AR084862A1 - Formas solidas de inhibidor de girasa (r) 1-etil-3-[5-[2-(1-hidroxi-1-metil-etil)pirimidin-5-il]-7-(tetrahidrofuran-2-il)-1h-benzimidazol-2-il]urea - Google Patents

Formas solidas de inhibidor de girasa (r) 1-etil-3-[5-[2-(1-hidroxi-1-metil-etil)pirimidin-5-il]-7-(tetrahidrofuran-2-il)-1h-benzimidazol-2-il]urea

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Publication number
AR084862A1
AR084862A1 ARP120100139A ARP120100139A AR084862A1 AR 084862 A1 AR084862 A1 AR 084862A1 AR P120100139 A ARP120100139 A AR P120100139A AR P120100139 A ARP120100139 A AR P120100139A AR 084862 A1 AR084862 A1 AR 084862A1
Authority
AR
Argentina
Prior art keywords
solid
xprd
etil
salt
degrees
Prior art date
Application number
ARP120100139A
Other languages
English (en)
Inventor
Brian Luisi
Yusheng Liao
Mariusz Krawiec
Dean Shannon
Original Assignee
Vertex Pharma
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45615044&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR084862(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR084862A1 publication Critical patent/AR084862A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Formas sólidas de los compuestos de fórmula (1) y sales farmacéuticamente aceptables de los mismos que inhiben girasa bacterial y/o Topo IV y composiciones farmacéuticas que comprende dichas composiciones y sales. Estos compuestos y sales son útiles en el tratamiento de una infección bacterial.Reivindicación 2: El sólido compuesto de acuerdo con la reivindicación 1, en donde dicho sólido es una base libre de forma I sólida. Reivindicación 8: Una sal de ácido clorhídrico del compuesto de la fórmula (1). Reivindicación 9: La sal clorhidrato de acuerdo con la reivindicación 8 en forma sólida. Reivindicación 10: La sal clorhidrato de acuerdo con la reivindicación 9, en donde dicha sal es una forma sólida II. Reivindicación 11: La forma sólida II de acuerdo con la reivindicación 10, en donde dicha forma sólida II se caracteriza por un patrón de difracción de polvos por rayos X (XPRD) que comprende al menos tres posiciones de pico aproximadas (grados 2q ± 0,2) cuando se miden usando radiación Cu Ka, seleccionados del grupo que consiste en 7,0, 9,1, 11,5, 12,3, 12,4, 13,5, 16,4, 17,2, 17,9, 18,2, 19,0, 19,5, 20,6, 20,9, 22,4, 23,0, 23,5, 24,0, 24,5, 26,0, 26,5, 27,1, 27,4, 28,5, 29,4, 30,8, 33,0, cuando el XPRD se recolecta de aproximadamente 5 a aproximadamente 38 grados 2q. Reivindicación 16: El compuesto de sal clorhidrato sólido de acuerdo con la reivindicación 9, en donde dicha sal clorhidrato del compuesto de la fórmula (1) es una forma sólida III. Reivindicación 17: La forma sólida III de acuerdo con la reivindicación 16, en donde dicha forma III se caracteriza por un patrón de difracción de polvos por rayos X (XPRD) que comprende al menos tres posiciones de pico aproximadas (grados 2q ± 0,2) cuando se miden usando radiación Cu Ka, seleccionados del grupo que consiste en 6,9, 9,1, 11,0, 11,7, 12,3, 15,8, 16,9, 18,1, 18,9, 19,8, 20,9, 22,7, 23,4, 24,1, 24,8, 25,3, 27,7, 28,5, 29,5 y 31,4, cuando el XPRD se recolecta de aproximadamente 5 a aproximadamente 38 grados 2q. Reivindicación 21: El compuesto sólido de acuerdo con la reivindicación 1, en donde dicho sólido es una sal amorfa de mesilato de la forma IV. Reivindicación 22: La sal de mesilato amorfa sólida de la forma IV de acuerdo con la reivindicación 21, que se caracteriza por un patrón de difracción de polvos por rayos X (XPRD) usando radiación Cu Ka, caracterizada por un halo amplio sin pico de difracción no discernible.
ARP120100139A 2011-01-14 2012-01-16 Formas solidas de inhibidor de girasa (r) 1-etil-3-[5-[2-(1-hidroxi-1-metil-etil)pirimidin-5-il]-7-(tetrahidrofuran-2-il)-1h-benzimidazol-2-il]urea AR084862A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161433161P 2011-01-14 2011-01-14

Publications (1)

Publication Number Publication Date
AR084862A1 true AR084862A1 (es) 2013-06-26

Family

ID=45615044

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100139A AR084862A1 (es) 2011-01-14 2012-01-16 Formas solidas de inhibidor de girasa (r) 1-etil-3-[5-[2-(1-hidroxi-1-metil-etil)pirimidin-5-il]-7-(tetrahidrofuran-2-il)-1h-benzimidazol-2-il]urea

Country Status (17)

Country Link
US (2) US8481552B2 (es)
EP (1) EP2663558A1 (es)
JP (1) JP2014507413A (es)
KR (1) KR101897950B1 (es)
CN (1) CN103384666A (es)
AR (1) AR084862A1 (es)
AU (1) AU2012205416B2 (es)
BR (1) BR112013017977A2 (es)
CA (1) CA2824401A1 (es)
CL (1) CL2013002026A1 (es)
IL (1) IL227407B (es)
MX (1) MX351555B (es)
RU (1) RU2013137753A (es)
SG (1) SG191924A1 (es)
TW (1) TW201309676A (es)
WO (1) WO2012097270A1 (es)
ZA (1) ZA201305230B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103384666A (zh) 2011-01-14 2013-11-06 沃泰克斯药物股份有限公司 固体形式的促旋酶抑制剂（r）-1-乙基-3-[5-[2-（1-羟基-1-甲基-乙基）嘧啶-5-基]-7-（四氢呋喃-2-基）-1氢-苯并咪唑-2-基]脲
ES2545516T3 (es) * 2011-01-14 2015-09-11 Vertex Pharmaceuticals Incorporated Inhibidores de la pirimidina girasa y la topoisomerasa IV
SG191945A1 (en) * 2011-01-14 2013-08-30 Vertex Pharma Process of making gyrase and topoisomerase iv inhibitors
CN103403000B (zh) * 2011-01-14 2017-05-31 斯派罗吹耐姆公司 固体形式的促旋酶抑制剂（r）‑1‑乙基‑3‑[6‑氟‑5‑[2‑（1‑羟基‑1‑甲基‑乙基）嘧啶‑5‑基]‑7‑（四氢呋喃‑2‑基）‑1氢‑苯并咪唑‑2‑基]脲
US9125922B2 (en) * 2011-06-20 2015-09-08 Vertex Pharmaceuticals Incorporated Phosphate esters of gyrase and topoisomerase inhibitors
WO2014015105A1 (en) * 2012-07-18 2014-01-23 Vertex Pharmaceuticals Incorporated Solid forms of (r)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1h-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof
US9572809B2 (en) 2012-07-18 2017-02-21 Spero Trinem, Inc. Combination therapy to treat Mycobacterium diseases
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SG191945A1 (en) * 2011-01-14 2013-08-30 Vertex Pharma Process of making gyrase and topoisomerase iv inhibitors
CN103384666A (zh) 2011-01-14 2013-11-06 沃泰克斯药物股份有限公司 固体形式的促旋酶抑制剂（r）-1-乙基-3-[5-[2-（1-羟基-1-甲基-乙基）嘧啶-5-基]-7-（四氢呋喃-2-基）-1氢-苯并咪唑-2-基]脲
CN103403000B (zh) * 2011-01-14 2017-05-31 斯派罗吹耐姆公司 固体形式的促旋酶抑制剂（r）‑1‑乙基‑3‑[6‑氟‑5‑[2‑（1‑羟基‑1‑甲基‑乙基）嘧啶‑5‑基]‑7‑（四氢呋喃‑2‑基）‑1氢‑苯并咪唑‑2‑基]脲
US9125922B2 (en) * 2011-06-20 2015-09-08 Vertex Pharmaceuticals Incorporated Phosphate esters of gyrase and topoisomerase inhibitors
WO2014015105A1 (en) * 2012-07-18 2014-01-23 Vertex Pharmaceuticals Incorporated Solid forms of (r)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1h-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof
US9572809B2 (en) * 2012-07-18 2017-02-21 Spero Trinem, Inc. Combination therapy to treat Mycobacterium diseases

Also Published As

Publication number Publication date
US8481552B2 (en) 2013-07-09
KR101897950B1 (ko) 2018-09-12
IL227407B (en) 2018-01-31
US20120184741A1 (en) 2012-07-19
BR112013017977A2 (pt) 2019-09-24
SG191924A1 (en) 2013-08-30
MX351555B (es) 2017-10-19
WO2012097270A1 (en) 2012-07-19
CA2824401A1 (en) 2012-07-19
MX2013008163A (es) 2013-08-27
EP2663558A1 (en) 2013-11-20
NZ612912A (en) 2015-10-30
AU2012205416A1 (en) 2013-08-01
IL227407A0 (en) 2013-09-30
KR20140037029A (ko) 2014-03-26
ZA201305230B (en) 2014-11-26
AU2012205416B2 (en) 2017-02-02
CL2013002026A1 (es) 2013-12-27
RU2013137753A (ru) 2015-02-20
US20130317222A1 (en) 2013-11-28
JP2014507413A (ja) 2014-03-27
CN103384666A (zh) 2013-11-06
TW201309676A (zh) 2013-03-01

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