[go: up one dir, main page]

PE20181144A1 - Derivados de heteroarilo como inhibidores de parp - Google Patents

Derivados de heteroarilo como inhibidores de parp

Info

Publication number
PE20181144A1
PE20181144A1 PE2018000206A PE2018000206A PE20181144A1 PE 20181144 A1 PE20181144 A1 PE 20181144A1 PE 2018000206 A PE2018000206 A PE 2018000206A PE 2018000206 A PE2018000206 A PE 2018000206A PE 20181144 A1 PE20181144 A1 PE 20181144A1
Authority
PE
Peru
Prior art keywords
halogen
independently selected
oxo
nitro
compounds
Prior art date
Application number
PE2018000206A
Other languages
English (en)
Inventor
Navnath Popat Karche
Ajay Ramchandra Tilekar
Sanjay Pralhad Kurhade
Ganesh Rajaram Jadhav
Nishant Ramniwasji Gupta
Neelima Sinha
Venkata P Palle
Rajender Kumar Kamboj
Original Assignee
Lupin 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
Application filed by Lupin Ltd filed Critical Lupin Ltd
Publication of PE20181144A1 publication Critical patent/PE20181144A1/es

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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/255—Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
    • 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/498—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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se refiere a compuestos de formula general (I), donde las rayas discontinuas son un enlace sencillo o doble; X e Y son independientemente C o N; el anillo Ar es seleccionado de a) un anillo heteroaromatico de 6 miembros que contiene de 1 a 2 atomos de N, siendo X e Y carbono y b) un anillo heteroaromatico de 5 miembros que contiene de 1 a 2 heteroatomos seleccionados de N, O y S, en el que tanto X como Y no se seleccionan como N al mismo tiempo; R1 es seleccionado independientemente de halogeno, nitro, ciano, entre otros; R2 es H, halogeno, nitro, entre otros; R3 es seleccionado independientemente de halogeno y alquilo sustituido o no sustituido, entre otros; R4 es seleccionado independientemente como alquilo sustituido o no sustituido, o dos R4 en el mismo carbono forman un oxo (=o), entre otros; el anillo B es cicloalquilo, heterociclilo, entre otros; R5 se selecciona independientemente de halogeno, nitro, entre otros; p es seleccionado de 0, 1 y 2; q, r, s se seleccionan de 0, 1, 2 y 3. Tambien se refiere a composiciones farmaceuticas que comprenden el compuesto de formula (I), su tautomero, estereoisomero o sal del mismo. Son compuestos preferidos: (R)-4-(4-(3-(5-oxo-5,6-dihidro-1,6-naftiridin-7-il)ciclopent-2-en-1-il)piperazin-1-il)benzonitrilo, (R)-4-(4-(3-(3-fluoro-5-oxo-5,6-dihidro-1,6-naftiridin-7-il)ciclopent-2-en-1-il)piperazin-1-il)benzonitrilo, entre otros. Dichos compuestos son inhibidores de la poli(ADP-ribosa)polimerasa (PARP) y son utiles en el tratamiento o prevencion de enfermedades o trastornos cancerigenos tales como cancer de higado, melanoma, entre otros
PE2018000206A 2015-08-17 2016-08-13 Derivados de heteroarilo como inhibidores de parp PE20181144A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN3111MU2015 2015-08-17
IN3588MU2015 2015-09-21
IN201621000832 2016-01-08

Publications (1)

Publication Number Publication Date
PE20181144A1 true PE20181144A1 (es) 2018-07-17

Family

ID=56920883

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018000206A PE20181144A1 (es) 2015-08-17 2016-08-13 Derivados de heteroarilo como inhibidores de parp

Country Status (21)

Country Link
US (1) US20200101068A1 (es)
EP (1) EP3337802A1 (es)
JP (1) JP2018523679A (es)
KR (1) KR20180037265A (es)
CN (1) CN107922409A (es)
AU (1) AU2016308717A1 (es)
BR (1) BR112018002465A2 (es)
CA (1) CA2991232A1 (es)
CL (1) CL2018000338A1 (es)
CO (1) CO2018001268A2 (es)
CR (1) CR20180168A (es)
CU (1) CU20180019A7 (es)
EA (1) EA033613B1 (es)
HK (1) HK1255269A1 (es)
IL (1) IL256808A (es)
MA (1) MA42659A (es)
MX (1) MX2018001871A (es)
PE (1) PE20181144A1 (es)
PH (1) PH12018500360A1 (es)
SV (1) SV2018005633A (es)
WO (1) WO2017029601A1 (es)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3009196C (en) 2016-01-08 2022-05-31 Arcus Biosciences, Inc. Modulators of 5'-nucleotidase, ecto and the use thereof
HUE058355T2 (hu) 2016-12-08 2022-07-28 Hoffmann La Roche Új izoxazolil-éter származékok, mint a gaba a alfa5 pam
US10737259B2 (en) 2018-08-31 2020-08-11 Pall Corporation Salt tolerant anion exchange medium
US11045773B2 (en) 2018-08-31 2021-06-29 Pall Corporation Salt tolerant porous medium
BR112021024131A2 (pt) * 2019-05-31 2022-01-11 Haisco Pharmaceuticals Pte Ltd Derivado de anel inibidor de btk, método de preparação para o mesmo e aplicação farmacêutica do mesmo
US11633416B1 (en) 2020-03-06 2023-04-25 Arcus Biosciences, Inc. Oral formulations of CD73 compounds
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
IL299612A (en) 2020-07-02 2023-03-01 Incyte Corp Tricyclic urea compounds as JAK2 V617F inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
CN112062770A (zh) * 2020-08-21 2020-12-11 台州学院 一种稠环二氢吡啶酮的制备方法
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
US11958861B2 (en) 2021-02-25 2024-04-16 Incyte Corporation Spirocyclic lactams as JAK2 V617F inhibitors
WO2022222964A1 (zh) * 2021-04-23 2022-10-27 成都百裕制药股份有限公司 吡啶衍生物及其在医药上的应用
PE20241129A1 (es) * 2021-10-01 2024-05-24 Xinthera Inc Inhibidores de parp1 de azetidina y pirrolidina y usos de estos
CN118804916B (zh) 2022-01-21 2025-04-01 新特拉有限公司 Parp1抑制剂及其用途
KR20240149429A (ko) * 2022-02-16 2024-10-14 듀크 스트리트 바이오 리미티드 약학적 화합물
EP4493558A1 (en) 2022-03-17 2025-01-22 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
IL316278A (en) 2022-04-28 2024-12-01 Xinthera Inc TRICYCLIC PARP1 INHIBITORS AND THEIR USES
WO2024050370A1 (en) * 2022-08-30 2024-03-07 1Cbio, Inc. Heterocyclic compounds and methods of use thereof
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
GB2630970A (en) * 2023-06-15 2024-12-18 Duke Street Bio Ltd PARP1 inhibitor compounds
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
GB2634233A (en) * 2023-10-02 2025-04-09 Duke Street Bio Ltd PARP1 inhibitor compounds
GB2634228A (en) * 2023-10-02 2025-04-09 Duke Street Bio Ltd PARP1 inhibitor compounds
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025091346A1 (en) * 2023-11-01 2025-05-08 Suzhou Eoc Medical Research Co., Ltd. Parp inhibitors and uses thereof
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
US5019369A (en) 1984-10-22 1991-05-28 Vestar, Inc. Method of targeting tumors in humans
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
RU2199534C2 (ru) 1997-10-14 2003-02-27 Мицубиси Фарма Корпорейшн СОЕДИНЕНИЕ ПИПЕРАЗИНА, ИНГИБИТОР ПРОДУЦИРОВАНИЯ TNF-α И /ИЛИ ПРОМОТОР ПРОДУЦИРОВАНИЯ IL-10 И СРЕДСТВО ДЛЯ ПРОФИЛАКТИКИ ИЛИ ЛЕЧЕНИЯ БОЛЕЗНЕЙ НА ЕГО ОСНОВЕ
KR100804564B1 (ko) 2000-10-30 2008-02-20 쿠도스 파마슈티칼스 리미티드 프탈라지논 유도체
EP1397350B1 (en) * 2001-05-08 2007-02-28 Kudos Pharmaceuticals Limited Isoquinolinone derivatives as parp inhibitors
EP1396488A1 (en) * 2001-05-23 2004-03-10 Mitsubishi Pharma Corporation Fused heterocyclic compound and medicinal use thereof
AUPR975601A0 (en) 2001-12-24 2002-01-31 Fujisawa Pharmaceutical Co., Ltd. Quinazolinone derivatives
AUPS019702A0 (en) 2002-01-29 2002-02-21 Fujisawa Pharmaceutical Co., Ltd. Condensed heterocyclic compounds
DE10313319A1 (de) 2003-03-25 2004-10-07 Basf Ag Verfahren zur Hydroformylierung
UY32277A (es) 2008-12-02 2010-05-31 Glaxo Group Ltd Derivados de n-{[1r,4s,6r)-3-(2-piridinilcarbonil)-3-azabiciclo[4.1.0-il}metil}-2heteroarilamina y uso de los mismos
US20120077814A1 (en) 2010-09-10 2012-03-29 Zhong Wang Sulfonamide, sulfamate, and sulfamothioate derivatives
US8883789B2 (en) 2011-12-14 2014-11-11 Boehringer Ingelheim International Gmbh Piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors
HUE030067T2 (en) 2012-03-28 2017-04-28 Merck Patent Gmbh Bicyclic pyrazinone derivatives
WO2014009872A1 (en) 2012-07-09 2014-01-16 Lupin Limited Tetrahydroquinazolinone derivatives as parp inhibitors
EP3160466A4 (en) 2014-06-25 2017-12-27 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2016012956A1 (en) 2014-07-24 2016-01-28 Lupin Limited Isoquinolinone derivatives as parp inhibitors

Also Published As

Publication number Publication date
IL256808A (en) 2018-03-29
CN107922409A (zh) 2018-04-17
CA2991232A1 (en) 2017-02-23
MA42659A (fr) 2018-06-27
JP2018523679A (ja) 2018-08-23
MX2018001871A (es) 2018-05-28
BR112018002465A2 (pt) 2018-09-18
WO2017029601A1 (en) 2017-02-23
EA201890473A1 (ru) 2018-07-31
PH12018500360A1 (en) 2018-08-29
CL2018000338A1 (es) 2018-07-20
CR20180168A (es) 2018-06-27
US20200101068A1 (en) 2020-04-02
AU2016308717A1 (en) 2018-01-25
CO2018001268A2 (es) 2018-06-20
EP3337802A1 (en) 2018-06-27
SV2018005633A (es) 2018-04-11
EA033613B1 (ru) 2019-11-08
HK1255269A1 (zh) 2019-08-09
KR20180037265A (ko) 2018-04-11
CU20180019A7 (es) 2018-06-05

Similar Documents

Publication Publication Date Title
PE20181144A1 (es) Derivados de heteroarilo como inhibidores de parp
CR20160548A (es) Nuevos Derivados de Pirazolo Pirimidina y su Uso como Inhibidores de MALT1
UY37795A (es) Sulfonilureas y sulfoniltioureas útiles como inhibidores de nlrp3
PE20212247A1 (es) Compuestos de 3-((3-aminofenil)amino)piperidina-2,6-diona sustituida, composiciones de estos y metodos de tratamiento con estos
EA201691428A1 (ru) Бициклические гетероциклические производные в качестве ингибиторов irak4
GEP20217248B (en) 2,4,5-trisubstituted 1,2,4-triazolones useful as inhibitors of dhodh
AR065015A1 (es) Derivados de antranilamida, composiciones farmaceuticas que los contienen, y usos para el tratamiento del cancer
WO2015200677A3 (en) Prmt5 inhibitors and uses thereof
MX2016016538A (es) Derivados de quinazolinona como inhibidores de fosfatidilinositol 3-cinasa.
MX2016016516A (es) Inhibidores de fosfatidilinositol 3-cinasa.
MX2016016530A (es) Inhibidores de fosfatidilinositol 3-quinasa.
PH12016501440A1 (en) Novel heterocyclic compounds
EA201691401A1 (ru) Индазольные соединения в качестве ингибиторов irak4
PE20190811A1 (es) Derivados de pirazolopirimidinas como inhibidor de quinasa
PE20190656A1 (es) Compuestos de tiazolo-piridina sustituida como inhibidores de malt1
JP2016536363A5 (es)
PE20190337A1 (es) NUEVOS DERIVADOS DE PIRROLO [2,3-d]PIRIMIDA, UN PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
MX2016016528A (es) Inhibidores de fosfatidilinositol 3-quinasa.
AR077935A1 (es) Derivados de 3-amino-5 fenil-5,6-dihidro-2h-(1,4)oxazina
EA202091120A2 (ru) Производные 2,4-тиазолинидона в лечении расстройств центральной нервной системы
PE20170946A1 (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
MX2018008095A (es) Compuestos heterociclicos triciclicos condensados como inhibidores de integrasa del vih.
NZ726638A (en) Phosphatidylinositol 3-kinase inhibitors
SA519401322B1 (ar) مركبات أريل كربوكساميد غير متجانسة كمثطبات لكيناز بروتين سيرين/ ثريونين متداخل مع المستقبل 2
EA201000101A1 (ru) Производные пиримидина 934