CA2901022C - Substituted pyridine compounds as inhibitors of histone demethylases - Google Patents

Substituted pyridine compounds as inhibitors of histone demethylases Download PDF

Info

Publication number
CA2901022C
CA2901022C CA2901022A CA2901022A CA2901022C CA 2901022 C CA2901022 C CA 2901022C CA 2901022 A CA2901022 A CA 2901022A CA 2901022 A CA2901022 A CA 2901022A CA 2901022 C CA2901022 C CA 2901022C
Authority
CA
Canada
Prior art keywords
pyridin
methyl
substituted
cycloalkyl
dimethylamino
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CA2901022A
Other languages
English (en)
French (fr)
Other versions
CA2901022A1 (en
Inventor
Marc Labelle
Thomas Boesen
Qasim Khan
Ramkrishna Reddy VAKITI
Utpal SHARMA
Ying Yang
Mukund Mehrotra
Neerja Saraswat
Farman ULLAH
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gilead Sciences Inc
Original Assignee
Gilead Sciences 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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of CA2901022A1 publication Critical patent/CA2901022A1/en
Application granted granted Critical
Publication of CA2901022C publication Critical patent/CA2901022C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—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
    • A61K31/5355—Non-condensed oxazines 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
    • A61K31/535—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
    • A61K31/537—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 spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/06—Oxalic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/06—Oxalic acid
    • C07C55/07—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265—Citric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/46—Oxygen atoms
    • C07D213/48—Aldehydo radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/62—Three oxygen atoms, e.g. ascorbic acid
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2901022A 2013-02-27 2014-02-26 Substituted pyridine compounds as inhibitors of histone demethylases Active CA2901022C (en)

Applications Claiming Priority (15)

Application Number Priority Date Filing Date Title
US201361770058P 2013-02-27 2013-02-27
US201361770067P 2013-02-27 2013-02-27
US201361770065P 2013-02-27 2013-02-27
DKPA201370114 2013-02-27
DKPA201370114 2013-02-27
US61/770,065 2013-02-27
US61/770,058 2013-02-27
DKPA201370113 2013-02-27
DKPA201370115 2013-02-27
DKPA201370115 2013-02-27
DKPA201370113 2013-02-27
US61/770,067 2013-02-27
US201461931126P 2014-01-24 2014-01-24
US61/931,126 2014-01-24
PCT/EP2014/053674 WO2014131777A1 (en) 2013-02-27 2014-02-26 Inhibitors of histone demethylases

Publications (2)

Publication Number Publication Date
CA2901022A1 CA2901022A1 (en) 2014-09-04
CA2901022C true CA2901022C (en) 2021-05-04

Family

ID=51427545

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2901022A Active CA2901022C (en) 2013-02-27 2014-02-26 Substituted pyridine compounds as inhibitors of histone demethylases

Country Status (23)

Country Link
US (2) US9650339B2 (enExample)
EP (2) EP2961736B1 (enExample)
JP (2) JP6514117B2 (enExample)
KR (1) KR102229992B1 (enExample)
CN (1) CN105263906B (enExample)
AP (1) AP2015008676A0 (enExample)
AU (2) AU2014222756B2 (enExample)
BR (1) BR112015020650A2 (enExample)
CA (1) CA2901022C (enExample)
CL (1) CL2015002394A1 (enExample)
CR (1) CR20150507A (enExample)
EA (1) EA030451B1 (enExample)
ES (1) ES2670864T3 (enExample)
IL (1) IL240439A0 (enExample)
MD (1) MD20150085A2 (enExample)
MX (1) MX2015011097A (enExample)
PE (1) PE20151667A1 (enExample)
PH (1) PH12015501868A1 (enExample)
PL (1) PL2961736T3 (enExample)
SG (2) SG10201707027SA (enExample)
SI (1) SI2961736T1 (enExample)
TR (1) TR201808599T4 (enExample)
WO (1) WO2014131777A1 (enExample)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MD20150043A2 (ro) 2012-10-02 2015-08-31 Epitherapeutics Aps Inhibitori ai histon-demetilazelor
PE20151667A1 (es) 2013-02-27 2015-11-27 Epitherapeutics Aps Inhibidores de histona desmetilasas
WO2015153498A1 (en) * 2014-03-31 2015-10-08 Epitherapeutics, Aps Inhibitors of histone demethylases
SG11201701182VA (en) 2014-08-27 2017-03-30 Gilead Sciences Inc Compounds and methods for inhibiting histone demethylases
EP3212647B1 (en) 2014-10-29 2019-04-03 Dong-A ST Co., Ltd. Novel pyridopyrimidinone compounds for modulating the catalytic activity of histone lysine demethylases (kdms)
EP3283076A1 (en) * 2015-04-14 2018-02-21 Gilead Sciences, Inc. Methods of treating hepatitis b virus
WO2017099829A1 (en) * 2015-12-11 2017-06-15 The General Hospital Corporation Compositions and methods for treating drug-tolerant glioblastoma
BR102017010009A2 (pt) 2016-05-27 2017-12-12 Gilead Sciences, Inc. Compounds for the treatment of hepatitis b virus infection
SG11201809893WA (en) 2016-05-27 2018-12-28 Gilead Sciences Inc Methods for treating hepatitis b virus infections using ns5a, ns5b or ns3 inhibitors
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
EP3507288B1 (en) 2016-09-02 2020-08-26 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
AU2017318601B2 (en) 2016-09-02 2020-09-03 Gilead Sciences, Inc. Toll like receptor modulator compounds
US10662416B2 (en) 2016-10-14 2020-05-26 Precision Biosciences, Inc. Engineered meganucleases specific for recognition sequences in the hepatitis B virus genome
TWI820984B (zh) 2017-01-31 2023-11-01 美商基利科學股份有限公司 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型
JOP20180008A1 (ar) 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
WO2018222831A1 (en) * 2017-05-31 2018-12-06 The Children's Medical Center Corporation TARGETING LYSINE DEMETHYLASES (KDMs) AS A THERAPEUTIC STRATEGY FOR DIFFUSE LARGE B-CELL LYMPHOMA
AU2018328308A1 (en) 2017-09-06 2020-04-16 Translational Drug Development, Llc Aminobenzimidazole derivatives, treatments, and methods of inhibiting histone deacetylase
CN111511754B (zh) 2017-12-20 2023-09-12 捷克共和国有机化学与生物化学研究所 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸
KR102492187B1 (ko) 2017-12-20 2023-01-27 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 3'3' 사이클릭 다이뉴클레오티드
WO2019154261A1 (zh) * 2018-02-09 2019-08-15 南京明德新药研发股份有限公司 与kmd5通路相关的吡啶衍生物
TWI796596B (zh) 2018-02-13 2023-03-21 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
KR102526964B1 (ko) 2018-02-26 2023-04-28 길리애드 사이언시즈, 인코포레이티드 Hbv 복제 억제제로서의 치환된 피롤리진 화합물
EP3774883A1 (en) 2018-04-05 2021-02-17 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis b virus protein x
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW201945388A (zh) 2018-04-12 2019-12-01 美商精密生物科學公司 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
US20190359645A1 (en) 2018-05-03 2019-11-28 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide
MX2021000100A (es) 2018-07-13 2021-03-25 Gilead Sciences Inc Inhibidores de muerte programada-1 (pd-1)/ ligando de muerte programada 1 (pd-l1).
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
CA3106548A1 (en) * 2018-08-06 2020-02-13 Dana-Farber Cancer Institute, Inc. Histone demethylase 5 inhibitors and uses thereof
JP7158577B2 (ja) 2018-10-24 2022-10-21 ギリアード サイエンシーズ， インコーポレイテッド Ｐｄ－１／ｐｄ－ｌ１阻害剤
KR102658602B1 (ko) 2018-10-31 2024-04-19 길리애드 사이언시즈, 인코포레이티드 Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물
HRP20240541T1 (hr) 2018-10-31 2024-07-05 Gilead Sciences, Inc. Supstituirani spojevi 6-azabenzimidazola kao inhibitori hpk1
CN109852662B (zh) * 2018-12-25 2021-02-19 华南农业大学 组蛋白甲基化H3K4me3在猪卵巢颗粒细胞中的应用
WO2020178768A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
DK3934757T3 (da) 2019-03-07 2023-04-17 Inst Of Organic Chemistry And Biochemistry Ascr V V I 2'3'-cykliske dinukleotider og prodrugs deraf
AU2020231115B2 (en) 2019-03-07 2025-02-20 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202212339A (zh) 2019-04-17 2022-04-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
KR102776925B1 (ko) 2019-06-25 2025-03-11 길리애드 사이언시즈, 인코포레이티드 Flt3l-fc 융합 단백질 및 사용 방법
WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
WO2021034804A1 (en) 2019-08-19 2021-02-25 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
FI4037708T3 (fi) 2019-09-30 2024-10-31 Gilead Sciences Inc Hbv-rokotteita ja menetelmiä, hbv:n hoitamiseksi
EP4567109A3 (en) 2019-12-06 2025-09-17 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome
US11718637B2 (en) 2020-03-20 2023-08-08 Gilead Sciences, Inc. Prodrugs of 4′-C-substituted-2-halo-2′- deoxyadenosine nucleosides and methods of making and using the same
EP4192474B1 (en) 2020-08-07 2025-09-10 Gilead Sciences, Inc. Prodrugs of phosphonamide nucleotide analogues and their pharmaceutical use
TW202406932A (zh) 2020-10-22 2024-02-16 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
TW202310852A (zh) 2021-05-13 2023-03-16 美商基利科學股份有限公司 ＴＬＲ８調節化合物及抗ＨＢＶ ｓｉＲＮＡ療法之組合
CN117355531A (zh) 2021-06-23 2024-01-05 吉利德科学公司 二酰基甘油激酶调节化合物
CN117480155A (zh) 2021-06-23 2024-01-30 吉利德科学公司 二酰基甘油激酶调节化合物
US11999733B2 (en) 2021-06-23 2024-06-04 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
KR20240005901A (ko) 2021-06-23 2024-01-12 길리애드 사이언시즈, 인코포레이티드 디아실글리세롤 키나제 조절 화합물
WO2025240242A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2025240244A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies comprising bulevirtide and lonafarnib for use in the treatment of hepatitis d virus infection
WO2025240243A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with bulevirtide and an inhibitory nucleic acid targeting hepatitis b virus
WO2025240246A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
LU88769I2 (fr) 1982-07-23 1996-11-05 Zeneca Ltd Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R))
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
AU3732889A (en) * 1988-11-11 1990-05-28 Banyu Pharmaceutical Co., Ltd. Substituted allylamine derivatives, process for their preparation and their use
JPH03173865A (ja) * 1988-11-11 1991-07-29 Banyu Pharmaceut Co Ltd 置換アリルアミン誘導体、その製造法及びその用途
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
AU716610B2 (en) 1996-08-30 2000-03-02 Novartis Ag Method for producing epothilones, and intermediate products obtained during the production process
DE69724269T2 (de) 1996-09-06 2004-06-09 Obducat Ab Verfahren für das anisotrope ätzen von strukturen in leitende materialien
US5874438A (en) 1996-10-11 1999-02-23 Bayer Aktiengesellschaft 2,2'-bridged bis-2,4-diaminoquinazolines
US5756517A (en) * 1996-10-25 1998-05-26 Bayer Aktiengesellschaft Use of bisquinoline compounds in the treatment of cerebral disorders
DK1367057T3 (da) 1996-11-18 2009-01-19 Biotechnolog Forschung Gmbh Epothiloner E og F
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
CA2322157C (en) 1998-02-25 2012-05-29 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
EP1135470A2 (en) 1998-11-20 2001-09-26 Kosan Biosciences, Inc. Recombinant methods and materials for producing epothilone and epothilone derivatives
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
KR20050044407A (ko) * 2001-11-08 2005-05-12 엘란 파마슈티칼스, 인크. N,n'-치환-1,3-디아미노-2-히드록시프로판 유도체
PL230179B1 (pl) 2002-03-13 2018-09-28 Array Biopharma Inc N3 Alkilowane pochodne benzoimidazolu, kompozycja je zawierająca oraz ich zastosowanie do wytwarzania leku do leczenia zaburzeń hiperproliferacyjnych
WO2006129842A1 (ja) * 2005-06-01 2006-12-07 Banyu Pharmaceutical Co., Ltd. オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
US20080021024A1 (en) 2006-06-29 2008-01-24 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors
SA109300195B1 (ar) 2008-03-28 2013-04-20 Astrazeneca Ab تركيبة صيدلانية جديدة مضادة للسرطان
JP2012507556A (ja) 2008-10-29 2012-03-29 サートリス ファーマシューティカルズ， インコーポレイテッド サーチュインモジュレーターとしてのピリジン、二環式ピリジンおよび関連するアナログ
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
AU2010279359A1 (en) 2009-08-07 2012-02-16 The Wistar Institute Compositions containing JARID1B inhibitors and methods for treating cancer
SI2545045T1 (sl) 2010-03-10 2016-05-31 Incyte Holdings Corporation Derivati piperidin-4-ila kot zaviralci JAK1
US9365553B2 (en) 2010-05-27 2016-06-14 Aska Pharmaceutical Co., Ltd. Heterocyclic compound and H1 receptor antagonist
WO2012007007A1 (en) 2010-07-15 2012-01-19 Epitherapeutics Aps Inhibitors of hdme
US20130303545A1 (en) 2010-09-30 2013-11-14 Tamara Maes Cyclopropylamine derivatives useful as lsd1 inhibitors
GB201112607D0 (en) 2011-07-22 2011-09-07 Glaxo Group Ltd Novel compounds
WO2012071469A2 (en) * 2010-11-23 2012-05-31 Nevada Cancer Institute Histone demethylase inhibitors and uses thereof for treatment o f cancer
JP5813855B2 (ja) 2011-03-25 2015-11-17 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ Ｌｓｄ１阻害剤としてのシクロプロピルアミン
BR112014003382B1 (pt) * 2011-08-15 2022-03-15 University Of Utah Research Foundation Análogos de (e)-n-(1-feniletilideno) benzo-hidrazida substituída como inibidores de histona desmetilase e composições farmacêuticas compreendendo-os
CN102585150B (zh) 2012-02-01 2013-09-04 嘉兴学院 织物涂饰用阴离子水性聚氨酯分散体的制备方法
WO2013123411A1 (en) 2012-02-17 2013-08-22 Board Of Regents, The University Of Texas System Methods for diagnosing and treating cancer
MD20150043A2 (ro) 2012-10-02 2015-08-31 Epitherapeutics Aps Inhibitori ai histon-demetilazelor
EP3763367A1 (en) 2012-12-06 2021-01-13 Celgene Quanticel Research, Inc. Pyridine-pyrazole derivatives as histone demethylase inhibitors
PL2934145T3 (pl) 2012-12-19 2018-04-30 Celgene Quanticel Research, Inc. Inhibitory demetylazy histonowej
US11639333B2 (en) 2012-12-21 2023-05-02 Celgene Quanticel Research, Inc Histone demethylase inhibitors
PE20151667A1 (es) 2013-02-27 2015-11-27 Epitherapeutics Aps Inhibidores de histona desmetilasas
JP6332654B2 (ja) 2013-03-15 2018-05-30 セルジーン クオンティセル リサーチ，インク． ヒストンデメチラーゼ阻害剤
WO2015035062A1 (en) 2013-09-05 2015-03-12 Genentech, Inc. Antiproliferative compounds
WO2015153498A1 (en) 2014-03-31 2015-10-08 Epitherapeutics, Aps Inhibitors of histone demethylases

Also Published As

Publication number Publication date
IL240439A0 (en) 2015-09-24
AU2014222756A1 (en) 2015-08-27
PE20151667A1 (es) 2015-11-27
JP2018127486A (ja) 2018-08-16
HK1220460A1 (zh) 2017-05-05
EP3170811A1 (en) 2017-05-24
CL2015002394A1 (es) 2015-12-28
US20140371214A1 (en) 2014-12-18
AP2015008676A0 (en) 2015-08-31
EP2961736B1 (en) 2018-04-11
AU2014222756B2 (en) 2018-07-26
US9650339B2 (en) 2017-05-16
EA201591382A1 (ru) 2016-01-29
CN105263906B (zh) 2018-11-23
CR20150507A (es) 2015-11-20
WO2014131777A1 (en) 2014-09-04
EP2961736A1 (en) 2016-01-06
BR112015020650A2 (pt) 2017-07-18
JP6514117B2 (ja) 2019-05-15
ES2670864T3 (es) 2018-06-01
CA2901022A1 (en) 2014-09-04
SG10201707027SA (en) 2017-09-28
MD20150085A2 (ro) 2016-02-29
CN105263906A (zh) 2016-01-20
US9221801B2 (en) 2015-12-29
SG11201506717UA (en) 2015-09-29
MX2015011097A (es) 2016-03-09
TR201808599T4 (tr) 2018-07-23
AU2018205204A1 (en) 2018-08-02
JP2016509047A (ja) 2016-03-24
KR20150123894A (ko) 2015-11-04
HK1218539A1 (en) 2017-02-24
PL2961736T3 (pl) 2018-08-31
US20160237037A1 (en) 2016-08-18
SI2961736T1 (en) 2018-06-29
PH12015501868A1 (en) 2015-12-07
KR102229992B1 (ko) 2021-03-19
EA030451B1 (ru) 2018-08-31

Similar Documents

Publication Publication Date Title
CA2901022C (en) Substituted pyridine compounds as inhibitors of histone demethylases
EP2903968B1 (en) Inhibitors of histone demethylases
CA2957947A1 (en) Compounds and methods for inhibiting histone demethylases
AU2018200982A1 (en) Inhibitors of histone demethylases
HK1236522A1 (en) Ethyl pyridine-4-carboxylate compound as inhibitor of histone demethylases
HK1218539B (en) Inhibitors of histone demethylases
Class et al. Patent application title: INHIBITORS OF HISTONE DEMETHYLASES
HK1223612B (en) Inhibitors of histone demethylases
HK1207373B (en) Inhibitors of histone demethylases
HK1235404A1 (en) Inhibitors of histone demethylases
OA17463A (en) Inhibitors of histone demethylases.
HK1220460B (zh) 组蛋白脱甲基酶的抑制剂
HK1247920B (zh) 组蛋白去甲基化酶抑制剂

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20190226