ECSP055768A - Derivados de azol-pirimidina condensados - Google Patents
Derivados de azol-pirimidina condensadosInfo
- Publication number
- ECSP055768A ECSP055768A EC2005005768A ECSP055768A ECSP055768A EC SP055768 A ECSP055768 A EC SP055768A EC 2005005768 A EC2005005768 A EC 2005005768A EC SP055768 A ECSP055768 A EC SP055768A EC SP055768 A ECSP055768 A EC SP055768A
- Authority
- EC
- Ecuador
- Prior art keywords
- pi3k
- diseases
- disease
- present
- derivatives
- Prior art date
Links
- DDWJFSYHYPDQEL-UHFFFAOYSA-N pyrimidine;1h-pyrrole Chemical class C=1C=CNC=1.C1=CN=CN=C1 DDWJFSYHYPDQEL-UHFFFAOYSA-N 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 5
- 108091007960 PI3Ks Proteins 0.000 abstract 4
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 abstract 4
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 abstract 4
- 201000010099 disease Diseases 0.000 abstract 3
- 230000000694 effects Effects 0.000 abstract 3
- 208000035475 disorder Diseases 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 208000028867 ischemia Diseases 0.000 abstract 2
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000023328 Basedow disease Diseases 0.000 abstract 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 abstract 1
- 208000006029 Cardiomegaly Diseases 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 206010012438 Dermatitis atopic Diseases 0.000 abstract 1
- 208000005189 Embolism Diseases 0.000 abstract 1
- 208000015023 Graves' disease Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 208000012659 Joint disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical class C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 1
- 208000001647 Renal Insufficiency Diseases 0.000 abstract 1
- 206010040070 Septic Shock Diseases 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 201000008937 atopic dermatitis Diseases 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 230000004957 immunoregulator effect Effects 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 201000006370 kidney failure Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000002107 myocardial effect Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 230000007170 pathology Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 208000002815 pulmonary hypertension Diseases 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 206010039083 rhinitis Diseases 0.000 abstract 1
- 230000036303 septic shock Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P37/08—Antiallergic 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención se refiere a nuevos derivados de azolpirimidina condensados, a procedimientos para su preparación y a preparaciones farmacéuticas que los contienen. Los derivados de azolpirimidina condensados de la presente invención presentan una mayor potencia para la inhibición de la fosfatidilinositol-3-quinasa (PI3K), especialmente para la inhibición de la PI3K-? y pueden usarse para la profilaxis y tratamiento de enfermedades asociadas con la actividad de PI3K y particularmente con la actividad de PI3K-?. Más específicamente, los derivados de azol de la presente invención son útiles para el tratamiento y profilaxis de las siguientes enfermedades: trastornos inflamatorios e inmunorreguladores tales como asma, dermatitis atópica, rinitis, enfermedades alérgicas, enfermedad pulmonar obstructiva crónica (COPD), choque séptico, enfermedades de las articulaciones, patologías autoinmunes tales como artritis reumatoide, y enfermedad de Graves, cáncer, trastornos de contractilidad del miocardio, insuficiencia cardíaca, tromboembolia, isquemia y aterosclerosis. Los compuestos de la presente invención también son útiles para la hipertensión pulmonar, insuficiencia renal, hipertrofia cardíaca así como trastornos neurodegenerativos tales como enfermedad de Parkinson, enfermedad de Alzheimer, diabetes e isquemia focal, ya que las enfermedades también están relacionadas con la actividad de PI3K en un ser humano o animal.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02021861 | 2002-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP055768A true ECSP055768A (es) | 2005-08-11 |
Family
ID=32039115
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2005005768A ECSP055768A (es) | 2002-09-30 | 2005-04-28 | Derivados de azol-pirimidina condensados |
| EC2011005768A ECSP11005768A (es) | 2002-09-30 | 2011-02-07 | Derivados de azol-pirimidina condensados |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2011005768A ECSP11005768A (es) | 2002-09-30 | 2011-02-07 | Derivados de azol-pirimidina condensados |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US7511041B2 (es) |
| EP (2) | EP1549652B1 (es) |
| JP (1) | JP4790266B2 (es) |
| KR (1) | KR101059652B1 (es) |
| CN (1) | CN100384846C (es) |
| AR (2) | AR041426A1 (es) |
| AT (2) | ATE411996T1 (es) |
| AU (1) | AU2003293310B2 (es) |
| BR (1) | BRPI0314830B8 (es) |
| CA (1) | CA2499134C (es) |
| CY (2) | CY1109790T1 (es) |
| DE (1) | DE60324296D1 (es) |
| DK (2) | DK2042504T3 (es) |
| EC (2) | ECSP055768A (es) |
| ES (2) | ES2367141T3 (es) |
| HR (2) | HRP20131159B1 (es) |
| IL (1) | IL166855A (es) |
| MA (1) | MA27483A1 (es) |
| MX (1) | MXPA05001808A (es) |
| MY (1) | MY140756A (es) |
| NO (1) | NO331457B1 (es) |
| NZ (1) | NZ539062A (es) |
| PE (1) | PE20050089A1 (es) |
| PL (1) | PL226562B1 (es) |
| PT (2) | PT2042504E (es) |
| RU (1) | RU2326881C9 (es) |
| SI (2) | SI2042504T1 (es) |
| TW (1) | TWI327570B (es) |
| UA (1) | UA82205C2 (es) |
| UY (1) | UY28001A1 (es) |
| WO (1) | WO2004029055A1 (es) |
| ZA (1) | ZA200503306B (es) |
Families Citing this family (88)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| ZA200706595B (en) | 2003-08-29 | 2008-06-25 | Mitsui Chemicals Inc | Insecticide for agricultural or horticultural use and method of use thereof |
| LT2612862T (lt) | 2004-05-13 | 2017-01-25 | Icos Corporation | Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai |
| US7691888B2 (en) | 2004-10-07 | 2010-04-06 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-indazole |
| WO2006040645A1 (en) * | 2004-10-11 | 2006-04-20 | Ranbaxy Laboratories Limited | N-(3,5-dichloropyridin-4-yl)-2,4,5-alkoxy and 2,3,4-alkoxy benzamide derivatives as pde-iv (phophodiesterase type-iv) inhibitors for the treatment of inflammatory diseases such as asthma |
| JP2008537120A (ja) | 2005-04-14 | 2008-09-11 | ザ トラスティーズ オブ ボストン ユニバーシティ | 分類予測を使用した肺障害についての診断 |
| WO2007016979A2 (en) * | 2005-07-29 | 2007-02-15 | 4Sc Ag | NOVEL HETEROCYCLIC NF-κB INHIBITORS |
| JP2009529329A (ja) | 2006-03-09 | 2009-08-20 | トラスティーズ オブ ボストン ユニバーシティ | 鼻腔上皮細胞の遺伝子発現プロファイルを用いた、肺疾患のための診断および予後診断の方法 |
| US7517995B2 (en) | 2006-04-06 | 2009-04-14 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-cyclopentapyrazole |
| US7691868B2 (en) | 2006-04-06 | 2010-04-06 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-quinazoline |
| PL2041139T3 (pl) * | 2006-04-26 | 2012-05-31 | Hoffmann La Roche | Związki farmaceutyczne |
| WO2008064244A2 (en) * | 2006-11-20 | 2008-05-29 | The Trustees Of Columbia University In The City Of New York | Phosphoinositide modulation for the treatment of neurodegenerative diseases |
| AR064106A1 (es) * | 2006-12-05 | 2009-03-11 | Bayer Schering Pharma Ag | Derivados de 2,3-dihidroimidazo [1,2-c] quinazolina sustituida utiles para el tratamiento de enfermedades y trastornos hiper-proliferativos asociados con la angiogenesis |
| EP1953163A1 (en) | 2007-02-01 | 2008-08-06 | Boehringer Ingelheim Pharma GmbH & Co. KG | Pteridinone derivatives as PI3-kinases inhibitors |
| WO2008148023A2 (en) * | 2007-05-23 | 2008-12-04 | Medical College Of Georgia Research Institute, Inc. | Compositions and methods for treating neurological disorders |
| JP2010539239A (ja) * | 2007-09-17 | 2010-12-16 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Pi3キナーゼ阻害剤としてのピリドピリミジン誘導体 |
| CN101990577A (zh) * | 2007-09-19 | 2011-03-23 | 波士顿大学理事会 | 鉴定肺病药物开发的新途径 |
| CA2713388C (en) * | 2008-01-14 | 2016-03-29 | William Scott | Sulfone substituted 2,3-dihydroimidazo [1,2-c] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis |
| WO2009094224A1 (en) | 2008-01-25 | 2009-07-30 | Millennium Pharmaceuticals, Inc. | Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| US20090227575A1 (en) * | 2008-03-04 | 2009-09-10 | Wyeth | 7H-PYRROLO[2,3-H]QUINAZOLINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESIS |
| US20110105457A1 (en) * | 2008-04-18 | 2011-05-05 | Shionogi & Co., Ltd. | Heterocyclic compound having inhibitory activity on pi3k |
| EP2303890A4 (en) * | 2008-06-19 | 2012-04-11 | Progenics Pharm Inc | INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE |
| EP2168583A1 (en) * | 2008-09-24 | 2010-03-31 | Bayer Schering Pharma Aktiengesellschaft | Use of substituted 2,3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma |
| EP2168582A1 (en) | 2008-09-24 | 2010-03-31 | Bayer Schering Pharma Aktiengesellschaft | Combinations of substituted 2,3-dihydroimidazo[1,2-c]quinazolines |
| US8791131B2 (en) * | 2008-09-30 | 2014-07-29 | Pfizer Inc. | Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions |
| PL2364983T3 (pl) * | 2008-11-11 | 2014-04-30 | Jeil Pharmaceutical Co Ltd | Nowa pochodna tricykliczna lub jej farmaceutycznie dopuszczalne sole, sposób jej wytwarzania, oraz zawierająca ją kompozycja farmaceutyczna |
| US9492449B2 (en) | 2008-11-13 | 2016-11-15 | Gilead Calistoga Llc | Therapies for hematologic malignancies |
| KR20170060179A (ko) | 2008-11-13 | 2017-05-31 | 길리아드 칼리스토가 엘엘씨 | 혈액 종양에 대한 요법 |
| US10236078B2 (en) | 2008-11-17 | 2019-03-19 | Veracyte, Inc. | Methods for processing or analyzing a sample of thyroid tissue |
| US9495515B1 (en) | 2009-12-09 | 2016-11-15 | Veracyte, Inc. | Algorithms for disease diagnostics |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| JP2012516329A (ja) * | 2009-01-30 | 2012-07-19 | 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 | Pi3k阻害剤としてのヘテロアリールおよびその使用 |
| AU2010229968A1 (en) | 2009-03-24 | 2011-10-13 | Gilead Calistoga Llc | Atropisomers of2-purinyl-3-tolyl-quinazolinone derivatives and methods of use |
| JP2012524126A (ja) | 2009-04-20 | 2012-10-11 | ギリアド カリストガ リミテッド ライアビリティ カンパニー | 固形腫瘍の治療方法 |
| RS53830B1 (sr) * | 2009-04-30 | 2015-06-30 | Glaxo Group Limited | Indazoli supstituisani oksazolom kao inhibitori pi3-kinaze |
| EP3360978A3 (en) | 2009-05-07 | 2018-09-26 | Veracyte, Inc. | Methods for diagnosis of thyroid conditions |
| CA2768843A1 (en) | 2009-07-21 | 2011-01-27 | Gilead Calistoga Llc | Treatment of liver disorders with pi3k inhibitors |
| KR20120063515A (ko) * | 2009-09-09 | 2012-06-15 | 아빌라 테라퓨틱스, 인크. | Pi3 키나제 억제제 및 이들의 용도 |
| EA201201414A8 (ru) * | 2010-04-16 | 2013-12-30 | Байер Интеллектчуал Проперти Гмбх | КОМБИНАЦИИ, СОДЕРЖАЩИЕ ЗАМЕЩЕННЫЕ 2,3-ДИГИДРОИМИДАЗО[1,2-c]ХИНАЗОЛИНЫ |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| JP2013538840A (ja) | 2010-10-01 | 2013-10-17 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 置換n−(2−アリールアミノ)アリールスルホンアミドを含有する組み合わせ |
| UA113280C2 (xx) * | 2010-11-11 | 2017-01-10 | АМІНОСПИРТЗАМІЩЕНІ ПОХІДНІ 2,3-ДИГІДРОІМІДАЗО$1,2-c]ХІНАЗОЛІНУ, ПРИДАТНІ ДЛЯ ЛІКУВАННЯ ГІПЕРПРОЛІФЕРАТИВНИХ ПОРУШЕНЬ І ЗАХВОРЮВАНЬ, ПОВ'ЯЗАНИХ З АНГІОГЕНЕЗОМ | |
| CN103339133B (zh) * | 2010-11-11 | 2016-06-15 | 拜耳知识产权有限责任公司 | 烷氧基取代的2,3-二氢咪唑并[1,2-c]喹唑啉 |
| US9675616B2 (en) | 2010-11-11 | 2017-06-13 | Bayer Intellectual Property Gmbh | Arylaminoalcohol-substituted 2,3-dihydroimidazo[1,2-C]quinolines |
| JO3733B1 (ar) | 2011-04-05 | 2021-01-31 | Bayer Ip Gmbh | استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة |
| EP2508525A1 (en) | 2011-04-05 | 2012-10-10 | Bayer Pharma Aktiengesellschaft | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts |
| ES2848273T3 (es) | 2012-03-05 | 2021-08-06 | Gilead Calistoga Llc | Formas polimórficas de (S)-2-(1-(9H-purin-6-ilamino)propilo)-5-fluoro-3-fenilquinazolina-4(3H)-ona |
| EP2968988A4 (en) | 2013-03-14 | 2016-11-16 | Allegro Diagnostics Corp | METHOD FOR EVALUATING A COPD STATUS |
| HK1214533A1 (zh) | 2013-03-15 | 2016-07-29 | 基因泰克公司 | 治疗癌症和预防癌症耐药性的方法 |
| US11976329B2 (en) | 2013-03-15 | 2024-05-07 | Veracyte, Inc. | Methods and systems for detecting usual interstitial pneumonia |
| AP2015008750A0 (en) | 2013-04-08 | 2015-09-30 | Bayer Pharma AG | Use of substituted 2,3-dihydroimidazo[1,2-c] quinazolines for treating lymphomas |
| TWI710558B (zh) | 2013-05-01 | 2020-11-21 | 瑞士商赫孚孟拉羅股份公司 | 二雜芳基化合物及其用途 |
| WO2015027431A1 (en) | 2013-08-29 | 2015-03-05 | Merck Sharp & Dohme Corp. | 2,2-difluorodioxolo a2a receptor antagonists |
| EP3083630B1 (en) | 2013-12-20 | 2019-08-21 | Gilead Calistoga LLC | Process methods for phosphatidylinositol 3-kinase inhibitors |
| JP2017500319A (ja) | 2013-12-20 | 2017-01-05 | ギリアード カリストガ エルエルシー | (s)−2−(1−(9h−プリン−6−イルアミノ)プロピル)−5−フルオロ−3−フェニルキナゾリン−4(3h)−オンの塩酸塩の多形形態 |
| US11021467B2 (en) | 2014-06-13 | 2021-06-01 | Gilead Sciences, Inc. | Phosphatidylinositol 3-kinase inhibitors |
| US12297505B2 (en) | 2014-07-14 | 2025-05-13 | Veracyte, Inc. | Algorithms for disease diagnostics |
| CN114606309A (zh) | 2014-11-05 | 2022-06-10 | 威拉赛特公司 | 使用机器学习和高维转录数据的诊断系统和方法 |
| EP3018131A1 (en) * | 2014-11-07 | 2016-05-11 | Bayer Pharma Aktiengesellschaft | Synthesis of copanlisib and its dihydrochloride salt |
| EP3018127A1 (en) | 2014-11-07 | 2016-05-11 | Bayer Pharma Aktiengesellschaft | Synthesis of copanlisib and its dihydrochloride salt |
| EA201791974A1 (ru) | 2015-03-09 | 2018-05-31 | Байер Фарма Акциенгезельшафт | Комбинации, содержащие замещенный 2,3-дигидроимидазо[1,2-с]хиназолин |
| CN105130998B (zh) * | 2015-09-25 | 2017-07-28 | 苏州立新制药有限公司 | 库潘尼西的制备方法 |
| CN105130997B (zh) * | 2015-09-25 | 2017-12-05 | 苏州明锐医药科技有限公司 | 一种库潘尼西的制备方法 |
| WO2017153220A1 (en) | 2016-03-08 | 2017-09-14 | Bayer Pharma Aktiengesellschaft | 2—amino—n— [7—methoxy—2, 3-dihydroimidazo-[1, 2-c] quinazolin-5-yl] pyrimidine—5—carboxamides |
| EP3219329A1 (en) | 2016-03-17 | 2017-09-20 | Bayer Pharma Aktiengesellschaft | Combinations of copanlisib |
| US20190292600A1 (en) | 2016-05-12 | 2019-09-26 | Trustees Of Boston University | Nasal epithelium gene expression signature and classifier for the prediction of lung cancer |
| WO2018009915A1 (en) | 2016-07-08 | 2018-01-11 | Trustees Of Boston University | Gene expression-based biomarker for the detection and monitoring of bronchial premalignant lesions |
| WO2018054782A1 (en) | 2016-09-23 | 2018-03-29 | Bayer Pharma Aktiengesellschaft | Combination of pi3k-inhibitors |
| AU2017376766A1 (en) | 2016-12-14 | 2019-06-06 | Tva (Abc), Llc | HSP90-targeting conjugates and formulations thereof |
| CA3054249A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combinations of copanlisib with anti-pd-1 antibody |
| CA3068324A1 (en) | 2017-06-28 | 2019-01-03 | Bayer Consumer Care Ag | Combination of a pi3k-inhibitor with an androgen receptor antagonist |
| WO2019048527A1 (en) | 2017-09-08 | 2019-03-14 | Bayer Pharma Aktiengesellschaft | COPANLISIB FORMULATIONS |
| EP3498266A1 (en) | 2017-12-15 | 2019-06-19 | Bayer Consumer Care AG | Formulations of copanlisib |
| EP3684772B1 (en) * | 2017-09-20 | 2023-12-06 | ABM Therapeutics Corporation | Cyclic iminopyrimidine derivatives as kinase inhibitors |
| US11351156B2 (en) | 2017-10-13 | 2022-06-07 | Inserm | Combination treatment of pancreatic cancer |
| WO2019101871A1 (en) | 2017-11-23 | 2019-05-31 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | A new marker for predicting the sensitivity to pi3k inhibitors |
| WO2019105734A1 (en) | 2017-11-28 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib |
| WO2019105835A1 (en) | 2017-11-29 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib and anetumab ravtansine |
| WO2019197269A1 (en) | 2018-04-11 | 2019-10-17 | Bayer Aktiengesellschaft | Combinations of copanlisib with triazolone derivatives and their use in the treatment of cancer |
| CN112789279B (zh) * | 2018-07-27 | 2023-09-29 | 上海翰森生物医药科技有限公司 | 含三并环类衍生物抑制剂、其制备方法和应用 |
| CN109053554B (zh) * | 2018-08-01 | 2020-07-28 | 江苏八巨药业有限公司 | 一种使用催化剂合成3-乙酰吡啶的方法 |
| US20210187134A1 (en) | 2018-08-28 | 2021-06-24 | Bayer As | Combination of pi3k-inhibitors and targeted thorium conjugates |
| EP3866805A1 (en) | 2018-10-16 | 2021-08-25 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
| CA3118493A1 (en) | 2018-11-05 | 2020-05-14 | Iovance Biotherapeutics, Inc. | Expansion of tils utilizing akt pathway inhibitors |
| BR112021011894A2 (pt) | 2018-12-21 | 2021-09-08 | Daiichi Sankyo Company, Limited | Composição farmacêutica |
| WO2020164997A1 (en) | 2019-02-12 | 2020-08-20 | Bayer Aktiengesellschaft | Combination of pi3k-inhibitors |
| CN114621236B (zh) * | 2022-04-25 | 2024-06-18 | 河南湾流生物科技有限公司 | 一种喹啉类饲料添加剂的制备方法 |
| WO2025087879A2 (en) | 2023-10-23 | 2025-05-01 | Institut National de la Santé et de la Recherche Médicale | Suppressing the pi3kgamma/akt signalling pathway for the treatment of acute myeloid leukemia |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3644354A (en) * | 1968-09-16 | 1972-02-22 | Sandoz Ag | 5-substituted-2 3-dihydroimidazo(1 2-c)quinazolines |
| US4287341A (en) | 1979-11-01 | 1981-09-01 | Pfizer Inc. | Alkoxy-substituted-6-chloro-quinazoline-2,4-diones |
| NZ234186A (en) * | 1989-07-07 | 1991-10-25 | Janssen Pharmaceutica Nv | Imidazo quinazolin-one derivatives and pharmaceutical compositions |
| CN1033644C (zh) * | 1993-01-02 | 1996-12-25 | 瑞安大药厂股份有限公司 | 3-取代甲基-2,3-二氢咪唑并[1,2-c]喹唑啉衍生物,其制备与用途 |
| FI970588A7 (fi) | 1994-08-12 | 1997-04-11 | Wellstat Therapeutics Corp | Menetelmät verenmyrkytyksen tai tulehdussairauksien hoitamiseksi oksipuriininukleosideillä |
| JP4431638B2 (ja) * | 1996-01-29 | 2010-03-17 | アメリカ合衆国 | ジヒドロピリジン―、ピリジン―、ベンゾピラン―オン―およびトリアゾロキナゾリン誘導体、それらの製造およびそれらのアデノシン受容体アンタゴニストとしての用途 |
| US5932584A (en) * | 1997-05-06 | 1999-08-03 | National Science Council | Optically active 2,3-dihydroimidazo(1,2-C) quinazoline derivatives, the preparation and antihypertensive use thereof |
| DE60144277D1 (de) | 2000-04-25 | 2011-05-05 | Icos Corp | Hemmer der menschlichen phosphatidyl-inositol-3-kinase delta |
| AU5261001A (en) * | 2000-04-27 | 2001-11-12 | Imperial Cancer Research Technology Ltd | Condensed heteroaryl derivatives |
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