EA029052B1 - Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с - Google Patents

Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с Download PDF

Info

Publication number
EA029052B1
EA029052B1 EA201500923A EA201500923A EA029052B1 EA 029052 B1 EA029052 B1 EA 029052B1 EA 201500923 A EA201500923 A EA 201500923A EA 201500923 A EA201500923 A EA 201500923A EA 029052 B1 EA029052 B1 EA 029052B1
Authority
EA
Eurasian Patent Office
Prior art keywords
alkyl
alkylene
independently
independently selected
ring
Prior art date
Application number
EA201500923A
Other languages
English (en)
Russian (ru)
Other versions
EA201500923A1 (ru
Inventor
Ральф Андерскевиц
Маттиас Грауэрт
Марк Грундль
Петер Вильхельм Хебель
Торстен Ост
Александер Пауч
Штефан Петерс
Флориан Биндер
Виктор Винтоняк
Original Assignee
Бёрингер Ингельхайм Интернациональ Гмбх
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 Бёрингер Ингельхайм Интернациональ Гмбх filed Critical Бёрингер Ингельхайм Интернациональ Гмбх
Publication of EA201500923A1 publication Critical patent/EA201500923A1/ru
Publication of EA029052B1 publication Critical patent/EA029052B1/ru

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
    • A61K31/397—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
    • 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
    • C07D403/02—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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
EA201500923A 2013-03-14 2014-03-12 Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с EA029052B1 (ru)

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 (2)

Publication Number Publication Date
EA201500923A1 EA201500923A1 (ru) 2016-03-31
EA029052B1 true EA029052B1 (ru) 2018-02-28

Family

ID=50272622

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201500923A EA029052B1 (ru) 2013-03-14 2014-03-12 Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с

Country Status (27)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2825646C1 (ru) * 2023-09-04 2024-08-28 федеральное государственное бюджетное учреждение "Санкт-Петербургский научно-исследовательский институт фтизиопульмонологии" Министерства здравоохранения Российской Федерации 8-(4-Метил-4Н-1,2,4-триазол-3-ил)-6-(метилсульфонил)-2-(5-нитро-2-фуроил)-2,6-диазаспиро[3.4]октан, обладающий противотуберкулезной активностью в отношении возбудителя туберкулеза с множественной лекарственной устойчивостью, и способ его получения

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2689526T3 (es) 2013-03-14 2018-11-14 Janssen Pharmaceutica Nv Moduladores de P2X7
EP3112366B1 (en) 2013-03-14 2018-02-28 Janssen Pharmaceutica NV P2x7 modulators
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
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 Ｐ２ｘ７調控劑
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 Ｐ２ｘ７調節劑
NO2699580T3 (enExample) 2014-01-24 2018-02-24
WO2015140717A1 (en) 2014-03-18 2015-09-24 Iteos Therapeutics Novel 3-indol substituted derivatives, pharmaceutical compositions and methods for use
JP6529575B2 (ja) * 2014-08-01 2019-06-12 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 置換オキセタンおよびそれらのカテプシンｃの阻害薬としての使用
US20180118749A1 (en) 2014-09-12 2018-05-03 Janssen Pharmaceutica Nv P2x7 modulators
PL3191487T3 (pl) * 2014-09-12 2020-03-31 Boehringer Ingelheim International Gmbh Spirocykliczne inhibitory katepsyny C
EP3191492B1 (en) 2014-09-12 2019-01-09 Janssen Pharmaceutica NV P2x7 modulators
UY36547A (es) 2015-02-05 2016-06-01 Bayer Cropscience Ag Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas
AU2016227618B2 (en) * 2015-03-05 2020-06-04 Neuprozyme Therapeutics ApS Peptidyl nitril compounds as dipeptidyl peptidase I inhibitors
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
CA2994604A1 (en) 2015-08-07 2017-02-16 Bayer Cropscience Aktiengesellschaft 2-(het)aryl-substituted condensed heterocyclic derivatives as pest control agents
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
CA3039203A1 (en) 2016-10-03 2018-04-12 Sigilon Therapeutics, Inc. Compounds, devices, and uses thereof
EP3824906A1 (en) 2016-12-21 2021-05-26 Amgen Inc. Anti-tnf alpha antibody formulations
EP3641757A4 (en) * 2017-06-23 2021-03-24 New York Society for the Ruptured and Crippled Maintaining the Hospital for Special Surgery COMPOSITION, USES, AND METHOD OF TREATMENTAL DISC DEGENERATION BY A HEDGEHOG SOUND PATH
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
KR102738945B1 (ko) 2018-03-01 2024-12-04 아스트라제네카 에이비이 (2s)-n-｛(1s)-1-시아노-2-[4-(3-메틸-2-옥소-2,3-디하이드로-1,3-벤족사졸-5-일)페닐]에틸｝-1,4-옥사제판-2-카복스아미드를 포함하는 약학 조성물
WO2019169245A1 (en) 2018-03-02 2019-09-06 Sigilon Therapeutics, Inc. Biocompatible hydrogel capsules and process for preparing same
JP2021515767A (ja) 2018-03-07 2021-06-24 バイエル・アクチエンゲゼルシヤフト Ｅｒｋ５阻害剤の同定及び使用
JP7534219B2 (ja) 2018-04-04 2024-08-14 シギロン セラピューティクス， インコーポレイテッド 移植可能な粒子及び関連方法
KR20210032431A (ko) 2018-07-17 2021-03-24 인스메드 인코포레이티드 루푸스 신염을 치료하기 위한 특정 (2s)-n-[(1s)-1-시아노-2-페닐에틸]-1,4-옥사제판-2-카복스아미드
CA3111309A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
JOP20210058A1 (ar) 2018-09-28 2021-03-24 Janssen Pharmaceutica Nv مُعدلات ليباز أُحادِيُّ الجلِيسِريد
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
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CA3156100A1 (en) 2019-09-30 2021-04-08 Janssen Pharmaceutica Nv Radiolabelled mgl pet ligands
MX2022011902A (es) 2020-03-26 2023-01-04 Janssen Pharmaceutica Nv Moduladores de la monoacilglicerol lipasa.
CA3181285A1 (en) 2020-07-20 2022-01-27 Jessica BASSO Methods for extracting neutrophil serine proteases and treating dipeptidyl peptidase 1-mediated conditions
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
EP4257588A4 (en) * 2020-12-04 2024-10-16 Reistone Biopharma Company Limited SMALL MOLECULE INHIBITOR OF CATHEPSIN C AND ITS MEDICINAL USE
CN116783189A (zh) * 2021-02-05 2023-09-19 南京明德新药研发有限公司 含1，4-氧杂氮杂环庚烷的并环类衍生物
JP2024516826A (ja) * 2021-04-29 2024-04-17 インスメッド インコーポレイテッド 嚢胞性線維症を治療するためのある特定のｎ－（１－シアノ－２－フェニルエチル）－１，４－オキサゼパン－２－カルボキサミド
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
CN117279889B (zh) * 2022-04-28 2025-04-25 深圳湾实验室 经取代的氟硫酸盐及其用途
CN119317620A (zh) 2022-06-13 2025-01-14 亚力维克希斯股份有限公司 氮杂环烷基羰基环状胺化合物
EP4634162A1 (en) 2022-12-16 2025-10-22 Syngenta Crop Protection AG Benzimidazole derivatives
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
CN120584108A (zh) 2023-01-06 2025-09-02 英斯梅德股份有限公司 新型可逆dpp1抑制剂及其用途
WO2025167969A1 (en) * 2024-02-07 2025-08-14 Insmed Incorporated Dipeptidyl peptidase 1 inhibitors and uses thereof
WO2025214073A1 (en) * 2024-04-12 2025-10-16 Insmed Incorporated Dipeptidyl peptidase 1 inhibitors and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2013041497A1 (en) * 2011-09-19 2013-03-28 Boehringer Ingelheim International Gmbh Substituted n- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin c

Family Cites Families (44)

* 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
EP1372655B1 (en) 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. 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
US20070099958A1 (en) 2003-06-18 2007-05-03 Prozymex A/S Protease inhibitors
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
CA2552713A1 (en) * 2004-01-08 2005-07-21 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
WO2006096807A1 (en) 2005-03-08 2006-09-14 Janssen Pharmaceutica N.V. Aza-bridged-bicyclic amino acid derivatives as alpha 4 integrin antagonists
US20090247560A1 (en) 2006-09-28 2009-10-01 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
EA201000958A1 (ru) 2007-12-12 2010-12-30 Астразенека Аб Пептидилнитрилы и их применение в качестве ингибиторов дипептидилпептидазы i
EP2427445A1 (en) 2009-05-07 2012-03-14 AstraZeneca AB Substituted 1-cyanoethylheterocyclylcarboxamide compounds 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
WO2013160418A1 (en) 2012-04-27 2013-10-31 Glaxo Group Limited Novel compounds
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
PE20150400A1 (es) 2012-05-22 2015-03-27 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
WO2014052699A1 (en) 2012-09-28 2014-04-03 Cephalon, Inc. Azaquinazoline inhibitors of atypical protein kinase c
JP2015533134A (ja) 2012-10-09 2015-11-19 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 錠剤の機械的安定性に適切な少なくとも１種の水和物形成活性物質及び／又はアジュバントを含有する機械的に安定な錠剤、特にアルギニン含有錠剤の製造における選択的に水分調整された打錠材料の使用
NZ706739A (en) 2012-10-15 2018-11-30 Epizyme Inc Substituted benzene compounds
AU2013331496B2 (en) 2012-10-16 2017-07-27 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of ROR-gamma-t
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
WO2014100620A2 (en) 2012-12-21 2014-06-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9233974B2 (en) 2012-12-21 2016-01-12 Gilead Sciences, Inc. Antiviral compounds
CN105026372B (zh) 2012-12-21 2018-06-05 赛尔基因昆蒂赛尔研究公司 组蛋白脱甲基酶抑制剂
KR20150119012A (ko) 2013-02-08 2015-10-23 셀진 아빌로믹스 리서치, 인코포레이티드 Erk 억제제 및 이의 용도
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
AU2014229313B2 (en) 2013-03-14 2016-07-28 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
US20140275082A1 (en) 2013-03-14 2014-09-18 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 Ｐ２ｘ７調節劑
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
RU2667509C2 (ru) 2013-03-14 2018-09-21 Ньюлинк Джинетикс Корпорейшин Трициклические соединения в качестве ингибиторов иммуносупрессии, опосредуемой метаболизированием триптофана
JO3383B1 (ar) 2013-03-14 2019-03-13 Lilly Co Eli مثبطات cdc7
WO2016003723A1 (en) 2014-07-03 2016-01-07 Bridgestone Americas Tire Operations, Llc Sidewall decoration on rim guard
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
AR101696A1 (es) 2014-09-12 2017-01-04 Lilly Co Eli Compuestos de azetidiniloxifenilpirrolidina
PT3191476T (pt) 2014-09-12 2019-01-17 Glaxosmithkline Ip No 2 Ltd Derivados de tetra-hidroquinolina como inibidores de bromodomínio

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2013041497A1 (en) * 2011-09-19 2013-03-28 Boehringer Ingelheim International Gmbh Substituted n- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin c

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2825646C1 (ru) * 2023-09-04 2024-08-28 федеральное государственное бюджетное учреждение "Санкт-Петербургский научно-исследовательский институт фтизиопульмонологии" Министерства здравоохранения Российской Федерации 8-(4-Метил-4Н-1,2,4-триазол-3-ил)-6-(метилсульфонил)-2-(5-нитро-2-фуроил)-2,6-диазаспиро[3.4]октан, обладающий противотуберкулезной активностью в отношении возбудителя туберкулеза с множественной лекарственной устойчивостью, и способ его получения

Also Published As

Publication number Publication date
MX2015011799A (es) 2016-01-08
KR102295740B1 (ko) 2021-09-01
BR112015019720B1 (pt) 2023-01-03
IL240030B (en) 2020-07-30
JP2018009024A (ja) 2018-01-18
PH12015501964A1 (en) 2016-01-04
IL240030A0 (en) 2015-09-24
US20160081982A1 (en) 2016-03-24
HUE053431T2 (hu) 2021-07-28
SG11201507382QA (en) 2015-10-29
CN105026395B (zh) 2018-07-20
AP2015008601A0 (en) 2015-07-31
US20150105375A1 (en) 2015-04-16
AU2014230814A1 (en) 2015-07-30
DK2970283T3 (da) 2021-01-25
TN2015000381A1 (en) 2017-01-03
CA2903569A1 (en) 2014-09-18
KR20150128722A (ko) 2015-11-18
CN108707140B (zh) 2022-07-22
ES2845473T3 (es) 2021-07-26
JP6689805B2 (ja) 2020-04-28
PE20151727A1 (es) 2015-12-17
NZ710034A (en) 2020-06-26
US20140275025A1 (en) 2014-09-18
EP2970283A1 (en) 2016-01-20
JP2016516020A (ja) 2016-06-02
CA2903569C (en) 2023-04-11
GEP201706780B (en) 2017-11-27
CN105026395A (zh) 2015-11-04
US20170266160A1 (en) 2017-09-21
MX363936B (es) 2019-04-09
EA201500923A1 (ru) 2016-03-31
US20200138780A1 (en) 2020-05-07
JP6218860B2 (ja) 2017-10-25
WO2014140075A1 (en) 2014-09-18
CN108707140A (zh) 2018-10-26
TW201522307A (zh) 2015-06-16
US20210260027A1 (en) 2021-08-26
HK1211579A1 (en) 2016-05-27
EP2970283B1 (en) 2020-11-11
BR112015019720B8 (pt) 2023-10-10
US9713606B2 (en) 2017-07-25
UY35391A (es) 2014-09-30
US8987249B2 (en) 2015-03-24
BR112015019720A2 (pt) 2017-07-18
AU2014230814B2 (en) 2017-12-21
PL2970283T3 (pl) 2021-05-31
US10238633B2 (en) 2019-03-26
PH12015501964B1 (en) 2019-07-17
CL2015002301A1 (es) 2016-06-03
US20230310373A1 (en) 2023-10-05
US20190167636A1 (en) 2019-06-06

Similar Documents

Publication Publication Date Title
EA029052B1 (ru) Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с
EP3215156B1 (en) Inhibitors of tryptophan-2,3-dioxygenase or indoleamine-2,3-dioxygenase
EP2870150B1 (en) Heterocyclic modulators of lipid synthesis
EP2468729B1 (en) Novel indazole derivative
EA024817B1 (ru) Замещенные n-[1-циано-2-(фенил)этил]-2- азабицикло[2.2.1]гептан-3-карбоксамидные ингибиторы катепсина с
US9440960B2 (en) Substituted oxetanes and their use as inhibitors of cathepsin C
JP6441831B2 (ja) カテプシンｃの置換２−アザ−ビシクロ［２．２．２］オクタン−３−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤
JP2012504632A (ja) Ｃ型肝炎ウイルス阻害剤
JP6441830B2 (ja) カテプシンｃの置換２−アザ−ビシクロ［２．２．１］ヘプタン−３−カルボン酸（シアノ−メチル）−アミド阻害剤
JP6437929B2 (ja) カテプシンｃの置換二環式１−カルボン酸（ベンジル−シアノ−メチル）−アミド阻害剤
KR20150061644A (ko) 지방산 신타아제 저해제로서의 히드로피롤로피롤 유도체
HUE034415T2 (en) Use of indole derivatives for the treatment of cancer
EA024201B1 (ru) Ингибиторы вируса гепатита с
WO2015073864A1 (en) Ebna1 inhibitors and their method of use
WO2018021977A1 (en) Glycine metabolism modulators and uses thereof
TW201713622A (zh) 含氮雜環化合物
AU2011336700B2 (en) 4-substituted-cyclohexylamino-4-piperidinyl-acetamide antagonists of CCR2
US20250074906A1 (en) Azaindole derivative that inhibits h-pgds
WO2022184049A1 (zh) Plk4抑制剂及其用途
WO2017198159A1 (zh) 含桥环的咪唑衍生物
US20150329493A1 (en) Omega-amino acid derivatives of benzene, pyridine, and pyridazine compounds
HK1208445B (en) Heterocyclic modulators of lipid synthesis
MXPA06005983A (en) Azole-based kinase inhibitors

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KG TJ TM