PE20160931A1 - Macrociclos de diarilo como moduladores de la proteina quinasa - Google Patents
Macrociclos de diarilo como moduladores de la proteina quinasaInfo
- Publication number
- PE20160931A1 PE20160931A1 PE2016000959A PE2016000959A PE20160931A1 PE 20160931 A1 PE20160931 A1 PE 20160931A1 PE 2016000959 A PE2016000959 A PE 2016000959A PE 2016000959 A PE2016000959 A PE 2016000959A PE 20160931 A1 PE20160931 A1 PE 20160931A1
- Authority
- PE
- Peru
- Prior art keywords
- modulators
- protein kinase
- diaryl
- macrocycles
- diaryl macrocycles
- Prior art date
Links
- -1 DIARYL MACROCYCLES Chemical class 0.000 title 1
- 102000001253 Protein Kinase Human genes 0.000 title 1
- 108060006633 protein kinase Proteins 0.000 title 1
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- YCWSUKQGVSGXJO-NTUHNPAUSA-N nifuroxazide Chemical group C1=CC(O)=CC=C1C(=O)N\N=C\C1=CC=C([N+]([O-])=O)O1 YCWSUKQGVSGXJO-NTUHNPAUSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged 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
- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
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- 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
-
- 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
- A61P37/06—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
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Communicable Diseases (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Transplantation (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
Abstract
La presente invencion se refiere a ciertos compuestos macrociclicos de diarilo de formula (I-A), donde el anillo A' y B' son entre otros arilo, heteroarilo; L1 y L2 son entre otros -O-; R3' y R4' son entre otros halogeno; R7' es entre otros H, alquilo C2-C6; m' es 2 a 5; n' es 2 a 4; p' es 0 a 4 y q' es 0 a 4, composiciones farmaceuticas que los contienen y metodos para utilizarlos, incluidos los metodos para el tratamiento de cancer, enfermedades neurologicas, enfermedades autoinmunes e inflamacion.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461931506P | 2014-01-24 | 2014-01-24 | |
US201462049326P | 2014-09-11 | 2014-09-11 | |
US201562106301P | 2015-01-22 | 2015-01-22 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20160931A1 true PE20160931A1 (es) | 2016-09-21 |
Family
ID=53682127
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2016000959A PE20160931A1 (es) | 2014-01-24 | 2015-01-23 | Macrociclos de diarilo como moduladores de la proteina quinasa |
Country Status (32)
Country | Link |
---|---|
US (6) | US9714258B2 (es) |
EP (6) | EP3572416B1 (es) |
JP (5) | JP6490713B2 (es) |
KR (1) | KR102402179B1 (es) |
CN (3) | CN110317213B (es) |
AP (1) | AP2016009383A0 (es) |
AU (2) | AU2015209239B2 (es) |
CA (1) | CA2936079C (es) |
CL (1) | CL2016001876A1 (es) |
CY (1) | CY1121850T1 (es) |
DK (3) | DK3572416T3 (es) |
EA (2) | EA031863B1 (es) |
ES (2) | ES2735729T3 (es) |
FI (1) | FI3636649T3 (es) |
HK (1) | HK1231407A1 (es) |
HR (2) | HRP20221518T1 (es) |
HU (2) | HUE060554T2 (es) |
IL (2) | IL246860B (es) |
LT (3) | LT3636649T (es) |
MX (2) | MX2016009588A (es) |
MY (1) | MY193524A (es) |
NZ (2) | NZ722375A (es) |
PE (1) | PE20160931A1 (es) |
PH (1) | PH12016501463A1 (es) |
PL (3) | PL3636649T3 (es) |
PT (3) | PT3572416T (es) |
RS (3) | RS65417B1 (es) |
SG (2) | SG10202000191YA (es) |
SI (2) | SI3097107T1 (es) |
UA (1) | UA121206C2 (es) |
WO (1) | WO2015112806A2 (es) |
ZA (2) | ZA201604654B (es) |
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CN103965200B (zh) | 2008-09-22 | 2016-06-08 | 阵列生物制药公司 | 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物 |
LT3372605T (lt) | 2008-10-22 | 2022-02-10 | Array Biopharma, Inc. | Pakeistieji pirazolo[1,5-a]pirimidino junginiai, kaip trk kinazės inhibitoriai |
AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
KR102132405B1 (ko) | 2010-05-20 | 2020-07-09 | 어레이 바이오파마 인크. | Trk 키나제 저해제로서의 매크로시클릭 화합물 |
MY193524A (en) | 2014-01-24 | 2022-10-18 | Turning Point Therapeutics Inc | Diaryl macrocycles as modulators of protein kinases |
RS64122B1 (sr) | 2014-11-16 | 2023-05-31 | Array Biopharma Inc | Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogensulfata |
US10758525B2 (en) | 2015-01-22 | 2020-09-01 | MyoKardia, Inc. | 4-methylsulfonyl-substituted piperidine urea compounds |
TN2017000502A1 (en) | 2015-06-01 | 2019-04-12 | Loxo Oncology Inc | Methods of diagnosing and treating cancer |
KR102599788B1 (ko) * | 2015-07-02 | 2023-11-07 | 터닝 포인트 테라퓨틱스, 인크. | 단백질 키나제의 조절물질로서 키랄 디아릴 매크로사이클 |
LT3319969T (lt) * | 2015-07-06 | 2024-06-10 | Turning Point Therapeutics, Inc. | Diarilo makrociklo polimorfas |
LT3322706T (lt) | 2015-07-16 | 2021-03-10 | Array Biopharma, Inc. | Pakeistieji pirazolo[1,5-a]piridino junginiai, kaip ret kinazės inhibitoriai |
JP6817287B2 (ja) * | 2015-07-21 | 2021-01-20 | ターニング・ポイント・セラピューティクス・インコーポレイテッドTurning Point Therapeutics,Inc. | キラルジアリール大環状分子及びその使用 |
BR112018008357A2 (pt) | 2015-10-26 | 2018-11-27 | Array Biopharma Inc | mutações de ponto em câncer resistente a inibidor de trk e métodos relacionados às mesmas |
WO2017106505A1 (en) * | 2015-12-15 | 2017-06-22 | University Of South Florida | Gas5 binding compounds, formulations, and uses thereof |
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TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
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TWI808958B (zh) * | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
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CN107586796B (zh) * | 2017-07-20 | 2021-08-06 | 暨明医药科技(苏州)有限公司 | (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法 |
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TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
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