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

التركيبات الصيدلانية لمثبط CDK4 / 6 ومثبط B-Raf

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

Family Applications (1)

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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PE20151785A1 (es) 2013-03-21 2015-12-20 Novartis Ag Terapia de combinacion
JP2018502089A (ja) * 2014-12-23 2018-01-25 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Ｒａｆ阻害剤及びａｕｒｏｒａキナーゼ阻害剤の組み合わせ
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
EP3279201B1 (en) * 2015-04-01 2019-10-23 Crystal Pharmatech Co., Ltd. Cdk inhibitor, eutectic crystal of mek inhibitor, and preparation method therefor
WO2017037574A1 (en) * 2015-08-28 2017-03-09 Novartis Ag Combinations of the cdk4/6 inhibitor lee011 and the mek1/2 inhibitor trametinib, optionally further comprising the pi3k inhibitor byl719 to treat cancer
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
HUE060653T2 (hu) * 2016-06-03 2023-04-28 Array Biopharma Inc Gyógyászati kombinációk
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CN109715163B (zh) 2016-09-19 2022-11-22 诺华股份有限公司 包含raf抑制剂和erk抑制剂的治疗组合
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TWI798218B (zh) 2017-05-02 2023-04-11 瑞士商諾華公司 組合療法
WO2018218633A1 (en) 2017-06-02 2018-12-06 Beijing Percans Oncology Co. Ltd. Combination therapies for treating cancers
WO2019136451A1 (en) 2018-01-08 2019-07-11 G1 Therapeutics, Inc. G1t38 superior dosage regimes
JP2021514359A (ja) 2018-02-15 2021-06-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． キナーゼ阻害剤としての複素環式化合物
WO2019195959A1 (en) * 2018-04-08 2019-10-17 Cothera Biosciences, Inc. Combination therapy for cancers with braf mutation
WO2020010280A1 (en) * 2018-07-06 2020-01-09 Memorial Sloan Kettering Cancer Center Combination therapy with mek inhibitor and cdk4/6 inhibitor to treat pancreatic cancer
CA3123510A1 (en) * 2018-12-20 2020-06-25 Novartis Ag Combination therapy with a raf inhibitor and a cdk4/6 inhibitor for use in the treatment of cancer
EP4563150A3 (en) 2019-05-13 2025-07-23 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
TW202114667A (zh) * 2019-09-11 2021-04-16 大陸商江蘇恒瑞醫藥股份有限公司 Mek抑制劑與cdk4/6抑制劑聯合在製備治療腫瘤的藥物中的用途
EP4073065B1 (en) 2019-12-10 2025-02-19 F. Hoffmann-La Roche AG New methylquinazolinone derivatives
JP2023525100A (ja) * 2020-05-12 2023-06-14 ノバルティス アーゲー Ｃｒａｆ阻害剤を含む治療的組み合わせ
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
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WO2011130232A1 (en) 2010-04-13 2011-10-20 Novartis Ag Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor and an mtor inhibitor for treating cancer

Also Published As

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

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