KR102416358B1 - 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체 - Google Patents

암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체 Download PDF

Info

Publication number
KR102416358B1
KR102416358B1 KR1020167028920A KR20167028920A KR102416358B1 KR 102416358 B1 KR102416358 B1 KR 102416358B1 KR 1020167028920 A KR1020167028920 A KR 1020167028920A KR 20167028920 A KR20167028920 A KR 20167028920A KR 102416358 B1 KR102416358 B1 KR 102416358B1
Authority
KR
South Korea
Prior art keywords
delete delete
certain embodiments
compound
substituents
optionally substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
KR1020167028920A
Other languages
English (en)
Korean (ko)
Other versions
KR20170004968A (ko
Inventor
윈 롱
Original Assignee
카펠라 테라퓨틱스, 인크.
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=52997514&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR102416358(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 카펠라 테라퓨틱스, 인크. filed Critical 카펠라 테라퓨틱스, 인크.
Priority to KR1020227022282A priority Critical patent/KR102663309B1/ko
Publication of KR20170004968A publication Critical patent/KR20170004968A/ko
Application granted granted Critical
Publication of KR102416358B1 publication Critical patent/KR102416358B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/04—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with only hydrogen atoms, halogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon 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
    • C07D401/14—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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D405/14—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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
KR1020167028920A 2014-03-20 2015-03-19 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체 Active KR102416358B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020227022282A KR102663309B1 (ko) 2014-03-20 2015-03-19 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461968225P 2014-03-20 2014-03-20
US61/968,225 2014-03-20
PCT/US2015/021455 WO2015143148A1 (en) 2014-03-20 2015-03-19 Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020227022282A Division KR102663309B1 (ko) 2014-03-20 2015-03-19 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체

Publications (2)

Publication Number Publication Date
KR20170004968A KR20170004968A (ko) 2017-01-11
KR102416358B1 true KR102416358B1 (ko) 2022-07-07

Family

ID=52997514

Family Applications (3)

Application Number Title Priority Date Filing Date
KR1020167028920A Active KR102416358B1 (ko) 2014-03-20 2015-03-19 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체
KR1020227022282A Active KR102663309B1 (ko) 2014-03-20 2015-03-19 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체
KR1020247014448A Pending KR20240064750A (ko) 2014-03-20 2015-03-19 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체

Family Applications After (2)

Application Number Title Priority Date Filing Date
KR1020227022282A Active KR102663309B1 (ko) 2014-03-20 2015-03-19 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체
KR1020247014448A Pending KR20240064750A (ko) 2014-03-20 2015-03-19 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체

Country Status (16)

Country Link
US (4) US10005765B2 (enExample)
EP (2) EP3922630A1 (enExample)
JP (3) JP6577012B2 (enExample)
KR (3) KR102416358B1 (enExample)
CN (3) CN114989140B (enExample)
AU (1) AU2015231202B9 (enExample)
CA (2) CA3175724C (enExample)
DK (1) DK3119762T3 (enExample)
ES (1) ES2891734T3 (enExample)
IL (3) IL291000B2 (enExample)
MX (2) MX377384B (enExample)
PT (1) PT3119762T (enExample)
RU (2) RU2021101430A (enExample)
SG (1) SG11201607706SA (enExample)
TW (2) TWI807150B (enExample)
WO (1) WO2015143148A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220100081A (ko) * 2014-03-20 2022-07-14 카펠라 테라퓨틱스, 인크. 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
AU2015231215B2 (en) 2014-03-20 2019-07-18 Capella Therapeutics, Inc. Benzimidazole derivatives as ERBB tyrosine kinase inhibitors for the treatment of cancer
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
JP2018513853A (ja) 2015-04-10 2018-05-31 アラクセス ファーマ エルエルシー 置換キナゾリン化合物およびその使用方法
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
EP4353311A3 (en) 2015-07-20 2024-07-17 The Brigham and Women's Hospital, Inc. Shear-thinning compositions as an intravascular embolic agent
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10590108B2 (en) 2015-09-23 2020-03-17 Capella Therapeutics, Inc. Benzimidazoles for use in the treatment of cancer and inflammatory diseases
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356339A1 (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
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
CA3005089A1 (en) 2015-11-16 2017-05-26 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
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
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140600A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused hetero-hetero bicyclic compounds and methods of use thereof
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 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
US10736897B2 (en) 2017-05-25 2020-08-11 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
BR112019024674A2 (pt) 2017-05-25 2020-06-16 Araxes Pharma Llc Inibidores covalentes da kras
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
EP3755694B1 (en) * 2018-02-21 2023-04-05 Boehringer Ingelheim International GmbH New benzimidazole compounds and derivatives as egfr inhibitors
CN108191861B (zh) * 2018-03-01 2020-10-02 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-反式-2,4-戊二烯酰胺
JP2021532157A (ja) 2018-08-01 2021-11-25 アラクセス ファーマ エルエルシー がんを処置するための複素環式スピロ化合物およびその使用方法
CA3112043A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
CN111747950B (zh) * 2019-03-29 2024-01-23 深圳福沃药业有限公司 用于治疗癌症的嘧啶衍生物
CN114007698B (zh) 2019-06-24 2024-01-09 勃林格殷格翰国际有限公司 作为egfr抑制剂的大环化合物和衍生物
CA3195035A1 (en) * 2020-10-12 2022-04-21 Dana Farber Cancer Institute, Inc. Covalent egfr inhibitors and methods of use thereof
EP4237423B1 (en) 2020-11-02 2024-12-11 Boehringer Ingelheim International GmbH Substituted 1h-pyrazolo[4,3-c]pyridines and derivatives as egfr inhibitors
WO2022117051A1 (zh) * 2020-12-03 2022-06-09 北京鞍石生物科技有限责任公司 大环化合物及其制备方法和应用
EP4572754A1 (en) 2022-08-15 2025-06-25 Nalo Therapeutics, Inc. N-(1-((r)-1-acryloylazepan-3-yl)-7-chloro-6-(((r)-tetrahydrofuran-3-yl)oxy)-1h-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (nx-019) for use in the treatment of egfr mutant cancer
WO2025175145A1 (en) 2024-02-14 2025-08-21 Nalo Therapeutics, Inc. N-(1-((r)-1-acryloylazepan-3-yl)-7-chloro-6-(((r)-tetrahydrofuran-3-yl)oxy)-1h-b enzo[d]imidazol-2-yl)-2-methylisonicotinamide (nx-019) for use in the treatment of egfr mutant cancer

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013184766A1 (en) * 2012-06-06 2013-12-12 Irm Llc Compounds and compositions for modulating egfr activity
WO2013184757A1 (en) * 2012-06-06 2013-12-12 Irm Llc Compounds and compositions for modulating egfr activity
WO2014036016A1 (en) * 2012-08-31 2014-03-06 Principia Biopharma Inc. Benzimidazole derivatives as itk inhibitors

Family Cites Families (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
US4328245A (en) 1981-02-13 1982-05-04 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4410545A (en) 1981-02-13 1983-10-18 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4409239A (en) 1982-01-21 1983-10-11 Syntex (U.S.A.) Inc. Propylene glycol diester solutions of PGE-type compounds
HU196714B (en) 1984-10-04 1989-01-30 Monsanto Co Process for producing non-aqueous composition comprising somatotropin
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
US5612059A (en) 1988-08-30 1997-03-18 Pfizer Inc. Use of asymmetric membranes in delivery devices
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
PH30995A (en) 1989-07-07 1997-12-23 Novartis Inc Sustained release formulations of water soluble peptides.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5585112A (en) 1989-12-22 1996-12-17 Imarx Pharmaceutical Corp. Method of preparing gas and gaseous precursor-filled microspheres
IT1246382B (it) 1990-04-17 1994-11-18 Eurand Int Metodo per la cessione mirata e controllata di farmaci nell'intestino e particolarmente nel colon
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
US5543390A (en) 1990-11-01 1996-08-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University Covalent microparticle-drug conjugates for biological targeting
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
TW333456B (en) 1992-12-07 1998-06-11 Takeda Pharm Ind Co Ltd A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide.
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
US6274552B1 (en) 1993-03-18 2001-08-14 Cytimmune Sciences, Inc. Composition and method for delivery of biologically-active factors
US5985307A (en) 1993-04-14 1999-11-16 Emory University Device and method for non-occlusive localized drug delivery
US5523092A (en) 1993-04-14 1996-06-04 Emory University Device for local drug delivery and methods for using the same
US6087324A (en) 1993-06-24 2000-07-11 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6004534A (en) 1993-07-23 1999-12-21 Massachusetts Institute Of Technology Targeted polymerized liposomes for improved drug delivery
US5958458A (en) 1994-06-15 1999-09-28 Dumex-Alpharma A/S Pharmaceutical multiple unit particulate formulation in the form of coated cores
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
US5759542A (en) 1994-08-05 1998-06-02 New England Deaconess Hospital Corporation Compositions and methods for the delivery of drugs by platelets for the treatment of cardiovascular and other diseases
US5660854A (en) 1994-11-28 1997-08-26 Haynes; Duncan H Drug releasing surgical implant or dressing material
US6316652B1 (en) 1995-06-06 2001-11-13 Kosta Steliou Drug mitochondrial targeting agents
US5798119A (en) 1995-06-13 1998-08-25 S. C. Johnson & Son, Inc. Osmotic-delivery devices having vapor-permeable coatings
EP0835101B1 (en) 1995-06-27 2004-06-09 Takeda Chemical Industries, Ltd. Method of producing sustained-release preparation
TW448055B (en) 1995-09-04 2001-08-01 Takeda Chemical Industries Ltd Method of production of sustained-release preparation
JP2909418B2 (ja) 1995-09-18 1999-06-23 株式会社資生堂 薬物の遅延放出型マイクロスフイア
US6039975A (en) 1995-10-17 2000-03-21 Hoffman-La Roche Inc. Colon targeted delivery system
US5980945A (en) 1996-01-16 1999-11-09 Societe De Conseils De Recherches Et D'applications Scientifique S.A. Sustained release drug formulations
TW345603B (en) 1996-05-29 1998-11-21 Gmundner Fertigteile Gmbh A noise control device for tracks
US6264970B1 (en) 1996-06-26 2001-07-24 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6419961B1 (en) 1996-08-29 2002-07-16 Takeda Chemical Industries, Ltd. Sustained release microcapsules of a bioactive substance and a biodegradable polymer
US6139865A (en) 1996-10-01 2000-10-31 Eurand America, Inc. Taste-masked microcapsule compositions and methods of manufacture
US6375987B1 (en) 1996-10-01 2002-04-23 Gattefossé, S.A. Process for the manufacture of pharmaceutical composition with modified release of active principle comprising the matrix
CA2217134A1 (en) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Sustained release formulation
EP0839525B1 (en) 1996-10-31 2004-08-04 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6131570A (en) 1998-06-30 2000-10-17 Aradigm Corporation Temperature controlling device for aerosol drug delivery
DE19648576C2 (de) 1996-11-23 1999-08-12 Lohmann Therapie Syst Lts Lutschtablette zur modifizierten Freisetzung von Wirkstoffen im Gastrointestinaltrakt
EP0946169B1 (en) 1996-12-20 2003-02-26 Takeda Chemical Industries, Ltd. Method of producing a sustained-release preparation
US5891474A (en) 1997-01-29 1999-04-06 Poli Industria Chimica, S.P.A. Time-specific controlled release dosage formulations and method of preparing same
US6120751A (en) 1997-03-21 2000-09-19 Imarx Pharmaceutical Corp. Charged lipids and uses for the same
US6060082A (en) 1997-04-18 2000-05-09 Massachusetts Institute Of Technology Polymerized liposomes targeted to M cells and useful for oral or mucosal drug delivery
US5990146A (en) 1997-08-20 1999-11-23 Warner-Lambert Company Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
US6350458B1 (en) 1998-02-10 2002-02-26 Generex Pharmaceuticals Incorporated Mixed micellar drug deliver system and method of preparation
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
US6048736A (en) 1998-04-29 2000-04-11 Kosak; Kenneth M. Cyclodextrin polymers for carrying and releasing drugs
KR19990085365A (ko) 1998-05-16 1999-12-06 허영섭 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법
US7169410B1 (en) 1998-05-19 2007-01-30 Sdg, Inc. Targeted liposomal drug delivery system
MA26659A1 (fr) 1998-08-06 2004-12-20 Pfizer Dérivés de benzimidazole nouveaux, compositions pharmaceutiques les contenant et procédé pour leur préparation.
AU770645B2 (en) 1998-11-02 2004-02-26 Alkermes Pharma Ireland Limited Multiparticulate modified release composition
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6271359B1 (en) 1999-04-14 2001-08-07 Musc Foundation For Research Development Tissue-specific and pathogen-specific toxic agents and ribozymes
AU770600B2 (en) * 1999-10-07 2004-02-26 Amgen, Inc. Triazine kinase inhibitors
US6623756B1 (en) 2000-04-27 2003-09-23 Noveon Ip Holdings Corp. Directly compressed solid dosage articles
EP1313473A2 (en) 2000-08-30 2003-05-28 Pfizer Products Inc. Sustained release formulations for growth hormone secretagogues
BR0205509A (pt) 2001-07-27 2003-06-24 Yamanouchi Pharma Co Ltd Composição compreendendo partìculas finas de liberação prolongada para comprimidos de rápida desintegração na cavidade bucal e método de fabricação da mesma
JP2005509604A (ja) 2001-09-28 2005-04-14 マクニール−ピーピーシー・インコーポレイテッド 菓子組成物を含む剤形
ATE511840T1 (de) 2001-10-09 2011-06-15 Amgen Inc Imidazolderivate als entzündungshemmende mittel
JP2005514386A (ja) 2001-12-19 2005-05-19 アストラゼネカ・アクチエボラーグ 新規フィルム・コーティング
US6958161B2 (en) 2002-04-12 2005-10-25 F H Faulding & Co Limited Modified release coated drug preparation
US7485322B2 (en) 2002-12-24 2009-02-03 Lek Pharmaceuticals D.D. Modified release pharmaceutical composition
US7427414B2 (en) 2006-01-18 2008-09-23 Astron Research Limited Modified release oral dosage form using co-polymer of polyvinyl acetate
CN101631779A (zh) * 2006-12-12 2010-01-20 先灵公司 含有三环系统的天冬氨酰蛋白酶抑制剂
CL2008003062A1 (es) * 2007-11-09 2010-02-19 Schering Corp Compuestos derivados de pirazoles espiro conjugados, inhibidores de la actividad de ksp kinesina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de enfermedades proliferativas.
EP2265270A1 (en) 2008-02-04 2010-12-29 OSI Pharmaceuticals, Inc. 2-aminopyridine kinase inhibitors
FR2952552B1 (fr) 2009-11-19 2012-01-13 Commissariat Energie Atomique Dispositif de recuperation de nanopoudres et de poudres ultrafines contenues dans un gaz
MX2012008049A (es) 2010-01-12 2012-08-01 Hoffmann La Roche Compuestos heterociclicos triciclicos, composiciones y metodos de uso de los mismos,.
WO2011099832A2 (en) 2010-02-12 2011-08-18 Crystalgenomics, Inc. Novel benzimidazole compound, preparation method thereof and pharmaceutical composition comprising the same
BR112013002879A2 (pt) 2010-08-05 2016-05-31 Amgen Inc compostos de benizmidazol e azabenzimidazol que inibem a quinase de linfoma anaplásico
US20150306086A1 (en) 2011-11-14 2015-10-29 Tesaro, Inc. Modulating certain tyrosine kinases
CA2854188A1 (en) 2011-11-14 2013-05-23 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitors with braf inhibitors
CA2871540A1 (en) 2012-05-10 2013-11-14 Synta Pharmaceuticals Corp. Treating cancer with hsp90 inhibitory compounds
WO2013186229A1 (en) 2012-06-11 2013-12-19 Ucb Pharma S.A. Tnf -alpha modulating benzimidazoles
WO2014001464A1 (en) 2012-06-27 2014-01-03 4Sc Discovery Gmbh Bifluorodioxalane-amino-benzimidazole kinase inhibitors for the treatment of cancer, autoimmuneinflammation and cns disorders
WO2015134210A1 (en) 2014-03-03 2015-09-11 Principia Biopharma, Inc. BENZIMIDAZOLE DERIVATIVES AS RLK and ITK INHIBITORS
ES2891734T3 (es) 2014-03-20 2022-01-31 Capella Therapeutics Inc Derivados de bencimidazol como inhibidores de tirosina quinasa ERBB para el tratamiento del cáncer
AU2015231215B2 (en) 2014-03-20 2019-07-18 Capella Therapeutics, Inc. Benzimidazole derivatives as ERBB tyrosine kinase inhibitors for the treatment of cancer
CN104447765A (zh) 2014-12-31 2015-03-25 深圳铂立健医药有限公司 三环化合物及其药物组合物和应用
WO2016126819A1 (en) 2015-02-03 2016-08-11 Dolby Laboratories Licensing Corporation Optimized virtual scene layout for spatial meeting playback
US10590108B2 (en) 2015-09-23 2020-03-17 Capella Therapeutics, Inc. Benzimidazoles for use in the treatment of cancer and inflammatory diseases

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013184766A1 (en) * 2012-06-06 2013-12-12 Irm Llc Compounds and compositions for modulating egfr activity
WO2013184757A1 (en) * 2012-06-06 2013-12-12 Irm Llc Compounds and compositions for modulating egfr activity
WO2014036016A1 (en) * 2012-08-31 2014-03-06 Principia Biopharma Inc. Benzimidazole derivatives as itk inhibitors

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220100081A (ko) * 2014-03-20 2022-07-14 카펠라 테라퓨틱스, 인크. 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체
US11787788B2 (en) 2014-03-20 2023-10-17 Capella Therapeutics, Inc. Benzimidazole derivatives, and pharmaceutical compositions and methods of use thereof
KR102663309B1 (ko) * 2014-03-20 2024-05-03 카펠라 테라퓨틱스, 인크. 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체

Also Published As

Publication number Publication date
NZ724372A (en) 2021-06-25
EP3119762B1 (en) 2021-05-26
EP3119762B9 (en) 2021-10-20
CN114940673B (zh) 2025-03-18
MX2020012165A (es) 2021-01-29
US20170183330A1 (en) 2017-06-29
JP2017512833A (ja) 2017-05-25
RU2021101430A (ru) 2021-03-16
IL247852B (en) 2021-04-29
PT3119762T (pt) 2021-08-31
JP7073316B2 (ja) 2022-05-23
KR102663309B1 (ko) 2024-05-03
KR20170004968A (ko) 2017-01-11
MX2016012097A (es) 2017-04-27
MX377384B (es) 2025-03-10
CA2943220A1 (en) 2015-09-24
RU2016141052A3 (enExample) 2018-10-30
SG11201607706SA (en) 2016-10-28
US11787788B2 (en) 2023-10-17
US20180291012A1 (en) 2018-10-11
CN114940673A (zh) 2022-08-26
ES2891734T3 (es) 2022-01-31
US10647707B2 (en) 2020-05-12
CA3175724C (en) 2024-01-09
IL282651B (en) 2022-04-01
CA3175724A1 (en) 2015-09-24
AU2015231202B2 (en) 2019-08-22
EP3922630A1 (en) 2021-12-15
AU2015231202A1 (en) 2016-10-06
CN106536506A (zh) 2017-03-22
US20200291007A1 (en) 2020-09-17
TWI683813B (zh) 2020-02-01
IL291000B2 (en) 2024-04-01
KR20220100081A (ko) 2022-07-14
TW202028189A (zh) 2020-08-01
JP2020007327A (ja) 2020-01-16
IL282651A (en) 2021-06-30
DK3119762T3 (da) 2021-08-30
TWI807150B (zh) 2023-07-01
CN114989140B (zh) 2025-03-25
RU2741914C2 (ru) 2021-01-29
AU2015231202B9 (en) 2019-10-24
CN114989140A (zh) 2022-09-02
IL291000A (en) 2022-05-01
JP7394168B2 (ja) 2023-12-07
JP2022106967A (ja) 2022-07-20
JP6577012B2 (ja) 2019-09-18
US20250092028A1 (en) 2025-03-20
CA2943220C (en) 2024-01-16
TW201620896A (zh) 2016-06-16
IL291000B1 (en) 2023-12-01
US10005765B2 (en) 2018-06-26
RU2016141052A (ru) 2018-04-26
WO2015143148A1 (en) 2015-09-24
IL247852A0 (en) 2016-11-30
KR20240064750A (ko) 2024-05-13
EP3119762A1 (en) 2017-01-25

Similar Documents

Publication Publication Date Title
KR102416358B1 (ko) 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체
US11427565B2 (en) Benzimidazoles for use in the treatment of cancer and inflammatory diseases
KR102409739B1 (ko) 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체
HK40056179A (en) Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer
HK1233259B (en) Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20161018

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20200318

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20210826

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20220328

PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20220629

PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20220629

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20220630

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20250407

Start annual number: 4

End annual number: 4