[go: up one dir, main page]

AR076509A1 - Sal de abt-263 y formas en estado solido de la misma - Google Patents

Sal de abt-263 y formas en estado solido de la misma

Info

Publication number
AR076509A1
AR076509A1 ARP100101467A ARP100101467A AR076509A1 AR 076509 A1 AR076509 A1 AR 076509A1 AR P100101467 A ARP100101467 A AR P100101467A AR P100101467 A ARP100101467 A AR P100101467A AR 076509 A1 AR076509 A1 AR 076509A1
Authority
AR
Argentina
Prior art keywords
methyl
crystalline
abt
powder
compound
Prior art date
Application number
ARP100101467A
Other languages
English (en)
Inventor
Deliang Zhou
Thomas Borchardt
Paul Brackemeyer
Nathaniel Catron
Geoff Zhang
Rodger Henry
Xiaochun Lou
Matthew Ravn
Original Assignee
Abbott Lab
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
Application filed by Abbott Lab filed Critical Abbott Lab
Publication of AR076509A1 publication Critical patent/AR076509A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La ABT-263 bis-HCI y sus formas polimorficas cristalinas son ingredientes farmacéuticos activos apropiados para composiciones farmacéuticas utiles en el tratamiento de una enfermedad caracterizada por la sobreexpresion de una o más proteínas antiapoptoticas de la familia Bc1-2, por ejemplo, el cáncer. Se proveen además, procedimientos de preparacion de los mismos. Reivindicacion 1: Un compuesto caracterizado porque es bis-clorhidrato de N-(4-(4-((2-(4-clorofeniI)-5,5-dimetiI-1-ciclohex-1-en-1-iI)metil)piperazin-1-iI)benzoil)-4-(((1R)-3-(morfolin-4-il)-1-((fenilsulfanil)metil)propil)amino-3-((trifluorometil)sulfonil)bencenosulfonamida (ABT-263 bis-HCI). Reivindicacion 4: El compuesto de la reivindicacion 1 en su forma cristalina polimorfica 1, caracterizado porque al menos presenta picos en una o más cualesquiera de las siguientes posiciones en la difraccion de rayos X en polvo: 6,8, 7,2, 8,5, 18,5 y 18,7 °2theta +- 0,2s2theta. Reivindicacion 6: La forma polimorfica cristalina de la reivindicacion 4, caracterizada porque presenta un patron de difraccion de rayos X en polvo sustancialmente como el que se detalla en la siguiente tabla: Posicion del pico (°2theta)/ Intensidad relativa 6,8/59,0; 7,2/75,9; 8,5/14,3; 9,3/4,3; 11,2/6,5; 13,8/15,8; 14,0/17,7; 14,9/9,5; 16,7/17,5; 17,5/15,7; 18,2/52,2; 18,5/100,0; 18,7/95,4. Reivindicacion 7: El compuesto de la reivindicacion 1 en su forma cristalina polimorfica II, caracterizado porque al menos presenta un pico en la difraccion de rayos X en polvo en 3,7 o 7,4 s2theta +- 0,2 s2theta. Reivindicacion 9: La forma polimorfica cristalina de la reivindicacion 7, caracterizada porque presenta un patron de difraccion de rayos X en polvo sustancialmente como el que se detalla en la siguiente tabla: posicion del pico (s2theta)/ intensidad relativa: 3,7/6.0; 7,4/100,0; 12,1/5,3; 15,6/8,6; 16,1/16,2; 16,6/21,6; 18,3/70,2; 19,0/13,4. Reivindicacion 10: El compuesto de la reivindicacion 1, caracterizado porque toma la forma de un solvato cristalino que comprende ABT-263 bis-HCI solvatado con un solvente orgánico. Reivindicacion 11: El solvato de la reivindicacion 10, caracterizado porque el solvente orgánico se selecciona del grupo que consiste en etanol, 1-propanol, 2-propanol, 2-butanol, t-butanol, nitrometano, acetonitrilo, propionitrilo, formato de etilo, acetato de metilo, acetato de etilo, acetato de isopropilo, acetona, metil etil cetona, metil isopropil cetona, 1,4-dioxano, benceno, tolueno y éter butílico.
ARP100101467A 2009-04-30 2010-04-30 Sal de abt-263 y formas en estado solido de la misma AR076509A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US17427409P 2009-04-30 2009-04-30

Publications (1)

Publication Number Publication Date
AR076509A1 true AR076509A1 (es) 2011-06-15

Family

ID=42288743

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101467A AR076509A1 (es) 2009-04-30 2010-04-30 Sal de abt-263 y formas en estado solido de la misma

Country Status (17)

Country Link
US (1) US8362013B2 (es)
EP (1) EP2424849A1 (es)
JP (1) JP2012525433A (es)
KR (1) KR20120005538A (es)
CN (1) CN102414186A (es)
AR (1) AR076509A1 (es)
AU (1) AU2010242923A1 (es)
BR (1) BRPI1014369A2 (es)
CA (1) CA2758740A1 (es)
IL (1) IL215472A0 (es)
MX (1) MX2011011511A (es)
RU (1) RU2011148521A (es)
SG (1) SG175146A1 (es)
TW (1) TW201041882A (es)
UY (1) UY32598A (es)
WO (1) WO2010127190A1 (es)
ZA (1) ZA201107592B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100280031A1 (en) * 2009-04-30 2010-11-04 Paul David Lipid formulation of apoptosis promoter
US8362013B2 (en) 2009-04-30 2013-01-29 Abbvie Inc. Salt of ABT-263 and solid-state forms thereof
US8728516B2 (en) * 2009-04-30 2014-05-20 Abbvie Inc. Stabilized lipid formulation of apoptosis promoter
TWI471321B (zh) * 2009-06-08 2015-02-01 亞培公司 Bcl-2族群抑制劑之口服醫藥劑型
TWI532484B (zh) * 2009-06-08 2016-05-11 艾伯維有限公司 包含凋亡促進劑之固態分散劑
MX2012003408A (es) * 2009-09-20 2012-08-03 Abbott Lab Formas cristalinas de abt-263 y solvatos para uso para tratar enfermedades relacionadas con la proteina bcl-2.
CA2780177A1 (en) * 2009-12-22 2011-06-30 Abbott Laboratories Abt-263 capsule
UA113500C2 (xx) 2010-10-29 2017-02-10 Одержані екструзією розплаву тверді дисперсії, що містять індукуючий апоптоз засіб
CN102584744B (zh) * 2011-01-06 2015-07-01 上海药明康德新药开发有限公司 4-(4-((2-(4-氯苯基)-5,5-二甲基环己基-1-烯)甲基)哌嗪-1-基)苯甲酸的合成方法
MX2016001304A (es) 2013-07-30 2016-04-07 Gilead Connecticut Inc Polimorfo de inhibidores de syk.
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
CA2939121C (en) * 2014-01-28 2020-11-24 Mayo Foundation For Medical Education And Research Effective treatment of osteoarthritis, pulmonary disease, ophthalmic disease, and atherosclerosis by removing senescent cells at the site of the disease
WO2015157120A1 (en) * 2014-04-06 2015-10-15 Abraxis Bioscience, Llc Combination therapy comprising nanoparticles of a taxane and albumin with abt-263 in methods for treating cancer
MX2017000610A (es) 2014-07-14 2017-04-27 Gilead Sciences Inc Metodos combinados para tratar canceres.
TW201639573A (zh) 2015-02-03 2016-11-16 吉李德科學股份有限公司 有關治療癌症之合併治療
US20180133212A1 (en) 2016-11-03 2018-05-17 Gilead Sciences, Inc. Combination of a bcl-2 inhibitor and a bromodomain inhibitor for treating cancer
CN115028640A (zh) 2017-08-25 2022-09-09 吉利德科学公司 Syk抑制剂的多晶型物
KR20210131372A (ko) 2019-02-22 2021-11-02 크로노스 바이오, 인코포레이티드 Syk 억제제로서의 축합된 피라진의 고체 형태
JP2022553820A (ja) 2019-11-05 2022-12-26 アッヴィ・インコーポレイテッド 骨髄線維症及びmpn関連障害をナビトクラクスで処置する際に使用するための投与レジメン
US20230165806A1 (en) * 2021-11-19 2023-06-01 Board Of Regents, The University Of Texas System Topical Therapy of Skin Fibrosis and Melanoma

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US630663A (en) * 1899-05-01 1899-08-08 Wallace George Cook Combined hay and stock rack.
US5665379A (en) 1990-09-28 1997-09-09 Pharmacia & Upjohn Aktiebolag Lipid particle forming matrix, preparation and use thereof
US5536729A (en) 1993-09-30 1996-07-16 American Home Products Corporation Rapamycin formulations for oral administration
IL111004A (en) 1993-09-30 1998-06-15 American Home Prod Oral formulations of rapamycin
US5759548A (en) 1993-11-30 1998-06-02 Lxr Biotechnology Inc. Compositions which inhibit apoptosis, methods of purifying the compositions and uses thereof
GB9405304D0 (en) 1994-03-16 1994-04-27 Scherer Ltd R P Delivery systems for hydrophobic drugs
US5538737A (en) 1994-11-30 1996-07-23 Applied Analytical Industries, Inc. Oral compositions of H2 -antagonists
US6964946B1 (en) 1995-10-26 2005-11-15 Baker Norton Pharmaceuticals, Inc. Oral pharmaceutical compositions containing taxanes and methods of treatment employing the same
BE1011899A6 (fr) 1998-04-30 2000-02-01 Ucb Sa Compositions pharmaceutiques gelifiables utilisables.
US6294192B1 (en) 1999-02-26 2001-09-25 Lipocine, Inc. Triglyceride-free compositions and methods for improved delivery of hydrophobic therapeutic agents
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
US6309663B1 (en) 1999-08-17 2001-10-30 Lipocine Inc. Triglyceride-free compositions and methods for enhanced absorption of hydrophilic therapeutic agents
US7973161B2 (en) 2003-11-13 2011-07-05 Abbott Laboratories Apoptosis promoters
DK1888550T3 (da) 2005-05-12 2014-09-29 Abbvie Bahamas Ltd Apoptosepromotorer
JP2009513642A (ja) * 2005-10-25 2009-04-02 アボット・ラボラトリーズ 低水溶解度の薬剤を含む製剤およびそれの使用方法
CN101939008A (zh) 2007-12-06 2011-01-05 雅培制药有限公司 用于治疗癌症的abt-263经口组合物
CN101220008B (zh) 2008-01-21 2011-04-27 中国科学院广州生物医药与健康研究院 化合物abt-263的合成方法
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
US20100278921A1 (en) 2009-04-30 2010-11-04 Fischer Cristina M Solid oral formulation of abt-263
US8362013B2 (en) 2009-04-30 2013-01-29 Abbvie Inc. Salt of ABT-263 and solid-state forms thereof
US20100297194A1 (en) 2009-04-30 2010-11-25 Nathaniel Catron Formulation for oral administration of apoptosis promoter
US8728516B2 (en) 2009-04-30 2014-05-20 Abbvie Inc. Stabilized lipid formulation of apoptosis promoter
EP2442789A1 (en) 2009-06-18 2012-04-25 Abbott Laboratories Stable nanoparticulate drug suspension
MX2012003408A (es) 2009-09-20 2012-08-03 Abbott Lab Formas cristalinas de abt-263 y solvatos para uso para tratar enfermedades relacionadas con la proteina bcl-2.
CN101798292A (zh) 2010-03-29 2010-08-11 无锡好芳德药业有限公司 ABT-263衍生的新型Bcl-2蛋白抑制剂的制备

Also Published As

Publication number Publication date
US20100305125A1 (en) 2010-12-02
EP2424849A1 (en) 2012-03-07
MX2011011511A (es) 2011-11-18
IL215472A0 (en) 2011-12-29
KR20120005538A (ko) 2012-01-16
RU2011148521A (ru) 2013-06-10
WO2010127190A1 (en) 2010-11-04
CA2758740A1 (en) 2010-11-04
US8362013B2 (en) 2013-01-29
BRPI1014369A2 (pt) 2016-04-05
SG175146A1 (en) 2011-11-28
AU2010242923A1 (en) 2011-11-17
UY32598A (es) 2010-12-31
TW201041882A (en) 2010-12-01
CN102414186A (zh) 2012-04-11
ZA201107592B (en) 2012-06-27
JP2012525433A (ja) 2012-10-22

Similar Documents

Publication Publication Date Title
AR076509A1 (es) Sal de abt-263 y formas en estado solido de la misma
MX2021009763A (es) Derivados de 3-(1-oxo-5-(piperidin-4-il)isoindolin-2-il)piperidina -2,6-diona y usos de los mismos.
EA202192029A1 (ru) Замещенные производные 3-(1-оксоизоиндолин-2-ил)пиперидин-2,6-диона и варианты их применения
PE20190811A1 (es) Derivados de pirazolopirimidinas como inhibidor de quinasa
WO2015058163A3 (en) Heteromaromatic compounds useful for the treatment of prolferative diseases
WO2018136202A3 (en) Compounds and methods for cdk8 modulation and indications therefor
PE20170189A1 (es) Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1
CY1113395T1 (el) Σταθερη φαρμακευτικη συνθεση που περιεχει πυριμιδινη-σουλφαμιδη
EP4295852A3 (en) Piperidine derivatives as inhibitors of cyclin dependent kinase 7 (cdk7)
PE20131143A1 (es) Nuevas aminopirazoloquinazolinas
UY26872A1 (es) Derivados de la 4- fenil piridina
CY1112886T1 (el) Ανοσοκατασταλτικος παραγοντας ο οποιος περιλαμβανει μια ετεροκυκλικη ενωση ως δραστικο συστατικο
CU23550B7 (es) Derivados de pirrolo-pirazol sustituidos como inhibidores de quinasa
UY27617A1 (es) 2 - (piridin -2 - ilamino) - pirido (2,3-d ) pirimidin -7 onas
AR084639A1 (es) Formas polimorficas de acido 2-(5-bromo-4-(4-ciclopropilnaftalen-1-il)-4h-1,2,4-triazol-3-iltio)acetico y usos del mismo
CR9221A (es) Procesos para preparar eteres aromaticos
MX392270B (es) Oxisteroles sustituidos en c7 y metodos de uso de los mismos.
ATE455103T1 (de) Als antikoagulationsmittel geeignete phenylglycinamid- und pyridylglycinamidderivate
EP2205088A4 (en) NAPHTHALIN-BASED INHIBITORS OF ANTI-APOPTOTIC PROTEINS
AR068528A1 (es) Formas solidas de n-(5-tert-butil-isoxazol-3-il)-n'-(4(7-(2-morfolin-4-il-etoxi) imidazol(2,1-b)(1,3)benzotiazol-2-il)fenil)urea, composiciones con las mismas y usos de los mismos
AR058587A1 (es) Compuestos de pirrolo-1,5-naftiridinona,su uso como agentes antibacterianos, composiciones farmaceuticas que los contienen y compuestos intermediarios para preparar dichos compuestos
BRPI0510231A (pt) composto, polimorfo cristalino, cossolvato em metanol e água, cossolvato em metanol-água, cossolvato em etanol-água, composição farmacêutica, método para administrar um agente ativo, método para preparar a forma i do snac, método para preparar a forma ii de snac, método para preparar a forma iii de snac, método para preparar a forma iv de snac, método para preparar a forma v de snac, método para preparar a forma vi de snac, composição farmacêutica e método para preparar snac amorfo
PE20191236A1 (es) Compuestos de pirazolopirimidina y metodos de uso de los mismos
CO2021016433A2 (es) Derivados heterocíclicos condensados
CL2020002550A1 (es) Compuestos de pirazol sustituidos con heteroarilo y uso farmacéutico de los mismos.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal