JO3776B1 - التركيبات الصيدلانية لمثبط CDK4 / 6 ومثبط B-Raf - Google Patents

التركيبات الصيدلانية لمثبط CDK4 / 6 ومثبط B-Raf

Info

Publication number
JO3776B1
JO3776B1 JOP/2013/0223A JOP20130223A JO3776B1 JO 3776 B1 JO3776 B1 JO 3776B1 JO P20130223 A JOP20130223 A JO P20130223A JO 3776 B1 JO3776 B1 JO 3776B1
Authority
JO
Jordan
Prior art keywords
inhibitor
cdk4
raf
pharmaceutical combinations
combination
Prior art date
Application number
JOP/2013/0223A
Other languages
English (en)
Inventor
Loo Alice
Stuart Darrin
Delach Scott
Kim Sunkyu
Caponigro Giordano
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Application granted granted Critical
Publication of JO3776B1 publication Critical patent/JO3776B1/ar

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    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—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
    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

<strong><span dir="RTL">توليفة صيدلية تشتمل على (أ) مثبط </span>CDK4/6<span dir="RTL"> (ب) مثبط </span>B-Raf<span dir="RTL">، واختيارياً (ج) مثبط </span>MEK 1/2<span dir="RTL">؛ تحضيرات مشتركة وتركيبات صيدلية منها؛ استخدامات هذه التوليفة فى معالجة الأمراض التكاثرية؛ وطرق علاج مريض يعانى من مرض تكاثرى تشتمل على وصف كمية فعالة علاجياً من هذه التوليفة.</span></strong>
JOP/2013/0223A 2012-07-26 2013-07-25 التركيبات الصيدلانية لمثبط CDK4 / 6 ومثبط B-Raf JO3776B1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261676134P 2012-07-26 2012-07-26
US201361830911P 2013-06-04 2013-06-04

Publications (1)

Publication Number Publication Date
JO3776B1 true JO3776B1 (ar) 2021-01-31

Family

ID=48917729

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Application Number Title Priority Date Filing Date
JOP/2013/0223A JO3776B1 (ar) 2012-07-26 2013-07-25 التركيبات الصيدلانية لمثبط CDK4 / 6 ومثبط B-Raf

Country Status (15)

Country Link
US (1) US9700557B2 (ar)
EP (1) EP2877174B1 (ar)
JP (1) JP6320379B2 (ar)
KR (1) KR102113363B1 (ar)
CN (1) CN104507474B (ar)
AR (1) AR091876A1 (ar)
AU (1) AU2013295771B2 (ar)
CA (1) CA2874860C (ar)
ES (1) ES2778059T3 (ar)
IN (1) IN2015DN00376A (ar)
JO (1) JO3776B1 (ar)
MX (1) MX360045B (ar)
RU (1) RU2685250C2 (ar)
TW (1) TWI599357B (ar)
WO (1) WO2014018725A1 (ar)

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EP3327144B1 (en) * 2013-02-25 2020-03-25 Novartis AG Novel androgen receptor mutation
DK2976106T3 (da) * 2013-03-21 2021-06-14 Array Biopharma Inc Kombinationsterapi, som omfatter en b-raf-hæmmer og en anden hæmmer
WO2016106357A1 (en) * 2014-12-23 2016-06-30 Millennnium Pharmaceuticals, Inc. Combination of raf inhibitors and aurora kinase inhibitors
WO2016155670A1 (zh) * 2015-04-01 2016-10-06 苏州晶云药物科技有限公司 一种cdk抑制剂和mek抑制剂的共晶及其制备方法
CN105753869B (zh) * 2015-04-01 2018-09-25 苏州晶云药物科技有限公司 一种cdk抑制剂和mek抑制剂的共晶及其制备方法
CN108135905A (zh) * 2015-08-28 2018-06-08 诺华股份有限公司 用于治疗癌症的cdk4/6抑制剂lee011、mek1/2抑制剂曲美替尼以及可任选还包括pi3k抑制剂byl719的组合
CN105732642B (zh) * 2015-11-18 2018-09-25 苏州晶云药物科技有限公司 一种cdk抑制剂和mek抑制剂的共晶及其制备方法
BR112018074941A2 (pt) * 2016-06-03 2019-03-12 Caponigro Giordano combinações farmacêuticas
US20190175598A1 (en) * 2016-08-23 2019-06-13 Eisai R&D Management Co., Ltd. Combination therapies for the treatment of hepatocellular carcinoma
EP3515446B1 (en) 2016-09-19 2023-12-20 Novartis AG Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
WO2018081211A1 (en) * 2016-10-26 2018-05-03 Li George Y Deuterated 7-cyclopentyl-n, n-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7h-pyrrolo[2,3-d]pyrimdine-6-carboxamide
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
US11266653B2 (en) 2017-05-02 2022-03-08 Novartis Ag Combination therapy
WO2018218633A1 (en) 2017-06-02 2018-12-06 Beijing Percans Oncology Co. Ltd. Combination therapies for treating cancers
SG11202005937QA (en) 2018-01-08 2020-07-29 G1 Therapeutics Inc G1t38 superior dosage regimes
KR20200131246A (ko) 2018-02-15 2020-11-23 누베이션 바이오 인크. 키나제 억제제로서의 헤테로시클릭 화합물
WO2019195959A1 (en) * 2018-04-08 2019-10-17 Cothera Biosciences, Inc. Combination therapy for cancers with braf mutation
US11633401B2 (en) 2018-07-06 2023-04-25 Memorial Sloan Kettering Cancer Center Combination therapy with MEK inhibitor and CDK4/6 inhibitor to treat pancreatic cancer
CN113453671A (zh) * 2018-12-20 2021-09-28 诺华股份有限公司 用于治疗癌症的Raf抑制剂和CDK4/6抑制剂的组合疗法
ES3025633T3 (en) 2019-05-13 2025-06-09 Novartis Ag New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
WO2021047573A1 (zh) * 2019-09-11 2021-03-18 江苏恒瑞医药股份有限公司 一种mek抑制剂与cdk4/6抑制剂联合在制备治疗肿瘤的药物中的用途
FI4073065T3 (fi) 2019-12-10 2025-04-16 Hoffmann La Roche Uusia metyylikinatsolinonijohdannaisia
WO2021229439A1 (en) * 2020-05-12 2021-11-18 Novartis Ag Therapeutic combinations comprising a craf inhibitor
CA3257280A1 (en) 2022-05-25 2023-11-30 Msd International Gmbh COMBINATION OF A BRAF INHIBITOR, AN EGFR INHIBITOR AND A PD-1 ANTAGONIST FOR THE TREATMENT OF COLORECTAL CANCER MSI-H/DMMR, WITH BRAF V600E MUTATION
WO2025003956A1 (en) 2023-06-30 2025-01-02 Pfizer Inc. High drug loading formulations of encorafenib

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EA019094B1 (ru) 2008-08-22 2014-01-30 Новартис Аг Пирролопиримидины и их применение
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Also Published As

Publication number Publication date
IN2015DN00376A (ar) 2015-06-12
TWI599357B (zh) 2017-09-21
EP2877174B1 (en) 2020-01-01
WO2014018725A1 (en) 2014-01-30
HK1210721A1 (en) 2016-05-06
MX360045B (es) 2018-10-19
CN104507474A (zh) 2015-04-08
KR20150036146A (ko) 2015-04-07
RU2015106524A (ru) 2016-09-20
BR112014033118A8 (pt) 2023-01-31
CA2874860A1 (en) 2014-01-30
BR112014033118A2 (pt) 2017-06-27
KR102113363B1 (ko) 2020-05-21
CN104507474B (zh) 2018-01-02
AU2013295771A1 (en) 2014-12-11
JP6320379B2 (ja) 2018-05-09
ES2778059T3 (es) 2020-08-07
CA2874860C (en) 2020-06-23
JP2015523397A (ja) 2015-08-13
MX2015001122A (es) 2015-04-08
AU2013295771B2 (en) 2016-08-11
AR091876A1 (es) 2015-03-04
EP2877174A1 (en) 2015-06-03
US9700557B2 (en) 2017-07-11
TW201412316A (zh) 2014-04-01
US20150164897A1 (en) 2015-06-18
RU2685250C2 (ru) 2019-04-17

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