CN101094853B - 可用作蛋白激酶抑制剂的吡唑并[1,5-a]嘧啶 - Google Patents
可用作蛋白激酶抑制剂的吡唑并[1,5-a]嘧啶 Download PDFInfo
- Publication number
- CN101094853B CN101094853B CN2005800450252A CN200580045025A CN101094853B CN 101094853 B CN101094853 B CN 101094853B CN 2005800450252 A CN2005800450252 A CN 2005800450252A CN 200580045025 A CN200580045025 A CN 200580045025A CN 101094853 B CN101094853 B CN 101094853B
- Authority
- CN
- China
- Prior art keywords
- alkyl
- group
- compound
- aliphatic
- independently
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 *C=CC=CC=CC(c1c2ncc(*)c[n]2nc1N)=CC=CC(I)=* Chemical compound *C=CC=CC=CC(c1c2ncc(*)c[n]2nc1N)=CC=CC(I)=* 0.000 description 4
- ZWVRTWAMDOBDSL-UHFFFAOYSA-N CN1C(C2C(N)=NCNC2N)=CC=CC1 Chemical compound CN1C(C2C(N)=NCNC2N)=CC=CC1 ZWVRTWAMDOBDSL-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
-
- 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
- A61P1/18—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
- 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
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
-
- 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
- A61P17/10—Anti-acne agents
-
- 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
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- 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
- 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
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Biochemistry (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Virology (AREA)
- Ophthalmology & Optometry (AREA)
- Child & Adolescent Psychology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62544604P | 2004-11-04 | 2004-11-04 | |
| US60/625,446 | 2004-11-04 | ||
| PCT/US2005/040344 WO2006052913A1 (en) | 2004-11-04 | 2005-11-04 | PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101094853A CN101094853A (zh) | 2007-12-26 |
| CN101094853B true CN101094853B (zh) | 2011-07-13 |
Family
ID=35809833
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2005800450252A Expired - Fee Related CN101094853B (zh) | 2004-11-04 | 2005-11-04 | 可用作蛋白激酶抑制剂的吡唑并[1,5-a]嘧啶 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7528138B2 (https=) |
| EP (1) | EP1812440B1 (https=) |
| JP (2) | JP5030229B2 (https=) |
| KR (1) | KR20070090172A (https=) |
| CN (1) | CN101094853B (https=) |
| AT (1) | ATE482213T1 (https=) |
| AU (1) | AU2005304784B2 (https=) |
| CA (1) | CA2586375A1 (https=) |
| DE (1) | DE602005023763D1 (https=) |
| DK (1) | DK1812440T3 (https=) |
| ES (1) | ES2354824T3 (https=) |
| IL (1) | IL182893A0 (https=) |
| MX (1) | MX337817B (https=) |
| NO (1) | NO20072795L (https=) |
| NZ (1) | NZ555236A (https=) |
| PT (1) | PT1812440E (https=) |
| RU (1) | RU2417996C2 (https=) |
| SI (1) | SI1812440T1 (https=) |
| WO (1) | WO2006052913A1 (https=) |
| ZA (1) | ZA200704476B (https=) |
Families Citing this family (108)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0104140D0 (sv) * | 2001-12-07 | 2001-12-07 | Astrazeneca Ab | Novel Compounds |
| PT1812440E (pt) * | 2004-11-04 | 2011-01-25 | Vertex Pharma | Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases |
| SI1853588T1 (sl) * | 2005-02-16 | 2008-10-31 | Astrazeneca Ab | Kemične spojine |
| US20090156617A1 (en) * | 2005-05-12 | 2009-06-18 | Northrup Alan B | Tyrosine kinase inhibitors |
| US20080287437A1 (en) * | 2005-05-16 | 2008-11-20 | Astrazeneca Ab | Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors |
| WO2007046867A2 (en) * | 2005-05-19 | 2007-04-26 | Xenon Pharmaceuticals Inc. | Piperidine derivatives and their uses as therapeutic agents |
| EP2354140A1 (en) * | 2005-05-20 | 2011-08-10 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
| JP2009513615A (ja) * | 2005-10-28 | 2009-04-02 | アストラゼネカ アクチボラグ | 癌の治療においてチロシンキナーゼ阻害剤として使用するための4−(3−アミノピラゾール)ピリミジン誘導体 |
| SG10202003901UA (en) | 2005-12-13 | 2020-05-28 | Incyte Holdings Corp | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors |
| GB0601638D0 (en) * | 2006-01-27 | 2006-03-08 | Merck Sharp & Dohme | Therapeutic treatment |
| US8198448B2 (en) | 2006-07-14 | 2012-06-12 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| PE20080403A1 (es) | 2006-07-14 | 2008-04-25 | Amgen Inc | Derivados heterociclicos fusionados y metodos de uso |
| US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| CA2668286C (en) | 2006-11-03 | 2014-09-16 | Pharmacyclics, Inc. | Bruton's tyrosine kinase activity probe and method of using |
| MX2009010127A (es) * | 2007-03-22 | 2009-11-05 | Vertex Pharma | Compuestos utiles como inhibidores de janus cinasas. |
| JP2010524911A (ja) * | 2007-04-18 | 2010-07-22 | アストラゼネカ アクチボラグ | 5−アミノピラゾール−3−イル−3H−イミダゾ[4,5−b]ピリジン誘導体と癌の治療のためのその使用 |
| UA99459C2 (en) * | 2007-05-04 | 2012-08-27 | Астразенека Аб | 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer |
| WO2008135786A1 (en) * | 2007-05-04 | 2008-11-13 | Astrazeneca Ab | Amino-thiazolyl- pyrimidine derivatives and their use for the treatment of cancer |
| KR20150036210A (ko) | 2007-06-13 | 2015-04-07 | 인사이트 코포레이션 | 야누스 키나제 억제제(R)―3―(4―(7H―피롤로[2,3-d]피리미딘―4―일)―1H―피라졸―1―일)―3―사이클로펜틸프로판니트릴의 염 |
| KR20100087298A (ko) * | 2007-09-28 | 2010-08-04 | 교와 핫꼬 기린 가부시키가이샤 | 피부 질환의 예방 및/또는 치료제 |
| UA104849C2 (uk) * | 2007-11-16 | 2014-03-25 | Інсайт Корпорейшн | 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus |
| AU2008343813B2 (en) * | 2007-12-19 | 2012-04-12 | Amgen Inc. | Inhibitors of PI3 kinase |
| CN101932583A (zh) * | 2007-12-19 | 2010-12-29 | 沃泰克斯药物股份有限公司 | 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类 |
| JP5638961B2 (ja) * | 2008-03-13 | 2014-12-10 | ザ ジェネラル ホスピタル コーポレイション | Bmpシグナル伝達経路のインヒビター |
| KR20110017445A (ko) * | 2008-06-11 | 2011-02-21 | 아스트라제네카 아베 | 암 및 골수증식성 장애의 치료에 유용한 트리시클릭 2,4-디아미노-l,3,5-트리아진 유도체 |
| JP5746032B2 (ja) * | 2008-09-19 | 2015-07-08 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | 3,4−ジヒドロ−2H−ピロロ[1,2−a]ピラジン−1−オン誘導体 |
| WO2010033941A1 (en) | 2008-09-22 | 2010-03-25 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| BRPI0919488A2 (pt) * | 2008-09-30 | 2015-12-01 | Astrazeneca Ab | composto, uso de um composto, método para tratar câncer em um animal de sangue quente, composição farmacêutica, e, processo para preparar um composto |
| EP2348860B1 (en) * | 2008-10-31 | 2015-05-27 | Genentech, Inc. | Pyrazolopyrimidine jak inhibitor compounds and methods |
| GB0821913D0 (en) | 2008-12-02 | 2009-01-07 | Price & Co | Antibacterial compounds |
| AR076794A1 (es) | 2009-05-22 | 2011-07-06 | Incyte Corp | Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen |
| SI2432472T1 (sl) * | 2009-05-22 | 2019-11-29 | Incyte Holdings Corp | 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK |
| CA2762479A1 (en) * | 2009-05-28 | 2010-12-02 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-met protein kinase |
| LT3141252T (lt) | 2009-06-17 | 2018-11-12 | Vertex Pharmaceuticals Inc. | Gripo virusų replikacijos inhibitoriai |
| UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| NZ598985A (en) | 2009-09-04 | 2013-07-26 | Biogen Idec Inc | Bruton's tyrosine kinase inhibitors |
| EP3354652B1 (en) | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| US20130096160A1 (en) * | 2010-04-14 | 2013-04-18 | Secretary, Department Of Health And Human Services | Arylthiazolyl piperidines and related compounds as modulators of survival motor neuron (smn) protein production |
| NZ604306A (en) | 2010-05-17 | 2015-02-27 | Incozen Therapeutics Pvt Ltd | Novel 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of protein kinases |
| ME03376B (me) | 2010-05-20 | 2020-01-20 | Array Biopharma Inc | Makrociklička jedinjenja kао inhibiтori trk kinaze |
| PE20130216A1 (es) | 2010-05-21 | 2013-02-27 | Incyte Corp | Formulacion topica para un inhibidor de jak |
| GB2480814A (en) * | 2010-06-01 | 2011-12-07 | Summit Corp Plc | Compounds for the treatment of clostridium difficile-associated disease |
| ES2803556T3 (es) | 2010-06-01 | 2021-01-27 | Summit Oxford Ltd | Compuestos para el tratamiento de enfermedades asociadas a clostridium difficile |
| PE20140146A1 (es) | 2010-11-19 | 2014-02-06 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
| US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
| RU2013132681A (ru) * | 2010-12-16 | 2015-01-27 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы репликации вирусов гриппа |
| MX354412B (es) * | 2011-06-10 | 2018-03-05 | Merck Patent Gmbh | Composiciones y metodos para la produccion de compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton. |
| CN103797010B (zh) | 2011-06-20 | 2016-02-24 | 因塞特控股公司 | 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物 |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
| WO2013028263A1 (en) * | 2011-08-24 | 2013-02-28 | Glaxosmithkline Llc | Pyrazolopyrimidine derivatives as pi3 kinase inhibitors |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| CN107082779A (zh) | 2012-03-30 | 2017-08-22 | 理森制药股份公司 | 作为c‑met 蛋白激酶调节剂的新化合物 |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| AR091273A1 (es) * | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | Inhibidores de pirimidinil tirosina quinasa |
| WO2014028829A1 (en) * | 2012-08-16 | 2014-02-20 | The Scripps Research Institute | Novel kappa opioid ligands |
| PH12020551186B1 (en) | 2012-11-15 | 2024-03-20 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| WO2014081996A1 (en) * | 2012-11-23 | 2014-05-30 | Glaxosmithkline Llc | Novel compounds as diacylglycerol acyltransferase inhibitors |
| SI2941432T1 (en) | 2012-12-07 | 2018-07-31 | Vertex Pharmaceuticals Incorporated | 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR |
| TW201501713A (zh) * | 2013-03-01 | 2015-01-16 | Kyowa Hakko Kirin Co Ltd | 眼炎症性疾病之預防及/或治療劑 |
| RS62867B1 (sr) | 2013-03-06 | 2022-02-28 | Incyte Holdings Corp | Postupci i intermedijeri za dobijanje inhibitora jak |
| WO2014160203A2 (en) | 2013-03-14 | 2014-10-02 | The Brigham And Women's Hospital, Inc. | Bmp inhibitors and methods of use thereof |
| EP2970288A1 (en) * | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| WO2014143240A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| US8957078B2 (en) | 2013-03-15 | 2015-02-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2014175370A1 (ja) * | 2013-04-25 | 2014-10-30 | 塩野義製薬株式会社 | ピロリジン誘導体およびそれらを含有する医薬組成物 |
| SMT202000315T1 (it) | 2013-08-07 | 2020-07-08 | Incyte Corp | Forme di dosaggio a rilascio prolungato per un inibitore di jak1 |
| JP6618901B2 (ja) | 2013-11-13 | 2019-12-11 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | インフルエンザウイルスの複製の阻害剤を調製する方法 |
| LT3068776T (lt) | 2013-11-13 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Gripo virusų replikacijos inhibitoriai |
| WO2015073267A1 (en) * | 2013-11-15 | 2015-05-21 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| CN104650092B (zh) * | 2013-11-16 | 2017-11-10 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| PT3077397T (pt) | 2013-12-06 | 2020-01-22 | Vertex Pharma | Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo |
| JP2017516850A (ja) | 2014-05-23 | 2017-06-22 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Jak阻害剤である5−クロロ−2−ジフルオロメトキシフェニルピラゾロピリミジン化合物 |
| US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
| MX373102B (es) | 2014-06-05 | 2020-04-17 | Vertex Pharma | Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparación de tal compuesto y diferentes formas sólidas del mismo. |
| SG11201610500WA (en) | 2014-06-17 | 2017-01-27 | Vertex Pharma | Method for treating cancer using a combination of chk1 and atr inhibitors |
| US10513521B2 (en) | 2014-07-15 | 2019-12-24 | The Brigham And Women's Hospital, Inc. | Compositions and methods for inhibiting BMP |
| CN113354649B (zh) | 2014-11-16 | 2024-12-10 | 阵列生物制药公司 | 一种新的晶型 |
| EP3294735B8 (en) | 2015-05-13 | 2022-01-05 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| EP3294717B1 (en) | 2015-05-13 | 2020-07-29 | Vertex Pharmaceuticals Inc. | Methods of preparing inhibitors of influenza viruses replication |
| AU2016331955B2 (en) | 2015-09-30 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| FI3439662T3 (fi) | 2016-04-04 | 2024-09-04 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| EP3458456B1 (en) | 2016-05-18 | 2020-11-25 | Loxo Oncology Inc. | Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| PL3484888T3 (pl) * | 2016-07-18 | 2023-06-26 | University Health Network | Stałe postacie inhibitora TTK |
| JP7214632B2 (ja) | 2016-07-21 | 2023-01-30 | バイオジェン エムエー インク. | ブルトン型チロシンキナーゼ阻害剤のコハク酸塩形態および組成物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| EP3615538B1 (en) | 2017-04-27 | 2024-02-07 | The Brigham and Women's Hospital, Inc. | Novel alk2 inhibitors and methods for inhibiting bmp signaling |
| PL233595B1 (pl) * | 2017-05-12 | 2019-11-29 | Celon Pharma Spolka Akcyjna | Pochodne pirazolo[1,5-a]pirymidyny jako inhibitory kinazy JAK |
| MX387969B (es) | 2017-05-22 | 2025-03-19 | Hoffmann La Roche | Composiciones y compuestos terapéuticos, y métodos para su uso. |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| BR112020015396A2 (pt) | 2018-01-29 | 2020-12-08 | Merck Patent Gmbh | Inididores de gcn2 e usos dos mesmos |
| JP7229257B2 (ja) * | 2018-01-29 | 2023-02-28 | メルク パテント ゲーエムベーハー | Gcn2阻害剤およびその使用 |
| SG11202007164UA (en) | 2018-01-30 | 2020-08-28 | Incyte Corp | Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| SMT202400306T1 (it) | 2018-03-30 | 2024-09-16 | Incyte Corp | Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak. |
| EP3870181B1 (en) * | 2018-10-26 | 2024-08-14 | Keros Therapeutics, Inc. | Crystal forms of an alk2 inhibitor |
| CA3124088A1 (en) * | 2018-12-20 | 2020-06-25 | Incyte Corporation | Imidazopyridazine and imidazopyridine compounds as inhibitors of activin receptor-like kinase-2 |
| US12508262B2 (en) | 2020-04-30 | 2025-12-30 | Keros Therapeutics, Inc. | Methods of using ALK2 inhibitors |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| WO2022098812A1 (en) | 2020-11-04 | 2022-05-12 | Keros Therapeutics, Inc. | Methods of treating iron overload |
| EP4392418A4 (en) * | 2021-08-24 | 2025-06-18 | The Johns Hopkins University | Compositions and methods for treating proteotoxicity-associated diseases |
| CN116987083A (zh) * | 2022-04-25 | 2023-11-03 | 杭州健崃生物科技有限公司 | 吡唑并[1,5-a]嘧啶衍生物及其制备方法和用途 |
| KR102912267B1 (ko) | 2023-04-20 | 2026-01-15 | 한국화학연구원 | 신규한 헤테로고리 화합물 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 포함하는 바이러스성 질환의 예방 또는 치료용 약학적 조성물 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002501532A (ja) * | 1997-05-30 | 2002-01-15 | メルク エンド カンパニー インコーポレーテッド | 新規血管形成阻害薬 |
| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| US6245759B1 (en) * | 1999-03-11 | 2001-06-12 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| GB0103926D0 (en) * | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| US7550470B2 (en) * | 2002-12-11 | 2009-06-23 | Merck & Co. Inc. | Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors |
| PT1812440E (pt) * | 2004-11-04 | 2011-01-25 | Vertex Pharma | Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases |
-
2005
- 2005-11-04 PT PT05816516T patent/PT1812440E/pt unknown
- 2005-11-04 RU RU2007120518/04A patent/RU2417996C2/ru not_active IP Right Cessation
- 2005-11-04 EP EP05816516A patent/EP1812440B1/en not_active Expired - Lifetime
- 2005-11-04 CN CN2005800450252A patent/CN101094853B/zh not_active Expired - Fee Related
- 2005-11-04 US US11/266,935 patent/US7528138B2/en not_active Expired - Fee Related
- 2005-11-04 ES ES05816516T patent/ES2354824T3/es not_active Expired - Lifetime
- 2005-11-04 DE DE602005023763T patent/DE602005023763D1/de not_active Expired - Lifetime
- 2005-11-04 NZ NZ555236A patent/NZ555236A/en not_active IP Right Cessation
- 2005-11-04 ZA ZA200704476A patent/ZA200704476B/xx unknown
- 2005-11-04 WO PCT/US2005/040344 patent/WO2006052913A1/en not_active Ceased
- 2005-11-04 KR KR1020077012308A patent/KR20070090172A/ko not_active Ceased
- 2005-11-04 AU AU2005304784A patent/AU2005304784B2/en not_active Ceased
- 2005-11-04 AT AT05816516T patent/ATE482213T1/de active
- 2005-11-04 MX MX2007005439A patent/MX337817B/es active IP Right Grant
- 2005-11-04 CA CA002586375A patent/CA2586375A1/en not_active Abandoned
- 2005-11-04 JP JP2007540144A patent/JP5030229B2/ja not_active Expired - Fee Related
- 2005-11-04 DK DK05816516.8T patent/DK1812440T3/da active
- 2005-11-04 SI SI200531195T patent/SI1812440T1/sl unknown
-
2007
- 2007-05-01 IL IL182893A patent/IL182893A0/en unknown
- 2007-06-01 NO NO20072795A patent/NO20072795L/no not_active Application Discontinuation
-
2008
- 2008-10-29 JP JP2008278235A patent/JP2009067803A/ja active Pending
Non-Patent Citations (3)
| Title |
|---|
| Mohamed Hilmy ELNAGDI et al.Synthesis of substituted Azaindenes:synthesis ofnewpyrazolo-[1,5-a]pyrimidine derivatives.BULL.CHEM.SOC.JPN63 6.1990,63(6),1854-1856. |
| Mohamed Hilmy ELNAGDI et al.Synthesis of substituted Azaindenes:synthesis ofnewpyrazolo-[1,5-a]pyrimidine derivatives.BULL.CHEM.SOC.JPN63 6.1990,63(6),1854-1856. * |
| Yuh-Wen Ho.studies on the synthesis of new 3-(3,5-diamino-1-substituted-pyrazol-4-yl)azo-thieno[2,3-b]pyridines and 3-(2-amino-5,7-disubtituted-pyrazolo[1,5-a]pyrimidine-3-yl)azo-thieno[2,3-b]pyridines.Journal of the Chinese Chemical Society46.1999,46955-962. * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2006052913A1 (en) | 2006-05-18 |
| EP1812440B1 (en) | 2010-09-22 |
| ZA200704476B (en) | 2008-09-25 |
| RU2007120518A (ru) | 2008-12-10 |
| MX337817B (es) | 2011-11-04 |
| DE602005023763D1 (de) | 2010-11-04 |
| US7528138B2 (en) | 2009-05-05 |
| AU2005304784B2 (en) | 2011-03-24 |
| US20060135537A1 (en) | 2006-06-22 |
| ATE482213T1 (de) | 2010-10-15 |
| CN101094853A (zh) | 2007-12-26 |
| JP2009067803A (ja) | 2009-04-02 |
| ES2354824T3 (es) | 2011-03-18 |
| CA2586375A1 (en) | 2006-05-18 |
| AU2005304784A1 (en) | 2006-05-18 |
| SI1812440T1 (sl) | 2011-04-29 |
| JP2008519059A (ja) | 2008-06-05 |
| MX2007005439A (es) | 2008-02-19 |
| NZ555236A (en) | 2010-10-29 |
| NO20072795L (no) | 2007-06-01 |
| JP5030229B2 (ja) | 2012-09-19 |
| PT1812440E (pt) | 2011-01-25 |
| DK1812440T3 (da) | 2011-01-31 |
| HK1113569A1 (en) | 2008-10-10 |
| IL182893A0 (en) | 2007-08-19 |
| EP1812440A1 (en) | 2007-08-01 |
| RU2417996C2 (ru) | 2011-05-10 |
| KR20070090172A (ko) | 2007-09-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101094853B (zh) | 可用作蛋白激酶抑制剂的吡唑并[1,5-a]嘧啶 | |
| TWI444379B (zh) | 有用於作為Raf激酶抑制劑之化合物 | |
| EP1562938B1 (en) | Heteroaryl-pyrimidine derivatives as jak inhibitors | |
| CN1934113B (zh) | 可用作蛋白激酶抑制剂的组合物 | |
| AU2007284562B2 (en) | Using PI3K and MEK modulators in treatments of cancer | |
| JP2008519059A5 (https=) | ||
| CN101547924B (zh) | 抑制有丝分裂的化合物 | |
| CN101039933B (zh) | 可用作蛋白激酶抑制剂的二氨基三唑化合物 | |
| CN101460499A (zh) | 可用作janus激酶抑制剂的去氮杂嘌呤 | |
| TW201004940A (en) | Heteroaryl compounds and uses thereof | |
| CA2935867A1 (en) | Heteroaryls and uses thereof | |
| CN105367503A (zh) | 杂芳基化合物和其用途 | |
| JP2011528026A6 (ja) | 新規化学化合物 | |
| CN101801971A (zh) | 可用作janus激酶抑制剂的脱氮嘌呤 | |
| JP2010532312A (ja) | 1−h−ピラゾロ(3,4b)ピリミジン誘導体および有糸分裂キナーゼの調節剤としてのその使用 | |
| CA2946130A1 (en) | Quinoxaline compounds and uses thereof | |
| EP3013813A1 (en) | Heteroaromatic compounds and their use as dopamine d1 ligands | |
| JP2023508978A (ja) | エクトヌクレオチドピロホスファターゼ/ホスホジエステラーゼ1(enpp1)モジュレーター及びその使用 | |
| TW201605832A (zh) | 作為p97錯合物之抑制劑之單環嘧啶/吡啶化合物 | |
| CN101291926A (zh) | 可用作Tec家族非受体酪氨酸激酶抑制剂的3,5-二取代的吡啶-2-酮 | |
| CN101228160A (zh) | 可用作蛋白激酶抑制剂的吖吲哚 | |
| HK1113569B (en) | Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases | |
| CN101573365A (zh) | 可用作蛋白激酶抑制剂的化合物 | |
| OA17657A (en) | Heteroaromatic compounds and their use as Dopamine DI ligands |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 1113569 Country of ref document: HK |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: GR Ref document number: 1113569 Country of ref document: HK |
|
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20110713 Termination date: 20121104 |