HUE030413T2 - Szubsztituált pirazolo[1,5-a]pirimidin vegyületek mint TRK kináz inhibitorok elõállításának köztitermékei - Google Patents
Szubsztituált pirazolo[1,5-a]pirimidin vegyületek mint TRK kináz inhibitorok elõállításának köztitermékei Download PDFInfo
- Publication number
- HUE030413T2 HUE030413T2 HUE13197815A HUE13197815A HUE030413T2 HU E030413 T2 HUE030413 T2 HU E030413T2 HU E13197815 A HUE13197815 A HU E13197815A HU E13197815 A HUE13197815 A HU E13197815A HU E030413 T2 HUE030413 T2 HU E030413T2
- Authority
- HU
- Hungary
- Prior art keywords
- pyrrolidin
- pyrazolo
- pyrimidin
- mmol
- difluorophenyl
- Prior art date
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- 239000000543 intermediate Substances 0.000 title description 9
- LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical class N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 title description 8
- 229940043355 kinase inhibitor Drugs 0.000 title description 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 title description 3
- 238000004519 manufacturing process Methods 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 265
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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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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]
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- C07D519/02—Ergot alkaloids of the cyclic peptide type
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (3)
- Szabadalmi igénypontok1, Vegyülsi, amely a kővetkező csoportból vart kjváiasKtvá: - alábbi képietö vegyidet:vagy ennek gyógyszerészeti jog elfogadható sója, és - alábbi képietö vegyüleí:vagy mmk gyógyszéréSxetiíeg elfogadható sója,
- 2, Egy m, 1 - igénypont szerinti vegyüleí, amely az - alábbi képietö vegyüléí:vagy ennek gyógy szerésKetlisg elfogadható sója;
- 3, Egy az i , igénypont szerinti vegyidet, amely ax - alábbi képiét« vegyit let:vagy ennek gyógyszerészetiíeg -elfogadható sója. 119476-14Ő97A FO/TÈ
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HUE16166461A HUE037716T2 (hu) | 2008-10-22 | 2009-10-21 | Szubsztituált pirazolo[l,5-a]pirimidin vegyületek mint TRK kináz inhibitorok |
HUE18151233A HUE057625T2 (hu) | 2008-10-22 | 2009-10-21 | TRK kináz inhibitor szubsztituált pirazolo[1,5-a]pirimidin vegyületek |
HUS2000006C HUS000512I2 (hu) | 2008-10-22 | 2020-03-11 | Larotrektinib és/vagy gyógyszerészetileg elfogadható sói, elõnyösen larotrektinib-szulfát, beleértve a larotrektinib-hidrogénszulfátot |
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HUE16166461A HUE037716T2 (hu) | 2008-10-22 | 2009-10-21 | Szubsztituált pirazolo[l,5-a]pirimidin vegyületek mint TRK kináz inhibitorok |
HUE18151233A HUE057625T2 (hu) | 2008-10-22 | 2009-10-21 | TRK kináz inhibitor szubsztituált pirazolo[1,5-a]pirimidin vegyületek |
HUS2000006C HUS000512I2 (hu) | 2008-10-22 | 2020-03-11 | Larotrektinib és/vagy gyógyszerészetileg elfogadható sói, elõnyösen larotrektinib-szulfát, beleértve a larotrektinib-hidrogénszulfátot |
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EP (4) | EP3106463B3 (hu) |
JP (5) | JP5600111B2 (hu) |
KR (5) | KR101853026B1 (hu) |
CN (2) | CN103509017B (hu) |
AR (2) | AR074052A1 (hu) |
AU (1) | AU2009308465B2 (hu) |
BR (1) | BRPI0919873B8 (hu) |
CA (1) | CA2741313C (hu) |
CL (1) | CL2011000880A1 (hu) |
CO (1) | CO6440551A2 (hu) |
CR (1) | CR20110261A (hu) |
CY (4) | CY1118199T1 (hu) |
DK (4) | DK2350071T3 (hu) |
ES (4) | ES2669581T7 (hu) |
HK (2) | HK1160640A1 (hu) |
HR (3) | HRP20211722T1 (hu) |
HU (4) | HUE030413T2 (hu) |
IL (3) | IL212341A0 (hu) |
LT (4) | LT2725028T (hu) |
LU (1) | LUC00150I2 (hu) |
ME (1) | ME03010B (hu) |
MX (1) | MX2011004204A (hu) |
MY (1) | MY169791A (hu) |
NL (1) | NL301033I2 (hu) |
NO (2) | NO3106463T3 (hu) |
NZ (1) | NZ592809A (hu) |
PL (4) | PL2725028T3 (hu) |
PT (4) | PT3372605T (hu) |
RS (3) | RS57221B2 (hu) |
RU (1) | RU2018131134A (hu) |
SG (3) | SG196855A1 (hu) |
SI (4) | SI3106463T1 (hu) |
SM (2) | SMT201800244T1 (hu) |
TR (1) | TR201807039T4 (hu) |
TW (4) | TWI639605B (hu) |
UA (1) | UA106054C2 (hu) |
UY (1) | UY32192A (hu) |
WO (1) | WO2010048314A1 (hu) |
Families Citing this family (135)
Publication number | Priority date | Publication date | Assignee | Title |
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JP5503655B2 (ja) | 2008-09-22 | 2014-05-28 | アレイ バイオファーマ、インコーポレイテッド | Trkキナーゼ阻害剤としての置換イミダゾ[1,2b]ピリダジン化合物 |
SI3106463T1 (en) * | 2008-10-22 | 2018-08-31 | Array Biopharma, Inc. | Compounds of substituted pyrazolo (1,5-) pyrimidine as inhibitors of TRK kinase |
AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
TWI510487B (zh) | 2010-04-21 | 2015-12-01 | Plexxikon Inc | 用於激酶調節的化合物和方法及其適應症 |
KR101852169B1 (ko) | 2010-05-20 | 2018-04-26 | 어레이 바이오파마 인크. | Trk 키나제 저해제로서의 매크로시클릭 화합물 |
WO2012034095A1 (en) * | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
US8637516B2 (en) | 2010-09-09 | 2014-01-28 | Irm Llc | Compounds and compositions as TRK inhibitors |
US9102671B2 (en) * | 2011-02-25 | 2015-08-11 | Novartis Ag | Compounds and compositions as TRK inhibitors |
MX369142B (es) * | 2011-05-13 | 2019-10-30 | Array Biopharma Inc | Compuestos intermediarios de fórmula ii, útiles en la preparación de compuestos derivados de pirrolidinil como inhibidores de cinasa trka. |
US9045478B2 (en) * | 2011-12-12 | 2015-06-02 | Dr. Reddy's Laboratories Ltd. | Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (Trk) inhibitors |
NZ630721A (en) * | 2012-03-09 | 2016-12-23 | Lexicon Pharmaceuticals Inc | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use |
WO2014078331A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
UA117573C2 (uk) | 2012-11-13 | 2018-08-27 | Ерей Біофарма Інк. | Біциклічні сполуки сечовини, тіосечовини, гуанідину й ціаногуанідину, придатні для лікування болю |
US9981959B2 (en) | 2012-11-13 | 2018-05-29 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
UA116455C2 (uk) | 2012-11-13 | 2018-03-26 | Еррей Біофарма Інк. | Сполуки n-піролідинілсечовини, n'-піразолілсечовини, тіосечовини, гуанідину та ціаногуанідину як інгібітори кінази trka |
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