PE20171242A1 - Dispersiones solidas extruidas por fusion que contienen un agente inductor de apoptosis - Google Patents
Dispersiones solidas extruidas por fusion que contienen un agente inductor de apoptosisInfo
- Publication number
- PE20171242A1 PE20171242A1 PE2017001230A PE2017001230A PE20171242A1 PE 20171242 A1 PE20171242 A1 PE 20171242A1 PE 2017001230 A PE2017001230 A PE 2017001230A PE 2017001230 A PE2017001230 A PE 2017001230A PE 20171242 A1 PE20171242 A1 PE 20171242A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- compound
- methoxy
- solid
- extruded
- Prior art date
Links
- 230000004927 fusion Effects 0.000 title 1
- 239000007962 solid dispersion Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- -1 4 - {[2- (4-chlorophenyl) -4,4-dimethylcyclohex-1-en-1-yl] methyl} piperazin-1-yl Chemical group 0.000 abstract 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 239000007787 solid Substances 0.000 abstract 3
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 abstract 2
- 239000006185 dispersion Substances 0.000 abstract 2
- 239000011159 matrix material Substances 0.000 abstract 2
- 239000008247 solid mixture Substances 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 abstract 1
- 102000051485 Bcl-2 family Human genes 0.000 abstract 1
- 108700038897 Bcl-2 family Proteins 0.000 abstract 1
- 206010027406 Mesothelioma Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000006907 apoptotic process Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 238000001816 cooling Methods 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000001939 inductive effect Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000001613 neoplastic effect Effects 0.000 abstract 1
- 239000008180 pharmaceutical surfactant Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 239000004094 surface-active agent Substances 0.000 abstract 1
Classifications
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- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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- 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
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
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- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- 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
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- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
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- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
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- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Inorganic Chemistry (AREA)
- Molecular Biology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Biochemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biophysics (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se refiere a dispersiones solidas extruidas por fusion que contienen un agente inductor de apoptosis de formula (I), donde R0 es halo; R1 y R2 son H, metilo o metoxi; R3 y R4 son metilo o metoxi si R1 y R2 son H, o son H si R1 y R2 son metilo o metoxi; A1 y A2 son CH o N; R5 es C1-C4 alquilo o haloalquilo, entre otros; X es -O- o -NH-; Y es -(CH2)n-; n es 0, 1, 2 o 3; R6 es un anillo carbociclico o heterociclico de entre 3 y 7 miembros opcionalmente sustituido, entre otros. Es un compuesto seleccionado 4-(4-{[2-(4-clorofenil)-4,4-dimetilciclohex-1-en-1-il]metil}piperazin-1-il)-2-(1H-indol-5-iloxi)-N-({3-nitro-4-[(1-tetrahidro-2H-piran-4-ilpiperidin-4-il)amino]fenil}sulfonil)benzamida; entre otros. Dicho compuesto es un inhibidor de la familia de las proteinas Bcl-2 disperso en una matriz solida que comprende (a) un vehiculo polimerico soluble en agua farmaceuticamente aceptable y (b) un agente tensioactivo farmaceuticamente aceptable. Tambien se refiere a un proceso de preparacion que comprende someter a una temperatura elevada el compuesto de formula I, (a) y (b), para proveer una mezcla semisolida extruible; extrudir la mezcla semisolida; y enfriar el extrudido resultante para proveer una matriz solida que comprende el vehiculo polimerico y el agente tensioactivo y en el cual esta disperso el compuesto en una forma esencialmente no cristalina. Dichas dispersiones son utiles en el tratamiento de enfermedades neoplasicas tales como cancer, mesotelioma, entre otras
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US40852710P | 2010-10-29 | 2010-10-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20171242A1 true PE20171242A1 (es) | 2017-08-24 |
Family
ID=44903438
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2017001230A PE20171242A1 (es) | 2010-10-29 | 2011-10-05 | Dispersiones solidas extruidas por fusion que contienen un agente inductor de apoptosis |
PE2013000918A PE20140381A1 (es) | 2010-10-29 | 2011-10-05 | Dispersiones solidas extruidas por fusion que contienen un agente inductor de apoptosis |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2013000918A PE20140381A1 (es) | 2010-10-29 | 2011-10-05 | Dispersiones solidas extruidas por fusion que contienen un agente inductor de apoptosis |
Country Status (40)
Country | Link |
---|---|
US (2) | US20120108590A1 (es) |
EP (3) | EP2613769B1 (es) |
JP (2) | JP5902187B2 (es) |
KR (2) | KR101957137B1 (es) |
CN (2) | CN108175749B (es) |
AR (2) | AR083656A1 (es) |
AU (1) | AU2011361704B2 (es) |
BR (1) | BR112013010524A8 (es) |
CA (1) | CA2813985C (es) |
CL (1) | CL2013001120A1 (es) |
CO (1) | CO6781472A2 (es) |
CR (2) | CR20180289A (es) |
CY (1) | CY1119993T1 (es) |
DK (1) | DK2613769T3 (es) |
DO (2) | DOP2013000092A (es) |
EC (2) | ECSP13012647A (es) |
ES (1) | ES2647583T3 (es) |
GT (1) | GT201300102A (es) |
HK (1) | HK1243761A1 (es) |
HR (1) | HRP20171884T1 (es) |
HU (1) | HUE035169T2 (es) |
IL (2) | IL226215A (es) |
LT (1) | LT2613769T (es) |
ME (1) | ME02942B (es) |
MX (2) | MX362113B (es) |
MY (1) | MY189224A (es) |
NO (1) | NO2613769T3 (es) |
NZ (1) | NZ608907A (es) |
PE (2) | PE20171242A1 (es) |
PL (1) | PL2613769T3 (es) |
PT (1) | PT2613769T (es) |
RS (1) | RS56718B1 (es) |
RU (2) | RU2633353C1 (es) |
SG (2) | SG189477A1 (es) |
SI (1) | SI2613769T1 (es) |
TW (2) | TWI535699B (es) |
UA (1) | UA113500C2 (es) |
UY (3) | UY33692A (es) |
WO (1) | WO2012121758A1 (es) |
ZA (2) | ZA201302669B (es) |
Families Citing this family (51)
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US8546399B2 (en) | 2009-05-26 | 2013-10-01 | Abbvie Inc. | Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases |
US20220315555A1 (en) | 2009-05-26 | 2022-10-06 | Abbvie Inc. | Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases |
US9034875B2 (en) | 2009-05-26 | 2015-05-19 | Abbvie Inc. | Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases |
US8628554B2 (en) | 2010-06-13 | 2014-01-14 | Virender K. Sharma | Intragastric device for treating obesity |
US10420665B2 (en) | 2010-06-13 | 2019-09-24 | W. L. Gore & Associates, Inc. | Intragastric device for treating obesity |
US10010439B2 (en) | 2010-06-13 | 2018-07-03 | Synerz Medical, Inc. | Intragastric device for treating obesity |
US9526648B2 (en) | 2010-06-13 | 2016-12-27 | Synerz Medical, Inc. | Intragastric device for treating obesity |
UA113500C2 (xx) | 2010-10-29 | 2017-02-10 | Одержані екструзією розплаву тверді дисперсії, що містять індукуючий апоптоз засіб | |
RU2598345C2 (ru) | 2010-10-29 | 2016-09-20 | Эббви Инк. | Твердые дисперсии, содержащие средства, вызывающие апоптоз |
PT2642999T (pt) | 2010-11-23 | 2017-01-05 | Abbvie Ireland Unlimited Co | Métodos de tratamento que utilizam inibidores seletivos de bcl-2 |
BR112013012740A2 (pt) | 2010-11-23 | 2016-09-13 | Abbvie Inc | sais e formas cristalinas de um agente que induz apoptose |
WO2012177927A1 (en) | 2011-06-21 | 2012-12-27 | Mayo Foundation For Medical Education And Research | Transgenic animals capable of being induced to delete senescent cells |
MX2014007093A (es) | 2011-12-13 | 2014-10-13 | Buck Inst For Res On Aging | Metodos para mejorar terapias medicas. |
WO2013158664A2 (en) | 2012-04-17 | 2013-10-24 | Kythera Biopharmaceuticals, Inc. | Use of engineered viruses to specifically kill senescent cells |
US9901081B2 (en) | 2012-08-23 | 2018-02-27 | Buck Institute For Research On Aging | Transgenic mouse for determining the role of senescent cells in cancer |
US9901080B2 (en) | 2012-08-23 | 2018-02-27 | Buck Institute For Research On Aging | Transgenic mouse having a transgene that converts a prodrug into a cytotoxic compound in senescent cells |
WO2014039855A1 (en) | 2012-09-07 | 2014-03-13 | Genentech, Inc. | Combination therapy of a type ii anti-cd20 antibody with a selective bcl-2 inhibitor |
WO2014048782A1 (en) * | 2012-09-27 | 2014-04-03 | Basf Se | A storage-stable dust-free homogeneous particulate formulation comprising at least one water-soluble vitamin e-derivative and at least one hydrophilic polymer |
UY39847A (es) | 2013-03-13 | 2022-09-30 | Abbvie Ireland Unlimited Co | Procesos para la preparación de un agente inductor de la apoptosis |
AR095265A1 (es) | 2013-03-13 | 2015-09-30 | Abbvie Inc | Procesos para la preparación de un agente inductor de la apoptosis |
US20140275082A1 (en) | 2013-03-14 | 2014-09-18 | Abbvie Inc. | Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases |
AU2015211021B2 (en) | 2014-01-28 | 2020-07-02 | Buck Institute For Research On Aging | Methods and compositions for killing senescent cells and for treating senescence-associated diseases and disorders |
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