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AR124662A2 - Formulaciones inmunosupresoras - Google Patents

Formulaciones inmunosupresoras

Info

Publication number
AR124662A2
AR124662A2 ARP220100086A ARP220100086A AR124662A2 AR 124662 A2 AR124662 A2 AR 124662A2 AR P220100086 A ARP220100086 A AR P220100086A AR P220100086 A ARP220100086 A AR P220100086A AR 124662 A2 AR124662 A2 AR 124662A2
Authority
AR
Argentina
Prior art keywords
carbon atoms
alkyl
halogen
substituted
cycloalkyl
Prior art date
Application number
ARP220100086A
Other languages
English (en)
Inventor
Philippe Bouillot
Emeric Reynaud
Original Assignee
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=44022942&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR124662(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR124662A2 publication Critical patent/AR124662A2/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • 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
    • 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
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

La presente invención se refiere a una composición farmacéutica en fase sólida, la cual comprende uno o más excipientes farmacéuticamente aceptables, y un ingrediente farmacéutico activo (“API”), el cual es un compuesto de la fórmula (1) o (2), o una sal, solvato o hidrato farmacológicamente aceptable del mismo, en donde el ingrediente farmacéutico activo (API) no se expone a un compuesto básico. Reivindicación 1: Una composición farmacéutica en fase sólida, la cual comprende uno o más excipientes farmacéuticamente aceptables, y un ingrediente farmacéutico activo (“API”), el cual es un compuesto de la fórmula (1) o (2), o una sal, solvato o hidrato farmacológicamente aceptable del mismo, en donde el ingrediente farmacéutico activo (API) no se expone a un compuesto básico, en donde: A es COOR⁵, OPO(OR⁵)₂, PO(OR⁵)₂, SO₂OR⁵, POR⁵OR⁵ ó 1H-tetrazol-5-ilo, en donde R⁵ es H o un grupo formador de éster; W es un enlace, alquileno de 1 a 3 átomos de carbono, o alquenileno de 2 a 3 átomos de carbono; Y es arilo de 6 a 10 átomos de carbono, o heteroarilo de 3 a 9 átomos de carbono opcionalmente sustituido por 1 a 3 radicales seleccionados a partir de halógeno, NO₂, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono; alquilo de 1 a 6 átomos de carbono sustituido por halógeno, y alcoxilo de 1 a 6 átomos de carbono sustituido por halógeno; Z se selecciona a partir de: los compuestos del grupo de fórmulas (3); en donde los asteriscos de Z indican el punto de unión entre -C(R³)-(R⁴)- y A de la fórmula (1) o (2), respectivamente; R⁶ se selecciona a partir de hidrógeno y alquilo de 1 a 6 átomos de carbono; y J¹ y J² son independientemente metileno o un heteroátomo seleccionado a partir de S, O y NR⁵; en donde R⁵ se selecciona a partir de hidrógeno y alquilo de 1 a 6 átomos de carbono; y cualquier alquileno de Z puede estar adicionalmente sustituido por uno a tres radicales seleccionados a partir de halógeno, hidroxilo, alquilo de 1 a 6 átomos de carbono; o R⁶ se puede unir a un átomo de carbono de Y para formar un anillo de 5 a 7 miembros; R¹ es arilo de 6 a 10 átomos de carbono, o heteroarilo de 3 a 9 átomos de carbono opcionalmente sustituido por alquilo de 1 a 6 átomos de carbono, arilo de 6 a 10 átomos de carbono, arilo de 6 a 10 átomos de carbono-alquilo de 1 a 4 átomos de carbono, heteroarilo de 3 a 9 átomos de carbono, heteroarilo de 3 a 9 átomos de carbono-alquilo de 1 a 4 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono-alquilo de 1 a 4 átomos de carbono, hetero-cicloalquilo de 3 a 8 átomos de carbono, o hetero-cicloalquilo de 3 a 8 átomos de carbono-alquilo de 1 a 4 átomos de carbono; en donde cualquier arilo, heteroarilo, cicloalquilo o hetero-cicloalquilo de R¹ puede estar sustituido por 1 a 5 grupos seleccionados a partir de halógeno, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, y alquilo de 1 a 6 átomos de carbono o alcoxilo de 1 a 6 átomos de carbono sustituido por halógeno; R² es H, alquilo de 1 a 6 átomos de carbono, alquilo de 1 a 6 átomos de carbono sustituido por halógeno, alquenilo de 2 a 6 átomos de carbono, o alquinilo de 2 a 6 átomos de carbono; y cada uno de R³ ó R⁴ es independientemente H, halógeno, OH, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, o alquilo de 1 a 6 átomos de carbono o alcoxilo de 1 a 6 átomos de carbono sustituido por halógeno. Reivindicación 3: Una composición de la reivindicación 1, en donde el ingrediente farmacéutico activo (API) es el ácido 1-{4-[1-(4-ciclohexil-3-trifluoro-metil-benciloxi-imino)-etil]-2-etil-bencil}-azetidin-3-carboxílico, o una sal farmacéuticamente aceptable. Reivindicación 10: Una tableta que comprende una mezcla comprimida que consiste en ácido 1-{4-[1-(4-ciclohexil-3-trifluoro-metil-benciloxi-imino)-etil]-2-etil-bencil}-azetidin-3-carboxílico, o una sal farmacéuticamente aceptable del mismo, y uno o más excipientes no básicos, estando el ácido 1-{4-[1-(4-ciclohexil-3-trifluoro-metil-benciloxi-imino)-etil]-2-etil-bencil}-azetidin-3-carboxílico, o una sal farmacéuticamente aceptable, en la forma de partículas que tienen un diámetro X₉₀ de 10 micras a 200 micras.
ARP220100086A 2011-01-07 2022-01-17 Formulaciones inmunosupresoras AR124662A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11150431 2011-01-07

Publications (1)

Publication Number Publication Date
AR124662A2 true AR124662A2 (es) 2023-04-19

Family

ID=44022942

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP120100047A AR084801A1 (es) 2011-01-07 2012-01-06 Formulaciones inmunosupresoras
ARP220100086A AR124662A2 (es) 2011-01-07 2022-01-17 Formulaciones inmunosupresoras

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP120100047A AR084801A1 (es) 2011-01-07 2012-01-06 Formulaciones inmunosupresoras

Country Status (36)

Country Link
US (4) US20130273161A1 (es)
EP (2) EP3590507A1 (es)
JP (2) JP6111202B2 (es)
KR (2) KR101951966B1 (es)
CN (1) CN103458877B (es)
AR (2) AR084801A1 (es)
AU (1) AU2012204835B2 (es)
BR (1) BR112013017302B1 (es)
CA (1) CA2823616C (es)
CL (1) CL2013001979A1 (es)
CO (1) CO6761402A2 (es)
CY (1) CY1122182T1 (es)
DK (1) DK2661261T3 (es)
EA (1) EA026144B9 (es)
EC (1) ECSP13012812A (es)
ES (1) ES2751920T3 (es)
GT (1) GT201300178A (es)
HR (1) HRP20191842T1 (es)
HU (1) HUE045612T2 (es)
IL (1) IL227094B (es)
JO (1) JO3619B1 (es)
LT (1) LT2661261T (es)
MA (1) MA34897B1 (es)
MX (2) MX371290B (es)
MY (1) MY161162A (es)
PE (1) PE20140216A1 (es)
PH (1) PH12013501442B1 (es)
PL (1) PL2661261T3 (es)
PT (1) PT2661261T (es)
SG (1) SG191286A1 (es)
SI (1) SI2661261T1 (es)
TN (1) TN2013000257A1 (es)
TW (2) TWI610672B (es)
UA (1) UA114283C2 (es)
WO (1) WO2012093161A1 (es)
ZA (1) ZA201304465B (es)

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Also Published As

Publication number Publication date
PL2661261T3 (pl) 2020-01-31
EA201391018A1 (ru) 2013-11-29
ECSP13012812A (es) 2013-09-30
MX357304B (es) 2018-07-04
GT201300178A (es) 2014-12-30
UA114283C2 (uk) 2017-05-25
ZA201304465B (en) 2014-02-26
PH12013501442B1 (en) 2018-04-20
JP2017141248A (ja) 2017-08-17
JP6111202B2 (ja) 2017-04-05
TW201609092A (zh) 2016-03-16
CL2013001979A1 (es) 2013-11-22
IL227094B (en) 2019-03-31
CO6761402A2 (es) 2013-09-30
KR102166885B1 (ko) 2020-10-19
AU2012204835B2 (en) 2015-07-09
PH12013501442A1 (en) 2013-09-09
PT2661261T (pt) 2019-10-25
US20250084034A1 (en) 2025-03-13
MX2013007909A (es) 2013-08-29
EP2661261A1 (en) 2013-11-13
AR084801A1 (es) 2013-06-26
CA2823616C (en) 2019-01-29
TWI583380B (zh) 2017-05-21
NZ612420A (en) 2015-05-29
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