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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/14—Heterocyclic 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
    • C07D295/155—Heterocyclic 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (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)

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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
US20100280031A1 (en) * 2009-04-30 2010-11-04 Paul David Lipid formulation of apoptosis promoter
TWI471321B (zh) * 2009-06-08 2015-02-01 Abbott Gmbh & Co Kg 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
CN102695702A (zh) 2009-09-20 2012-09-26 雅培制药有限公司 用于治疗bcl-2蛋白相关疾病的abt-263晶体形式和溶剂化物
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
PT3027618T (pt) 2013-07-30 2020-10-12 Kronos Bio Inc Polimorfo de inibidores de syk
TWI662037B (zh) 2013-12-23 2019-06-11 美商基利科學股份有限公司 脾酪胺酸激酶抑制劑
SG10201805670QA (en) * 2014-01-28 2018-08-30 Buck Inst Res Aging Methods and compositions for killing senescent cells and for treating senescence-associated diseases and disorders
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
NZ726365A (en) 2014-07-14 2018-06-29 Gilead Sciences Inc Combinations for treating cancers
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
WO2018085069A1 (en) 2016-11-03 2018-05-11 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
CN115279375A (zh) 2019-11-05 2022-11-01 艾伯维公司 用于以navitoclax治疗骨髓纤维化和mpn相关病症的给药方案
US20230157970A1 (en) * 2021-11-19 2023-05-25 Board Of Regents, The University Of Texas System Targeted Therapy of Kidney Fibrosis

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Also Published As

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

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