WO2012116349A3 - Novel cocrystals of ezetimibe - Google Patents

Novel cocrystals of ezetimibe Download PDF

Info

Publication number
WO2012116349A3
WO2012116349A3 PCT/US2012/026658 US2012026658W WO2012116349A3 WO 2012116349 A3 WO2012116349 A3 WO 2012116349A3 US 2012026658 W US2012026658 W US 2012026658W WO 2012116349 A3 WO2012116349 A3 WO 2012116349A3
Authority
WO
WIPO (PCT)
Prior art keywords
novel
fluorophenyl
cocrystal
cocrystals
relates
Prior art date
Application number
PCT/US2012/026658
Other languages
French (fr)
Other versions
WO2012116349A2 (en
Inventor
Scott L. Childs
Nathan BARISHANSKY
Shreenivas Reddy LINGIREDDY
Original Assignee
Amplio Pharma, Llc
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 Amplio Pharma, Llc filed Critical Amplio Pharma, Llc
Publication of WO2012116349A2 publication Critical patent/WO2012116349A2/en
Publication of WO2012116349A3 publication Critical patent/WO2012116349A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Abstract

The invention relates to a novel L-proline cocrystal of l-(4-fluorophenyl)-3(R)-[3-(4- fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone. The invention further relates to a novel imidazole cocrystal of l-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)- 3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone. The preparation and characterization of the novel cocrystals according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel L- proline and/or novel imidazole cocrystal, and the therapeutic use of the novel cocrystals to treat and/or prevent various disorders and/or conditions, including primary hypercholesterolemia, mixed hyperlipidemia and homozygous familial sitosterolemia.
PCT/US2012/026658 2011-02-26 2012-02-24 Novel cocrystals of ezetimibe WO2012116349A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161447049P 2011-02-26 2011-02-26
US61/447,049 2011-02-26

Publications (2)

Publication Number Publication Date
WO2012116349A2 WO2012116349A2 (en) 2012-08-30
WO2012116349A3 true WO2012116349A3 (en) 2013-02-14

Family

ID=46721491

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2012/026658 WO2012116349A2 (en) 2011-02-26 2012-02-24 Novel cocrystals of ezetimibe

Country Status (1)

Country Link
WO (1) WO2012116349A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2841655A1 (en) * 2011-07-26 2013-01-31 Basf Se Multicomponent crystalline system of ezetimibe and proline
CN105001138A (en) * 2015-07-28 2015-10-28 郑州大学 Ezetimibe and maleic acid pharmaceutical co-crystal and preparation method thereof
JP7186460B2 (en) * 2017-08-07 2022-12-09 エナンティア，エセ．エレ． Co-crystal of 2-[(1R,6R)-6-isopropenyl-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene-1,3-diol
US20190177258A1 (en) * 2017-12-11 2019-06-13 Artelo Biosciences, Inc. New solid forms of cannabidiol and uses thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040176335A1 (en) * 2003-01-21 2004-09-09 Childs Scott L. Novel cocrystallization
US20050171080A1 (en) * 2003-12-23 2005-08-04 Dr. Reddy's Laboratories, Inc. Polymorphs of ezetimibe and process for preparation thereof
US20060160785A1 (en) * 2004-12-03 2006-07-20 Judith Aronhime Ezetimibe polymorphs
US20060234996A1 (en) * 2005-04-14 2006-10-19 Itai Adin Novel crystalline form of ezetimibe and processes for the preparation thereof
US20090143316A1 (en) * 2006-04-05 2009-06-04 Astellas Pharma Inc. Cocrystal of c-glycoside derivative and l-proline

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040176335A1 (en) * 2003-01-21 2004-09-09 Childs Scott L. Novel cocrystallization
US20050171080A1 (en) * 2003-12-23 2005-08-04 Dr. Reddy's Laboratories, Inc. Polymorphs of ezetimibe and process for preparation thereof
US20060160785A1 (en) * 2004-12-03 2006-07-20 Judith Aronhime Ezetimibe polymorphs
US20060234996A1 (en) * 2005-04-14 2006-10-19 Itai Adin Novel crystalline form of ezetimibe and processes for the preparation thereof
US20090143316A1 (en) * 2006-04-05 2009-06-04 Astellas Pharma Inc. Cocrystal of c-glycoside derivative and l-proline

Also Published As

Publication number Publication date
WO2012116349A2 (en) 2012-08-30

Similar Documents

Publication Publication Date Title
WO2007120824A3 (en) Processes for the synthesis of azetidinone
WO2010017545A3 (en) Triazole compounds that modulate hsp90 activity
WO2008027542A3 (en) 5-substituted isoindoline compounds
EA201792046A1 (en) ANDROGEN RECEPTOR MODULATORS AND THEIR APPLICATION
WO2010108074A3 (en) Inhibitors of pi3 kinase
WO2008097428A3 (en) Compounds and compositions as modulators of gpr119 activity
EP2966065A3 (en) Hydroxylated and methoxylated cyclopenta [d] pyrimidines as akt protein kinase inhibitors
WO2007119106A3 (en) Processes for preparing intermediate compounds useful for the preparation of ezetimibe
WO2007138282A3 (en) Bi-aryl or aryl-heteroaryl substituted indoles
MX2012008285A (en) Voltage-gated sodium channel blockers.
MX346608B (en) 5-substituted isoindoline compounds.
MX2010009752A (en) Oxadiazoanthracene compounds for the treatment of diabetes.
PH12014501199A1 (en) Substituted 4-phenyl - pyridines for the treatment of nk-1 receptor related diseases
WO2006086562A3 (en) Phenylazetidinone derivatives
MXPA05012680A (en) Novel substituted 3-sulfur indoles.
WO2009106980A3 (en) Indazole derivatives
WO2012116349A3 (en) Novel cocrystals of ezetimibe
MX2010003949A (en) Substituted n-phenyl-bipyrrolidine carboxamides and therapeutic use thereof.
MX355325B (en) Quinazoline carboxamide azetidines.
WO2013033037A3 (en) Novel antiprion compounds
ATE532789T1 (en) DIHYDROTHIENOPYRIMIDINES AS ACT PROTEIN KINASE INHIBITORS
WO2009025785A3 (en) Cb2 receptor ligands for the treatment of pain
MY148807A (en) Substituted n-phenyl-bipyrrolidine ureas and therapeutic use thereof
GEP20135806B (en) Lactams as beta secretase inhibitors
MX2012001134A (en) Compositions and methods for inhibition of the jak pathway.

Legal Events

Date Code Title Description
NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 12748912

Country of ref document: EP

Kind code of ref document: A2