * 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
US8999975B2 (en) 2011-09-19 2015-04-07 Boehringer Ingelheim International Gmbh Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C
PE20142400A1 (es) 2012-04-27 2015-02-04 Glaxo Group Ltd Compuestos novedosos
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
MX2014014234A (es) 2012-05-22 2015-05-07 Genentech Inc Benzamidas n-sustituidas y su uso en el tratamiento del dolor.
US8859774B2 (en) 2012-05-25 2014-10-14 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
JO3459B1 (ar) 2012-09-09 2020-07-05 H Lundbeck As تركيبات صيدلانية لعلاج مرض الزهايمر
TWI608013B (zh) 2012-09-17 2017-12-11 西蘭製藥公司 升糖素類似物
TWI663165B (zh) 2012-09-28 2019-06-21 美商伊格尼塔公司 非典型蛋白質激酶ｃ之氮雜喹唑啉抑制劑
US20140100236A1 (en) 2012-10-09 2014-04-10 Boehringer Ingelheim International Gmbh Use of selectively moisture-adjusted tabletting material in the production of mechanically stable tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing tablets
MY180311A (en) 2012-10-15 2020-11-28 Epizyme Inc Substituted benzene compounds
SI2909192T1 (sl) 2012-10-16 2017-08-31 Janssen Pharmaceutica Nv Metilensko vezani kinolinilni modulatorji za ROR-gama-t
CN107936039A (zh) 2012-11-01 2018-04-20 因赛特公司 作为jak抑制剂的三环稠合噻吩衍生物
US9233974B2 (en) 2012-12-21 2016-01-12 Gilead Sciences, Inc. Antiviral compounds
WO2014100818A1 (en) 2012-12-21 2014-06-26 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
CA2895239C (en) 2012-12-21 2020-10-27 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EA201591051A1 (ru) 2013-02-08 2016-06-30 Селджен Авиломикс Рисерч, Инк. Ингибиторы erk и варианты их применения
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 Ｐ２ｘ７調節劑
US20140275082A1 (en) 2013-03-14 2014-09-18 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
JO3383B1 (ar) 2013-03-14 2019-03-13 Lilly Co Eli مثبطات cdc7
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
MX355945B (es) 2013-03-14 2018-05-07 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
AU2014230814B2 (en) * 2013-03-14 2017-12-21 Boehringer Ingelheim International Gmbh Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C
SG10201707545XA (en) 2013-03-14 2017-10-30 Newlink Genetics Corp Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization
JP2017521308A (ja) 2014-07-03 2017-08-03 ブリヂストン アメリカズ タイヤ オペレーションズ、 エルエルシー リムガード上のサイドウォールの装飾
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
TW201625591A (zh) 2014-09-12 2016-07-16 美國禮來大藥廠 吖丁啶基氧苯基吡咯啶化合物
HUE041694T2 (hu) 2014-09-12 2019-05-28 Glaxosmithkline Ip No 2 Ltd Tetrahidrokvinolin származékok mint bromodomén inhibitorok

Also Published As

Publication number Publication date
US20140275025A1 (en) 2014-09-18
BR112015019720B8 (pt) 2023-10-10
CN108707140A (zh) 2018-10-26
PH12015501964B1 (en) 2019-07-17
US20210260027A1 (en) 2021-08-26
EP2970283A1 (en) 2016-01-20
IL240030A0 (en) 2015-09-24
NZ710034A (en) 2020-06-26
US20200138780A1 (en) 2020-05-07
PL2970283T3 (pl) 2021-05-31
TN2015000381A1 (en) 2017-01-03
AU2014230814A1 (en) 2015-07-30
US20190167636A1 (en) 2019-06-06
JP6689805B2 (ja) 2020-04-28
CN108707140B (zh) 2022-07-22
PE20151727A1 (es) 2015-12-17
KR20150128722A (ko) 2015-11-18
US20160081982A1 (en) 2016-03-24
JP2016516020A (ja) 2016-06-02
JP2018009024A (ja) 2018-01-18
US10238633B2 (en) 2019-03-26
EA201500923A1 (ru) 2016-03-31
WO2014140075A1 (en) 2014-09-18
US20170266160A1 (en) 2017-09-21
CL2015002301A1 (es) 2016-06-03
BR112015019720A2 (pt) 2017-07-18
KR102295740B1 (ko) 2021-09-01
DK2970283T3 (da) 2021-01-25
TW201522307A (zh) 2015-06-16
MX2015011799A (es) 2016-01-08
US8987249B2 (en) 2015-03-24
ES2845473T3 (es) 2021-07-26
CN105026395B (zh) 2018-07-20
PH12015501964A1 (en) 2016-01-04
IL240030B (en) 2020-07-30
EA029052B1 (ru) 2018-02-28
CA2903569A1 (en) 2014-09-18
US20150105375A1 (en) 2015-04-16
UY35391A (es) 2014-09-30
US9713606B2 (en) 2017-07-25
MX363936B (es) 2019-04-09
HK1211579A1 (en) 2016-05-27
HUE053431T2 (hu) 2021-07-28
EP2970283B1 (en) 2020-11-11
AU2014230814B2 (en) 2017-12-21
CA2903569C (en) 2023-04-11
AP2015008601A0 (en) 2015-07-31
BR112015019720B1 (pt) 2023-01-03
US20230310373A1 (en) 2023-10-05
CN105026395A (zh) 2015-11-04
JP6218860B2 (ja) 2017-10-25
GEP201706780B (en) 2017-11-27

Similar Documents

Publication Publication Date Title
IL240030A0 (en) 2-aza-bicyclo[1.2.2]heptane-3-carboxylic acid (benzyl-cyano-methyl)-modified amides inhibitors of cathepsin c
IL268340A (en) Glucosylceramide synthase inhibitors for the treatment of diseases
IL245408B (en) Converted benzamides for the treatment of arthropods
IL243976A0 (en) kdm1a inhibitors for disease treatment
IL262879A (en) Modified seraphins for the treatment of bleeding disorders
EP3016603A4 (en) Steerable fastener for bone
SG11201600473UA (en) Amino acid derivatives
EP2967049A4 (en) Methods, compounds, and compositions for the treatment of angiotensin-related diseases
EP2833886A4 (en) SUBSTITUTED QUINOLINES AS INHIBITORS OF BRUTON TYROSINE KINASES
EP3130592A4 (en) Analogues of 4h-pyrazolo[1,5- ]benzimidazole compound as parp inhibitors
RS62021B1 (sr) Terapijski sistem za krioablaciju
PL2985275T3 (pl) Sposób oczyszczania kwasu beta-hydroksy-beta-metylomasłowego
EP3033331A4 (en) Process for the purification of diaminophenothiazinium compounds
IL243038A0 (en) A method for the preparation of pyrrolidine-2-carboxylic acid derivatives
GB2583319B (en) Integrated nanospray system
EP3054996A4 (en) High purity therapeutic bone agents
EP2994156A4 (en) Compounds, compositions and methods for the treatment of diseases through inhibiting tgf- activity
EP2997009A4 (en) Process for the preparation of arformoterol or salt thereof
IN2013MU04056A (enrdf_load_stackoverflow)
GB201323123D0 (en) Method for the preparation of biopolymers
PL3030561T3 (pl) N-cyjanometyloamidy jako inhibitory kinaz janusowych
EP2963026A4 (en) SUBSTITUTED (R) -3- (4-METHYLARBAMOYL-3-FLUORO-PHENYLAMINO-) TETRAHYDROFURAN-3-ENCARBOXYLIC ACID (VARIANTS) AND ESTER THEREOF, METHOD FOR THE PRODUCTION AND USE THEREOF
EP3090742A4 (en) Use of compounds produced from arrabidaea brachypoda extracts as anti-ulcerogenic agents
TH1501001800A (th) โครงย่อยสำหรับส่วนลำตัวลิ้น