MD4800B1 - Compuşi de aminopirimidinil ca inhibitori de JAK - Google Patents

Compuşi de aminopirimidinil ca inhibitori de JAK

Info

Publication number
MD4800B1
MD4800B1 MDA20170016A MD20170016A MD4800B1 MD 4800 B1 MD4800 B1 MD 4800B1 MD A20170016 A MDA20170016 A MD A20170016A MD 20170016 A MD20170016 A MD 20170016A MD 4800 B1 MD4800 B1 MD 4800B1
Authority
MD
Moldova
Prior art keywords
compounds
jak inhibitors
aminopyrimidinyl
aminopyrimidinyl compounds
jak
Prior art date
Application number
MDA20170016A
Other languages
English (en)
Russian (ru)
Other versions
MD20170016A2 (ro
MD4800C1 (ro
Inventor
Эндрю ФЕНСАМ
Ариамала Гопалсами
Бриан С. ГЕРСТЕНБЕРГЕР
Иван Викторович Ефремов
Чжао-Куй ВАНЬ
Бетси ПИРС
Жан-Батист ТЕЛЛЬЕ
Джон И. ТРУДЖИЛЛО
Лиин ЧЖАН
Син
Эддин Сайях
Original Assignee
Pfizer Inc.
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=54148580&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MD4800(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Inc. filed Critical Pfizer Inc.
Publication of MD20170016A2 publication Critical patent/MD20170016A2/ro
Publication of MD4800B1 publication Critical patent/MD4800B1/ro
Publication of MD4800C1 publication Critical patent/MD4800C1/ro

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04NPICTORIAL COMMUNICATION, e.g. TELEVISION
    • H04N7/00Television systems
    • H04N7/18Closed-circuit television [CCTV] systems, i.e. systems in which the video signal is not broadcast
    • H04N7/188Capturing isolated or intermittent images triggered by the occurrence of a predetermined event, e.g. an object reaching a predetermined position

Abstract

Invenţia se referă la compuşi de aminopirimidinil cu formula generală (I):(I),sau la sărurile farmaceutic acceptabile ale acestora, unde substituenţii sunt definiţi în descriere. De asemenea, sunt dezvăluite metode de tratament cu inhibitori ai Kinazei Janus (JAK), compoziţii farmaceutice ce conţin compuşii conform invenţiei şi combinaţii cu alţi agenţi terapeutici.
MDA20170016A 2014-08-21 2015-08-07 Compuşi de aminopirimidinil ca inhibitori de JAK MD4800C1 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462039969P 2014-08-21 2014-08-21
PCT/IB2015/056021 WO2016027195A1 (en) 2014-08-21 2015-08-07 Aminopyrimidinyl compounds as jak inhibitors

Publications (3)

Publication Number Publication Date
MD20170016A2 MD20170016A2 (ro) 2017-08-31
MD4800B1 true MD4800B1 (ro) 2022-03-31
MD4800C1 MD4800C1 (ro) 2022-10-31

Family

ID=54148580

Family Applications (1)

Application Number Title Priority Date Filing Date
MDA20170016A MD4800C1 (ro) 2014-08-21 2015-08-07 Compuşi de aminopirimidinil ca inhibitori de JAK

Country Status (48)

Country Link
US (5) US9663526B2 (ro)
EP (1) EP3183247B9 (ro)
JP (1) JP6218260B2 (ro)
KR (1) KR101877189B1 (ro)
CN (1) CN107074867B (ro)
AP (1) AP2017009748A0 (ro)
AR (1) AR101599A1 (ro)
AU (1) AU2015304883B2 (ro)
BR (1) BR112017003054B1 (ro)
CA (1) CA2900855C (ro)
CL (1) CL2017000406A1 (ro)
CO (1) CO2017001603A2 (ro)
CR (1) CR20170066A (ro)
CU (1) CU24435B1 (ro)
CY (1) CY1119771T1 (ro)
DK (1) DK3183247T3 (ro)
DO (1) DOP2017000048A (ro)
EA (1) EA032609B1 (ro)
EC (1) ECSP17010156A (ro)
ES (1) ES2655971T3 (ro)
GE (1) GEP20197003B (ro)
GT (1) GT201700035A (ro)
HR (1) HRP20171913T1 (ro)
HU (1) HUE035553T2 (ro)
IL (1) IL250709B (ro)
LT (1) LT3183247T (ro)
MA (1) MA40587A (ro)
MD (1) MD4800C1 (ro)
ME (1) ME02856B (ro)
MX (1) MX2017002241A (ro)
MY (1) MY192109A (ro)
NI (1) NI201700020A (ro)
NO (1) NO2721710T3 (ro)
NZ (1) NZ729005A (ro)
PE (1) PE20171177A1 (ro)
PH (1) PH12017500276A1 (ro)
PL (1) PL3183247T3 (ro)
PT (1) PT3183247T (ro)
RS (1) RS56807B1 (ro)
SG (1) SG11201700957WA (ro)
SI (1) SI3183247T1 (ro)
SV (1) SV2017005384A (ro)
TN (1) TN2017000044A1 (ro)
TW (1) TWI583681B (ro)
UA (1) UA117976C2 (ro)
UY (1) UY36275A (ro)
WO (1) WO2016027195A1 (ro)
ZA (1) ZA201701005B (ro)

Families Citing this family (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2419610C2 (ru) 2005-05-26 2011-05-27 Ньюрон Системз, Инк. Композиции и способы лечения заболевания сетчатки
MX2015009383A (es) 2013-01-23 2016-03-17 Aldeyra Therapeutics Inc Enfermedades relacionadas con aldehido toxico y tratamiento.
WO2015155332A1 (en) 2014-04-11 2015-10-15 Boehringer Ingelheim International Gmbh Spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one derivatives and their use as mdm2-p53 inhibitors
WO2016001376A1 (en) 2014-07-03 2016-01-07 Boehringer Ingelheim International Gmbh New spiro[3h-indole-3,2´-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors
ES2739697T3 (es) 2014-08-21 2020-02-03 Boehringer Ingelheim Int Nuevos compuestos y derivados de espiro[3H-indol-3,2-pirrolidin]-2(1H)-ona como inhibidores de MDM2-p53
NO2721710T3 (ro) 2014-08-21 2018-03-31
CN108135907A (zh) 2015-08-21 2018-06-08 奥尔德拉医疗公司 氘化化合物和其用途
US9938257B2 (en) 2015-09-11 2018-04-10 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
TWI737635B (zh) 2015-10-09 2021-09-01 德商百靈佳殷格翰國際股份有限公司 作為mdm2-p53抑制劑之新穎螺﹝3h-吲哚-3,2´-吡咯啶﹞-2(1h)-酮化合物及其衍生物
BR112018072168A2 (pt) * 2016-04-28 2019-02-12 Theravance Biopharma R&D Ip, Llc compostos derivados da pirimidina como inibidores da quinase jak
CA3022665A1 (en) 2016-05-09 2017-11-16 Aldeyra Therapeutics, Inc. Combination treatment of ocular inflammatory disorders and diseases
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
EP3512519A1 (en) 2016-09-14 2019-07-24 Gilead Sciences, Inc. Syk inhibitors
TWI763722B (zh) * 2016-10-14 2022-05-11 美商林伯士拉克許米公司 Tyk2抑制劑及其用途
WO2018170476A1 (en) 2017-03-16 2018-09-20 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
WO2018195471A1 (en) 2017-04-21 2018-10-25 Gilead Sciences, Inc. Syk inhibitors in combination with hypomethylating agents
CN108864057B (zh) * 2017-05-16 2020-03-31 山东大学 含有4-氨基吡唑结构的jak与hdac双靶点抑制剂及其制备方法和应用
CN109422753B (zh) * 2017-09-03 2021-12-31 上海美志医药科技有限公司 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物
CA3077362A1 (en) 2017-10-10 2019-04-18 Aldeyra Therapeutics, Inc. Treatment of inflammatory disorders
EA202091016A1 (ru) * 2017-10-27 2020-07-17 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Пиримидиновое соединение в качестве ингибитора jak киназы
JP7254076B2 (ja) 2017-11-19 2023-04-07 サンシャイン・レイク・ファーマ・カンパニー・リミテッド 置換ヘテロアリール化合物及び使用方法
EP3749667A1 (en) 2018-02-05 2020-12-16 Alkermes, Inc. Compounds for the treatment of pain
EP3825303A4 (en) 2018-07-17 2022-07-06 Nippon Chemiphar Co., Ltd. T-CALCIUM CHANNEL BLOCKERS
AU2019319740A1 (en) 2018-08-06 2021-03-25 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
TW202035375A (zh) 2018-09-25 2020-10-01 美商卡都瑞恩醫藥有限責任公司 胺基嘧啶化合物
WO2020068846A1 (en) * 2018-09-25 2020-04-02 Heterocyclic Compound Heterocyclic compound
GB201816369D0 (en) 2018-10-08 2018-11-28 Sareum Ltd Pharmaceutical compounds
CN109364248B (zh) * 2018-10-16 2021-05-18 哈尔滨医科大学 ENaC及其抑制剂在预防、缓解和/或治疗动脉粥样硬化中的应用
AR116592A1 (es) * 2018-10-17 2021-05-26 Lilly Co Eli Tratamiento de la colangitis biliar primaria y la colangitis esclerosante primaria con baricitinib
AU2020222083B2 (en) * 2019-02-15 2022-11-17 Pfizer Inc. Crystalline pyrimidinyl-3,8-diazabicyclo(3.2.1)octanylmethanone compound and use thereof
CN111658628B (zh) * 2019-03-08 2022-03-01 中国科学院动物研究所 Gli2抑制剂的用途以及抑制gli2的化合物的筛选方法
US20220185816A1 (en) 2019-03-14 2022-06-16 Shanghai Synergy Pharmaceutical Sciences Co., Ltd Jak kinase inhibitor, preparation method for same, and applications thereof in field of medicine
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
JPWO2020203609A1 (ro) 2019-03-29 2020-10-08
TW202106681A (zh) 2019-04-24 2021-02-16 美商施萬生物製藥研發Ip有限責任公司 用於治療皮膚疾病之嘧啶jak抑制劑
US11155549B2 (en) 2019-04-24 2021-10-26 Theravance Biopharma R&D Ip, Llc Ester and carbonate pyrimidine compounds as JAK kinase inhibitors
WO2020222773A1 (en) 2019-04-30 2020-11-05 Celgene Corporation Combination therapies comprising apremilast and tyk2 inhibitors
KR20220046593A (ko) * 2019-08-09 2022-04-14 더 내셔널 인스티튜츠 오브 파마슈티컬 알앤디 컴퍼니 리미티드 가교된 헤테로사이클일-치환된 피리미딘 화합물, 이의 제조 방법, 및 이의 약학 용도
AU2020347561A1 (en) 2019-09-11 2022-04-14 Pfizer Inc. Treatment of hidradenitis with JAK inhibitors
CN110862376A (zh) * 2019-10-24 2020-03-06 嘉兴特科罗生物科技有限公司 一种小分子化合物
CA3159348A1 (en) 2019-11-08 2021-05-14 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113372364A (zh) * 2020-03-10 2021-09-10 明慧医药(上海)有限公司 一类jak激酶抑制剂及其制备和应用
CN115397815A (zh) * 2020-03-17 2022-11-25 江苏恒瑞医药股份有限公司 稠合二环类衍生物、其制备方法及其在医药上的应用
EP4125900A1 (en) 2020-04-04 2023-02-08 Pfizer Inc. Methods of treating coronavirus disease 2019
GB202005114D0 (en) 2020-04-07 2020-05-20 Sareum Ltd Crystalline Forms of a Pharmaceutical Compound
CN111423420A (zh) * 2020-04-30 2020-07-17 广州博济医药生物技术股份有限公司 作为己酮糖激酶抑制剂的并环化合物
CN113698403B (zh) * 2020-05-21 2022-06-28 南京亘泰医药技术有限公司 (1r,4r,7r)-7-氨基-2-氮杂双环[2,2,1]庚烷衍生物及制备方法
US20240018155A1 (en) * 2020-06-09 2024-01-18 Crystal Pharmatech Co., Ltd. New crystal form of p-toluenesulfonate salt of diazabicyclic compound and preparation method therefor
TWI782599B (zh) * 2020-07-02 2022-11-01 美商輝瑞股份有限公司 胺基嘧啶基衍生物
AR122756A1 (es) 2020-07-02 2022-10-05 Pfizer Preparación de un derivado de pirimidinil-3,8-diazabiciclo[3.2.1]octanilmetanona y sal de este
CA3189561A1 (en) 2020-07-17 2022-01-20 Pfizer Inc. Stable pharmaceutical topical formulation containing immunosuppressant for treating dermatological conditions
AU2021341508A1 (en) 2020-09-10 2023-05-25 Precirix N.V. Antibody fragment against fap
EP4279485A1 (en) * 2021-01-14 2023-11-22 The National Institutes of Pharmaceutical R&D Co., Ltd Bridged heterocyclyl-substituted pyrimidine compounds, preparation method and medical use thereof
CN114835717A (zh) * 2021-02-01 2022-08-02 杭州领业医药科技有限公司 Brepocitinib甲苯磺酸盐的晶型及其制备方法和用途
JP2024511979A (ja) 2021-03-15 2024-03-18 メイズ セラピューティクス, インコーポレイテッド グリコーゲンシンターゼ1(gys1)の阻害剤及びその使用方法
CN113999239B (zh) * 2021-07-14 2022-11-11 上海凌富药物研究有限公司 一种二氮杂桥化合物的合成方法
CN113698409B (zh) * 2021-08-10 2022-07-19 上海凌凯医药科技有限公司 一种多用途的二氮杂双环类化合物、制备方法及在合成药物中的应用
CN113461687B (zh) * 2021-08-10 2022-04-19 四川大学华西医院 2,8-氮杂-[4,5]十螺环酮衍生物及其制备方法和用途
CN117940410A (zh) * 2021-09-17 2024-04-26 江苏恒瑞医药股份有限公司 一种稠合二环类衍生物的可药用盐、晶型及其制备方法
WO2023076161A1 (en) 2021-10-25 2023-05-04 Kymera Therapeutics, Inc. Tyk2 degraders and uses thereof
CN114181097A (zh) * 2021-12-10 2022-03-15 广东嘉博制药有限公司 一种盐酸甲氧明的合成方法
WO2023178001A1 (en) * 2022-03-17 2023-09-21 Pfizer Inc. Methods, dosage regimens, and compositions for treating hidradenitis
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
WO2023213801A1 (en) 2022-05-02 2023-11-09 Precirix N.V. Pre-targeting
CN116396298A (zh) * 2023-06-06 2023-07-07 四川维亚本苑生物科技有限公司 CDK Ligand-1的中间体XII及CDK Ligand-1的制备方法

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4131139A1 (de) 1991-09-19 1993-03-25 Bayer Ag Verfahren zur herstellung von 1-fluor-cyclopropan-1-carbonsaeure
CN1930112B (zh) 2004-03-31 2010-06-23 第一制药株式会社 1,2-顺式-2-氟环丙烷-1-甲酸酯类的制造方法
JPWO2006109846A1 (ja) 2005-04-06 2008-11-20 武田薬品工業株式会社 トリアゾール誘導体およびその用途
BRPI0617241A2 (pt) 2005-10-13 2016-11-08 Glaxo Group Ltd composto ou um sal ou solvato do mesmo, composição farmacêutica, método para tratar uma doença ou condição mediada por atividade syk inadequada em um mamífero, e, uso de um composto ou um sal ou solvato farmaceuticamente aceitável do mesmo
NL2000323C2 (nl) * 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
EP1973911B1 (en) * 2006-01-17 2016-01-13 Vertex Pharmaceuticals Incorporated Azaindoles useful for the treatment of (inter alia) proliferative, cardiac, neurodegenerative, autoimmune or inflammatory disorders
WO2008032033A1 (en) * 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
CN101595103A (zh) * 2006-09-14 2009-12-02 阿斯利康(瑞典)有限公司 嘧啶衍生物
TW200904437A (en) * 2007-02-14 2009-02-01 Janssen Pharmaceutica Nv 2-aminopyrimidine modulators of the histamine H4 receptor
RU2009140319A (ru) * 2007-04-02 2011-05-10 Палау Фарма С.А. (Es) Производные пирролпиримидина
US8188083B2 (en) 2007-06-28 2012-05-29 Abbott Laboratories Triazolopyridazines
US8076491B2 (en) 2007-08-21 2011-12-13 Senomyx, Inc. Compounds that inhibit (block) bitter taste in composition and use thereof
EP2307387B1 (en) 2008-07-16 2013-11-20 F. Hoffmann-La Roche AG Novel heterocyclyl compounds for treatment of cardiovascular disease
WO2010075273A1 (en) * 2008-12-23 2010-07-01 Schering Corporation Bicyclic heterocycle derivatives and methods of use thereof
AR077465A1 (es) 2009-07-08 2011-08-31 Leo Pharma As Derivados de pirrolopirimidina como inhibidores de receptores jak y protein tirosin quinasas y uso farmaceutico de los mismos
JP2013534233A (ja) 2010-08-20 2013-09-02 セルゾーム リミティッド 選択的jak阻害剤としてのヘテロシクリルピラゾロピリミジン類似体
WO2013043962A1 (en) 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Cyanomethylpyrazole carboxamides as janus kinase inhibitors
EP2791347A2 (en) 2011-12-16 2014-10-22 Invista Technologies S.à.r.l. METHODS OF PRODUCING 6-CARBON CHEMICALS VIA CoA-DEPENDENT CARBON CHAIN ELONGATION ASSOCIATED WITH CARBON STORAGE
ES2739697T3 (es) 2014-08-21 2020-02-03 Boehringer Ingelheim Int Nuevos compuestos y derivados de espiro[3H-indol-3,2-pirrolidin]-2(1H)-ona como inhibidores de MDM2-p53
NO2721710T3 (ro) 2014-08-21 2018-03-31

Also Published As

Publication number Publication date
RS56807B1 (sr) 2018-04-30
KR101877189B1 (ko) 2018-07-10
BR112017003054A2 (pt) 2017-11-21
ES2655971T9 (es) 2018-09-14
IL250709A0 (en) 2017-04-30
TWI583681B (zh) 2017-05-21
TW201609706A (zh) 2016-03-16
KR20170036109A (ko) 2017-03-31
GT201700035A (es) 2019-10-10
EP3183247B1 (en) 2017-11-29
US20200330477A1 (en) 2020-10-22
US9663526B2 (en) 2017-05-30
LT3183247T (lt) 2018-01-25
US11197867B2 (en) 2021-12-14
CR20170066A (es) 2017-07-17
SI3183247T1 (en) 2018-02-28
SV2017005384A (es) 2017-07-10
AU2015304883B2 (en) 2018-05-10
PT3183247T (pt) 2018-01-18
PH12017500276A1 (en) 2017-07-03
CL2017000406A1 (es) 2017-10-06
MY192109A (en) 2022-07-27
HRP20171913T1 (hr) 2018-02-09
CU24435B1 (es) 2019-09-04
NI201700020A (es) 2017-05-02
SG11201700957WA (en) 2017-03-30
CA2900855A1 (en) 2016-02-21
CY1119771T1 (el) 2018-06-27
JP2017524022A (ja) 2017-08-24
EP3183247B9 (en) 2018-07-25
CU20170015A7 (es) 2017-06-05
TN2017000044A1 (en) 2018-07-04
EA201700077A1 (ru) 2017-07-31
CA2900855C (en) 2022-03-15
AU2015304883A1 (en) 2017-03-02
NO2721710T3 (ro) 2018-03-31
ES2655971T3 (es) 2018-02-22
US10463675B2 (en) 2019-11-05
WO2016027195A1 (en) 2016-02-25
BR112017003054B1 (pt) 2023-04-11
MX2017002241A (es) 2017-05-03
US10980815B2 (en) 2021-04-20
ZA201701005B (en) 2019-07-31
MA40587A (fr) 2017-06-28
CN107074867A (zh) 2017-08-18
US20170239264A1 (en) 2017-08-24
HUE035553T2 (hu) 2018-05-02
ME02856B (me) 2018-04-20
PE20171177A1 (es) 2017-08-22
CO2017001603A2 (es) 2017-05-10
UY36275A (es) 2016-04-01
EA032609B1 (ru) 2019-06-28
ECSP17010156A (es) 2017-11-30
JP6218260B2 (ja) 2017-10-25
UA117976C2 (uk) 2018-10-25
NZ729005A (en) 2020-06-26
US20200038409A1 (en) 2020-02-06
DK3183247T3 (en) 2018-01-15
IL250709B (en) 2019-05-30
US20160052930A1 (en) 2016-02-25
US20210377495A1 (en) 2021-12-02
GEP20197003B (en) 2019-07-25
MD20170016A2 (ro) 2017-08-31
MD4800C1 (ro) 2022-10-31
AR101599A1 (es) 2016-12-28
CN107074867B (zh) 2019-10-22
PL3183247T3 (pl) 2018-03-30
AP2017009748A0 (en) 2017-02-28
DOP2017000048A (es) 2017-06-30
EP3183247A1 (en) 2017-06-28

Similar Documents

Publication Publication Date Title
MD4800B1 (ro) Compuşi de aminopirimidinil ca inhibitori de JAK
PH12018502125A1 (en) Bipyrazole derivatives as jak inhibitors
PH12016501972A1 (en) Bicyclic-fused heteroaryl or aryl compounds and their use as irak4 inhibitors
MD4650B1 (ro) Derivaţi de chinazolină utilizaţi în tratamentul HIV
MX2016013689A (es) Compuestos 4-amino-imidazoquinolina.
MD4820C1 (ro) Compuşi dihidroizochinolinonici substituiţi
MY197698A (en) Oxysterols and methods of use thereof
EA201891063A1 (ru) Производные дигидроимидазопиразинона, применимые в лечении рака
MX2016015565A (es) Ciertos inhibidores de la proteina quinasa.
MX2017004618A (es) Inhibidores de la biosintesis de sulfato de heparano para el tratamiento de enfermedades.
TW201613864A (en) Novel compounds
MD20170011A2 (ro) Compuşi imidazopiridazinici
PH12017500595B1 (en) Aldosterone synthase inhibitors
MX2018005004A (es) Compuestos de indazol substituidos como inhibidores de rorgammat y sus usos.
EA201700356A1 (ru) Новые циклопропанбензофуранилпиридопиразиндионы
MD20160111A2 (ro) Derivaţi diheterociclici legaţi de cicloalchil
MX2017002544A (es) Derivados de isoquinolinona utiles en el tratamiento contra el cancer.
PH12016502480A1 (en) Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases
MX2017002627A (es) Derivados de polieteres macrociclicos de n-aril-2-amino-4-aril-pir imidina como inhibidores de ftl3 y jak.
MX2018004879A (es) Nuevos derivados de piridona y su uso como inhibidores de quinasas.
MX2017013103A (es) Metodos para el tratamiento de trastornos cardiovasculares.
MX2017002747A (es) Derivados de polieteres macrociclicos de n-aril-triciclopirimidin- 2-amino como inhibidores de ftl3 y jak.
MY192305A (en) Bipyrazole derivatives as jak inhibitors

Legal Events

Date Code Title Description
FG4A Patent for invention issued