BR112016002496A2 - composto de fórmula i, composição farmacêutica, método para inibição de kdm1a, método para tratamento de uma doença mediada por globina, método para atingir um efeito em um paciente, e, método para inibir pelo menos uma função de kdm1a - Google Patents

composto de fórmula i, composição farmacêutica, método para inibição de kdm1a, método para tratamento de uma doença mediada por globina, método para atingir um efeito em um paciente, e, método para inibir pelo menos uma função de kdm1a

Info

Publication number
BR112016002496A2
BR112016002496A2 BR112016002496A BR112016002496A BR112016002496A2 BR 112016002496 A2 BR112016002496 A2 BR 112016002496A2 BR 112016002496 A BR112016002496 A BR 112016002496A BR 112016002496 A BR112016002496 A BR 112016002496A BR 112016002496 A2 BR112016002496 A2 BR 112016002496A2
Authority
BR
Brazil
Prior art keywords
kdm1a
inhibiting
treating
globin
achieving
Prior art date
Application number
BR112016002496A
Other languages
English (en)
Other versions
BR112016002496B1 (pt
Inventor
Young Rienhoff Hugh Jr
M Mccall John
Clare Michael
Original Assignee
Imago Biosciences 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 Imago Biosciences Inc filed Critical Imago Biosciences Inc
Publication of BR112016002496A2 publication Critical patent/BR112016002496A2/pt
Publication of BR112016002496B1 publication Critical patent/BR112016002496B1/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4453Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/90Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

trata-se de novos compostos e composições e sua aplicação como produtos farmacêuticos para o tratamento de doenças. métodos de inibição de kdm1a, métodos para aumentar a expressão de gene de gama globina e métodos para induzir a diferenciação de células cancerosas em um indivíduo humano ou animal são também fornecidos para o tratamento de doenças, tais como leucemia mieloide aguda.
BR112016002496-6A 2013-08-06 2014-08-06 Composto e composição farmacêutica BR112016002496B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361862759P 2013-08-06 2013-08-06
US61/862,759 2013-08-06
US201461954276P 2014-03-17 2014-03-17
US61/954,276 2014-03-17
PCT/US2014/049906 WO2015021128A1 (en) 2013-08-06 2014-08-06 Kdm1a inhibitors for the treatment of disease

Publications (2)

Publication Number Publication Date
BR112016002496A2 true BR112016002496A2 (pt) 2017-08-01
BR112016002496B1 BR112016002496B1 (pt) 2022-07-12

Family

ID=52461899

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112016002496-6A BR112016002496B1 (pt) 2013-08-06 2014-08-06 Composto e composição farmacêutica

Country Status (15)

Country Link
US (4) US9790195B2 (pt)
EP (1) EP3030323B1 (pt)
JP (1) JP6521967B2 (pt)
KR (1) KR102255778B1 (pt)
CN (1) CN105592888A (pt)
AU (1) AU2014306149B2 (pt)
BR (1) BR112016002496B1 (pt)
CA (1) CA2920257C (pt)
DK (1) DK3030323T3 (pt)
ES (1) ES2734209T3 (pt)
IL (1) IL243976B (pt)
MX (1) MX2016001587A (pt)
NZ (1) NZ716427A (pt)
WO (1) WO2015021128A1 (pt)
ZA (1) ZA201600901B (pt)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9388123B2 (en) * 2012-11-28 2016-07-12 Kyoto University LSD1-selective inhibitor having lysine structure
DK3030323T3 (da) 2013-08-06 2019-07-15 Imago Biosciences Inc Kdm1a-inhibitorer til behandlingen af sygdom
US11369577B2 (en) 2014-11-26 2022-06-28 IEO—Istituto Europeo di Oncologia S.r.l. Reprogramming-based models of neurodevelopmental disorders and uses thereof
MX2017010291A (es) 2015-02-12 2017-12-07 Imago Biosciences Inc Inhibidores de kdm1a para el tratamiento de enfermedades.
CA2987876A1 (en) 2015-06-12 2016-12-15 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
TWI765860B (zh) 2015-08-12 2022-06-01 美商英塞特公司 Lsd1抑制劑之鹽
MA43318A (fr) 2015-11-27 2018-10-03 Taiho Pharmaceutical Co Ltd Nouveau composé de biphényle ou un sel de celui-ci
US20190091256A1 (en) * 2016-03-02 2019-03-28 Beth Israel Deaconess Medical Center Therapeutic targets for lin-28-expressing cancers
AU2017233898B2 (en) 2016-03-15 2022-12-15 Oryzon Genomics, S.A. Combinations of LSD1 inhibitors for use in the treatment of solid tumors
US11034991B2 (en) 2016-03-16 2021-06-15 Oryzon Genomics S.A. Methods to determine KDM1A target engagement and chemoprobes useful therefor
CN109477993B (zh) 2016-06-07 2023-03-28 J大卫格莱斯顿研究机构 β-羟基丁酸酯和丁二醇的中链脂肪酸酯和组合物及其使用方法
WO2018035259A1 (en) * 2016-08-16 2018-02-22 Imago Biosciences, Inc. Methods and processes for the preparation of kdm1a inhibitors
US20190256929A1 (en) 2016-11-03 2019-08-22 Oryzon Genomics, S.A. Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents
US20190256930A1 (en) 2016-11-03 2019-08-22 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
JP6843979B2 (ja) 2017-05-26 2021-03-17 大鵬薬品工業株式会社 新規なビフェニル化合物又はその塩
RU2765153C2 (ru) 2017-05-26 2022-01-26 Тайхо Фармасьютикал Ко., Лтд. Усилитель противоопухолевого эффекта с применением нового соединения бифенила
AU2018276611B2 (en) * 2017-05-31 2022-01-06 Taiho Pharmaceutical Co., Ltd. Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1
JP7442095B2 (ja) 2017-07-21 2024-03-04 バック・インスティテュート・フォー・リサーチ・オン・エイジング ベータ-ヒドロキシブチレート及びブタンジオールのs-エナンチオマー並びにその使用方法
AU2018309372A1 (en) 2017-08-03 2020-01-30 Oryzon Genomics, S.A. Methods of treating behavior alterations
CN107828747B (zh) * 2017-10-23 2020-11-03 中山大学附属第六医院 一种多肽及其编码基因和用途
US11578059B2 (en) 2018-05-11 2023-02-14 Imago Biosciences. Inc. KDM1A inhibitors for the treatment of disease
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
WO2020152280A1 (en) * 2019-01-24 2020-07-30 Fundación Pública Andaluza Progreso Y Salud Lsd1 inhibitors for use in the treatment of type 2 diabetes
MX2021011256A (es) 2019-03-20 2021-10-01 Oryzon Genomics Sa Metodos de tratamiento del trastorno limite de la personalidad.
CN113631164A (zh) 2019-03-20 2021-11-09 奥莱松基因组股份有限公司 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法
CN114341366A (zh) 2019-07-05 2022-04-12 奥莱松基因组股份有限公司 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法
MX2022007113A (es) * 2019-12-09 2022-07-11 Imago Biosciences Inc Inhibidores de la desmetilasa de la histona especifica de la lisina para el tratamiento de las neoplasias mieloproliferativas.
EP4319732A1 (en) 2021-04-08 2024-02-14 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors for treating myeloid cancers
WO2023069884A1 (en) * 2021-10-18 2023-04-27 Imago Biosciences, Inc. Kdm1a inhibitors for the treatment of disease
WO2023217758A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors
WO2023217784A1 (en) 2022-05-09 2023-11-16 Oryzon Genomics, S.A. Methods of treating nf1-mutant tumors using lsd1 inhibitors

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2581523A1 (en) 2004-09-24 2006-04-06 Idenix (Cayman) Limited Methods and compositions for treating flaviviruses, pestiviruses and hepacivirus
US8314087B2 (en) 2007-02-16 2012-11-20 Amgen Inc. Nitrogen-containing heterocyclyl ketones and methods of use
CN101842361B (zh) 2007-06-27 2013-06-05 阿斯利康(瑞典)有限公司 吡嗪酮衍生物及其在治疗肺病中的用途
WO2009036404A2 (en) 2007-09-13 2009-03-19 Codexis, Inc. Ketoreductase polypeptides for the reduction of acetophenones
CN101883846A (zh) 2007-10-01 2010-11-10 科德克希思公司 用于生成氮杂环丁酮的还原酶多肽
US8288141B2 (en) 2008-08-27 2012-10-16 Codexis, Inc. Ketoreductase polypeptides for the production of 3-aryl-3-hydroxypropanamine from a 3-aryl-3-ketopropanamine
WO2010043721A1 (en) 2008-10-17 2010-04-22 Oryzon Genomics, S.A. Oxidase inhibitors and their use
EP2177502A1 (en) 2008-10-17 2010-04-21 Oryzon Genomics, S.A. Compounds and their use
WO2010143582A1 (ja) 2009-06-11 2010-12-16 公立大学法人名古屋市立大学 フェニルシクロプロピルアミン誘導体及びlsd1阻害剤
MX338041B (es) 2009-09-25 2016-03-30 Oryzon Genomics Sa Inhibidores de demetilasa-1 especificos de lisina y su uso.
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
ES2607081T3 (es) 2010-04-19 2017-03-29 Oryzon Genomics, S.A. Inhibidores de desmetilasa específica de lisina-1 y su uso
PL2560949T3 (pl) 2010-04-20 2017-01-31 Università Degli Studi Di Roma "La Sapienza" Pochodne tranylocyprominy jako inhibitory demetylazy histonowej LSD1 i/lub LSD2
LT2598482T (lt) 2010-07-29 2018-07-10 Oryzon Genomics, S.A. Demetilazės lsd1 inhibitoriai arilciklopropilamino pagrindu ir jų medicininis panaudojimas
EP2598480B1 (en) 2010-07-29 2019-04-24 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
WO2012034116A2 (en) 2010-09-10 2012-03-15 The Johns Hopkins University Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders
JP2013540767A (ja) 2010-10-07 2013-11-07 ザ ジェイ. デヴィッド グラッドストーン インスティテューツ 免疫不全ウイルス転写を調節するための組成物および方法
WO2012045883A1 (en) 2010-10-08 2012-04-12 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
WO2012071469A2 (en) 2010-11-23 2012-05-31 Nevada Cancer Institute Histone demethylase inhibitors and uses thereof for treatment o f cancer
WO2012107499A1 (en) 2011-02-08 2012-08-16 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
WO2012107498A1 (en) * 2011-02-08 2012-08-16 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative disorders
EP2688568B1 (en) 2011-03-25 2019-06-19 Glaxosmithkline Intellectual Property (No. 2) Limited Cyclopropylamines as lsd1 inhibitors
KR20140052018A (ko) 2011-08-09 2014-05-02 다케다 야쿠힌 고교 가부시키가이샤 시클로프로판아민 화합물
BR112014009306B1 (pt) 2011-10-20 2021-07-20 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1
CA2849564C (en) 2011-10-20 2020-10-20 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
US9388123B2 (en) 2012-11-28 2016-07-12 Kyoto University LSD1-selective inhibitor having lysine structure
EP2740474A1 (en) 2012-12-05 2014-06-11 Instituto Europeo di Oncologia S.r.l. Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
WO2014164867A1 (en) 2013-03-11 2014-10-09 Imago Biosciences Kdm1a inhibitors for the treatment of disease
CA2916533C (en) * 2013-06-25 2022-12-20 University Of Canberra Methods and compositions for modulating cancer stem cells
DK3030323T3 (da) 2013-08-06 2019-07-15 Imago Biosciences Inc Kdm1a-inhibitorer til behandlingen af sygdom
SG10201806849WA (en) 2014-02-13 2018-09-27 Incyte Corp Cyclopropylamines as lsd1 inhibitors
EP3134519B1 (en) 2014-04-22 2018-06-06 c-LEcta GmbH Ketoreductases
EA030946B1 (ru) 2014-06-27 2018-10-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы лизин-специфической деметилазы-1
MX2017010291A (es) 2015-02-12 2017-12-07 Imago Biosciences Inc Inhibidores de kdm1a para el tratamiento de enfermedades.
WO2017079753A1 (en) 2015-11-05 2017-05-11 Imago Biosciences, Inc. Lysine-specific histone demethylase as a novel therapeutic target in myeloproliferative neoplasms
JP6916795B2 (ja) 2015-12-29 2021-08-11 ミラティ セラピューティクス, インコーポレイテッド Lsd1阻害剤
CN109153636B (zh) 2016-05-09 2021-10-22 朱比连特埃皮科尔有限责任公司 作为双重lsd1/hdac抑制剂的环丙基-酰胺化合物
WO2018035249A1 (en) 2016-08-16 2018-02-22 Imago Biosciences, Inc. Compositions and methods for producing stereoisomerically pure aminocyclopropanes
WO2018035259A1 (en) 2016-08-16 2018-02-22 Imago Biosciences, Inc. Methods and processes for the preparation of kdm1a inhibitors
WO2018106984A1 (en) 2016-12-09 2018-06-14 Constellation Pharmaceuticals, Inc. Markers for personalized cancer treatment with lsd1 inhibitors
US11578059B2 (en) 2018-05-11 2023-02-14 Imago Biosciences. Inc. KDM1A inhibitors for the treatment of disease

Also Published As

Publication number Publication date
IL243976A0 (en) 2016-04-21
AU2014306149A1 (en) 2016-02-18
DK3030323T3 (da) 2019-07-15
US20170334873A1 (en) 2017-11-23
EP3030323A4 (en) 2017-01-11
US20200095214A1 (en) 2020-03-26
ES2734209T3 (es) 2019-12-04
MX2016001587A (es) 2016-08-05
US10370346B2 (en) 2019-08-06
KR102255778B1 (ko) 2021-05-24
BR112016002496B1 (pt) 2022-07-12
US20160257662A1 (en) 2016-09-08
US20210147373A1 (en) 2021-05-20
US10882835B2 (en) 2021-01-05
US11655226B2 (en) 2023-05-23
AU2014306149B2 (en) 2019-09-19
EP3030323B1 (en) 2019-04-24
US9790195B2 (en) 2017-10-17
CA2920257C (en) 2023-02-21
KR20160045079A (ko) 2016-04-26
IL243976B (en) 2020-07-30
JP2016531121A (ja) 2016-10-06
NZ716427A (en) 2021-07-30
JP6521967B2 (ja) 2019-05-29
WO2015021128A1 (en) 2015-02-12
CA2920257A1 (en) 2015-02-12
EP3030323A1 (en) 2016-06-15
ZA201600901B (en) 2022-11-30
CN105592888A (zh) 2016-05-18

Similar Documents

Publication Publication Date Title
BR112016002496A2 (pt) composto de fórmula i, composição farmacêutica, método para inibição de kdm1a, método para tratamento de uma doença mediada por globina, método para atingir um efeito em um paciente, e, método para inibir pelo menos uma função de kdm1a
BR112017017074A2 (pt) Compostos; sal; bis-tosilatos de n-((s)-5-((1r,2s)-2-(4- fluorofenil)ciclopropilamino)-1-(4-metilpiperazin-1- il)-1-oxopentan-2-il)-4-(1h-1,2,3-triazol-1-il)benzamida; sal de tosilato de um composto; sal de bis- tosilato de um composto; compostos, sais, polimorfos ou solvatos; composições farmacêuticas, método para inibição de kdm1a; métodos para tratamento de uma doença mediada por kdm1a ou globina; método para atingir um efeito em um paciente; método para inibir pelo menos uma função de kdm1a
CR20210387A (es) Inhibidores de kif18a
MX2017009571A (es) Inhibidores heterociclicos de itk para el tratamiento de la inflamacion y cancer.
MX2022005290A (es) Compuestos heterociclicos como inmunomoduladores.
MX2021007104A (es) Inhibidores de kif18a.
BR112018076534A2 (pt) compostos heterocíclicos como imunomoduladores
EA201891203A1 (ru) Гетероциклические соединения в качестве иммуномодуляторов
BR112019004100A2 (pt) compostos de biarila úteis como imunomoduladores
BR112013033182A2 (pt) compostos imidazopiridinil-aminopiridina substituída
CY1119387T1 (el) Τριαζολοπυραζινες ως αναστολεις brd4 για χρηση στην αντιμετωπιση καρκινου
MX2019007189A (es) Compuestos de amino-triazolopiridina y su uso en el trataniento del cancer.
PH12017500367B1 (en) Compounds that inhibit mcl-1 protein
BR112018070602A2 (pt) composto, composição farmacêutica, uso do composto, e, método para tratar uma doença ou distúrbio
PH12020552135A1 (en) Kdm1a inhibitors for the treatment of disease
BR112017000470A2 (pt) composto, composição farmacêutica, método para modular atividade, método para tratar uma afecção
BR112017027498A2 (pt) anticorpo, ácido nucleico, composto, composição, e, método para tratamento de um paciente com uma doença.
CR20150217A (es) Inhibidores de histona demetilasas
BR112016030730A8 (pt) composto
ECSP20046463A (es) Compuestos, composiciones y métodos para tratar enfermedades que involucren tejidos con enfermedades ácidas o hipóxicas
UY35827A (es) Derivados de triazolopirazina como inhibidores de la proteína brd4
BR112016015235A2 (pt) Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento
ECSP19051409A (es) Nuevo compuesto heterocíclico, su método de preparación y composición farmacéutica que lo comprende
BR112017026535A2 (pt) composto de fórmula estrutural i, enantiômero isolado, composição farmacêutica, método para inibir atividade do transportador de monocarboxilato mct4, método para inibir seletivamente atividade do transportador de monocarboxilato mct4, método para tratar um distúrbio mediado por transportador de monocarboxilato mct4 e uso de um composto
MX2017011277A (es) Inhibidores de glucosilceramida sintasa para el tratamiento de enfermedades.

Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 06/08/2014, OBSERVADAS AS CONDICOES LEGAIS