BR112014004631A2 - derivados de heterociclo bicíclico para o tratamento de hipertensão arterial pulmonar - Google Patents

derivados de heterociclo bicíclico para o tratamento de hipertensão arterial pulmonar

Info

Publication number
BR112014004631A2
BR112014004631A2 BR112014004631A BR112014004631A BR112014004631A2 BR 112014004631 A2 BR112014004631 A2 BR 112014004631A2 BR 112014004631 A BR112014004631 A BR 112014004631A BR 112014004631 A BR112014004631 A BR 112014004631A BR 112014004631 A2 BR112014004631 A2 BR 112014004631A2
Authority
BR
Brazil
Prior art keywords
treatment
arterial hypertension
pulmonary arterial
bicyclic heterocycle
heterocycle derivatives
Prior art date
Application number
BR112014004631A
Other languages
English (en)
Other versions
BR112014004631B1 (pt
Inventor
Michael Saunders Alex
Thomson Christopher
Janus Diana
Shaw Duncan
Bruce Ian
Christopher Loren Jon
Sviridenko Lilya
Furet Pascal
West Ryan
Lewis Sarah
Paul Collingwood Stephen
Chamoin Sylvie
Molteni Valentina
Furminger Vikki
Yeh Vince
Original Assignee
Irm Llc
Novartis Ag
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=47018333&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112014004631(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Irm Llc, Novartis Ag filed Critical Irm Llc
Publication of BR112014004631A2 publication Critical patent/BR112014004631A2/pt
Publication of BR112014004631B1 publication Critical patent/BR112014004631B1/pt

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

resumo patente de invenção: "derivados de heterociclo bicíclico para o tratamento de hipertensão arterial pulmonar". a presente invenção refere-se a derivados heterocíclicos bicíclicos de fórmula i úteis na inibição da atividade biológica mediada pelo receptor de pdgf. i em que a é ou ; e r1, r1a, r2, r3, r4, r5, r6 e x são como definidos aqui.
BR112014004631-0A 2011-09-01 2012-08-31 Derivados de heterociclo bicíclico, seus usos, combinação e composição farmacêuticas BR112014004631B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161530049P 2011-09-01 2011-09-01
US61/530,049 2011-09-01
US201261680119P 2012-08-06 2012-08-06
US61/680,119 2012-08-06
PCT/IB2012/054501 WO2013030802A1 (en) 2011-09-01 2012-08-31 Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension

Publications (2)

Publication Number Publication Date
BR112014004631A2 true BR112014004631A2 (pt) 2017-03-14
BR112014004631B1 BR112014004631B1 (pt) 2020-02-11

Family

ID=47018333

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112014004631-0A BR112014004631B1 (pt) 2011-09-01 2012-08-31 Derivados de heterociclo bicíclico, seus usos, combinação e composição farmacêuticas

Country Status (28)

Country Link
US (2) US8883819B2 (pt)
EP (1) EP2751108B1 (pt)
JP (1) JP5815870B2 (pt)
KR (1) KR101687082B1 (pt)
CN (2) CN105001218B (pt)
AP (1) AP3818A (pt)
AR (1) AR087755A1 (pt)
AU (1) AU2012303674B2 (pt)
BR (1) BR112014004631B1 (pt)
CA (1) CA2845753C (pt)
CL (1) CL2014000459A1 (pt)
CO (1) CO6900139A2 (pt)
CR (1) CR20140099A (pt)
EA (1) EA024068B1 (pt)
ES (1) ES2585048T3 (pt)
HK (1) HK1196126A1 (pt)
IL (1) IL231228A0 (pt)
MA (1) MA35364B1 (pt)
MX (1) MX360316B (pt)
PE (1) PE20141674A1 (pt)
PL (1) PL2751108T3 (pt)
PT (1) PT2751108T (pt)
SG (1) SG11201400253YA (pt)
TN (1) TN2014000067A1 (pt)
TW (1) TW201313718A (pt)
UY (1) UY34305A (pt)
WO (1) WO2013030802A1 (pt)
ZA (1) ZA201401294B (pt)

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US8883819B2 (en) 2011-09-01 2014-11-11 Irm Llc Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
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WO2015089137A1 (en) 2013-12-11 2015-06-18 Karos Pharmaceuticals, Inc. Acylguanidines as tryptophan hydroxylase inhibitors
CN105524058B (zh) 2014-10-21 2018-03-27 广州艾格生物科技有限公司 吡唑并[1,5‑a]吡啶类化合物及其应用
WO2016109501A1 (en) 2014-12-30 2016-07-07 Karos Pharmaceuticals, Inc. Amide compounds as tryptophan hydroxylase inhibitors
US9611201B2 (en) 2015-03-05 2017-04-04 Karos Pharmaceuticals, Inc. Processes for preparing (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol and 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone
GB201801355D0 (en) * 2018-01-26 2018-03-14 Enterprise Therapeutics Ltd Compounds
CN113227093A (zh) 2018-11-14 2021-08-06 阿尔塔万特科学公司 结晶螺环化合物、包含该化合物的剂型、用于疾病治疗的方法和再结晶方法
TW202136234A (zh) * 2019-12-13 2021-10-01 日商日本新藥股份有限公司 作為pdgf受體激酶抑制劑之化合物及組合物
JP7386124B2 (ja) 2020-05-28 2023-11-24 株式会社名村造船所 船舶
US20220031633A1 (en) * 2020-07-28 2022-02-03 Yale University Poly(amine-co-ester) polymeric particles for selective pulmonary delivery
EP4267585A1 (en) 2020-12-23 2023-11-01 Actelion Pharmaceuticals Ltd Pyrazolothiazole carboxamides and their uses as pdgfr inhibitors
TW202313053A (zh) 2021-07-30 2023-04-01 瑞士商艾克泰聯製藥有限公司 吡唑并嘧啶及其作為ｐｄｇｆｒ抑制劑之用途
CN113912530A (zh) * 2021-11-10 2022-01-11 山东汇海医药化工有限公司 一种4-aa中间体废液的处理方法
WO2023247596A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Pyrazolothiazole carboxamides and their uses as pdgfr inhibitors
WO2023247590A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Triazolopyridine and benzoisoxazole carboxamides and their uses as pdgfr inhibitors
WO2023247595A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Pyrazolopyrazine carboxamides and their uses as pdgfr inhibitors
WO2023247593A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Pyrrolopyridine carboxamides and their uses as pdgfr inhibitors
WO2024104968A1 (en) 2022-11-14 2024-05-23 Actelion Pharmaceuticals Ltd Pyrazolopyrrolopyridazines and their uses as pdgfr inhibitors

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