HRP20211372T1 - Amidi koji sadrže karbazol, karbamati, i uree kao modulatori kriptokroma - Google Patents

Amidi koji sadrže karbazol, karbamati, i uree kao modulatori kriptokroma Download PDF

Info

Publication number
HRP20211372T1
HRP20211372T1 HRP20211372TT HRP20211372T HRP20211372T1 HR P20211372 T1 HRP20211372 T1 HR P20211372T1 HR P20211372T T HRP20211372T T HR P20211372TT HR P20211372 T HRP20211372 T HR P20211372T HR P20211372 T1 HRP20211372 T1 HR P20211372T1
Authority
HR
Croatia
Prior art keywords
carbazol
hydroxypropyl
difluoro
cr8r9
cr11r12
Prior art date
Application number
HRP20211372TT
Other languages
English (en)
Inventor
Ross BERSOT
Paul Humphries
Original Assignee
Synchronicity Pharma, Inc.
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 Synchronicity Pharma, Inc. filed Critical Synchronicity Pharma, Inc.
Publication of HRP20211372T1 publication Critical patent/HRP20211372T1/hr

Links

Classifications

    • 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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • 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
    • C07D401/06—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 only aliphatic carbon atoms
    • 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
    • A61K31/435—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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles 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 ring system
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/118—Prognosis of disease development
    • 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T436/00—Chemistry: analytical and immunological testing
    • Y10T436/14—Heterocyclic carbon compound [i.e., O, S, N, Se, Te, as only ring hetero atom]
    • Y10T436/142222—Hetero-O [e.g., ascorbic acid, etc.]
    • Y10T436/143333—Saccharide [e.g., DNA, etc.]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Neurology (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Physics & Mathematics (AREA)
  • Molecular Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Pathology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)

Claims (19)

1. Spoj s formulom I [image] ili njegova farmaceutski prihvatljiva sol ili hidrat, pri čemu svaki od A, D, E, G, J, L, M, i Q je neovisno dušik ili ugljik; svaki od R1 i R2, kada A, D, E, G, J, L, M, ili Q je ugljik, je neovisno odabran iz niza koji sadrži vodik, halo, cijano, nitro, -CF3, -CHF2, -CH2F, trifluorometoksi, azido, hidroksil, (C1-C6)alkoksi, (C1-C6)alkil, (C2-C6)alkenil, (C2-C6)alkinil, -(C=O)-R8, -(C=O)-O-R8, -O-(C=O)-R8, -NR8(C=O)-R10, -(C=O)-NR8R9, -NR8R9, -NR8OR9, -S(O)cNR8R9, -S(O)d(C1-C8)alkil, -O-SO2-R8, NR8-S(O)c, -(CR8R9)d(3-10)-člani cikloalkil, -(CR8R9)e(C6-C10)aril, -(CR8R9)e(4-10)-člani heterociklil, -(CR8R9)f(C=O)(CR8R9)e(C6-C10)aril, -(CR8R9)f(C=O)(CR8R9)e(4-10)-člani heterociklil, -(CR8R9)eO(CR8R9)f(C6-C10)aril, -(CR8R9)eO(CR8R9)f(4-10)-člani heterociklil, -(CR8R9)fS(O)d(CR8R9)e(C6-C10)aril, i -(CR8R9)fS(O)d(CR8R9)e(4-10)-člani heterociklil; svaki od R3 i R5 je neovisno odabran iz niza koji sadrži vodik, cijano, -CF3, -CHF2, -CH2F, (C1-C6)alkil, (C2-C6)alkenil, (C2-C6)alkinil, -(C=O)-R8, -(C=O)-O-R8, -(C=O)-NR8R9, - S(O)cNR8R9, -S(O)d(C1-C8)alkil, -(CR8R9)d(3-10)-člani cikloalkil, -(CR8R9)e(C6-C10)aril, - (CR8R9)e(4-10)-člani heterociklil, -(CR8R9)f(C=O)(CR8R9)e(C6-C10)aril, - (CR8R9)t(C=O)(CR8R9)e(4-10)-člani heterociklil, -(CR8R9)eO(CR8R9)f(C6-C10)aril, - (CR8R9)eO(CR8R9)f(4-10)-člani heterociklil, -(CR8R9)fS(O)d(CR8R9)e(C6-C10)aril, i - (CR8R9)fS(O)d(CR8R9)e(4-10)-člani heterociklil; pri čemu je svaka od R3 skupina po izboru međusobno povezana kao 4-12 člani mono- ili biciklički prsten; pri čemu je svaka od R5 skupina po izboru međusobno povezana kao 4-12 člani mono- ili biciklički prsten; R4 je vodik, -CF3, -CHF2, -CH2F, (C1-C6)alkil, (C2-C6)alkenil, (C2-C6)alkinil, - (C=O)-R8, -(C=O)-O-R8, -(C=O)-NR8R9, -(CR8R9)d(3-10)-člani cikloalkil, -(CR8R9)e(C6-C10)aril, -(CR8R9)e(4-10)-člani heterociklil, -(CR8R9)f(C=O)(CR8R9)e(C6-C10)aril, - (CR8R9)f(C=O)(CR8R9)e(4-10)-člani heterociklil, -(CR8R9)eO(CR8R9)f(C6-C10)aril, - (CR8R9)eO(CR8R9)f(4-10)-člani heterociklil, -(CR8R9)fS(O)d(CR8R9)e(C6-C10)aril, i - (CR8R9)fS(O)d(CR8R9)e(4-10)-člani heterociklil; pri čemu R6 i R7 su međusobno spojeni kao pirolidinonski prsten, imidazolidinonski prsten ili 4-12-člani premošteni biciklički prsten; svaki od R8, R9 i R10 su neovisno odabrani iz niza koji sadrži vodik, (C1-C6)alkil, - (CR11R12)e(3-10)-člani cikloalkil, -(CR11R12)g(C6-C10)aril, i -(CR11R12)g(4-10)-člani heterociklil; bilo koji atomi ugljika iz (C1-C6)alkila, (3-10)-članog cikloalkila, (C6-C10)arila i (4-10)-članog heterociklila od navedenih R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, i R16 su neovisno po izboru supstituirani s 1 do 3 R14 supstituenta koji su svaki neovisno odabrani od halo, cijano, nitro, -CF3, -CHF2, -CH2F, trifluorometoksi, azido, hidroksil, -O-R15, (C1-C6)alkoksi, (C1-C6)alkil, (C2-C6)alkenil, (C2-C6)alkinil, -(C=O)-R11, - (C=O)-R15, -(C=O)-O-R11, -(C=O)-O-R15, -O-(C=O)-R11, -O-(C=O)-R15, -NR11(C=O)-R13, - (C=O)-NR11R12, -(C=O)-NR11R15, -NR11R12, -NR11R15, -NR11OR12, -NR11OR15, -S(O)cNR11R12, - S(O)cNR11R15, -S(O)d(C1-C6)alkil, -S(O)dR15, -O-SO2-R11, -O-SO2-R15, -NR11-S(O)c, -NR15-S(O)c, -(CR11R12)e(3-10)-člani cikloalkil, -(CR11R12)e(C6-C10)aril, -(CR11R12)e(4-10)-člani heterociklil, -(CR11R12)f(C=O)(CR11R12)e(C6-C10)aril, - (CR11R12)f(C=O)(CR11R12)e(4-10)-člani heterociklil, -(CR11R12)eO(CR11R12)f(C6-C10)aril, - (CR11R12)eO(CR11R12)f(4-10)-člani heterociklil, -(CR11R12)fS(O)d(CR11R12)e(C6-C10)aril, i -(CR11R12)fS(O)d(CR11R12)e(4-10)-člani heterociklil; bilo koji atomi ugljika iz (C1-C6)alkila, (3-10)-članog cikloalkila, (C6-C10)aril i (4-10)-članog heterociklila od navedenog R14 su neovisno po izboru supstituirani s 1 do 3 R16 supstituenta koji su svaki neovisno odabrani od halo, cijano, nitro, -CF3, -CHF2, -CH2F, trifluorometoksi, azido, (CH2)eOH, (C1-C6)alkoksi, (C1-C6)alkil, (C2-C6)alkenil, (C2-C6)alkinil, -(C=O)-R11, -(C=O)-R15, -(C=O)-O-R11, -(C=O)-O-R15, -O-(C=O)-R11, -O-(C=O)-R15, -NR11(C=O)-R13, -(C=O)-NR11R12, -NR11R12, i -NR11R15; bilo koji atomi dušika iz (4-10)-članog heterociklila od navedenih R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R14, i R15 su neovisno po izboru supstituirani s (C1-C6)alkil, (C2-C6)alkenil, (C2-C6)alkinil, -(C=O)-R11, -(C=O)-O-R11, -(C=O)-NR11R12, -(CR11R12)e(3-10)-člani cikloalkil, -(CR11R12)e(C6-C10)aril, -(CR11R12)e(4-10)-člani heterociklil, - (CR11R12)f(C=O)(CR11R12)e(C6-C10)aril, ili -(CR11R12)f(C=O)(CR11R12)e(4-10)-člani heterociklil; svaki R11, R12, i R13 su neovisno vodik ili (C1-C6)alkil; R15 je -(CR11R12)e(3-10)-člani cikloalkil, -(CR11R12)e(C6-C10)aril, ili -(CR11R12)e(4-10)-člani heterociklil; a i b su svaki neovisno 1, 2, 3, ili 4; c je 1 ili 2; d je 0, 1, ili 2; i e, f, i g su svaki neovisno 0, 1, 2, 3, 4, ili 5.
2. Spoj prema patentnom zahtjevu 1, naznačen time što svaki od A, D, E, G, J, L, M, i Q su ugljik; svaki od R1 i R2 je neovisno odabran od vodika ili halo; R4 je vodik ili (C1-C6)alkil, i R3 i R5 su vodik.
3. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj pojedinačni enantiomer koji ima (R)-konfiguraciju na C-3, svaki od A, D, E, G, J, L, M, i Q su ugljik; svaki od R1 i R2 je neovisno odabran od vodika ili halo; R4 je vodik ili (C1-C6)alkil, i R3 i R5 su vodik.
4. Spoj prema patentnom zahtjevu 1 naznačen time što je odabran iz skupine koja sadrži: 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-fluoropirolidin-2-on; 2-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-2-azabiciklo[2.2.1]heptan-3-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; (1R,4S)-2-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-2-azabiciklo[2.2.1]heptan-3-on; (R)-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; (R)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-fluoropirolidin-2-on; (S)-1-((S)-3-(9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fluoropirolidin-2-on; (R)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-4-metilimidazolidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)piperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)piperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)piperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)pirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)pirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fluoropirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-fluoropiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fluoropiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3,3-difluoropiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3,3-difluoropiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3,3-dimetilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3,3-dimetilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-etilpirolidin-2-on; 3-ciklopentil-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)pirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-fenilpiperidin-2-on; 3-ciklohexil-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)piperidin-2-on; 3-ciklohexil-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)piperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-izopropilpirolidin-2-on; 3-ciklopentil-l-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)piperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-etilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-izopropilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-izopropilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-metilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-metilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-metilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-metilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4,4-dimetilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-5-etilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-5-etilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-5-metilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-5-metilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-4-metilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-5-metilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-5-metilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-6-metilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-6-metilpiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4-izopropilpirolidin-2-on; 4-ciklopropil-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)pirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4-metilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-4-metilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4-etilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-4-etilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4,5-dimetilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4-metilpiperidin-2-on; 3-ciklobutil-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)pirolidin-2-on; 3-ciklobutil-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)piperidin-2-on; 3-ciklobutil-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)piperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-fenilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fenilpirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-metoksipiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3,3-difluoropirolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3,3-difluoropirolidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-3-metoksipiperidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-4-metilpiperidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-5-metilpiperidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-6-metilpiperidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-3-metilpiperidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-4-ciklopropilpirolidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksi-2-metilpropil)piperidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksi-2-metilpropil)pirolidin-2-on; 1-(3 -(9H-karbazol-9-il)-2-hidroksipropil)pirolidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-3,3-difluoropiperidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-3-fluoropiperidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-etilimidazolidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4-metilimidazolidin-2-on; 1-ciklohexil-3-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-fenilimidazolidin-2-on; 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-izopropilimidazolidin-2-on; 1-ciklopentil-3-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; 1-ciklopropil-3-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; 1-ciklobutil-3-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-3-ciklobutilimidazolidin-2-on; 1-(3 -(9H-karbazol-9-il)-2-hidroksipropil) -3 -ciklopropilimidazolidin-2-on; 1-(3-(9H-karbazol-9-il)-2-hidroksipropil)-3-izopropilimidazolidin-2-on; 3-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3,4-dihidrokinazolin-2(1H)-on; 3-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3,4-dihidrokinazolin-2(1H)-on; (1S,4R)-2-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-2-azabiciklo[2.2.1]heptan-3-on; (1S,4R)-2-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-2-azabiciklo[2.2.1]heptan-3-on; (1R,4S)-2-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-2-azabiciklo[2.2.1]heptan-3-on; (1R,4S)-2-((S)-3-(9H-karbazol-9-il)-2-hidroksipropil)-2-azabiciklo[2.2.1]heptan-3-on; (R)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-5-metilpirolidin-2-on; (S)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-5-metilpirolidin-2-on; (R)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-5-metilpirolidin-2-on; (S)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-5-metilpirolidin-2-on; (R)-1-((S)-3-(9H-karbazol-9-il)-2-hidroksipropil)-5-metilpirolidin-2-on; (S)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-metilpirolidin-2-on; (R)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-metilpirolidin-2-on; (S)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-3-metilpirolidin-2-on; (R)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-3-metilpirolidin-2-on; (S)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-3-fluoropirolidin-2-on; (R)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-3-fluoropirolidin-2-on; (S)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-3-fluoropirolidin-2-on; (R)-1-((S)-3-(9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fluoropirolidin-2-on; (S)-1-((S)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fluoropirolidin-2-on; (R)-1-((S)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fluoropirolidin-2-on; (R)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fluoropirolidin-2-on; (S)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksi-2-metilpropil)-3-fluoropirolidin-2-on; (S)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-5-metilpiperidin-2-on; (S)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-5-metilpiperidin-2-on; (R)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-5-metilpiperidin-2-on; (S)-1-((S)-3-(9H-karbazol-9-il)-2-hidroksipropil)-5-metilpiperidin-2-on; (R)-1-((S)-3-(9H-karbazol-9-il)-2-hidroksipropil)-5-metilpiperidin-2-on; (R)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-5-metilpiperidin-2-on; (S)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4-metilimidazolidin-2-on; (R)-1-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-4-metilimidazolidin-2-on; (S)-1-((R)-3-(9H-karbazol-9-il)-2-hidroksipropil)-4-metilimidazolidin-2-on; i njihova farmaceutski prihvatljiva sol ili hidrat.
5. Spoj prema patentnom zahtjevu 4 naznačen time što je 1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; ili njegova farmaceutski prihvatljiva sol ili hidrat.
6. Spoj prema patentnom zahtjevu 4 naznačen time što je (1R,4S)-2-((R)-3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)-2-azabiciklo[2.2.1]heptan-3-on; ili njegova farmaceutski prihvatljiva sol ili hidrat.
7. Spoj prema patentnom zahtjevu 4 naznačen time što je (R)-1-(3-(3,6-difluoro-9H-karbazol-9-il)-2-hidroksipropil)imidazolidin-2-on; ili njegova farmaceutski prihvatljiva sol ili hidrat.
8. Farmaceutski pripravak naznačen time što sadrži spoj prema patentnom zahtjevu 1, ili njegovu farmaceutski prihvatljiva sol ili hidrat, i farmaceutski prihvatljiv nosač, adjuvans ili razrjeđivač.
9. Farmaceutski pripravak prema patentnom zahtjevu 8, koji nadalje sadrži jedno ili više dodatnih terapijskih sredstava, pri čemu je navedeno jedno ili više dodatnih terapijskih sredstava odabrano iz skupine koju čine inhibitori DPP-IV, inhibitori SGLT2, metformin, sulfonilureje, pasireotid, ketokonazol, metirapon, mitotan, etomidat, mifepriston, inhibitori receptora epidermalnog faktora rasta, inhibitor aldosteron sintaze /11β-hidroksilaze LCI699, i levoketokonazol (COR-003).
10. Farmaceutski pripravak prema patentnom zahtjevu 8 naznačen time što je za uporabu u liječenju bolesti ili poremećaja posredovanih sa Cry kod subjekta, pri čemu je bolest ili poremećaj posredovan sa Cry odabran iz skupine koju čine dijabetes, dijabetičke komplikacije poput dijabetičke neuropatije, dijabetičke retinopatije, dijabetičke nefropatije, stvaranje katarakta, glaukom, dijabetička angiopatija, ateroskleroza; ne-alkoholni steatohepatitis (NASH); ne-alkoholna bolest masne jetre (NAFLD); astma; kronična opstruktivna plućna bolest (KOPB); metabolički sindrom; sindrom inzulinske rezistencije; pretilost; glaukom; Cushingov sindrom; psihotična depresija; Alzheimerova bolest; neuropatska bol; zlouporaba droga; osteoporoza; rak; makularna degeneracija; i miopatija.
11. Farmaceutski pripravak prema patentnom zahtjevu 8 naznačen time što je za uporabu u ublažavanju simptoma bolesti ili poremećaja posredovanih sa Cry kod subjekta, pri čemu je bolest ili poremećaj posredovan sa Cry odabran iz skupine koju čine dijabetes, dijabetičke komplikacije poput dijabetičke neuropatije, dijabetičke retinopatije, dijabetičke nefropatije, stvaranje katarakta, glaukom, dijabetička angiopatija, ateroskleroza; ne-alkoholni steatohepatitis (NASH); ne-alkoholna bolest masne jetre (NAFLD); astma; kronična opstruktivna plućna bolest (KOPB); metabolički sindrom; sindrom inzulinske rezistencije; pretilost; glaukom; Cushingov sindrom; psihotična depresija; Alzheimerova bolest; neuropatska bol; zlouporaba droga; osteoporoza; rak; makularna degeneracija; i miopatija.
12. Farmaceutski pripravak za uporabu prema patentnom zahtjevu 10 ili 11, naznačen time što nadalje sadrži jedno ili više dodatnih terapijskih sredstava, odabranih iz skupine koju čine inhibitori DPP-IV, inhibitori SGLT2, metformin, i sulfoniluree.
13. Farmaceutski pripravak za uporabu prema patentnom zahtjevu 12, naznačen time što je navedeno jedno ili više dodatnih terapijskih sredstava odabrano iz skupine koju čine pasireotid, ketokonazol, metirapon, mitotan, etomidat, mifepriston, inhibitori receptora epidermalnog faktora rasta, inhibitor aldosteron sintaze /11β-hidroksilaze LCI699, i levoketokonazol (COR-003).
14. Spoj prema patentnom zahtjevu 1, naznačen time što A, D, E, G, J, L, M, i Q su ugljik.
15. Spoj prema patentnom zahtjevu 1, naznačen time što R1 i R2 su vodik.
16. Spoj prema patentnom zahtjevu 1, naznačen time što R1 i R2 su fluor, i a i b su 1.
17. Spoj prema patentnom zahtjevu 1, naznačen time što R3 i R5 su vodik.
18. Spoj prema patentnom zahtjevu 1, naznačen time što R3, R4, i R5 su vodik.
19. Spoj prema patentnom zahtjevu 1, naznačen time što je prsten koji tvore R6 i R7 supstituiran isključivo s fluorom, metilnim skupinama, etilnim skupinama, izopropilnim skupinama, C3-6 cikloalkanima, ili fenilnim skupinama.
HRP20211372TT 2014-04-07 2021-08-30 Amidi koji sadrže karbazol, karbamati, i uree kao modulatori kriptokroma HRP20211372T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461976350P 2014-04-07 2014-04-07
PCT/US2015/024537 WO2015157182A1 (en) 2014-04-07 2015-04-06 Carbazole-containing amides, carbamates, and ureas as cryptochrome modulators
EP15719041.4A EP3129366B1 (en) 2014-04-07 2015-04-06 Carbazole-containing amides, carbamates, and ureas as cryptochrome modulators

Publications (1)

Publication Number Publication Date
HRP20211372T1 true HRP20211372T1 (hr) 2021-12-10

Family

ID=53008857

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20211372TT HRP20211372T1 (hr) 2014-04-07 2021-08-30 Amidi koji sadrže karbazol, karbamati, i uree kao modulatori kriptokroma

Country Status (22)

Country Link
US (6) US10005759B2 (hr)
EP (2) EP3939971A1 (hr)
JP (4) JP6601916B2 (hr)
KR (1) KR102224423B1 (hr)
CN (2) CN106458891B (hr)
AR (1) AR099970A1 (hr)
AU (1) AU2015244060B2 (hr)
CA (1) CA2944074C (hr)
DK (1) DK3129366T3 (hr)
ES (1) ES2886469T3 (hr)
HR (1) HRP20211372T1 (hr)
HU (1) HUE055547T2 (hr)
IL (1) IL248240B (hr)
LT (1) LT3129366T (hr)
MX (1) MX371096B (hr)
NZ (1) NZ724683A (hr)
PL (1) PL3129366T3 (hr)
RU (1) RU2705094C2 (hr)
SG (1) SG11201608020YA (hr)
SI (1) SI3129366T1 (hr)
TW (1) TWI690521B (hr)
WO (1) WO2015157182A1 (hr)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102136431B1 (ko) * 2012-05-11 2020-07-21 싱크로니시티 파마, 인크. 크립토크롬 조절제로서의 카르바졸-함유 술폰아미드
TWI690521B (zh) 2014-04-07 2020-04-11 美商同步製藥公司 作為隱花色素調節劑之含有咔唑之醯胺類、胺基甲酸酯類及脲類
US20190300875A1 (en) * 2016-07-11 2019-10-03 The Regents Of The University Of California Bic inhibitor of cry-cry and cry-cib oligomerization/clustering
US10906905B2 (en) 2016-10-14 2021-02-02 Jiangsu Hengrui Medicine Co., Ltd. Five-membered heteroaryl ring bridged ring derivative, preparation method therefor and medical use thereof
JP6835308B2 (ja) * 2016-10-19 2021-02-24 国立研究開発法人理化学研究所 クリプトクロムの機能を抑制するための組成物
US11713470B2 (en) * 2017-03-20 2023-08-01 University of Pittsburgh—of the Commonwealth System of Higher Education Targeted gene therapies for pain and other neuro-related disorders
SG11202008526VA (en) * 2018-03-22 2020-10-29 Aurigene Discovery Tech Ltd Substituted imidazolidin-2-one derivatives as prmt5 inhibitors
US20210267939A1 (en) * 2018-06-18 2021-09-02 Duke University Compositions and methods for treating nafld/nash and related disease phenotypes
WO2020113094A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CN111217741B (zh) * 2019-03-01 2022-03-15 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） 氟取代单咔唑类衍生物、其制备方法及应用
CN111285793B (zh) * 2019-03-01 2022-04-22 广州中医药大学(广州中医药研究院) 氟取代双分子咔唑衍生物、其制备方法及应用
AU2020232246A1 (en) 2019-03-04 2021-10-07 Strongbridge Dublin Limited Methods of treating disease with levoketoconazole
WO2021026185A1 (en) * 2019-08-08 2021-02-11 New York University Indole compounds as modulators of rage activity and uses thereof
CN112162028A (zh) * 2020-09-29 2021-01-01 中国农业科学院农业质量标准与检测技术研究所 一种用于草莓组织中维生素c的质谱成像方法
GB202106143D0 (en) * 2021-04-29 2021-06-16 Adaptive Diagnostics Ltd Determination of the presence of a target species
CN112986451B (zh) * 2021-05-06 2022-05-17 湖南师范大学 一种基于风味特征的杂交鱼类肉品质评价方法
CN113461674B (zh) * 2021-08-09 2022-05-13 山东农业大学 一种促进植物根系生长的酰胺类化合物及其制备方法和应用
EP4382529A1 (en) 2022-12-07 2024-06-12 Bayer Consumer Care AG A process for preparing pure (3s)-pyrrolidin-3-ol and pure (3s)-pyrrolidin-3-ol hydrochloride

Family Cites Families (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4302386A (en) 1978-08-25 1981-11-24 The Ohio State University Antigenic modification of polypeptides
US4105776A (en) 1976-06-21 1978-08-08 E. R. Squibb & Sons, Inc. Proline derivatives and related compounds
CA1178414A (en) 1978-02-08 1984-11-27 Toyo Boseki Kabushiki Kaisha (Trading Under The Name Of Toyobo Co., Ltd.) Packaging material having excellent seal packaging property
US4233402A (en) 1978-04-05 1980-11-11 Syva Company Reagents and method employing channeling
US4275149A (en) 1978-11-24 1981-06-23 Syva Company Macromolecular environment control in specific receptor assays
US4325952A (en) 1978-04-18 1982-04-20 Aziende Chimiche Riunite Angelini Francesco Method of treating abstinence syndrome with cycloaklyltriazoles
US4316906A (en) 1978-08-11 1982-02-23 E. R. Squibb & Sons, Inc. Mercaptoacyl derivatives of substituted prolines
IL58849A (en) 1978-12-11 1983-03-31 Merck & Co Inc Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them
US4276890A (en) 1979-04-11 1981-07-07 Fichera Anthony T Tobacco smoking inhibitor
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4508729A (en) 1979-12-07 1985-04-02 Adir Substituted iminodiacids, their preparation and pharmaceutical compositions containing them
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
MX7065E (es) 1980-06-06 1987-04-10 Sankyo Co Un procedimiento microbiologico para preparar derivados de ml-236b
US4376110A (en) 1980-08-04 1983-03-08 Hybritech, Incorporated Immunometric assays using monoclonal antibodies
US4344949A (en) 1980-10-03 1982-08-17 Warner-Lambert Company Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids
ZA817261B (en) 1980-10-23 1982-09-29 Schering Corp Carboxyalkyl dipeptides,processes for their production and pharmaceutical compositions containing them
US4337201A (en) 1980-12-04 1982-06-29 E. R. Squibb & Sons, Inc. Phosphinylalkanoyl substituted prolines
US4410520A (en) 1981-11-09 1983-10-18 Ciba-Geigy Corporation 3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
GB2128984B (en) 1982-05-12 1985-05-22 Hoffmann La Roche Diaza-bicyclic compounds
US4659678A (en) 1982-09-29 1987-04-21 Serono Diagnostics Limited Immunoassay of antigens
US4739073A (en) 1983-11-04 1988-04-19 Sandoz Pharmaceuticals Corp. Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof
US4727022A (en) 1984-03-14 1988-02-23 Syntex (U.S.A.) Inc. Methods for modulating ligand-receptor interactions and their application
US4780401A (en) 1984-04-09 1988-10-25 Ciba-Geigy Corporation Novel monoclonal antibodies to human renin and hybridoma cells, processes for their preparation and their applications
US4845079A (en) 1985-01-23 1989-07-04 Luly Jay R Peptidylaminodiols
US5066643A (en) 1985-02-19 1991-11-19 Sandoz Ltd. Fluorine and chlorine statine or statone containing peptides and method of use
US4894437A (en) 1985-11-15 1990-01-16 The Upjohn Company Novel renin inhibiting polypeptide analogs containing S-aryl-D- or L- or DL-cysteinyl, 3-(arylthio)lactic acid or 3-(arylthio)alkyl moieties
US4885292A (en) 1986-02-03 1989-12-05 E. R. Squibb & Sons, Inc. N-heterocyclic alcohol renin inhibitors
US4816463A (en) 1986-04-01 1989-03-28 Warner-Lambert Company Substituted diimidazo [1,5-a: 4',5'-d]pyridines having antihypertensive activity
CA1334092C (en) 1986-07-11 1995-01-24 David John Carini Angiotensin ii receptor blocking imidazoles
US4772684A (en) 1987-01-20 1988-09-20 Triton Biosciences, Inc. Peptides affecting blood pressure regulation
US4786653A (en) 1987-08-24 1988-11-22 Golwyn Daniel H Treatment of neurotransmitter-linked drug abuse
US4980283A (en) 1987-10-01 1990-12-25 Merck & Co., Inc. Renin-inhibitory pepstatin phenyl derivatives
US5089471A (en) 1987-10-01 1992-02-18 G. D. Searle & Co. Peptidyl beta-aminoacyl aminodiol carbamates as anti-hypertensive agents
US5034512A (en) 1987-10-22 1991-07-23 Warner-Lambert Company Branched backbone renin inhibitors
US5063207A (en) 1987-10-26 1991-11-05 Warner-Lambert Company Renin inhibitors, method for using them, and compositions containing them
US5055466A (en) 1987-11-23 1991-10-08 E. R. Squibb & Sons, Inc. N-morpholino derivatives and their use as anti-hypertensive agents
US5081127A (en) 1988-01-07 1992-01-14 E. I. Du Pont De Nemours And Company Substituted 1,2,3-triazole angiotensin II antagonists
US5036054A (en) 1988-02-11 1991-07-30 Warner-Lambert Company Renin inhibitors containing alpha-heteroatom amino acids
US4788189A (en) 1988-02-29 1988-11-29 Glazer Howard I Method to treat smoking withdrawal symptoms by potentiated central noradrenergic blocking
US5036053A (en) 1988-05-27 1991-07-30 Warner-Lambert Company Diol-containing renin inhibitors
DE3841520A1 (de) 1988-12-09 1990-06-13 Hoechst Ag Enzymhemmende harnstoffderivate von dipeptiden, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung
US5106835A (en) 1988-12-27 1992-04-21 American Cyanamid Company Renin inhibitors
DE4004820A1 (de) 1989-08-05 1991-04-25 Bayer Ag Renininhibitoren, verfahren zur herstellung und ihre verwendung in arzneimitteln
US5064825A (en) 1989-06-01 1991-11-12 Merck & Co., Inc. Angiotensin ii antagonists
US5744101A (en) 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5063208A (en) 1989-07-26 1991-11-05 Abbott Laboratories Peptidyl aminodiol renin inhibitors
US5098924A (en) 1989-09-15 1992-03-24 E. R. Squibb & Sons, Inc. Diol sulfonamide and sulfinyl renin inhibitors
US5104869A (en) 1989-10-11 1992-04-14 American Cyanamid Company Renin inhibitors
US5114937A (en) 1989-11-28 1992-05-19 Warner-Lambert Company Renin inhibiting nonpeptides
US5073566A (en) 1989-11-30 1991-12-17 Eli Lilly And Company Angiotensin ii antagonist 1,3-imidazoles and use thereas
US5750015A (en) 1990-02-28 1998-05-12 Soane Biosciences Method and device for moving molecules by the application of a plurality of electrical fields
US5075451A (en) 1990-03-08 1991-12-24 American Home Products Corporation Pyrrolimidazolones useful as renin inhibitors
US5064965A (en) 1990-03-08 1991-11-12 American Home Products Corporation Renin inhibitors
US5095119A (en) 1990-03-08 1992-03-10 American Home Products Corporation Renin inhibitors
US5085992A (en) 1990-07-19 1992-02-04 Merck & Co., Inc. Microbial transformation process for antihypertensive products
US5087634A (en) 1990-10-31 1992-02-11 G. D. Searle & Co. N-substituted imidazol-2-one compounds for treatment of circulatory disorders
US5071837A (en) 1990-11-28 1991-12-10 Warner-Lambert Company Novel renin inhibiting peptides
US5604260A (en) 1992-12-11 1997-02-18 Merck Frosst Canada Inc. 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
GB9602877D0 (en) 1996-02-13 1996-04-10 Merck Frosst Canada Inc 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors
US5538848A (en) 1994-11-16 1996-07-23 Applied Biosystems Division, Perkin-Elmer Corp. Method for detecting nucleic acid amplification using self-quenching fluorescence probe
JP2788677B2 (ja) 1994-01-10 1998-08-20 メルク フロスト カナダ インコーポレーテツド Ｃｏｘ−２阻害剤としてのフェニル複素環
US5521213A (en) 1994-08-29 1996-05-28 Merck Frosst Canada, Inc. Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2
ES2139959T3 (es) 1994-10-27 2000-02-16 Merck Frosst Canada Inc Derivados de estilbeno utiles como inhibidores de la ciclooxigenasa-2.
US5552422A (en) 1995-01-11 1996-09-03 Merck Frosst Canada, Inc. Aryl substituted 5,5 fused aromatic nitrogen compounds as anti-inflammatory agents
US5801155A (en) 1995-04-03 1998-09-01 Epoch Pharmaceuticals, Inc. Covalently linked oligonucleotide minor grove binder conjugates
US5691374A (en) 1995-05-18 1997-11-25 Merck Frosst Canada Inc. Diaryl-5-oxygenated-2-(5H) -furanones as COX-2 inhibitors
US5604253A (en) 1995-05-22 1997-02-18 Merck Frosst Canada, Inc. N-benzylindol-3-yl propanoic acid derivatives as cyclooxygenase inhibitors
US5639780A (en) 1995-05-22 1997-06-17 Merck Frosst Canada, Inc. N-benzyl indol-3-yl butanoic acid derivatives as cyclooxygenase inhibitors
US5643933A (en) 1995-06-02 1997-07-01 G. D. Searle & Co. Substituted sulfonylphenylheterocycles as cyclooxygenase-2 and 5-lipoxygenase inhibitors
US5733909A (en) 1996-02-01 1998-03-31 Merck Frosst Canada, Inc. Diphenyl stilbenes as prodrugs to COX-2 inhibitors
US5789413A (en) 1996-02-01 1998-08-04 Merck Frosst Canada, Inc. Alkylated styrenes as prodrugs to COX-2 inhibitors
GB9607503D0 (en) 1996-04-11 1996-06-12 Merck Frosst Canada Inc Bisaryl cyclobutenes derivatives as cyclooxygenase inhibitors
US5922742A (en) 1996-04-23 1999-07-13 Merck Frosst Canada Pyridinyl-2-cyclopenten-1-ones as selective cyclooxygenase-2 inhibitors
US5677318A (en) 1996-07-11 1997-10-14 Merck Frosst Canada, Inc. Diphenyl-1,2-3-thiadiazoles as anti-inflammatory agents
US5861419A (en) 1996-07-18 1999-01-19 Merck Frosst Canad, Inc. Substituted pyridines as selective cyclooxygenase-2 inhibitors
AR008331A1 (es) 1997-01-23 1999-12-29 Smithkline Beecham Corp Compuestos antagonistas de un receptor de il-8, uso de los mismos para la fabricacion de medicamentos, procedimiento para su obtencion, composicionesfarmaceuticas que los contienen
WO2001007654A1 (en) 1999-07-22 2001-02-01 The General Hospital Corporation Method for identifying compounds which modulate circadian rhythm
US6399631B1 (en) 1999-07-23 2002-06-04 Pfizer Inc. Carbazole neuropeptide Y5 antagonists
AU779635B2 (en) 1999-10-27 2005-02-03 Health Discovery Corporation Methods and devices for identifying patterns in biological systems and methods for uses thereof
NZ524171A (en) 2000-07-18 2006-09-29 Correlogic Systems Inc A process for discriminating between biological states based on hidden patterns from biological data
JP2004536276A (ja) 2000-11-16 2004-12-02 シファーゲン バイオシステムズ， インコーポレイテッド 質量スペクトルを分析する方法
US7113896B2 (en) 2001-05-11 2006-09-26 Zhen Zhang System and methods for processing biological expression data
US20020193950A1 (en) 2002-02-25 2002-12-19 Gavin Edward J. Method for analyzing mass spectra
US7026343B2 (en) * 2002-06-12 2006-04-11 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Pharmacologic inhibition of Myc function
US20040121305A1 (en) 2002-12-18 2004-06-24 Wiegand Roger Charles Generation of efficacy, toxicity and disease signatures and methods of use thereof
US20050101023A1 (en) 2003-03-28 2005-05-12 Rogers James A. Methods for diagnosing urinary tract and prostatic disorders
JP4705630B2 (ja) 2004-03-26 2011-06-22 エフ．ホフマン−ラ ロシュ アーゲー テトラヒドロカルバゾール及び誘導体
BRPI0514397A (pt) 2004-08-19 2008-06-10 Aventis Pharma Inc derivados de 3-ariltioindol-2-carboxamida e análogos destes como inibidores de caseìna cinase iépsilon
EP3327016B1 (en) 2006-04-07 2021-06-16 Vertex Pharmaceuticals Incorporated Preparation of modulators of atp-binding cassette transporters
CL2007003591A1 (es) 2006-12-12 2008-02-29 Wyeth Corp Compuestos derivados de sulfonamida ciclicos, inhibidores de retoma de monoamina; procedimiento de preparacion; composicion farmaceutica; y uso para el tratamiento o prevencion de disfuncion sexual, trastorno gastrointestinal, trastorno genitourinari
JP2011507910A (ja) * 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
UA107652C2 (en) * 2008-10-06 2015-02-10 Incuron Llc Carbazole compounds and therapeutic uses of the compounds
US9962368B2 (en) 2009-01-09 2018-05-08 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
US8604074B2 (en) * 2009-01-09 2013-12-10 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
US8362277B2 (en) 2009-01-09 2013-01-29 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
US9162980B2 (en) * 2009-01-09 2015-10-20 Board Of Regents Of The University Of Texas System Anti-depression compounds
AU2011274787B2 (en) * 2010-07-07 2016-06-16 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
US20130116445A1 (en) 2010-07-12 2013-05-09 Colorado State University Research Foundation Triazolium carbene catalysts and processes for asymmetric carbon-carbon bond formation
KR102136431B1 (ko) 2012-05-11 2020-07-21 싱크로니시티 파마, 인크. 크립토크롬 조절제로서의 카르바졸-함유 술폰아미드
CN104754941B (zh) * 2012-08-24 2018-02-27 得克萨斯州大学系统董事会 前神经原性化合物
WO2014039515A2 (en) * 2012-09-04 2014-03-13 University Of Massachusetts Antifungal agents and uses thereof
US9357781B2 (en) * 2013-05-03 2016-06-07 Inscent, Inc. Honeybee repellents and uses thereof
US9353078B2 (en) * 2013-10-01 2016-05-31 New York University Amino, amido and heterocyclic compounds as modulators of rage activity and uses thereof
TWI690521B (zh) 2014-04-07 2020-04-11 美商同步製藥公司 作為隱花色素調節劑之含有咔唑之醯胺類、胺基甲酸酯類及脲類

Also Published As

Publication number Publication date
EP3939971A1 (en) 2022-01-19
PL3129366T3 (pl) 2022-01-03
US20240190837A1 (en) 2024-06-13
AU2015244060B2 (en) 2019-08-01
KR102224423B1 (ko) 2021-03-05
JP2021155449A (ja) 2021-10-07
US10759777B2 (en) 2020-09-01
EP3129366B1 (en) 2021-06-09
ES2886469T3 (es) 2021-12-20
TW201605835A (zh) 2016-02-16
JP2017510611A (ja) 2017-04-13
RU2016143304A3 (hr) 2018-10-05
NZ724683A (en) 2023-03-31
SI3129366T1 (sl) 2022-01-31
CN110003172A (zh) 2019-07-12
MX2016013105A (es) 2017-05-23
CN110003172B (zh) 2022-04-01
JP2023154093A (ja) 2023-10-18
US20150284362A1 (en) 2015-10-08
WO2015157182A1 (en) 2015-10-15
AR099970A1 (es) 2016-08-31
LT3129366T (lt) 2021-09-27
JP6601916B2 (ja) 2019-11-06
RU2705094C2 (ru) 2019-11-05
US20210171495A1 (en) 2021-06-10
IL248240B (en) 2020-08-31
RU2016143304A (ru) 2018-05-07
US20220411399A1 (en) 2022-12-29
JP2019142959A (ja) 2019-08-29
US10214507B2 (en) 2019-02-26
IL248240A0 (en) 2016-11-30
US20180334446A1 (en) 2018-11-22
CA2944074C (en) 2023-04-04
TWI690521B (zh) 2020-04-11
MX371096B (es) 2020-01-16
US20190241540A1 (en) 2019-08-08
HUE055547T2 (hu) 2021-12-28
KR20160140909A (ko) 2016-12-07
CN106458891B (zh) 2019-04-09
CN106458891A (zh) 2017-02-22
DK3129366T3 (da) 2021-09-13
SG11201608020YA (en) 2016-10-28
EP3129366A1 (en) 2017-02-15
US10005759B2 (en) 2018-06-26
AU2015244060A1 (en) 2016-10-13
CA2944074A1 (en) 2015-10-15

Similar Documents

Publication Publication Date Title
HRP20211372T1 (hr) Amidi koji sadrže karbazol, karbamati, i uree kao modulatori kriptokroma
HRP20172000T1 (hr) Derivati piperidinil indola i njihova uporaba kao inhibitora komplementnog faktora b
HRP20171913T1 (hr) Aminopirimidinilni spojevi kao inhibitori jak
CA2849169C (en) Pyrazole carboxamides as janus kinase inhibitors
JP6318238B2 (ja) スルファモイルピロールアミド誘導体およびｂ型肝炎を処置するための医薬品としてのその使用
HRP20190668T1 (hr) Tetrazolonom supstituirani dihidropiridinonski mgat2 inhibitori
HRP20170112T1 (hr) Supstituirani spojevi piridin-2-karboksamida kao kinazni inhibitori signalne regulacije apoptoze
JP2016526576A5 (hr)
HRP20150173T1 (hr) Oksazolom supstituirani indazoli kao inhibitori pi3-kinaze
JP2016523911A5 (hr)
AR038420A1 (es) Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende
JP2014506877A5 (hr)
JP6412102B2 (ja) ヤヌスキナーゼ阻害剤としてのシクロアルキルニトリルピラゾロピリドン
JP2014505037A5 (hr)
RU2016112952A (ru) Производные индола и индазола
MX2007000030A (es) Derivados de piperidina como antagonistas de neuroquinina-1.
HRP20230643T1 (hr) Derivati benzimidazola kao modulatori receptora siroče gama (rory) povezanih s retinoidima i njihova farmaceutska upotreba
JP2019523266A5 (hr)
AU2014234909A1 (en) Acyclic cyanoethylpyrazolo pyridones as Janus kinase inhibitors
JP2016535042A5 (hr)
JP2016518344A5 (hr)
CN105189497B (zh) 作为janus激酶抑制剂的n-(2-氰基杂环基)吡唑并吡啶酮
JP2019519583A5 (hr)
US20170240567A1 (en) Ethyl n-boc piperidinyl pyrazolo pyridones as janus kinase inhibitors
KR20160008191A (ko) 신규한 (시아노-디메틸-메틸)-이속사졸 및 -[1,3,4]티아디아졸