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PE20050328A1 - Combinaciones de un bisfosfonato y un inhibidor de catepsina k - Google Patents

Combinaciones de un bisfosfonato y un inhibidor de catepsina k

Info

Publication number
PE20050328A1
PE20050328A1 PE2004000692A PE2004000692A PE20050328A1 PE 20050328 A1 PE20050328 A1 PE 20050328A1 PE 2004000692 A PE2004000692 A PE 2004000692A PE 2004000692 A PE2004000692 A PE 2004000692A PE 20050328 A1 PE20050328 A1 PE 20050328A1
Authority
PE
Peru
Prior art keywords
het
catepsin
carbamoil
cyanomethyl
piperazin
Prior art date
Application number
PE2004000692A
Other languages
English (en)
Inventor
Johann Zimmermann
Carsten Goessl
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34135094&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20050328(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20050328A1 publication Critical patent/PE20050328A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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

Landscapes

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

Abstract

SE REFIERE A UNA COMBINACION FARMACEUTICA QUE COMPRENDE UN BISFOSFONATO DE FORMULA I, EN DONDE X ES H, HIDROXILO, AMINO, ALCANOILO, ENTRE OTROS; R ES H o ALQUILO C1-C4; Rx ES UNA CADENA LATERAL QUE CONTIENE UN GRUPO AMINO OPCIONALMENTE SUSTITUIDO, O UN HETEROCICLO QUE CONTIENE N; Y (a) UN INHIBIDOR DE CATEPSINA K DE FORMULA V, ENTRE OTRAS CLASES DE INHIBIDORES DE CATEPSINA K, EN DONDE R1 ES ARILO, ARIL-ALQUILO INFERIOR, ALQUENILO INFERIOR, ENTRE OTROS; R2 Y R3 JUNTOS REPRESENTAN ALQUILENO INFERIOR, OPCIONALMENTE INTERRUMPIDO POR O, S, ENTRE OTROS, PARA FORMAR UN ANILLO CON EL C AL QUE SE UNEN; R4 Y R5 SON, INDEPENDIENTEMENTE ENTRE SI, H, ALQUILO INFERIOR, ARIL-ALQUILO INFERIOR, ENTRE OTROS; X1 ES C(O), C(S), S(O), S(O)2, ENTRE OTROS; Y ES O o S; L ES HET OPCIONALMENTE SUSTITUIDO, HET-CH2 o CH2-HET; HET ES UN HETEROATOMO SELECCIONADO DE O, N o S; X ES 0 o 1. SON INHIBIDORES DE CATEPSINA K PREFERIDOS: N-[1-(CIANOMETIL-CARBAMOIL)-CICLOHEXIL]-4-(PIPERAZIN-1-IL)-BENZAMIDA; N-[1-(CIANOMETIL-CARBAMOIL)-CICLOHEXIL]-4-(4-METIL-PIPERAZIN-1-IL)-BENZAMIDA; N-[1-(CIANOMETIL-CARBAMOIL)-CICLOHEXIL]-4-(4-ETIL-PIPERAZIN-1-IL)-BENZAMIDA. UNO DE LOS BIFOSFANATOS PREFERIDOS ES: ACIDO 2-(IMIDAZOL-1-IL)-1-HIDROXIETANO-1,1-DIFOSFONICO (ACIDO ZOLENDRONICO). ESTA PREPARACION FARMACEUTICA ES UTIL EN LA PREVENCION Y TRATAMIENTO DE METASTASIS OSEA, HIPERCALCEMIA INDUCIDA POR TUMOR, CRECIMIENTO DE TUMOR, PERDIDA OSEA INDUCIDA POR TUMOR Y ENFERMEDADES DE PERDIDA OSEA TAL COMO OSTEOPOROSIS
PE2004000692A 2003-07-21 2004-07-20 Combinaciones de un bisfosfonato y un inhibidor de catepsina k PE20050328A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US48892503P 2003-07-21 2003-07-21

Publications (1)

Publication Number Publication Date
PE20050328A1 true PE20050328A1 (es) 2005-06-16

Family

ID=34135094

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000692A PE20050328A1 (es) 2003-07-21 2004-07-20 Combinaciones de un bisfosfonato y un inhibidor de catepsina k

Country Status (21)

Country Link
US (1) US20060281714A1 (es)
EP (1) EP1651238A1 (es)
JP (1) JP2006528151A (es)
KR (1) KR20060037382A (es)
CN (1) CN100406016C (es)
AR (1) AR045728A1 (es)
AU (1) AU2004262903B2 (es)
BR (1) BRPI0412769A (es)
CA (1) CA2532948A1 (es)
CO (1) CO5680441A2 (es)
EC (1) ECSP066293A (es)
IL (1) IL172913A0 (es)
IS (1) IS8311A (es)
MA (1) MA27925A1 (es)
MX (1) MXPA06000790A (es)
NO (1) NO20060851L (es)
PE (1) PE20050328A1 (es)
RU (1) RU2006105100A (es)
TN (1) TNSN06021A1 (es)
TW (1) TW200510436A (es)
WO (1) WO2005014006A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20060107792A (ko) * 2003-11-19 2006-10-16 노파르티스 아게 중증 골 소실 질환의 치료를 위한 카텝신 ｋ 억제제의 용도
GB0427380D0 (en) * 2004-12-14 2005-01-19 Novartis Ag Organic compounds
US20080219996A1 (en) * 2005-09-26 2008-09-11 Thea Kalebic Molecular Markers Associated with Bone Metastasis
JPWO2009054454A1 (ja) * 2007-10-24 2011-03-03 国立大学法人 東京医科歯科大学 カテプシン阻害剤を有効成分として含有するＴｏｌｌ様受容体のシグナル伝達の調整剤
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
WO2018009417A1 (en) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
WO2018064119A1 (en) 2016-09-28 2018-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
US20210298890A1 (en) 2018-06-27 2021-09-30 Cirlo Gmbh Implants for recruiting and removing circulating tumor cells
WO2021122803A2 (en) 2019-12-17 2021-06-24 Cirlo Gmbh Tubular shaped elongated catheter device assemblies for interacting with components of bodily fluids, method for recovering cells, cell aggregates and exosomes from a tubular shaped elongated catheter device and smart tubular shaped elongated catheter device assemblies for monitoring interaction with components of bodily fluids
US20250281518A1 (en) * 2022-04-27 2025-09-11 The Regents Of The University Of California Methods and agents for preventing skeletal aging, osteoporosis and obesity

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5501969A (en) * 1994-03-08 1996-03-26 Human Genome Sciences, Inc. Human osteoclast-derived cathepsin
US6544767B1 (en) * 1994-10-27 2003-04-08 Axys Pharmaceuticals, Inc. Cathespin O2 protease
US6017926A (en) * 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
EP1100506A4 (en) * 1998-07-29 2002-06-26 Merck & Co Inc INTEGRIN RECEPTOR ANTAGONISTS
US5998390A (en) * 1998-09-28 1999-12-07 The Research Foundation Of State University Of New York Combination of bisphosphonate and tetracycline
CA2367348A1 (en) * 1999-03-15 2000-09-21 Axys Pharmaceuticals, Inc. Novel compounds and compositions as protease inhibitors
AU775079B2 (en) * 1999-05-21 2004-07-15 Novartis Ag Pharmaceutical compositions and uses
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
US6468559B1 (en) * 2000-04-28 2002-10-22 Lipocine, Inc. Enteric coated formulation of bishosphonic acid compounds and associated therapeutic methods
AR036375A1 (es) * 2001-08-30 2004-09-01 Novartis Ag Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos
JP4343690B2 (ja) * 2001-11-13 2009-10-14 メルク フロスト カナダ リミテツド プロテアーゼ阻害薬としてのシアノアルキルアミノ誘導体

Also Published As

Publication number Publication date
KR20060037382A (ko) 2006-05-03
BRPI0412769A (pt) 2006-09-26
RU2006105100A (ru) 2007-09-20
AR045728A1 (es) 2005-11-09
IL172913A0 (en) 2006-06-11
CO5680441A2 (es) 2006-09-29
CA2532948A1 (en) 2005-02-17
US20060281714A1 (en) 2006-12-14
MA27925A1 (fr) 2006-06-01
MXPA06000790A (es) 2006-04-07
JP2006528151A (ja) 2006-12-14
TW200510436A (en) 2005-03-16
WO2005014006A1 (en) 2005-02-17
NO20060851L (no) 2006-04-21
AU2004262903A1 (en) 2005-02-17
IS8311A (is) 2006-02-17
ECSP066293A (es) 2006-07-28
TNSN06021A1 (en) 2007-10-03
CN1826124A (zh) 2006-08-30
CN100406016C (zh) 2008-07-30
AU2004262903B2 (en) 2007-08-23
EP1651238A1 (en) 2006-05-03

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