HRP20230612T1 - Formulacije kopanlisiba - Google Patents

Formulacije kopanlisiba Download PDF

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Publication number
HRP20230612T1
HRP20230612T1 HRP20230612TT HRP20230612T HRP20230612T1 HR P20230612 T1 HRP20230612 T1 HR P20230612T1 HR P20230612T T HRP20230612T T HR P20230612TT HR P20230612 T HRP20230612 T HR P20230612T HR P20230612 T1 HRP20230612 T1 HR P20230612T1
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Croatia
Prior art keywords
copanlisib
solid containing
lyophilized solid
amount
containing copanlisib
Prior art date
Application number
HRP20230612TT
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English (en)
Inventor
Julia FREUNDLIEB
Tia JACOBS
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Bayer Pharma Aktiengesellschaft
Bayer Consumer Care Ag
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Publication date
Priority claimed from EP17207771.1A external-priority patent/EP3498266A1/en
Application filed by Bayer Pharma Aktiengesellschaft, Bayer Consumer Care Ag filed Critical Bayer Pharma Aktiengesellschaft
Publication of HRP20230612T1 publication Critical patent/HRP20230612T1/hr

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    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Luminescent Compositions (AREA)
  • Road Signs Or Road Markings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Claims (14)

1. Stabilna, liofilizirana krutina koja sadrži kopanlisib, pogodna za razrjeđivanje i za terapeutske primjene, te navedena krutina sadrži: • kopanlisib, naročito u količini prikladnoj kao terapijska doza, • jedno ili više sredstava za podešavanje pH, što je sredstvo za puferiranje koje se sastoji od slabe kiseline, kao što je na primjer limunska kiselina, i jake baze, kao što je na primjer natrijev hidroksid, i • sredstvo za povećanje volumena, pri čemu je navedeno sredstvo za povećanje volumena manitol, navedena krutina ima pH između 4 i 5 (uključivo) kada se rekonstituira s prikladnim razrjeđivačem, kao što je sterilna voda za injekcije ili sterilna vodena otopina natrijevog klorida, naročito na primjer 0.9% vodena otopina natrijevog klorida, navedena terapijska doza je 30, 45 ili 60 mg kopanlisiba.
2. Liofilizirana krutina koja sadrži kopanlisib prema zahtjevu 1, naznačena time što je navedeno pufersko sredstvo limunska kiselina i natrijev hidroksid.
3. Liofilizirana krutina koja sadrži kopanlisib prema zahtjevu 1 ili 2, koja sadrži limunsku kiselinu u količini od 0,7-75% m/m, naročito 1,5-30% m/m, naročito 2,98% m/m, navedene liofilizirane krutine koja sadrži kopanlisib.
4. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 3, koja sadrži natrijev hidroksid u količini od 0-6% m/m, naročito 3,3-4,0% m/m, naročito 3,7% m/m, navedene liofilizirane krutine koja sadrži kopanlisib.
5. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 4, koja sadrži natrijev hidroksid u količini od 0,01-6% m/m, naročito 3,3-4,0% m/m, naročito 3,7% m/m, navedene liofilizirane krutine koja sadrži kopanlisib.
6. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 5, koja sadrži manitol u količini od 15,4-82,1% m/m, naročito 30,8-82,1% m/m, naročito 61,6% m/m, navedene liofilizirane krutine koja sadrži kopanlisib.
7. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 6, koja sadrži navedenu slobodnu bazu kopanlisiba u količini od 7,7-92,4% m/m, naročito 7,7-61,6% m/m, naročito 30,8% m/m, liofilizirane krutine koja sadrži kopanlisib.
8. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 7, naznačena time što: • navedena terapijska doza kopanlisiba je u količini od 30,8% m/m navedene liofilizirane krutine koja sadrži kopanlisib, • navedena limunska kiselina je u količini od 2,98% m/m navedene liofilizirane krutine koja sadrži kopanlisib, • navedeni natrijev hidroksid je u količini od 3,7% m/m navedene liofilizirane krutine koja sadrži kopanlisib, i navedeni manitol je u količini od 61,6% m/m, navedene liofilizirane krutine koja sadrži kopanlisib, navedena liofilizirana krutina koja sadrži kopanlisib, kada se rekonstituira s prikladnim razrjeđivačem, kao što je sterilna voda za injekcije ili sterilna vodena otopina natrijevog klorida, na primjer naročito 0,9% vodena otopina natrijevog klorida, ima pH između 4 i 5 (uključivo).
9. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 8, naznačena time što: • navedena terapijska doza kopanlisiba je u količini od 30, 45 ili 60 mg, • navedena limunska kiselina je u količini od 5,8 mg, • navedeni natrijev hidroksid je u količini od 6,3 mg, i • navedeni manitol je u količini od 120 mg, navedena liofilizirana krutina koja sadrži kopanlisib, kada se rekonstituira s prikladnim razrjeđivačem, kao što je sterilna voda za injekcije ili sterilna vodena otopina natrijevog klorida, naročito na primjer 0,9% vodena otopina natrijevog klorida, ima pH između 4 i 5 (uključivo).
10. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 9, naznačena time što: • navedena terapijska doza kopanlisiba je u količini od 80 mg, • navedena limunska kiselina je u količini od 7,7 mg, • navedeni natrijev hidroksid je u količini od 8,4 mg, i • navedeni manitol je u količini od 160 mg, navedena liofilizirana krutina koja sadrži kopanlisib, kada se rekonstituira s prikladnim razrjeđivačem, kao što je sterilna voda za injekcije ili sterilna vodena otopina natrijevog klorida, naročito na primjer 0,9% vodena otopina natrijevog klorida, ima pH između 4 i 5 (uključivo).
11. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 10, naznačena time što je prah ili kolač.
12. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 11, naznačena time što je sadržana u jednom spremniku, naročito zatvorenom spremniku, naročito bočici za injekciju, točnije bočici za injekciju od 6 ml.
13. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 12, naznačena time što sadrži kopanlisib u količini od 68,4 mg.
14. Liofilizirana krutina koja sadrži kopanlisib prema bilo kojem od zahtjeva 1 do 13, za upotrebu u liječenju ili profilaksi raka, naročito ne-Hodgkinovog limfoma (NHL), kao što je 1. linija, 2. linija ili do 9 prethodnih tretmana, relapsirajućeg, refraktornog, indolentnog NHL, naročito folikularnog limfoma (FL), limfoma rubne zone (MZL), malog limfocitnog limfoma (SLL), limfoplazmocitoidne/Waldenströmove makroglobulinemije (LPL-WM), ili agresivnog NHL, naročito difuznog limfoma velikih B stanica (DLBCL), limfoma stanica plašta (MCL), perifernog T-staničnog limfoma (PTCL), transformiranog limfoma (TL), ili kronične limfocitne leukemije (CLL), kao monoterapija ili u kombinaciji s jednim ili više imunoterapijskih, kemoterapijskih ili imuno-kemoterapijskih sredstava protiv raka.
HRP20230612TT 2017-09-08 2018-09-06 Formulacije kopanlisiba HRP20230612T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP17190117 2017-09-08
EP17207771.1A EP3498266A1 (en) 2017-12-15 2017-12-15 Formulations of copanlisib
PCT/EP2018/073965 WO2019048527A1 (en) 2017-09-08 2018-09-06 COPANLISIB FORMULATIONS
EP18762107.3A EP3678644B1 (en) 2017-09-08 2018-09-06 Formulations of copanlisib

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HRP20230612T1 true HRP20230612T1 (hr) 2023-09-29

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US (1) US20200281932A1 (hr)
EP (1) EP3678644B1 (hr)
JP (2) JP2020533292A (hr)
KR (1) KR20200052326A (hr)
CN (1) CN111278430A (hr)
AU (1) AU2018328812A1 (hr)
BR (1) BR112020004545A2 (hr)
CA (1) CA3074890A1 (hr)
CL (1) CL2020000584A1 (hr)
CO (1) CO2020002628A2 (hr)
CR (1) CR20200111A (hr)
CU (1) CU24607B1 (hr)
DK (1) DK3678644T3 (hr)
DO (1) DOP2020000054A (hr)
ES (1) ES2950663T3 (hr)
FI (1) FI3678644T3 (hr)
GE (1) GEP20237486B (hr)
HR (1) HRP20230612T1 (hr)
HU (1) HUE063178T2 (hr)
IL (1) IL272857B2 (hr)
JO (1) JOP20200053A1 (hr)
LT (1) LT3678644T (hr)
MA (1) MA50068A (hr)
MX (1) MX2020002633A (hr)
NI (1) NI202000019A (hr)
PH (1) PH12020500448A1 (hr)
PL (1) PL3678644T3 (hr)
RS (1) RS64316B1 (hr)
SG (1) SG11202001696QA (hr)
SI (1) SI3678644T1 (hr)
TW (1) TWI794288B (hr)
UA (1) UA126817C2 (hr)
UY (1) UY37868A (hr)
WO (1) WO2019048527A1 (hr)
ZA (1) ZA202002378B (hr)

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Publication number Priority date Publication date Assignee Title
EP4070785B1 (en) 2021-04-06 2023-11-08 Synthon B.V. Lyophilized composition of copanlisib salt
CN115252613B (zh) * 2022-08-09 2024-01-12 北京清华长庚医院 药物组合物及其在逆转仑伐替尼耐药性中的用途
WO2024069239A1 (en) * 2022-09-28 2024-04-04 Urogen Pharma Ltd. Compositions comprising a thermoreversible hydrogel, and having an extended in-use period

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Publication number Priority date Publication date Assignee Title
NZ539062A (en) 2002-09-30 2007-05-31 Bayer Pharmaceuticals Corp Fused azole-pyrimidine derivatives exhibiting enhanced potency for phosphotidylinositol-3-kinase (P13K) inhibition
AR064106A1 (es) 2006-12-05 2009-03-11 Bayer Schering Pharma Ag Derivados de 2,3-dihidroimidazo [1,2-c] quinazolina sustituida utiles para el tratamiento de enfermedades y trastornos hiper-proliferativos asociados con la angiogenesis
EP2508525A1 (en) 2011-04-05 2012-10-10 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts
EP3018127A1 (en) 2014-11-07 2016-05-11 Bayer Pharma Aktiengesellschaft Synthesis of copanlisib and its dihydrochloride salt
CA3012951A1 (en) * 2016-02-01 2017-08-10 Bayer Pharma Aktiengesellschaft Copanlisib biomarkers
WO2017134000A1 (en) * 2016-02-01 2017-08-10 Bayer Pharma Aktiengesellschaft Copanlisib biomarkers

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IL272857A (en) 2020-04-30
UA126817C2 (uk) 2023-02-08
NI202000019A (es) 2020-08-28
TW201919636A (zh) 2019-06-01
IL272857B2 (en) 2024-03-01
SI3678644T1 (sl) 2023-08-31
AU2018328812A1 (en) 2020-03-12
MA50068A (fr) 2021-06-02
ZA202002378B (en) 2023-10-25
CO2020002628A2 (es) 2020-04-01
CU20200017A7 (es) 2020-11-30
EP3678644B1 (en) 2023-05-03
HUE063178T2 (hu) 2023-12-28
CN111278430A (zh) 2020-06-12
CA3074890A1 (en) 2019-03-14
WO2019048527A1 (en) 2019-03-14
CR20200111A (es) 2020-07-24
EP3678644A1 (en) 2020-07-15
DK3678644T3 (da) 2023-07-31
US20200281932A1 (en) 2020-09-10
DOP2020000054A (es) 2020-09-30
TWI794288B (zh) 2023-03-01
UY37868A (es) 2019-04-30
LT3678644T (lt) 2023-06-26
KR20200052326A (ko) 2020-05-14
JP2020533292A (ja) 2020-11-19
MX2020002633A (es) 2020-07-13
FI3678644T3 (fi) 2023-07-28
IL272857B1 (en) 2023-11-01
GEP20237486B (en) 2023-03-27
SG11202001696QA (en) 2020-03-30
CU24607B1 (es) 2022-06-06
ES2950663T3 (es) 2023-10-11
JP2023071917A (ja) 2023-05-23
RS64316B1 (sr) 2023-08-31
CL2020000584A1 (es) 2020-08-21
PL3678644T3 (pl) 2023-09-11
BR112020004545A2 (pt) 2020-09-08
PH12020500448A1 (en) 2021-02-08
JOP20200053A1 (ar) 2020-03-08

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