WO2011008809 CRYSTALLINE FREEBASE FORMS OF A BIPHENYL COMPOUND

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Publication Number WO/2011/008809

Publication Date 20.01.2011

International Application No. PCT/US2010/041903

International Filing Date 14.07.2010

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Applicants

THERAVANCE, INC. [US]/[US] (AllExceptUS)
WOOLLAM, Grahame [GB]/[GB] (UsOnly)

Inventors

WOOLLAM, Grahame

Agents

HAGENAH, Jeffrey A.

Priority Data

61/225,803

15.07.2009

Publication Language English (en)

Filing Language English (EN)

Designated States

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Title

(EN) CRYSTALLINE FREEBASE FORMS OF A BIPHENYL COMPOUND

(FR) FORMES À BASE LIBRE CRISTALLINE D'UN COMPOSÉ BIPHENYLE

Abstract

(EN) The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid l-(2-{[4-(4-carbamoylpiperidin-l-yImethyl)benzoyl]methylamino}ethyl)piperidin-4- yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.

(FR) L'invention concerne deux formes à base libre cristalline d'acide biphényl-2-ylcarbamique de l-(2-{[4-(4-carbamoylpipéridin-l-yIméthyl)benzoyl]méthylamino}éthyle)pipéridin-4-yl ester. L'invention concerne également des compositions pharmaceutiques contenant ces bases libres cristallines ou préparées au moyen de celles-ci; des procédés et des intermédiaires pour la préparation des bases libres cristallines; ainsi que des méthodes d'utilisation de ces bases libres cristallines dans le traitement d'un trouble pulmonaire.

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
44	Non-condensed pyridines; Hydrogenated derivatives thereof
445	Non-condensed piperidines, e.g. piperocaine

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
401	Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02	containing two hetero rings
12	linked by a chain containing hetero atoms as chain links

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11	Drugs for disorders of the respiratory system

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
44	Non-condensed pyridines; Hydrogenated derivatives thereof
445	Non-condensed piperidines, e.g. piperocaine

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
401	Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02	containing two hetero rings
12	linked by a chain containing hetero atoms as chain links

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1. WO2011008809 - CRYSTALLINE FREEBASE FORMS OF A BIPHENYL COMPOUND

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
B	GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200	Indexing scheme relating to specific properties of organic compounds
13	Crystalline forms, e.g. polymorphs

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9	Medicinal preparations characterised by special physical form
14	Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
16	Agglomerates; Granulates; Microbeadlets ; ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
1605	Excipients; Inactive ingredients
1617	Organic compounds, e.g. phospholipids, fats
1623	Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9	Medicinal preparations characterised by special physical form
14	Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
16	Agglomerates; Granulates; Microbeadlets ; ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
1605	Excipients; Inactive ingredients
1617	Organic compounds, e.g. phospholipids, fats
1623	Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules