PE20060742A1 - CRYSTALLINE SALTS OF N- [CYANOMETHYL-CARBAMOIL) -CYCLOHEXIL] -4- (PROPYL-PIPERAZI-1-NIL) -BENZAMIDE - Google Patents

CRYSTALLINE SALTS OF N- [CYANOMETHYL-CARBAMOIL) -CYCLOHEXIL] -4- (PROPYL-PIPERAZI-1-NIL) -BENZAMIDE

Info

Publication number
PE20060742A1
PE20060742A1 PE2005001441A PE2005001441A PE20060742A1 PE 20060742 A1 PE20060742 A1 PE 20060742A1 PE 2005001441 A PE2005001441 A PE 2005001441A PE 2005001441 A PE2005001441 A PE 2005001441A PE 20060742 A1 PE20060742 A1 PE 20060742A1
Authority
PE
Peru
Prior art keywords
salts
cyclohexil
carbamoil
piperazi
nil
Prior art date
Application number
PE2005001441A
Other languages
Spanish (es)
Inventor
Sabine Pfeffer
Frederik Nobs
Piotr H Karpinski
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20060742A1 publication Critical patent/PE20060742A1/en

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

REFERIDA A SALES CRISTALINAS DE N-[CIANOMETIL-CARBAMOIL)-CICLOHEXIL]-4-(PROPIL-PIPERAZI-1-NIL)-BENZAMIDA (COMPUESTO I). DICHAS SALES PUEDEN SER SALES DE ACETATO, LACTATO, MALONATO, FUMARATO, OXALATO, MALEATO, TARTRATO, SUCCINATO, BENZOATO, ENTRE OTRAS; LAS CUALES PRESENTAN CRISTALINIDAD Y OTRAS PROPIEDADES FISICO-QUIMICAS MEJORADAS. PARTICULARMENTE SE PREFIERE LA SAL MALEATO DE HIDROGENO DE DICHO COMPUESTO, QUE PRESENTA UN DISENO DE DIFRACCION DE POLVO DE RAYOS X CONTENIENDO PICOS CARACTERISTICOS COMO LOS VALORES 2 TETA, TALES COMO 7,6±0.3°C, 8,3±0,3°C, 8,5±0,3°C, 9,2±0,3°C, 9,5±0,3°C, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION. LAS SALES DEL COMPUESTO I SON INHIBIDORAS DE LA CATEPSINA K Y SON UTILES PARA EL TRATAMIENTO DE LA OSTEOPOROSIS, OSTEOARTRITIS, ARTRITIS REUMATOIDEA, ENTRE OTRASREFERRING TO CRYSTALLINE SALTS OF N- [CYANOMETIL-CARBAMOIL) -CYCLOHEXIL] -4- (PROPYL-PIPERAZI-1-NIL) -BENZAMIDE (COMPOUND I). SUCH SALTS MAY BE ACETATE, LACTATE, MALONATE, FUMARATE, OXALATE, MALEATE, TARTRATE, SUCCINATE, BENZOATE, AMONG OTHERS; WHICH PRESENT CRYSTALINITY AND OTHER IMPROVED PHYSICAL-CHEMICAL PROPERTIES. PARTICULARLY PREFERRED THE HYDROGEN MALEATE SALT OF SAID COMPOUND, WHICH HAS A DIFFRACTION DESIGN OF X-RAY DUST CONTAINING CHARACTERISTIC PEAKS SUCH AS 2 TETA VALUES, SUCH AS 7.6 ± 0.3 ° C, 8.3 ± 0.3 ° C, 8.5 ± 0.3 ° C, 9.2 ± 0.3 ° C, 9.5 ± 0.3 ° C, AMONG OTHERS. IT IS ALSO REFERRED TO A PREPARATION PROCEDURE. THE SALTS OF COMPOUND I ARE INHIBITORS OF CATEPSIN K AND ARE USEFUL FOR THE TREATMENT OF OSTEOPOROSIS, OSTEOARTHRITIS, RHEUMATOID ARTHRITIS, AMONG OTHERS

PE2005001441A 2004-12-14 2005-12-13 CRYSTALLINE SALTS OF N- [CYANOMETHYL-CARBAMOIL) -CYCLOHEXIL] -4- (PROPYL-PIPERAZI-1-NIL) -BENZAMIDE PE20060742A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0427380.1A GB0427380D0 (en) 2004-12-14 2004-12-14 Organic compounds

Publications (1)

Publication Number Publication Date
PE20060742A1 true PE20060742A1 (en) 2006-09-08

Family

ID=34090027

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005001441A PE20060742A1 (en) 2004-12-14 2005-12-13 CRYSTALLINE SALTS OF N- [CYANOMETHYL-CARBAMOIL) -CYCLOHEXIL] -4- (PROPYL-PIPERAZI-1-NIL) -BENZAMIDE

Country Status (6)

Country Link
AR (1) AR052161A1 (en)
GB (1) GB0427380D0 (en)
GT (1) GT200500365A (en)
PE (1) PE20060742A1 (en)
TW (1) TW200635910A (en)
WO (1) WO2006063762A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2678717A1 (en) * 2007-02-28 2008-09-04 Sanofi-Aventis Imaging probes
EP2262783A2 (en) * 2008-02-21 2010-12-22 Sanofi-Aventis Covalently binding imaging probes

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1273444C (en) * 1997-11-05 2006-09-06 诺瓦提斯公司 Dipeptide nitriles
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
PE20050328A1 (en) * 2003-07-21 2005-06-16 Novartis Ag COMBINATIONS OF A BISPHOSPHONATE AND A CATEPSIN K INHIBITOR
JP2007511548A (en) * 2003-11-19 2007-05-10 ノバルティス アクチエンゲゼルシャフト Use of cathepsin K inhibitors in severe bone loss diseases

Also Published As

Publication number Publication date
GB0427380D0 (en) 2005-01-19
GT200500365A (en) 2006-07-17
WO2006063762A1 (en) 2006-06-22
TW200635910A (en) 2006-10-16
AR052161A1 (en) 2007-03-07

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