PE20170331A1 - Derivados quinolina como inhibidores smo - Google Patents

Derivados quinolina como inhibidores smo

Info

Publication number
PE20170331A1
PE20170331A1 PE2016001704A PE2016001704A PE20170331A1 PE 20170331 A1 PE20170331 A1 PE 20170331A1 PE 2016001704 A PE2016001704 A PE 2016001704A PE 2016001704 A PE2016001704 A PE 2016001704A PE 20170331 A1 PE20170331 A1 PE 20170331A1
Authority
PE
Peru
Prior art keywords
quinoline derivatives
smo inhibitors
detailed below
smo
inhibitors
Prior art date
Application number
PE2016001704A
Other languages
English (en)
Inventor
Shuhui Chen
Lijuan Chen
Xiaoxin Chen
Yunhui Li
Hao Wu
Zhuowei Liu
Chaofeng Long
Changqing Wei
Jun Lin
Original Assignee
Guangdong Zhongsheng Pharmaceutical Co Ltd
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
Priority claimed from CN201410110890.1A external-priority patent/CN104945377A/zh
Application filed by Guangdong Zhongsheng Pharmaceutical Co Ltd filed Critical Guangdong Zhongsheng Pharmaceutical Co Ltd
Publication of PE20170331A1 publication Critical patent/PE20170331A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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 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
    • C07D215/38—Nitrogen atoms
    • 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
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Se refiere a derivados de quinolina de formula (I) o sales de los mismos, donde A es una de las formulas detalladas a continuacion; T11, T12 y T13 son N, C(R13); R11, R12 y R13 son H, F, Cl, entre otros; T21 a T26 son N, C(R25); R25 es H, Br, entre otros; L1 y L2 son N(R14), C(=O)N(R15), entre otros; R14 y R15 son H, cicloalquil C3-C6, entre otros; B es una de las formulas detalladas a continuacion; R31 a R35 son H, F, entre otros; E32 es N(R40), entre otros; R40 es H, entre otros. Es un compuesto preferido: 4-(2-(4-((3R,5R)-3,5-dimetilpiperidin-1-il)fenil)-4-metil-1-oxo-1,2-dihidroisoquinolin-5-il)benzonitrilo; entre otros. Dichos compuestos inhiben la via de Hedgehog siendo utiles en el tratamiento de enfermedades tal como el cancer
PE2016001704A 2014-03-24 2015-03-16 Derivados quinolina como inhibidores smo PE20170331A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201410110890.1A CN104945377A (zh) 2014-03-24 2014-03-24 作为smo抑制剂的喹啉衍生物
CN201510104908 2015-03-10

Publications (1)

Publication Number Publication Date
PE20170331A1 true PE20170331A1 (es) 2017-04-28

Family

ID=54193978

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001704A PE20170331A1 (es) 2014-03-24 2015-03-16 Derivados quinolina como inhibidores smo

Country Status (18)

Country Link
US (1) US9938292B2 (es)
EP (1) EP3124482B1 (es)
JP (1) JP6377245B2 (es)
KR (1) KR101910724B1 (es)
CN (1) CN106458974B (es)
AU (1) AU2015237050B2 (es)
BR (1) BR112016021730B1 (es)
CA (1) CA2943100C (es)
CL (1) CL2016002394A1 (es)
EC (1) ECSP16083602A (es)
IL (1) IL247970A (es)
MX (1) MX370438B (es)
NZ (1) NZ724691A (es)
PE (1) PE20170331A1 (es)
RU (1) RU2695815C9 (es)
SG (1) SG11201607973XA (es)
TW (1) TW201623242A (es)
WO (1) WO2015144001A1 (es)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI433674B (zh) 2006-12-28 2014-04-11 Infinity Discovery Inc 環杷明（ｃｙｃｌｏｐａｍｉｎｅ）類似物類
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
HRP20251395T1 (hr) 2015-06-04 2026-02-13 Sol-Gel Technologies Ltd. Topikalne formulacije za isporuku spojeva inhibitora hedgehog signalnog puta i njihova uporaba
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017015562A1 (en) * 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US20190112317A1 (en) 2015-10-05 2019-04-18 The Trustees Of Columbia University In The City Of New York Activators of autophagic flux and phospholipase d and clearance of protein aggregates including tau and treatment of proteinopathies
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
EP3377481A1 (en) 2015-11-16 2018-09-26 Araxes Pharma LLC 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
MX2021006804A (es) 2015-12-17 2023-01-13 Merck Patent Gmbh Antagonistas policiclicos del receptor 7/8 tipo toll (tlr7/8) y uso de los mismos en el tratamiento de trastornos inmunitarios.
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP4198031A1 (en) 2016-08-08 2023-06-21 Merck Patent GmbH Tlr7/8 antagonists and uses thereof
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
KR102688614B1 (ko) 2016-09-30 2024-07-26 삼성전자주식회사 이미지 처리 방법 및 이를 지원하는 전자 장치
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
CN109890793B (zh) 2016-11-11 2022-11-18 拜耳动物保健有限责任公司 新的抗蠕虫药喹啉-3-甲酰胺衍生物
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
JP7210483B2 (ja) 2017-06-30 2023-01-23 バイエル・アニマル・ヘルス・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 新規アザキノリン誘導体
UY38009A (es) * 2017-12-15 2019-07-31 Bayer Animal Health Gmbh Proceso para la preparación de derivados de quinolina
US11261192B2 (en) 2018-03-09 2022-03-01 Recurium Ip Holdings, Llc Substituted 1,2-dihydro-3H-pyrazolo[3,4-D]pyrimidin-3-ones
JP7403472B2 (ja) 2018-05-09 2023-12-22 バイエル・アニマル・ヘルス・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 新規キノリン誘導体
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
PE20211655A1 (es) 2018-10-31 2021-08-24 Gilead Sciences Inc Compuestos de 6-azabencimidazol sustituidos como inhibidores de hpk1
AU2019375983A1 (en) * 2018-11-09 2021-06-10 Vivace Therapeutics, Inc. Bicyclic compounds
IL287222B2 (en) 2019-04-16 2025-04-01 Vivace Therapeutics Inc Bicyclic compounds
TWI826690B (zh) 2019-05-23 2023-12-21 美商基利科學股份有限公司 經取代之烯吲哚酮化物及其用途
WO2020259556A1 (zh) * 2019-06-27 2020-12-30 南京明德新药研发有限公司 作为cdk9抑制剂的氮杂吲哚连吡唑类化合物
CN115298172B (zh) * 2020-03-27 2023-11-14 广东众生药业股份有限公司 一种作为smo抑制剂化合物的盐型、晶型及其制备方法
US20230242511A1 (en) * 2020-05-14 2023-08-03 Glixogen Therapeutics Ltd. Fused pyrazole and imidazole based compounds and use thereof as gli1 inhibitors
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
BR112023000047A2 (pt) 2020-07-02 2023-03-14 Incyte Corp Compostos de ureia tricíclicos como inibidores da v617f da jak2
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
EP4358948A4 (en) * 2021-06-25 2025-05-14 Cedilla Therapeutics, Inc. TEAD INHIBITORS AND USES THEREOF
KR20240163688A (ko) 2022-03-17 2024-11-19 인사이트 코포레이션 Jak2 v617f 억제제로서의 삼환계 우레아 화합물

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07173138A (ja) 1993-10-25 1995-07-11 Kyowa Hakko Kogyo Co Ltd キノリン誘導体
NZ325248A (en) * 1995-12-23 1999-09-29 Pfizer Res & Dev Quinoline and quinazoline compounds useful in therapy
GB9700504D0 (en) 1997-01-11 1997-02-26 Pfizer Ltd Pharmaceutical compounds
DE19738615A1 (de) * 1997-09-04 1999-03-11 Clariant Gmbh Neue Lichtschutzmittel auf Basis von sterisch gehinderten Aminen
DE10219037A1 (de) 2002-04-29 2003-11-06 Bayer Ag Herstellung und Verwendung von Iminodibernsteinsäureammoniummetallsalzen
AU2003301436A1 (en) * 2002-10-17 2004-05-04 Amgen Inc. Benzimidazole derivatives and their use as vanilloid receptor ligands
JP2005132834A (ja) * 2003-10-09 2005-05-26 Kyowa Hakko Kogyo Co Ltd キノリン誘導体
ATE444068T1 (de) * 2004-01-23 2009-10-15 Janssen Pharmaceutica Nv Chinolinderivate und ihre verwendung als mycobakterielle inhibitoren
KR20200019263A (ko) 2004-09-02 2020-02-21 제넨테크, 인크. 헤지호그 신호전달에 대한 피리딜 억제제
US20070054916A1 (en) * 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
DK2001474T3 (en) * 2006-03-16 2016-05-09 Second Genome Inc BICYCLOHETEROARYL COMPOUNDS AS P2X7 MODULATORS AND APPLICATIONS THEREOF
CA2645652A1 (en) * 2006-03-16 2007-09-27 Renovis, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
TWI464148B (zh) * 2006-03-16 2014-12-11 Evotec Us Inc 作為ｐ２ｘ7調節劑之雙環雜芳基化合物與其用途
UA93548C2 (uk) 2006-05-05 2011-02-25 Айерем Елелсі Сполуки та композиції як модулятори хеджхогівського сигнального шляху
WO2008012623A1 (en) * 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
KR20090130051A (ko) 2007-03-14 2009-12-17 엑셀리시스, 인코포레이티드 헤지호그 경로의 억제제
WO2010021381A1 (ja) * 2008-08-22 2010-02-25 武田薬品工業株式会社 縮合複素環誘導体およびその用途
CA2733533C (en) 2008-08-25 2013-12-17 Irm Llc Hedgehog pathway modulators
EP2334683B1 (en) 2008-08-29 2017-03-22 MSD Italia S.r.l. Saturated bicyclic heterocyclic derivatives as smo antagonists
GB0900484D0 (en) 2009-01-13 2009-02-11 Angeletti P Ist Richerche Bio Therapeutic agent
CN102573473B (zh) 2009-06-09 2015-05-27 加利福尼亚资本权益有限责任公司 用作hedgehog 信号转导抑制剂的异喹啉、喹啉和喹唑啉衍生物
TWI428332B (zh) * 2009-06-09 2014-03-01 Hoffmann La Roche 雜環抗病毒化合物
JP5739334B2 (ja) 2009-08-26 2015-06-24 武田薬品工業株式会社 縮合複素環誘導体およびその用途
WO2011097491A1 (en) * 2010-02-04 2011-08-11 Glaxosmithkline Llc Benzimidazole antiviral agents
TW201311149A (zh) * 2011-06-24 2013-03-16 Ishihara Sangyo Kaisha 有害生物防治劑
MX344308B (es) * 2011-11-03 2016-12-13 Merck Sharp & Dohme Derivados de quinolina carboxamida y quinolina carbonitrilo como moduladores alostericos negativos de mglur2, composiciones y su uso.
CN103694236B (zh) * 2013-01-15 2017-05-31 苏州开拓药业股份有限公司 一种嘧啶骨架具有刺猬通路拮抗剂活性的抗肿瘤化合物
UY35419A (es) * 2013-03-14 2014-10-31 Abbvie Inc Inhibidores de cdk9 quinasa de pirrolo (2,3- b) piridina

Also Published As

Publication number Publication date
JP2017509707A (ja) 2017-04-06
AU2015237050B2 (en) 2019-05-09
KR101910724B1 (ko) 2018-10-22
BR112016021730B1 (pt) 2022-09-06
MX370438B (es) 2019-12-13
WO2015144001A1 (zh) 2015-10-01
IL247970A0 (en) 2016-12-01
TW201623242A (zh) 2016-07-01
AU2015237050A8 (en) 2016-10-27
JP6377245B2 (ja) 2018-08-22
BR112016021730A2 (es) 2017-08-15
NZ724691A (en) 2018-02-23
MX2016012470A (es) 2017-05-23
RU2016141129A (ru) 2018-04-28
RU2695815C2 (ru) 2019-07-29
CN106458974B (zh) 2019-07-16
CA2943100C (en) 2017-04-04
AU2015237050A1 (en) 2016-10-20
US9938292B2 (en) 2018-04-10
KR20160127159A (ko) 2016-11-02
RU2695815C9 (ru) 2019-10-28
ECSP16083602A (es) 2017-01-31
IL247970A (en) 2017-07-31
US20170174703A1 (en) 2017-06-22
CA2943100A1 (en) 2015-10-01
CL2016002394A1 (es) 2018-05-04
EP3124482A4 (en) 2017-03-22
SG11201607973XA (en) 2016-11-29
RU2016141129A3 (es) 2018-04-28
EP3124482A1 (en) 2017-02-01
CN106458974A (zh) 2017-02-22
EP3124482B1 (en) 2019-09-11

Similar Documents

Publication Publication Date Title
ECSP16076566A (es) Compuestos de heteroarilo o arilo biciclicos fusionados y su aplicación a inhibidores de irak4
PH12016502382A1 (en) Substituted indazole compounds as irak4 inhibitors
MX2020001757A (es) Compuestos, sales de los mismos y metodos para el tratamiento de enfermedades.
MX2018002402A (es) Compuestos de heteroarilo o arilo biciclicos fusionados como moduladores de la quinasa 4 asociada al receptor de la interleucina 1 (irak4).
EA201890594A1 (ru) Арильные, гетероарильные и гетероциклические соединения для лечения заболеваний
PE20170695A1 (es) Compuestos de indol carboxamida utiles como inhibidores de cinasas
MX2017002670A (es) Inhibidores de glucosidasa.
EA201792205A1 (ru) Гетероциклические соединения как ингибиторы lsd1
EA201691579A1 (ru) Производные сульфамоилпирроламида и их применение в качестве медикаментов для лечения гепатита b
CU24419B1 (es) 2-(morfolin-4-il)-1,7-naftiridinas útiles en el tratamiento o la profilaxis de enfermedades hiperproliferativas
UY35617A (es) Inhibidores de la fosfatidilinositol 3-quinasa
EA201592200A1 (ru) Производные сульфамоилпирроламида и их применение в качестве медикаментов для лечения гепатита b
MX376271B (es) Compuestos heterocíclicos y usos de los mismos.
MX2016011035A (es) Compuestos arilo, heteroarilo y heterociclicos para el tratamiento de trastornos mediados por complemento.
PE20160200A1 (es) Inhibidores de bromodominios
MX374513B (es) Compuestos de morfolinona de ácido heteroarilo como inhibidores mdm2 para el tratamiento de cáncer.
CR20150472A (es) USO DE DERIVADOS DE PIRAZOLOPIRIMIDINA PARA EL TRATAMIENTO DE TRANSTORNOS RELACIONADOS CON LA PI3Kd
PE20160862A1 (es) Polimorfo de los inhibidores de la syk
UY35675A (es) Derivados sustituidos de quinazolin-4-ona
GEP20196942B (en) Heterocyclic compounds and their use as retinoidrelated orphan receptor (ror) gamma-t inhibitors
AR103680A1 (es) Inhibidores selectivos de bace1
UY35551A (es) Derivados heteroarilos como inhibidores de aldosterona sintasa
CO2019001181A2 (es) Compuestos de heteroarilcarboxamida como inhibidores de ripk2
MX2015009479A (es) Compuestos y metodos para tratar infecciones bacterianas.
UY36228A (es) Derivados de heteroarilo como inhibidores de aldosterona sintasa (cyp11b2) y composiciones farmacéuticas que los contienen