RU2406503C2 - Дигидроптеридиноны, предназначенные для лечения раковых заболеваний - Google Patents

Дигидроптеридиноны, предназначенные для лечения раковых заболеваний Download PDF

Info

Publication number
RU2406503C2
RU2406503C2 RU2007109109/15A RU2007109109A RU2406503C2 RU 2406503 C2 RU2406503 C2 RU 2406503C2 RU 2007109109/15 A RU2007109109/15 A RU 2007109109/15A RU 2007109109 A RU2007109109 A RU 2007109109A RU 2406503 C2 RU2406503 C2 RU 2406503C2
Authority
RU
Russia
Prior art keywords
use according
disease
group
tumors
polo
Prior art date
Application number
RU2007109109/15A
Other languages
English (en)
Other versions
RU2007109109A (ru
Inventor
Герд МУНЦЕРТ (DE)
Герд Мунцерт
Мартин ШТЕГМАЙЕР (DE)
Мартин Штегмайер
Original Assignee
Берингер Ингельхайм Интернациональ Гмбх
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=34926179&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2406503(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Берингер Ингельхайм Интернациональ Гмбх filed Critical Берингер Ингельхайм Интернациональ Гмбх
Publication of RU2007109109A publication Critical patent/RU2007109109A/ru
Application granted granted Critical
Publication of RU2406503C2 publication Critical patent/RU2406503C2/ru

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
    • A61K31/495—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
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Изобретение относится к области фармакологии и медицины и касается применения соединений общей формулы (1) для лечения заболеваний, характеризующихся аномальной пролиферацией клеток в организме человека или млекопитающего, не являющегося человеком, путем ингибирования polo-подобных киназ, как регуляторов митоза. Изобретение предоставляет высокоактивные противоопухолевые средства. 7 з.п. ф-лы, 2 табл.

Description

Текст описания приведен в факсимильном виде.
Figure 00000001
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
Figure 00000039
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
Figure 00000045
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049
Figure 00000050
Figure 00000051
Figure 00000052
Figure 00000053
Figure 00000054
Figure 00000055
Figure 00000056
Figure 00000057
Figure 00000058
Figure 00000059
Figure 00000060
Figure 00000061
Figure 00000062
Figure 00000063
Figure 00000064
Figure 00000065
Figure 00000066
Figure 00000067
Figure 00000068
Figure 00000069
Figure 00000070
Figure 00000071
Figure 00000072
Figure 00000073
Figure 00000074
Figure 00000075
Figure 00000076
Figure 00000077
Figure 00000078
Figure 00000079
Figure 00000080
Figure 00000081
Figure 00000082
Figure 00000083
Figure 00000084
Figure 00000085
Figure 00000086
Figure 00000087
Figure 00000088
Figure 00000089
Figure 00000090
Figure 00000091
Figure 00000092
Figure 00000093
Figure 00000094
Figure 00000095
Figure 00000096
Figure 00000097
Figure 00000098
Figure 00000099
Figure 00000100
Figure 00000101

Claims (7)

1. Применение соединения формулы (I)
Figure 00000102

в котором соединение выбрано из группы соединений, приведенных в представленной ниже таблице
Figure 00000103
     Пример R1 R2 Конфигурация R1 или R2 R3 R4 Ln-R5 m

27 Н
Figure 00000104
 R
Figure 00000105
Figure 00000106
Figure 00000107
 44 Н
Figure 00000104
 R
Figure 00000108
 Н
Figure 00000109
 46 Н
Figure 00000104
 R
Figure 00000108
Figure 00000110
Figure 00000109
 55 Н
Figure 00000104
 R
Figure 00000108
Figure 00000111
Figure 00000112
 58 Н
Figure 00000104
 R
Figure 00000108
Figure 00000111
Figure 00000113
 102 Н
Figure 00000104
 R
Figure 00000105
Figure 00000111
Figure 00000114
 103 Н
Figure 00000115
 R
Figure 00000108
Figure 00000111
Figure 00000114
 105 Н
Figure 00000115
 R
Figure 00000108
Figure 00000106
Figure 00000116

110 Н
Figure 00000104
 R
Figure 00000105
Figure 00000106
Figure 00000116
 115 Н
Figure 00000115
 R
Figure 00000117
Figure 00000111
Figure 00000118
 133 Н
Figure 00000104
 R
Figure 00000108
Figure 00000106
Figure 00000107
 134 Н
Figure 00000104
 R
Figure 00000108
Figure 00000106
Figure 00000119
 234 Н
Figure 00000120
 R
Figure 00000105
Figure 00000106
Figure 00000121
 240 Н
Figure 00000122
 R
Figure 00000117
Figure 00000111
Figure 00000123

где обозначения X1, X2, Х3, Х4 и Х5, использованные в таблице, в каждом случае обозначают связывание в положении в общей формуле, приведенной в таблице, а не соответствующие группы R1, R2, R3, R4 и L-R5, необязательно в форме его рацематов и необязательно в форме его фармакологически приемлемых солей присоединения с кислотами, сольватов или гидратов, для приготовления фармацевтической композиции, предназначенной для лечения заболеваний, характеризующихся аномальной пролиферацией клеток в организме человека или млекопитающего, не являющегося человеком, путем ингибирования polo-подобных киназ, как регуляторов митоза.
2. Применение по п.1, в котором polo-подобной киназой является ППК-1.
3. Применение по п.1 или 2, характеризующееся тем, что заболевание характеризуется неприемлемой пролиферацией, миграцией, апоптозом или ангиогенезом клеток.
4. Применение по любому из пп.1-3, характеризующееся тем, что заболеванием является рак, выбранный из группы, включающей карциномы, саркомы, меланомы, миелому, опухоли кроветворной системы, лимфомы и раковые заболевания детей.
5. Применение по п.4, характеризующееся тем, что раком является лейкоз.
6. Применение по любому из пп.1-5, характеризующееся тем, что заболеванием является рак, выбранный из группы, включающей смешанные опухоли, недифференцированные опухоли и их метастазы.
7. Применение по любому из пп.1-6, в котором активный ингредиент вводят перорально, энтерально, чрескожно, внутривенно, внутрибрюшинно или путем инъекции.
RU2007109109/15A 2004-08-14 2005-08-09 Дигидроптеридиноны, предназначенные для лечения раковых заболеваний RU2406503C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04019359 2004-08-14
EP04019359.1 2004-08-14

Publications (2)

Publication Number Publication Date
RU2007109109A RU2007109109A (ru) 2008-09-20
RU2406503C2 true RU2406503C2 (ru) 2010-12-20

Family

ID=34926179

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2007109109/15A RU2406503C2 (ru) 2004-08-14 2005-08-09 Дигидроптеридиноны, предназначенные для лечения раковых заболеваний

Country Status (18)

Country Link
US (2) US20060074088A1 (ru)
EP (3) EP2409706A1 (ru)
JP (2) JP2008509949A (ru)
KR (2) KR101353990B1 (ru)
CN (2) CN104055778A (ru)
AR (1) AR050694A1 (ru)
AU (1) AU2005274387B2 (ru)
BR (1) BRPI0513977A (ru)
CA (1) CA2575787C (ru)
ES (2) ES2975234T3 (ru)
IL (2) IL181304A (ru)
MX (2) MX343697B (ru)
NZ (1) NZ553722A (ru)
PL (1) PL3560499T3 (ru)
RU (1) RU2406503C2 (ru)
TW (1) TWI360420B (ru)
WO (1) WO2006018185A2 (ru)
ZA (1) ZA200700281B (ru)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6861422B2 (en) * 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
DE102004029784A1 (de) * 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
DE102004033670A1 (de) * 2004-07-09 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Pyridodihydropyrazinone, Verfahren zu Ihrer Herstellung und Ihre Verwendung als Arzneimittel
US20060035903A1 (en) * 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US7728134B2 (en) * 2004-08-14 2010-06-01 Boehringer Ingelheim International Gmbh Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
US7759485B2 (en) * 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060074088A1 (en) * 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
EP1630163A1 (de) * 2004-08-25 2006-03-01 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1632493A1 (de) * 2004-08-25 2006-03-08 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE102004058337A1 (de) * 2004-12-02 2006-06-14 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten
US7553639B2 (en) * 2006-01-31 2009-06-30 Elan Pharma International Limited Alpha-synuclein kinase
US7439358B2 (en) 2006-02-08 2008-10-21 Boehringer Ingelheim International Gmbh Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
TW200808325A (en) * 2006-07-06 2008-02-16 Astrazeneca Ab Novel compounds
MX2009004077A (es) 2006-10-19 2009-05-05 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
CA2672612A1 (en) 2006-12-14 2008-06-26 Vertex Pharmaceuticals Incorporated Compounds useful as protein kinase inhibitors
EP2185559A1 (en) * 2007-08-03 2010-05-19 Boehringer Ingelheim International GmbH Crystalline form of a dihydropteridione derivative
NZ584760A (en) 2007-09-25 2012-03-30 Takeda Pharmaceutical Polo-like kinase inhibitors
WO2009103010A2 (en) * 2008-02-13 2009-08-20 Elan Pharmaceuticals, Inc. Alpha-synuclein kinase
EP2100894A1 (en) 2008-03-12 2009-09-16 4Sc Ag Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors
EP2356122B1 (en) 2008-06-23 2019-03-20 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors
US20100075973A1 (en) * 2008-08-28 2010-03-25 Takeda Pharmaceutical Company Limited Polo-like kinase inhibitors
CN102020643A (zh) 2009-09-22 2011-04-20 上海恒瑞医药有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
JP2013515734A (ja) * 2009-12-23 2013-05-09 エラン ファーマシューティカルズ，インコーポレイテッド ポロ様キナーゼの阻害薬としてのプテリジノン
WO2011101369A1 (en) 2010-02-17 2011-08-25 Boehringer Ingelheim International Gmbh Dihydropteridinones, method for production and use thereof
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
CA2801074A1 (en) 2010-06-04 2011-12-08 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
US8546566B2 (en) 2010-10-12 2013-10-01 Boehringer Ingelheim International Gmbh Process for manufacturing dihydropteridinones and intermediates thereof
US9358233B2 (en) 2010-11-29 2016-06-07 Boehringer Ingelheim International Gmbh Method for treating acute myeloid leukemia
AR085406A1 (es) 2011-02-25 2013-09-25 Takeda Pharmaceutical Oxazinopteridinas y oxazinopteridinonas n-sustituidas
US20130131069A1 (en) * 2011-05-13 2013-05-23 Boehringer Ingelheim International Gmbh Method for treatment of solid malignancies including advanced or metastatic solid malignancies
US9370535B2 (en) 2011-05-17 2016-06-21 Boehringer Ingelheim International Gmbh Method for treatment of advanced solid tumors
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
US20150031699A1 (en) * 2013-07-26 2015-01-29 Boehringer Ingelheim International Gmbh Treatment of myelodysplastic syndrome
EP3066101B1 (en) 2013-11-08 2020-07-29 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
UY35945A (es) 2014-01-09 2015-08-31 Takeda Pharmaceutical Derivados de azaindol
JP2017504650A (ja) 2014-01-31 2017-02-09 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジアゼパン誘導体およびその使用
US20160347750A1 (en) * 2014-01-31 2016-12-01 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도
JP2017504651A (ja) 2014-01-31 2017-02-09 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジアゼパン誘導体の使用
CN106456653A (zh) 2014-02-28 2017-02-22 腾沙治疗公司 高胰岛素血症相关病症的治疗
CN106793775B (zh) * 2014-08-08 2020-06-02 达纳-法伯癌症研究所股份有限公司 二氢碟啶酮衍生物及其用途
JP2017526741A (ja) 2014-08-08 2017-09-14 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジアゼパン誘導体およびその使用
US9867831B2 (en) 2014-10-01 2018-01-16 Boehringer Ingelheim International Gmbh Combination treatment of acute myeloid leukemia and myelodysplastic syndrome
SG11201703414VA (en) 2014-10-27 2017-05-30 Tensha Therapeutics Inc Bromodomain inhibitors
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
HK1256419A1 (zh) 2015-09-11 2019-09-20 达纳-法伯癌症研究所股份有限公司 乙酰胺噻吩並三唑並二氮雜環庚三烯及其用途
PE20181287A1 (es) 2015-09-11 2018-08-07 Dana Farber Cancer Inst Inc Ciano tienotriazolpirazinas y usos de las mismas
SG10201913450PA (en) 2015-11-25 2020-03-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
DE102017005089A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2002125451A (ru) * 2000-02-23 2004-01-10 Астразенека Аб (Se) Птеридиновые соединения для лечения псориаза

Family Cites Families (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL8303657A (nl) 1983-10-24 1985-05-17 Pharmachemie Bv Voor injectie geschikte, stabiele, waterige, zoutzuur bevattende oplossing van cisplatine, alsmede werkwijze ter bereiding daarvan.
DE3537761A1 (de) * 1985-10-24 1987-04-30 Bayer Ag Infusionsloesungen der 1-cyclopropyl-6-fluor-1,4-dihydro-4-oxo-7- (1-piperazinyl)-chinolin-3-carbonsaeure
ES2058527T3 (es) 1988-06-16 1994-11-01 Smith Kline French Lab Derivados de pirimidina condensados procedimiento y compuestos intermedios para su preparacion y composiciones farmaceuticas que los contienen.
FR2645152B1 (fr) 1989-03-30 1991-05-31 Lipha 3h-pteridinones-4, procedes de preparation et medicaments les contenant
CA2029651C (en) 1989-11-17 2000-06-06 David D. Davey Tricyclic pteridinones and a process for their preparation
US5198547A (en) * 1992-03-16 1993-03-30 South Alabama Medical Science Foundation, Usa Process for N5-formylating tetrahydropteridines
TW274550B (ru) * 1992-09-26 1996-04-21 Hoechst Ag
EP1195372A1 (en) * 1994-04-18 2002-04-10 Mitsubishi Pharma Corporation N-heterocyclic substituted benzamide derivatives with antihypertensive activity
CO4410190A1 (es) 1994-09-19 1997-01-09 Lilly Co Eli 3-[4-(2-AMINOETOXI)-BENZOIL]-2-ARIL-6-HIDROXIBENZO [b] TIOFENO CRISTALINO
IL117923A (en) 1995-05-03 2000-06-01 Warner Lambert Co Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds
BR9609083A (pt) * 1995-05-19 1999-02-02 Novartis Ag Processo para a hidrogenação catalítica de compostos nitro aromáticos
US5698556A (en) * 1995-06-07 1997-12-16 Chan; Carcy L. Methotrexate analogs and methods of using same
WO1998011893A1 (en) 1996-09-23 1998-03-26 Eli Lilly And Company Olanzapine dihydrate d
NZ509297A (en) * 1998-08-11 2003-11-28 Pfizer Prod Inc Substituted 1,8-naphthyridin-4(1H)-ones as phosphodiesterase 4 inhibitors
AU2623900A (en) 1999-01-22 2000-08-07 American Home Products Corporation Compounds which inhibit leukocyte adhesion mediated by vla-4
WO2001019825A1 (en) 1999-09-15 2001-03-22 Warner-Lambert Company Pteridinones as kinase inhibitors
KR20020075805A (ko) 2000-03-06 2002-10-05 워너-램버트 캄파니 5-알킬피리도[2,3-ｄ]피리미딘 타이로신 카이나제 억제제
DE10018783A1 (de) 2000-04-15 2001-10-25 Fresenius Kabi De Gmbh Lagerstabile Infusionslösung des Ciprofloxacins mit verringertem Säuregehalt
US20020183292A1 (en) * 2000-10-31 2002-12-05 Michel Pairet Pharmaceutical compositions based on anticholinergics and corticosteroids
DE10058119A1 (de) * 2000-11-22 2002-05-23 Bayer Ag Pepinotan-Kit
US6756374B2 (en) 2001-01-22 2004-06-29 Hoffmann-La Roche Inc. Diaminothiazoles having antiproliferative activity
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
US20030055026A1 (en) * 2001-04-17 2003-03-20 Dey L.P. Formoterol/steroid bronchodilating compositions and methods of use thereof
US6806272B2 (en) * 2001-09-04 2004-10-19 Boehringer Ingelheim Pharma Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
NZ531928A (en) * 2001-09-04 2005-10-28 Boehringer Ingelheim Pharma Novel dihydropteridinones, method for producing the same and the use thereof as medicaments
ES2293965T3 (es) * 2001-12-14 2008-04-01 Laboratoires Serono Sa Metodo de inducir la ovulacion utilizando un modulador no polipeptidico de los niveles de camp.
JP2005538048A (ja) * 2002-05-03 2005-12-15 シエーリング アクチエンゲゼルシャフト チアゾリジノン類、それらの生成及び医薬剤としての使用
CA2493908A1 (en) 2002-08-08 2004-02-19 Smithkline Beecham Corporation Thiophene compounds
US6861422B2 (en) * 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
MXPA05009068A (es) * 2003-02-26 2005-10-19 Boehringer Ingelheim Pharma Dihidro-pteridinonas, metodo para la produccion y uso del mismo en la forma de farmacos.
ATE468859T1 (de) 2003-03-26 2010-06-15 Wyeth Llc Immunogene zusammensetzung und verfahren
AU2004231342A1 (en) 2003-04-14 2004-11-04 Vectura Ltd Dry power inhaler devices and dry power formulations for enhancing dosing efficiency
CA2552540A1 (en) * 2004-01-17 2005-07-28 Boehringer Ingelheim International Gmbh Use of substituted pteridines for the treatment of diseases of the respiratory tract
DE102004002557A1 (de) * 2004-01-17 2005-08-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verwendung von substituierten Pyrimido(5,4-d)pyrimidinen zur Behandlung von Atemwegserkrankungen
DE102004029784A1 (de) * 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
DE102004033670A1 (de) * 2004-07-09 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Pyridodihydropyrazinone, Verfahren zu Ihrer Herstellung und Ihre Verwendung als Arzneimittel
DE102004034623A1 (de) * 2004-07-16 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 6-Formyl-tetrahydropteridine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US20060058311A1 (en) * 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US7759485B2 (en) * 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060074088A1 (en) * 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US7728134B2 (en) * 2004-08-14 2010-06-01 Boehringer Ingelheim International Gmbh Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
EP1632493A1 (de) 2004-08-25 2006-03-08 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1630163A1 (de) * 2004-08-25 2006-03-01 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
WO2006021547A1 (de) * 2004-08-26 2006-03-02 Boehringer Ingelheim International Gmbh Pteridinone als plk (polo like kinase) inhibitoren
JP2008510771A (ja) * 2004-08-27 2008-04-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジヒドロプテリジノン、その製造方法および医薬薬剤としてのその使用
DE102004058337A1 (de) * 2004-12-02 2006-06-14 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten
EP1915155A1 (en) * 2005-08-03 2008-04-30 Boehringer Ingelheim International GmbH Dihydropteridinones in the treatment of respiratory diseases
US7439358B2 (en) 2006-02-08 2008-10-21 Boehringer Ingelheim International Gmbh Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
EP1994002A1 (en) * 2006-03-07 2008-11-26 AstraZeneca AB Piperidine derivatives, their process for preparation, their use as therapeutic agents and pharmaceutical compositions containing them
EP2185559A1 (en) * 2007-08-03 2010-05-19 Boehringer Ingelheim International GmbH Crystalline form of a dihydropteridione derivative

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2002125451A (ru) * 2000-02-23 2004-01-10 Астразенека Аб (Se) Птеридиновые соединения для лечения псориаза

Also Published As

Publication number Publication date
CA2575787C (en) 2013-12-24
CA2575787A1 (en) 2006-02-23
CN101022809A (zh) 2007-08-22
TWI360420B (en) 2012-03-21
KR20070044052A (ko) 2007-04-26
EP1778240B1 (en) 2020-03-25
WO2006018185A3 (en) 2006-04-13
CN104055778A (zh) 2014-09-24
NZ553722A (en) 2010-08-27
EP2409706A1 (en) 2012-01-25
ES2800308T3 (es) 2020-12-29
MX2007001851A (es) 2007-03-28
US8058270B2 (en) 2011-11-15
US20080221099A1 (en) 2008-09-11
KR20130043695A (ko) 2013-04-30
WO2006018185A8 (en) 2006-06-01
EP1778240A2 (en) 2007-05-02
IL181304A0 (en) 2007-07-04
BRPI0513977A (pt) 2008-05-20
EP3560499A1 (en) 2019-10-30
TW200612956A (en) 2006-05-01
US20060074088A1 (en) 2006-04-06
WO2006018185A2 (en) 2006-02-23
ZA200700281B (en) 2008-05-28
AU2005274387A1 (en) 2006-02-23
IL181304A (en) 2015-05-31
PL3560499T3 (pl) 2024-07-15
RU2007109109A (ru) 2008-09-20
AU2005274387B2 (en) 2011-03-17
KR101283378B1 (ko) 2013-07-08
IL227841A (en) 2016-04-21
JP2008509949A (ja) 2008-04-03
MX343697B (es) 2016-11-18
ES2975234T3 (es) 2024-07-04
KR101353990B1 (ko) 2014-01-22
EP3560499B1 (en) 2024-03-06
AR050694A1 (es) 2006-11-15
JP2012211178A (ja) 2012-11-01
IL227841A0 (en) 2013-09-30

Similar Documents

Publication Publication Date Title
RU2406503C2 (ru) Дигидроптеридиноны, предназначенные для лечения раковых заболеваний
RU2407532C2 (ru) Комбинации, предназначенные для лечения заболеваний, включающих пролиферацию клеток
MX2021000887A (es) Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer.
AU2014251087B2 (en) Formulations of oxabicycloheptanes and oxabicycloheptenes
AR028810A1 (es) Derivados de arilpiperazinil-ciclohexil indol, composiciones farmaceuticas que los comprenden y el uso de los mismos para la manufactura de medicamentos para el tratamiento de la depresion
KR930702292A (ko) 종양 치료 활성을 증대시키기 위한 퀴나졸린 유도체
RU2011104570A (ru) КОМБИНАЦИЯ (А) ИНГИБИТОРА ФОСФОИНОЗИТ-3-КИНАЗЫ И (Б) МОДУЛЯТОРА ПУТИ Ras/Raf/Mek
RU2013119705A (ru) Применение производного рапамицина
RU2008120408A (ru) Соединения, связывающие bir домены iap
ES2605586T3 (es) Análogos de etopósido para el tratamiento de tumores metastásicos
EP1663244A2 (en) Pteridine derivatives for the treatment of septic shock and tnf-alpha-related diseases.
JP2023506787A (ja) Ｐａｒｐ阻害薬と組み合わせたａｔｒ阻害薬の使用
JP2007511498A (ja) Ｅｔ−７４３とドキソルビシンとを使用することを含むガンの併用療法
JP2016523858A (ja) がんを治療するためのｂｔｋ阻害剤とフルオロウラシルとの併用
EP3442505A1 (en) Combinations for the treatment of neoplasms using quiescent cell targeting and egfr inhibitors
KR20120096053A (ko) 아르테미시닌계 약물 및 다른 화학요법제의 항암 조합물
CN106572989A (zh) 用于治疗骨髓增生异常综合征的蛋白磷酸酶2a抑制剂
SK11552003A3 (sk) Farmaceutické kombinácie obsahujúce combretastatín a protinádorové činidlo
KR20100031759A (ko) 흑색종의 치료
MX2023013225A (es) Inhibidores de la cinasa 4 similar a polo.
JP2007511509A (ja) Ｅｔ−７４３およびパクリタキセルの使用を含むガンの併用療法
US6355628B1 (en) Combination therapy using pentafluorobenzenesulfonamides
US20190231793A1 (en) Use of harringtonines in the treatment of breast cancer, in particular triple-negative breast cancer
US10668080B2 (en) Phosphaplatin compounds as therapeutic agents for treatment of bone or blood cancers
KR100869037B1 (ko) 치환된 아크릴로일 디스타마이신 유도체 및 알킬화제를 포함하는 항종양 조성물

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20180810