RS58040B1 - Prmt5 inhibitori i njihove upotrebe - Google Patents

Prmt5 inhibitori i njihove upotrebe

Info

Publication number
RS58040B1
RS58040B1 RS20181485A RSP20181485A RS58040B1 RS 58040 B1 RS58040 B1 RS 58040B1 RS 20181485 A RS20181485 A RS 20181485A RS P20181485 A RSP20181485 A RS P20181485A RS 58040 B1 RS58040 B1 RS 58040B1
Authority
RS
Serbia
Prior art keywords
prmt5 inhibitors
prmt5
inhibitors
Prior art date
Application number
RS20181485A
Other languages
English (en)
Inventor
Kenneth W Duncan
Richard Chesworth
Paula Ann Boriack-Sjodin
Michael John Munchhof
Lei Jin
Original Assignee
Epizyme 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49958717&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RS58040(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Epizyme Inc filed Critical Epizyme Inc
Publication of RS58040B1 publication Critical patent/RS58040B1/sr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/495—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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
    • C12N9/1007—Methyltransferases (general) (2.1.1.)
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Obesity (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
RS20181485A 2012-12-21 2013-12-20 Prmt5 inhibitori i njihove upotrebe RS58040B1 (sr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261745485P 2012-12-21 2012-12-21
US201361790525P 2013-03-15 2013-03-15
EP13821599.1A EP2935222B1 (en) 2012-12-21 2013-12-20 Prmt5 inhibitors and uses thereof
PCT/US2013/077235 WO2014100719A2 (en) 2012-12-21 2013-12-20 Prmt5 inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
RS58040B1 true RS58040B1 (sr) 2019-02-28

Family

ID=49958717

Family Applications (1)

Application Number Title Priority Date Filing Date
RS20181485A RS58040B1 (sr) 2012-12-21 2013-12-20 Prmt5 inhibitori i njihove upotrebe

Country Status (30)

Country Link
US (10) US9604930B2 (sr)
EP (3) EP4219465A3 (sr)
JP (1) JP6678455B2 (sr)
KR (2) KR102024417B1 (sr)
CN (1) CN105452226B (sr)
AU (1) AU2018202150B2 (sr)
BR (1) BR112015014590B1 (sr)
CA (1) CA2894228C (sr)
CL (1) CL2015001790A1 (sr)
CR (1) CR20150371A (sr)
CY (1) CY1121625T1 (sr)
DK (1) DK2935222T3 (sr)
DO (1) DOP2015000158A (sr)
EA (1) EA027908B1 (sr)
ES (1) ES2701069T3 (sr)
HK (1) HK1212690A1 (sr)
HR (1) HRP20182037T1 (sr)
HU (1) HUE040323T2 (sr)
IL (3) IL239296B (sr)
LT (1) LT2935222T (sr)
MX (1) MX2015008052A (sr)
PE (1) PE20151501A1 (sr)
PH (2) PH12015501351A1 (sr)
PL (1) PL2935222T3 (sr)
PT (1) PT2935222T (sr)
RS (1) RS58040B1 (sr)
SI (1) SI2935222T1 (sr)
UA (1) UA118548C2 (sr)
WO (1) WO2014100719A2 (sr)
ZA (1) ZA201505212B (sr)

Families Citing this family (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012170904A2 (en) * 2011-06-10 2012-12-13 Bytemobile, Inc. Adaptive bitrate management on progressive download with indexed media files
TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物
CA2899363A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2014100734A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2894130A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
CA2894126A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
MX2015008052A (es) 2012-12-21 2016-08-18 Epizyme Inc Inhibidores de prmt5 y sus usos.
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
CA2894542C (en) 2012-12-21 2023-10-31 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
WO2014110574A1 (en) 2013-01-14 2014-07-17 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
ME03780B (me) 2013-01-15 2021-04-20 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
BR112015022785A2 (pt) 2013-03-14 2017-07-18 Epizyme Inc composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
EP2970137A1 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
WO2014153208A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9394258B2 (en) 2013-03-14 2016-07-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9718816B2 (en) 2013-03-15 2017-08-01 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as CARM1 inhibitors and uses thereof
US9346802B2 (en) 2013-03-15 2016-05-24 Epizyme, Inc. CARM1 inhibitors and uses thereof
EP2970219B1 (en) 2013-03-15 2019-02-27 Epizyme, Inc. Carm1 inhibitors and uses thereof
CN105658653A (zh) 2013-08-23 2016-06-08 因赛特公司 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物
PE20161552A1 (es) 2014-06-17 2017-01-11 Pfizer Compuestos de dihidroisoquinolinona sustituida
WO2015200677A2 (en) * 2014-06-25 2015-12-30 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2952567A1 (en) 2014-06-25 2015-12-30 Glaxosmithkline Intellectual Property Development Limited Crystalline salts of (s)-6-((1-acetylpiperidin-4-yl)amino)-n-(3-(3,4-dihydroisoquinolin-2(1h)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide
US20170198006A1 (en) * 2014-06-25 2017-07-13 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
EP3177288A4 (en) * 2014-08-04 2018-04-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2016034671A1 (en) * 2014-09-03 2016-03-10 Ctxt Pty Ltd Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived prmt5-inhibitors
WO2016034673A1 (en) * 2014-09-03 2016-03-10 Ctxt Pty Ltd Tetrahydroisoquinoline derived prmt5-inhibitors
GB201415573D0 (en) * 2014-09-03 2014-10-15 Cancer Therapeutics Crc Pty Ltd Compounds
US20180010132A1 (en) 2014-09-11 2018-01-11 Novartis Ag Inhibition of prmt5 to treat mtap-deficiency-related diseases
US10479997B2 (en) 2014-12-01 2019-11-19 Novartis Ag Compositions and methods for diagnosis and treatment of prostate cancer
AR104326A1 (es) 2015-05-04 2017-07-12 Lilly Co Eli Compuestos nucleósidos 5-sustituidos
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
TWI730980B (zh) * 2015-08-26 2021-06-21 比利時商健生藥品公司 使用作為ｐｒｍｔ５抑制劑之新穎經６-６雙環芳香環取代之核苷類似物
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
CN105497034B (zh) * 2015-12-08 2018-08-07 暨南大学 一种通过靶向prmt5抑制骨肉瘤生长的组合物及其制备方法
GB201604031D0 (en) * 2016-03-09 2016-04-20 Ctxt Pty Ltd Compounds
GB201604029D0 (en) 2016-03-09 2016-04-20 Ctxt Pty Ltd Compounds
GB201604020D0 (en) * 2016-03-09 2016-04-20 Ctxt Pty Ltd Compounds
GB201604022D0 (en) 2016-03-09 2016-04-20 Ctxt Pty Ltd Compounds
GB201604027D0 (en) 2016-03-09 2016-04-20 Ctxt Pty Ltd Compounds
GB201604030D0 (en) * 2016-03-09 2016-04-20 Ctxt Pty Ltd Compounds
EP3426664B1 (en) 2016-03-10 2021-06-30 Janssen Pharmaceutica NV Substituted nucleoside analogues for use as prmt5 inhibitors
UA123637C2 (uk) 2016-03-10 2021-05-05 Янссен Фармацевтика Нв Заміщені аналоги нуклеозидів для застосування як інгібіторів prmt5
CA2969295A1 (en) 2016-06-06 2017-12-06 Pfizer Inc. Substituted carbonucleoside derivatives, and use thereof as a prmt5 inhibitor
US20180072718A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine compounds and uses thereof
KR102493644B1 (ko) 2016-09-14 2023-01-30 얀센 파마슈티카 엔.브이. 메닌-mll 상호작용의 스피로 바이사이클릭 억제제
EP3512858B1 (en) 2016-09-14 2023-11-08 Janssen Pharmaceutica NV Fused bicyclic inhibitors of menin-mll interaction
WO2018065365A1 (en) 2016-10-03 2018-04-12 Janssen Pharmaceutica Nv Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
CA3037998A1 (en) 2016-10-03 2018-04-12 Janssen Pharmaceutica Nv Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
JP2019537585A (ja) 2016-10-28 2019-12-26 アイカーン スクール オブ メディスン アット マウント シナイ Ｅｚｈ２媒介性がんを治療するための組成物および方法
CA3045243A1 (en) * 2016-12-01 2018-06-07 Glaxosmithkline Intellectual Property Development Limited Combination therapy
US11197857B2 (en) 2016-12-01 2021-12-14 Glaxosmithkline Intellectual Property Development Limited Combination therapy
WO2018106870A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
KR102513564B1 (ko) 2016-12-15 2023-03-22 얀센 파마슈티카 엔.브이. 메닌-mll 상호작용의 아제판 억제제
MX2019010150A (es) 2017-02-27 2019-10-21 Janssen Pharmaceutica Nv Uso de biomarcadores en la identificacion de pacientes con cancer que seran sensibles al tratamiento con un inhibidor de prmt5.
CN108570059B (zh) * 2017-03-09 2022-02-08 中国科学院上海药物研究所 一种具有prmt5抑制活性的化合物及其制备和应用
GB201704327D0 (en) * 2017-03-17 2017-05-03 Argonaut Therapeutics Ltd Compounds
AU2018313910B2 (en) * 2017-08-09 2022-12-08 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
CN111108105B (zh) 2017-09-22 2023-03-31 朱比兰特埃皮帕德有限公司 作为pad抑制剂的杂环化合物
SG11202003463XA (en) 2017-10-18 2020-05-28 Jubilant Epipad LLC Imidazo-pyridine compounds as pad inhibitors
CA3080677A1 (en) 2017-11-06 2019-05-09 Jubilant Prodel LLC Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
IL274762B2 (en) * 2017-11-24 2023-10-01 Jubilant Episcribe Llc Novel heterocyclic compounds as PRMT5 inhibitors
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
JP7352544B2 (ja) 2017-12-08 2023-09-28 ヤンセン ファーマシューティカ エヌ．ベー． 新規なスピロ二環式類似体
DK3724190T3 (da) 2017-12-13 2022-10-10 Lupin Ltd Substituerede bicykliske heterocykliske forbindelser som PRMT5 inhibitorer
US11396517B1 (en) 2017-12-20 2022-07-26 Janssen Pharmaceutica Nv Exo-aza spiro inhibitors of menin-MLL interaction
CA3091041A1 (en) * 2018-02-22 2019-08-29 Ichan School Of Medicine At Mount Sinai Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use
CA3092677A1 (en) 2018-03-06 2019-09-12 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (akt) degradation / disruption compounds and methods of use
US11591326B2 (en) 2018-03-09 2023-02-28 Pharmablock Sciences (Nanjing), Inc. Inhibitors of protein arginine methyltransferase 5 (PRMT5), pharmaceutical products thereof, and methods thereof
SG11202008950PA (en) 2018-03-13 2020-10-29 Jubilant Prodel LLC Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation
AU2019237329B2 (en) * 2018-03-22 2024-03-28 Aurigene Discovery Technologies Limited Substituted imidazolidin-2-one derivatives as PRMT5 inhibitors
US11365205B2 (en) 2018-03-22 2022-06-21 Aurigene Discovery Technologies Limited Imidazolidin-2-one compounds as PRMT5 modulators
WO2019219805A1 (en) 2018-05-16 2019-11-21 Ctxone Pty Ltd Combination therapy
US11077101B1 (en) 2018-07-18 2021-08-03 Tango Therapeutics, Inc. Compounds and methods of use
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
CA3118175A1 (en) * 2018-11-08 2020-05-14 Glaxosmithkline Intellectual Property Development Limited Combination of prmt5 inhibitors and bcl-2 inhibitors
WO2020182018A1 (zh) * 2019-03-12 2020-09-17 四川科伦博泰生物医药股份有限公司 氮杂环化合物、其制备方法及用途
US20230212143A9 (en) * 2019-03-29 2023-07-06 University Of Florida Research Foundation, Incorporated Prmt5 inhibitor compounds
CN111825656B (zh) * 2019-04-15 2023-03-31 南京药石科技股份有限公司 蛋白质精氨酸甲基转移酶5(prmt5)的抑制剂、其药学产品及其方法
TW202112375A (zh) 2019-06-06 2021-04-01 比利時商健生藥品公司 使用ｐｒｍｔ５抑制劑治療癌症之方法
EP3980417B1 (en) 2019-06-10 2023-09-27 Lupin Limited Prmt5 inhibitors
CR20220012A (es) 2019-06-12 2022-03-11 Janssen Pharmaceutica Nv Nuevos intermedios espirobiciclicos
KR20220027216A (ko) 2019-06-28 2022-03-07 에이엘에스 테라피 디벨럽먼트 인스티튜트 디펩타이드 반복 단백질의 억제
CN110585434B (zh) * 2019-10-11 2021-04-09 山东大学 Prmt5抑制剂在抗病毒中的应用
WO2021068953A1 (zh) 2019-10-12 2021-04-15 南京圣和药业股份有限公司 作为prmt5抑制剂的取代三环类化合物及其应用
JP2023504230A (ja) 2019-10-22 2023-02-02 ルピン・リミテッド Ｐｒｍｔ５阻害剤の組合せ医薬
CN112778275B (zh) * 2019-11-11 2023-05-12 石药集团中奇制药技术（石家庄）有限公司 金刚烷基prmt5抑制剂及其应用
CN110950841A (zh) * 2019-11-22 2020-04-03 济南大学 一类新型三唑类化合物的合成及应用
CN111018832A (zh) * 2019-11-26 2020-04-17 济南大学 一类含有四氢异喹啉结构的咪唑酮类化合物的制备及应用
KR102514245B1 (ko) * 2019-12-03 2023-03-29 한양대학교 에리카산학협력단 단백질 인산화 효소 저해 활성을 갖는 신규한 피라졸 유도체 및 이의 용도
AU2020394887A1 (en) 2019-12-03 2022-06-16 Lupin Limited Substituted nucleoside analogs as PRMT5 inhibitors
CA3160153A1 (en) * 2019-12-17 2021-06-24 Michelle Machacek Prmt5 inhibitors
US20230108114A1 (en) * 2019-12-17 2023-04-06 Merck Sharp & Dohme Llc Prmt5 inhibitors
CN113045543B (zh) * 2019-12-26 2023-05-12 石药集团中奇制药技术（石家庄）有限公司 一种prmt5抑制剂及其应用
EP4155301A1 (en) * 2020-06-02 2023-03-29 CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. 3,4-dihydroisoquinoline compound and use thereof
CN113754541A (zh) * 2020-06-02 2021-12-07 深圳湾实验室 靶向eb病毒核抗原蛋白的小分子抑制剂、制备方法及其应用
CN111592522B (zh) * 2020-06-17 2022-09-09 郑州大学 一种精氨酸甲基化转移酶5小分子抑制剂及其制备方法和用途
CN116568677A (zh) 2020-07-31 2023-08-08 探戈医药股份有限公司 可用于治疗mtap缺乏和/或mta累积癌症的哌啶-1-基-n-吡啶-3-基-2-氧代乙酰胺衍生物
CN116113626A (zh) 2020-09-04 2023-05-12 上海翊石医药科技有限公司 一种具有抗肿瘤活性的化合物及其用途
US20230365558A1 (en) * 2020-09-22 2023-11-16 Medshine Discovery Inc. Tetrahydroisoquinoline derivative and use thereof
WO2022237858A1 (zh) 2021-05-13 2022-11-17 上海翊石医药科技有限公司 一种具有抗肿瘤活性的化合物及其用途
GB202117230D0 (en) 2021-11-29 2022-01-12 Argonaut Therapeutics Ltd Peptide vaccine
WO2023104107A1 (zh) * 2021-12-08 2023-06-15 石药集团中奇制药技术（石家庄）有限公司 3,4-二氢异喹啉类化合物的盐及其应用
GB202203588D0 (en) 2022-03-15 2022-04-27 Argonaut Therapeutics Ltd Cancer diagnostic

Family Cites Families (183)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD68906A (sr)
DE63776C (de) A. RUPERT, Eisenbahn - Werkmeister, in Köln - Nippes, Escherstrafse 14 Verfahren und Vorrichtung eiserne Rohrwände mit Messing zu überziehen
GB1374366A (en) 1972-07-21 1974-11-20 Science Union & Cie Propanol derivatives and a process for their preparation
DE2361390A1 (de) * 1973-12-10 1975-06-19 Merck Patent Gmbh Isochinolinderivate und verfahren zu ihrer herstellung
US4026897A (en) 1974-01-31 1977-05-31 Otsuka Pharmaceutical Company 5-[1-Hydroxy-2-(substituted-amino)]alkyl-8-hydroxycarbostyril derivatives
CA1072359A (en) 1974-10-08 1980-02-26 Hiroyuki Konishi Method for controlling the growth of plants
HU179951B (en) 1979-10-11 1983-01-28 Chinoin Gyogyszer Es Vegyeszet Process for preparing 1,2,4-oxadiazolin-5-one derivatives and pharmaceutical compositions containing thereof
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
HU187922B (en) 1982-06-16 1986-03-28 May And Baker Ltd,Gb Process for preparing 3-/n,n-dimethyl-carbamoyl/-pyrazolo/1,5-a/-pyridine
DE3303344A1 (de) 1983-02-02 1984-08-02 Hoechst Ag, 6230 Frankfurt Verfahren zur herstellung von n-alkylierten aminosaeuren und deren estern
US4684459A (en) 1985-11-29 1987-08-04 The Dow Chemical Company Collector compositions for the froth flotation of mineral values
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
JPH07100688B2 (ja) * 1986-02-12 1995-11-01 大日本製薬株式会社 環状アミン誘導体
DE3631013A1 (de) * 1986-09-12 1988-03-24 Thomae Gmbh Dr K Neue naphthylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
DE3640641A1 (de) 1986-11-28 1988-07-14 Thomae Gmbh Dr K Neue heteroaromatische aminderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
CA1283827C (en) 1986-12-18 1991-05-07 Giorgio Cirelli Appliance for injection of liquid formulations
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
US4746655A (en) 1987-06-10 1988-05-24 A. H. Robins Company, Incorporated Fused aromatic-spiropiperidine oxazepinones(and thiones)
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
DE3804793A1 (de) 1988-02-16 1989-08-24 Hoechst Ag Renin-hemmende aminosaeurederivate
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
DE3839126A1 (de) 1988-11-19 1990-05-23 Hoechst Ag Renin-hemmende harnstoffderivate von dipeptiden, verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung
US5776963A (en) 1989-05-19 1998-07-07 Hoechst Marion Roussel, Inc. 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
GB9005318D0 (en) 1990-03-09 1990-05-02 Isis Innovation Antiarrhythmic agents
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
AU2228992A (en) 1991-07-08 1993-02-11 Glaxo Group Limited Thiazolidine derivatives and their use as anti-viral compounds
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
ES2103479T3 (es) 1992-07-10 1997-09-16 Glaxo Lab Sa Derivados de anilida.
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5514694A (en) 1992-09-21 1996-05-07 Georgia Tech Research Corp Peptidyl ketoamides
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5294621A (en) 1992-10-07 1994-03-15 Ortho Pharmaceutical Corporation Thieno tetrahydropyridines useful as class III antiarrhythmic agents
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
GB9402807D0 (en) * 1994-02-14 1994-04-06 Xenova Ltd Pharmaceutical compounds
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
US5693847A (en) 1995-04-19 1997-12-02 Vertex Pharmaceuticals Incorporated Heteroatom functionalized α-methyl ketones
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US5554621A (en) * 1995-06-07 1996-09-10 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: nitrogen heterocyclic derivatives
US6130217A (en) 1995-09-20 2000-10-10 Pfizer Inc Compounds enhancing antitumor activity of other cytotoxic agents
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
SE9600769D0 (sv) 1996-02-28 1996-02-28 Astra Ab Compounds useful as analgesic
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
GB9717576D0 (en) * 1997-08-19 1997-10-22 Xenova Ltd Pharmaceutical compounds
US5874449A (en) 1996-12-31 1999-02-23 Gpi Nil Holdings, Inc. N-linked sulfonamides of heterocyclic thioesters
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
US20020169101A1 (en) 1999-05-10 2002-11-14 Gonzalez Maria Isabel Treatment of sexual dysfunction
JP2003501431A (ja) * 1999-05-25 2003-01-14 ザ ペン ステート リサーチ ファウンデイション Ｄｎａメチル基転移酵素阻害剤
DK1216250T3 (da) 1999-09-14 2004-02-23 Aventis Pharma Inc Thienoisoxazolyl- og thienylpyrazolyl-phenoxy- substituerede propylderivater som D4-antagonister
US7253165B2 (en) 1999-09-14 2007-08-07 Aventis Pharmaceuticals Inc. Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as D4 antagonists
EE200200134A (et) 1999-09-14 2003-04-15 Aventis Pharmaceuticals Inc. D4 retseptori antagonistidena toimivad bensisoksasolüül-, püridoisoksasolüül- ja benstienüülfenoksüderivaadid
US7125903B1 (en) 1999-09-14 2006-10-24 Aventis Pharmaceuticals Inc. Thienoisoxazolyl-and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as D4 antagonists
IL150986A0 (en) 2000-03-14 2003-02-12 Actelion Pharmaceuticals Ltd 1,2,3,4,- tetrahydroisoquinoline derivatives
WO2002014277A1 (fr) 2000-08-10 2002-02-21 Tanabe Seiyaku Co., Ltd. Composes de biphenylcarboxamidoisoindoline, procedes de preparation de ceux-ci et produits intermediaires destines a la synthese de ceux-ci
NZ527276A (en) * 2001-03-27 2004-11-26 Actelion Pharmaceuticals Ltd 1,2,3,4-tetrahydroisoquinoline derivatives as urotensin II receptor antagonists
GEP20074221B (en) 2001-07-11 2007-10-25 Elan Pharm Inc N-(3-amino-2-hydroxy-propyl) substituted alkylamide compounds
WO2003018017A1 (en) 2001-08-27 2003-03-06 Arpida Ag 3-substituted 6,7-dihydroxytetrahydroisoquinoline derivatives for use as antibacterial agents
TWI259081B (en) 2001-10-26 2006-08-01 Sugen Inc Treatment of acute myeloid leukemia with indolinone compounds
SE0103644D0 (sv) 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic isoquinoline compounds
NZ533107A (en) 2001-11-08 2007-04-27 Upjohn Co N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives
US7338969B2 (en) 2002-03-08 2008-03-04 Quonova, Llc Modulation of pathogenicity
US7335779B2 (en) 2002-03-08 2008-02-26 Quonova, Llc Modulation of pathogenicity
CA2479618A1 (en) 2002-03-26 2003-10-09 William K. Hagmann Spirocyclic amides as cannabinoid receptor modulators
CA2480856A1 (en) 2002-04-05 2003-10-23 Merck & Co., Inc. Substituted aryl amides
US8013014B2 (en) 2002-07-05 2011-09-06 Georgia Tech Research Corporation Aza-peptide epoxides
CN100402529C (zh) 2002-09-09 2008-07-16 詹森药业有限公司 用于治疗orl-1受体介导疾病的羟基烷基取代的1,3,8-三氮杂螺[4,5]癸-4-酮衍生物
SE0300010D0 (sv) 2003-01-07 2003-01-07 Astrazeneca Ab Novel Compounds
WO2004078114A2 (en) 2003-02-28 2004-09-16 Encysive Pharmaceuticals Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-ii receptor antagonists.
WO2004078731A1 (fr) * 2003-03-06 2004-09-16 'chemical Diversity Research Institute', Ltd. Acides quinoline-carboxyliques et leurs derives et bibliotheque focalisee
US7408008B2 (en) 2003-12-09 2008-08-05 Janssen Pharmaceutica, N.V. Method of producing highly functionalized 1,3-diamino-propan-2-ols from solid support
EP1720855A4 (en) 2004-03-02 2008-12-17 Smithkline Beecham Corp HEMMER OF ACT ACTIVITY
WO2005087752A2 (en) 2004-03-09 2005-09-22 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamine aspartyl protease inhibitors
RU2266906C1 (ru) * 2004-04-29 2005-12-27 Общество с ограниченной ответственностью "Исследовательский Институт Химического Разнообразия" (ООО "Исследовательский Институт Химического Разнообразия") Анелированные карбамоилазагетероциклы, способы их получения (варианты), фармацевтическая композиция, фокусированная библиотека
WO2005118543A1 (ja) 2004-06-03 2005-12-15 Ono Pharmaceutical Co., Ltd. キナーゼ阻害薬およびその用途
EA200700117A1 (ru) 2004-06-24 2007-06-29 Инсайт Корпорейшн N-замещенные пиперидины и их применение в качестве фармацевтических препаратов
US20060009510A1 (en) 2004-07-09 2006-01-12 Pharmacia & Upjohn Company Llc Method of synthesizing indolinone compounds
JP2008007405A (ja) * 2004-12-07 2008-01-17 Takeda Chem Ind Ltd カルボキサミド誘導体
WO2007006547A1 (en) 2005-07-11 2007-01-18 Devgen N.V. Amide derivatives as kinase inhibitors
EP1910317B1 (en) 2005-07-20 2013-07-03 Eli Lilly And Company 1-amino linked compounds
GB0516723D0 (en) 2005-08-15 2005-09-21 Novartis Ag Organic compounds
CA2626549A1 (en) 2005-10-21 2007-04-26 University Of Alabama At Birmingham Small molecule inhibitors of hiv-1 capsid assembly
CA2644069A1 (en) 2006-02-28 2007-09-07 Helicon Therapeutics, Inc. Therapeutic piperazines as pde4 inhibitors
JP5306987B2 (ja) 2006-03-16 2013-10-02 エボテック （ユーエス） インコーポレイテッド Ｐ２ｘ７調節因子としてのビシクロへテロアリール化合物およびその使用
EP2027260B1 (en) 2006-05-05 2013-12-11 Cambridge Enterprise Limited Epigenetic regulatory complex for control of gene expression
WO2008063842A2 (en) 2006-11-02 2008-05-29 Aestus Therapeutics, Inc. Methods of treating neuropathic pain with agonists of ppar-gamma
CN101012223A (zh) 2006-11-13 2007-08-08 西安新安医药科技有限公司 用于治疗的奥硝唑衍生物、制备方法及用途
ATE547411T1 (de) 2006-12-04 2012-03-15 Jiangsu Simcere Pharmaceutical R & D Co Ltd 3-pyrrolo-cyclohexylen-2-dihydroindolinonderiva e und anwendungen davon
CN101157929B (zh) * 2007-02-02 2012-05-23 中国科学院上海有机化学研究所 番红霉素的生物合成基因簇
US20090099157A1 (en) 2007-02-15 2009-04-16 Ameriks Michael K Tetrahydro-pyrazolo-pyridine thioether modulators of cathepsin s
EP2137158A4 (en) 2007-02-28 2012-04-18 Methylgene Inc LOW-MOLECULAR INHIBITORS OF PROTEINARGININE METHYLTRANSFERASES (PRMTS)
US8273766B2 (en) * 2007-04-04 2012-09-25 Kowa Company, Ltd. Tetrahydroisoquinoline compound
DE102007020492A1 (de) 2007-04-30 2008-11-06 Grünenthal GmbH Substituierte Sulfonamid-Derivate
WO2008145398A1 (en) 2007-06-01 2008-12-04 Pfizer Italia S.R.L. 4-arylpyrrole substituted 2-indoline derivatives active as protein kinase inhibitors
ES2560529T3 (es) 2007-06-07 2016-02-19 Haplomic Technologies Pty Ltd. Métodos epigenéticos
WO2008154333A2 (en) 2007-06-08 2008-12-18 Asuragen, Inc. Mir-34 regulated genes and pathways as targets for therapeutic intervention
EP2014651A1 (en) 2007-07-12 2009-01-14 Exonhit Therapeutics SA Compounds and methods for modulating Rho GTPases
RU2345996C1 (ru) * 2007-07-17 2009-02-10 Андрей Александрович Иващенко Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения
NZ562237A (en) 2007-10-05 2011-02-25 Pacific Edge Biotechnology Ltd Proliferation signature and prognosis for gastrointestinal cancer
US20090093493A1 (en) 2007-10-09 2009-04-09 Francesco Berardi 1-phenylalcoxy-2-beta-phenylethyl derivatives as p-glycoprotein (p-gp) inhibitors useful in drug resistance events
MY167602A (en) 2007-11-01 2018-09-20 Acucela Inc Amine derivatives compounds for treating ophthalmic diseases and disorders
US8722851B2 (en) 2007-11-02 2014-05-13 Pain Therapeutics, Inc. Analgesia with minimal tolerance and dependence by a mu opioid receptor agonist that also binds filamin A
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
RU2371444C1 (ru) * 2008-01-24 2009-10-27 Андрей Александрович Иващенко ФУРО- И ТИЕНО[2,3-b]-ХИНОЛИН-2-КАРБОКСАМИДЫ, СПОСОБ ПОЛУЧЕНИЯ И ПРОТИВОТУБЕРКУЛЕЗНАЯ АКТИВНОСТЬ
WO2009126782A1 (en) 2008-04-11 2009-10-15 High Point Pharmaceuticals, Llc Histamine h3 receptor ligands
WO2010002994A1 (en) 2008-07-01 2010-01-07 Purdue Research Foundation Nonpeptide hiv-1 protease inhibitors
FR2933977B1 (fr) * 2008-07-18 2013-04-26 Centre Nat Rech Scient Derives heterocycliques utiles dans le traitement des maladies neurodegeneratives
CA2736229C (en) 2008-09-05 2015-06-09 Acucela Inc. Sulfur-linked compounds for treating opthalmic diseases and disorders
TWI486326B (zh) 2008-10-22 2015-06-01 Acucela Inc 用於治療眼疾和眼病變之連接氮之化合物
WO2010057101A2 (en) 2008-11-17 2010-05-20 Schering Corporation Compounds useful as hiv blockers
CA2755697A1 (en) 2009-03-17 2010-09-23 Daiichi Sankyo Company, Limited Amide derivative
US8309547B2 (en) 2009-04-28 2012-11-13 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
BRPI1011247A2 (pt) 2009-06-09 2016-06-21 California Capital Equity Llc derivados de isoquinolina, quinolina e quinazolina como inibidores de sinalização de hedgehog
AU2010273220B2 (en) 2009-07-13 2015-10-15 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
WO2011079236A1 (en) * 2009-12-22 2011-06-30 The Ohio State University Research Foundation Compositions and methods for cancer detection and treatment
GB0922332D0 (en) 2009-12-22 2010-02-03 Isis Innovation Method of treatment and screening method
EP2357176A1 (en) * 2010-01-15 2011-08-17 Hybrigenics S.A. Amidoacridine derivatives useful as selective inhibitors of ubiquitin specific protease 7
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
TWI513694B (zh) 2010-05-11 2015-12-21 Amgen Inc 抑制間變性淋巴瘤激酶的嘧啶化合物
JOP20190250A1 (ar) 2010-07-14 2017-06-16 Regeneron Pharma صيغ مستقرة تحتوي على الأجسام المضادة لمضاد عامل نمو الأعصاب
CA2815063C (en) 2010-10-18 2016-11-22 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
WO2012054896A1 (en) 2010-10-22 2012-04-26 Biotime Inc. Methods of modifying transcriptional regulatory networks in stem cells
WO2012082436A2 (en) 2010-12-03 2012-06-21 Epizyme, Inc. Modulators of histone methyltransferase, and methods of use thereof
BR112013013668A2 (pt) 2010-12-03 2016-09-06 Epizyme Inc moduladores 7-deazapurina de histona metiltransferase, e métodos de uso dos mesmos
CN103476944B (zh) 2011-03-25 2016-01-20 艾尔玛可科学（苏格兰）有限公司 荧光寿命表观遗传学测定
AU2012249322B2 (en) 2011-04-28 2018-01-04 Sloan-Kettering Institute For Cancer Research HSP90 combination therapy
KR102025142B1 (ko) 2011-07-08 2019-09-26 슬로안-케테링인스티튜트퍼캔서리서치 표지된 ｈｓｐ90 억제제의 용도
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
WO2013038378A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
WO2013052505A2 (en) 2011-10-03 2013-04-11 Celmatix, Inc. Methods and devices for assessing risk to a putative offspring of developing a condition
TWI577671B (zh) 2011-11-14 2017-04-11 Sunshine Lake Pharma Co Ltd Aminoquinazoline derivatives and salts thereof and methods of use thereof
US10214476B2 (en) 2011-12-30 2019-02-26 Ecole Nationale Superieure De Chimie De Clermont Ferrand Pain relief compounds
EP2833893B1 (en) 2012-04-03 2018-08-29 Reneuron Limited Stem cell microparticles
JP6566867B2 (ja) 2012-07-13 2019-08-28 ペイン セラピューティクス インコーポレイテッド 生きている患者でのアルツハイマー病アッセイ
CA2879322A1 (en) 2012-07-19 2014-01-23 Reneuron Limited Stem cell microparticles
US9585891B2 (en) 2012-09-25 2017-03-07 Merck Patent Gmbh Alpha hydroxy amides
NZ746054A (en) 2012-10-15 2020-07-31 Epizyme Inc Methods of treating cancer
US20140205669A1 (en) 2012-11-29 2014-07-24 The Penn State Research Foundation dhS1P AND USE OF SAME AS AN ANTICANCER THERAPEUTIC AND IMMUNOMODULATOR
JP2016511744A (ja) 2012-12-21 2016-04-21 エピザイム，インコーポレイティド Ｐｒｍｔ５を阻害する方法
CA2899363A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2894130A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
CA2894126A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
MX2015008052A (es) 2012-12-21 2016-08-18 Epizyme Inc Inhibidores de prmt5 y sus usos.
WO2014100734A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970137A1 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9394258B2 (en) 2013-03-14 2016-07-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153208A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP3363434A1 (en) 2013-03-14 2018-08-22 Epizyme Inc Arginine methyltransferase inhibitors and uses thereof
EP2970134B1 (en) 2013-03-14 2018-02-28 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
BR112015022785A2 (pt) 2013-03-14 2017-07-18 Epizyme Inc composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9346802B2 (en) 2013-03-15 2016-05-24 Epizyme, Inc. CARM1 inhibitors and uses thereof
EP2970219B1 (en) 2013-03-15 2019-02-27 Epizyme, Inc. Carm1 inhibitors and uses thereof
US9718816B2 (en) 2013-03-15 2017-08-01 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as CARM1 inhibitors and uses thereof
RU2673549C2 (ru) 2013-05-03 2018-11-28 Ф. Хоффманн-Ля Рош Аг Производные изохинолина, стимулирующие нейрогенез
US20170198006A1 (en) 2014-06-25 2017-07-13 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2015200677A2 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2952567A1 (en) 2014-06-25 2015-12-30 Glaxosmithkline Intellectual Property Development Limited Crystalline salts of (s)-6-((1-acetylpiperidin-4-yl)amino)-n-(3-(3,4-dihydroisoquinolin-2(1h)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide
EP3177288A4 (en) 2014-08-04 2018-04-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2016044585A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2016044650A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
WO2016044569A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Salts, co-crystals, amorphous forms, and crystalline forms of a co-activator-associated arginine methyltransferase 1 (carm1) inhibitor
WO2016044576A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Salts, co-crystals, amorphous forms, and crystalline forms of an arginine methyltransferase inhibitor
WO2016044626A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP3193608A4 (en) 2014-09-17 2018-05-02 Epizyme, Inc. Carm1 inhibitors and uses thereof
US20170283400A1 (en) 2014-09-17 2017-10-05 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2016044641A2 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
KR20170117479A (ko) 2015-02-11 2017-10-23 바실리어 파마슈티카 인터내셔널 리미티드 치환된 모노- 및 폴리아자나프탈렌 유도체 및 이의 용도
WO2017136699A1 (en) 2016-02-05 2017-08-10 Epizyme, Inc Arginine methyltransferase inhibitors and uses thereof
AR108326A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
GB201704476D0 (en) 2017-03-21 2017-05-03 Antabio Sas Chemical compounds

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