BR0308208A - Composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, métodos para inibir a atividade de catepsina em um mamìfero que disto necessita, para tratar ou prevenir uma doença, para tratar condições dependentes de catepsina em um mamìfero que disto necessita, para inibir ressorção óssea, para incrementar a densidade mineral óssea, e, para reduzir o risco de fraturas - Google Patents

Composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, métodos para inibir a atividade de catepsina em um mamìfero que disto necessita, para tratar ou prevenir uma doença, para tratar condições dependentes de catepsina em um mamìfero que disto necessita, para inibir ressorção óssea, para incrementar a densidade mineral óssea, e, para reduzir o risco de fraturas

Info

Publication number
BR0308208A
BR0308208A BR0308208-3A BR0308208A BR0308208A BR 0308208 A BR0308208 A BR 0308208A BR 0308208 A BR0308208 A BR 0308208A BR 0308208 A BR0308208 A BR 0308208A
Authority
BR
Brazil
Prior art keywords
pharmaceutical composition
mammal
need
treating
inhibiting
Prior art date
Application number
BR0308208-3A
Other languages
English (en)
Other versions
BRPI0308208B8 (pt
BRPI0308208B1 (pt
Inventor
Christopher I Bayly
Cameron Black
Serge Leger
Chun Sing Li
Dan Mckay
Christophe Mellon
Jacques Yves Gauthier
Cheuk Lau
Michel Therien
Vouy-Linh Truong
Michael J Green
Bernard L Hirschbein
James W Janc
James T Palmer
Chitra Baskaran
Original Assignee
Merck Frosst Canada Inc
Axys Pharm Inc
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=27807943&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR0308208(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Frosst Canada Inc, Axys Pharm Inc filed Critical Merck Frosst Canada Inc
Publication of BR0308208A publication Critical patent/BR0308208A/pt
Publication of BRPI0308208B1 publication Critical patent/BRPI0308208B1/pt
Publication of BRPI0308208B8 publication Critical patent/BRPI0308208B8/pt

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/17—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and doubly-bound oxygen atoms bound to the same acyclic carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • 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
    • A61P19/02—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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/24—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton
    • C07C255/25—Aminoacetonitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/24—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton
    • C07C255/29—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton containing cyano groups and acylated amino groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/45—Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C255/46—Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of non-condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/10—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/57—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D295/12—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 singly or doubly bound nitrogen atoms
    • C07D295/135—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 singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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 containing two hetero rings
    • C07D401/04—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 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Quinoline Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

"COMPOSTO, COMPOSIçãO FARMACêUTICA, PROCESSO PARA A PREPARAçãO DE UMA COMPOSIçãO FARMACêUTICA, MéTODOS PARA INIBIR A ATIVIDADE DE CATEPSINA EM UM MAMìFERO QUE DISTO NECESSITA, PARA TRATAR OU PREVENIR UMA DOENçA, PARA TRATAR CONDIçõES DEPENDENTES DE CATEPSINA EM UM MAMìFERO QUE DISTO NECESSITA, PARA INIBIR RESSORçãO óSSEA, PARA INCREMENTAR A DENSIDADE MINERAL óSSEA, E PARA REDUZIR O RISCO DE FRATURAS". Esta invenção refere-se a uma classe inédita de compostos que são inibidores de protease cisteina, incluindo, embora sem limitação, inibidores de catepsinas K, L, S e B. Estes compostos são úteis para tratar doenças em que se indica a inibição da ressorção óssea, como a osteoporose.
BRPI0308208A 2002-03-05 2003-02-28 compostos inibidores de catepsina cisteína protease e composições farmacêuticas compreendendo os mesmos BRPI0308208B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36181802P 2002-03-05 2002-03-05
US40870402P 2002-09-06 2002-09-06
PCT/US2003/006147 WO2003075836A2 (en) 2002-03-05 2003-02-28 Cathepsin cysteine protease inhibitors

Publications (3)

Publication Number Publication Date
BR0308208A true BR0308208A (pt) 2005-01-11
BRPI0308208B1 BRPI0308208B1 (pt) 2017-04-18
BRPI0308208B8 BRPI0308208B8 (pt) 2021-05-25

Family

ID=27807943

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0308208A BRPI0308208B8 (pt) 2002-03-05 2003-02-28 compostos inibidores de catepsina cisteína protease e composições farmacêuticas compreendendo os mesmos

Country Status (28)

Country Link
US (6) US20030232863A1 (pt)
EP (1) EP1482924B1 (pt)
JP (2) JP4201716B2 (pt)
KR (1) KR100975784B1 (pt)
CN (1) CN100430052C (pt)
AT (1) ATE395911T1 (pt)
AU (1) AU2003219953B8 (pt)
BR (1) BRPI0308208B8 (pt)
CA (1) CA2477657C (pt)
CL (1) CL2003001743A1 (pt)
CY (1) CY1111130T1 (pt)
DE (1) DE60321141D1 (pt)
DK (1) DK1482924T3 (pt)
EC (1) ECSP045261A (pt)
ES (1) ES2305452T3 (pt)
HK (1) HK1080375A1 (pt)
HR (1) HRP20040800B1 (pt)
IL (2) IL163748A0 (pt)
IS (1) IS2549B (pt)
MA (1) MA27295A1 (pt)
MX (1) MXPA04008621A (pt)
NO (1) NO335099B1 (pt)
NZ (1) NZ534583A (pt)
PL (1) PL215865B1 (pt)
PT (1) PT1482924E (pt)
RU (1) RU2312861C2 (pt)
SI (1) SI1482924T1 (pt)
WO (1) WO2003075836A2 (pt)

Families Citing this family (117)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9937531B2 (en) 2009-03-10 2018-04-10 Bookit Oy Ajanvarauspalvelu Method and system for delivery of goods
PT1469833T (pt) 2002-02-01 2021-07-13 Bend Res Inc Método para produzir dispersões de fármaco amorfo sólido seco por pulverização homogéneas utilizando aparelho de secagem por pulverização modificado
AU2003219953B8 (en) 2002-03-05 2008-09-25 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
WO2003077948A1 (fr) * 2002-03-19 2003-09-25 Kowa Co., Ltd. Myelome : medicaments preventifs/curatifs et methode de diagnostic
DE602004023838D1 (de) * 2003-04-24 2009-12-10 Merck & Co Inc Hemmer der akt aktivität
AU2004266740B2 (en) * 2003-08-21 2010-08-26 Merck Frosst Canada Ltd Cathepsin cysteine protease inhibitors
CN1842515A (zh) * 2003-08-27 2006-10-04 默克弗罗斯特加拿大有限公司 组织蛋白酶抑制剂
KR20060079143A (ko) * 2003-09-18 2006-07-05 액시스 파마슈티컬스 인코포레이티드 시스테인 프로테아제 억제제로서의 할로알킬 함유 화합물
NZ546504A (en) * 2003-10-24 2009-01-31 Aventis Pharma Inc Novel keto-oxadiazole derivatives as cathepsin inhibitors
EP1694647B1 (en) * 2003-12-12 2016-11-09 Merck Canada Inc. Cathepsin cysteine protease inhibitors
AU2005203820A1 (en) * 2004-01-08 2005-07-21 Merck Frosst Canada Ltd Cathepsin cysteine protease inhibitors
US7429674B2 (en) 2004-04-14 2008-09-30 Merck & Co. Inc.. Process for preparing fluoroleucine alkyl esters
CN1993314B (zh) * 2004-08-04 2011-11-02 默沙东公司 非对映异构选择性还原胺化方法
AU2005287046A1 (en) * 2004-09-17 2006-03-30 Bayer Schering Pharma Aktiengesellschaft Processes and intermediates for preparing cysteine protease inhibitors
TW200619206A (en) * 2004-09-29 2006-06-16 Anormed Inc Chemokine-binding heterocyclic compound salts, and methods of use thereof
AR055283A1 (es) * 2004-11-23 2007-08-15 Merck Frosst Canada Ltd Inhibidores de cisteinproteasa de catepsina
EP1817275A1 (en) 2004-12-01 2007-08-15 Schering Aktiengesellschaft Haloalkyl containing compounds as cysteine protease inhibitors
EP1819667B1 (en) 2004-12-02 2012-10-17 ViroBay, Inc. Sulfonamide compounds as cysteine protease inhibitors
EP1841419A4 (en) * 2005-01-19 2009-02-25 Merck Frosst Canada Ltd INHIBITORS OF CATHEPSIN K AND OBESITY
US20080125442A1 (en) * 2005-01-19 2008-05-29 Michael David Percival Cathepsin K Inhibitors and Atherosclerosis
WO2006093467A1 (en) * 2005-03-02 2006-09-08 Agency For Science, Technology And Research Conjugated organic molecules for molecular electronic devices
WO2007046842A2 (en) 2005-03-02 2007-04-26 Merck & Co., Inc. Composition for inhibition of cathepsin k
KR101447897B1 (ko) 2005-03-21 2014-10-07 비로베이, 인코포레이티드 시스테인 단백질분해효소 억제제로서의 알파 케토아미드화합물
MX2007011739A (es) * 2005-03-22 2008-03-14 Celera Genomics Compuestos que contienen sulfonilo como inhibidores de cisteina proteasa.
EP1891003A4 (en) 2005-06-02 2010-07-21 Merck Frosst Canada Ltd FLUORALKYLAMINE DERIVATIVES AS CATHEPSIN INHIBITORS
CN101267813A (zh) 2005-07-19 2008-09-17 第一三共株式会社 取代丙酰胺衍生物和含有其的药物组合物
WO2007012180A1 (en) * 2005-07-26 2007-02-01 Merck Frosst Canada Ltd. Papain family cysteine protease inhibitors for the treatment of parasitic diseases
RU2478620C2 (ru) 2006-06-01 2013-04-10 Санофи-Авентис Спироциклические нитрилы в качестве ингибиторов протеазы
US7622593B2 (en) * 2006-06-27 2009-11-24 The Procter & Gamble Company Human protein tyrosine phosphatase inhibitors and methods of use
US7893112B2 (en) * 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
ZA200902477B (en) * 2006-10-04 2010-08-25 Virobay Inc Di-fluoro containing compounds as cysteine protease inhibitors
WO2008080969A1 (en) * 2006-12-29 2008-07-10 Abbott Gmbh & Co. Kg Carboxamide compounds and their use as calpain inhibitors
US20090318560A1 (en) 2007-02-26 2009-12-24 Wayne Parent Formulations for cathepsin k inhibitors
US8273913B2 (en) 2007-04-02 2012-09-25 Merck Canada Inc. Amidation process for the preparation of cathepsin K inhibitors
KR20100023948A (ko) 2007-06-08 2010-03-04 닛뽕 케미파 가부시키가이샤 뇌동맥류의 치료 또는 예방약
WO2009054454A1 (ja) 2007-10-24 2009-04-30 National University Corporation Tokyo Medical And Dental University 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
EP2225196B1 (en) * 2007-11-29 2015-01-28 Merck Canada Inc. Cysteine protease inhibitors for the treatment of parasitic diseases
JPWO2009096198A1 (ja) * 2008-02-01 2011-05-26 一般社団法人ファルマＩｐ 新規ビアリール誘導体
BRPI0822420A2 (pt) * 2008-04-01 2014-10-07 Virobay Inc Composto, composição farmaceutica, e, métodos para tratar uma doença em uma animal e para tratar um paciente que passa por uma tarepia.
WO2009125861A1 (ja) * 2008-04-09 2009-10-15 帝人ファーマ株式会社 システインプロテアーゼ阻害剤
US20110065800A1 (en) * 2008-05-14 2011-03-17 Haihong Fan Formulations for cathepsin k inhibitors
JP5518997B2 (ja) 2009-04-20 2014-06-11 エフ．ホフマン−ラ ロシュ アーゲー カテプシン阻害薬としてのプロリン誘導体
US8324417B2 (en) * 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
US9051304B2 (en) * 2009-12-22 2015-06-09 AbbVie Deutschland GmbH & Co. KG Carboxamide compounds and their use as calpain inhibitors V
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
EP2675440B1 (en) * 2011-02-14 2020-03-25 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
US20130331597A1 (en) * 2011-03-02 2013-12-12 Guy Humphrey Amidation process
WO2012151319A1 (en) 2011-05-02 2012-11-08 Virobay, Inc. Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain
RU2013155509A (ru) 2011-05-16 2015-06-27 Байер Интеллектуэль Проперти Гмбх Применение ингибирования катепсина к для лечения и/или профилактики легочной гипертензии и/или сердечной недостаточности
US10023862B2 (en) 2012-01-09 2018-07-17 Arrowhead Pharmaceuticals, Inc. Organic compositions to treat beta-catenin-related diseases
EA036592B1 (ru) 2012-06-13 2020-11-26 Инсайт Холдингс Корпорейшн Замещенные трициклические соединения как ингибиторы fgfr
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
KR102279999B1 (ko) 2013-02-19 2021-07-22 노파르티스 아게 선택적 에스트로겐 수용체 분해제로서의 벤조티오펜 유도체 및 그의 조성물
RU2737434C2 (ru) 2013-03-13 2020-11-30 Форма Терапьютикс, Инк. Новые соединения и композиции для ингибирования fasn
WO2014172644A2 (en) 2013-04-19 2014-10-23 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2014184378A1 (en) 2013-05-16 2014-11-20 Sandoz Ag Tablet with increased drug load of odanacatib
EP2808012A1 (en) 2013-05-29 2014-12-03 ratiopharm GmbH Method for producing dosage form comprising odanacatib
JP6336973B2 (ja) 2013-06-14 2018-06-06 生化学工業株式会社 α−オキソアシルアミノカプロラクタム誘導体
WO2014199645A1 (ja) 2013-06-14 2014-12-18 生化学工業株式会社 α－オキソアシルアミノカプロラクタム体
WO2015006177A1 (en) * 2013-07-11 2015-01-15 Merck Sharp & Dohme Corp. Formulations for cathepsin k inhibitors with vitamin d
AU2014332250B2 (en) * 2013-10-08 2018-07-19 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2015092634A1 (en) 2013-12-16 2015-06-25 Novartis Ag 1,2,3,4-tetrahydroisoquinoline compounds and compositions as selective estrogen receptor antagonists and degraders
WO2015107494A1 (en) 2014-01-17 2015-07-23 Novartis Ag 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
EP3094627B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CZ2014941A3 (cs) 2014-12-19 2016-06-29 Zentiva, K.S. Příprava vysoce čistého intermediátu pro syntézu Odanacatibu
ES2895769T3 (es) 2015-02-20 2022-02-22 Incyte Corp Heterociclos bicíclicos como inhibidores de FGFR
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
JP6695353B2 (ja) 2015-03-25 2020-05-20 ノバルティス アーゲー Ｆｇｆｒ４阻害剤としてのホルミル化ｎ−複素環式誘導体
ES2824576T3 (es) 2015-06-19 2021-05-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
CN112625028A (zh) 2015-06-19 2021-04-09 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
WO2016203404A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
EP3342765B1 (en) * 2015-08-29 2021-09-15 Sunshine Lake Pharma Co., Ltd. Cathepsin k inhibitor and application thereof
EP3380455A1 (en) * 2015-11-26 2018-10-03 H. Hoffnabb-La Roche Ag Trypanosomes inhibitors
CN106866502B (zh) * 2015-12-10 2020-10-09 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途
DK3452465T3 (da) 2016-05-04 2021-02-08 Genoscience Pharma Substituerede 2,4-diaminoquinolinderivater til anvendelse til behandling af proliferative sygdomme
ES2810852T3 (es) 2016-06-14 2021-03-09 Novartis Ag Compuestos y composiciones para inhibir la actividad de shp2
JP7001068B2 (ja) * 2017-01-24 2022-01-19 アステラス製薬株式会社 フェニルジフルオロメチル置換プロリンアミド化合物
KR101916396B1 (ko) 2017-02-20 2018-11-08 서울대학교 산학협력단 항암제 또는 항균제로 사용될 수 있는 단백질분해효소 저해제
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
TW201912639A (zh) 2017-09-11 2019-04-01 美商克魯松藥物公司 Ｓｈｐ２之八氫環戊烷并[c]吡咯別構抑制劑
NL2020021B1 (en) * 2017-12-05 2019-06-13 Academisch Ziekenhuis Leiden Cathepsin inhibitors
WO2019112426A1 (en) * 2017-12-05 2019-06-13 ACADEMISCH ZIEKENHUIS LEIDEN (h.o.d.n. LUMC) Cathepsin inhibitors
EP3778576B1 (en) 2018-03-28 2024-04-17 Hanlim Pharmaceutical Co., Ltd. 2-cyanopyrimidin-4-yl carbamate or urea derivative or salt thereof, and pharmaceutical composition including same
CA3099287A1 (en) 2018-05-04 2019-11-07 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
MX2021003158A (es) 2018-09-18 2021-07-16 Nikang Therapeutics Inc Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2.
SG11202102981SA (en) 2018-09-25 2021-04-29 Black Diamond Therapeutics Inc Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use
EP3856349A1 (en) 2018-09-25 2021-08-04 Black Diamond Therapeutics, Inc. Tyrosine kinase inhibitor compositions, methods of making and methods of use
CN112839715A (zh) 2018-09-29 2021-05-25 诺华股份有限公司 抑制shp2活性化合物的制造方法
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
EP3873214A4 (en) 2018-10-29 2022-07-13 Forma Therapeutics, Inc. SOLID FORMS OF (4-(2-FLUORO-4-(1-METHYL-1H-BENZO[D]IMIDAZOL-5-YL)BENZOYL)PIPERAZIN-1-YL)(1-HYDROXYCYCLOPROPYL)METHANONE
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
EP3946332A1 (en) 2019-04-05 2022-02-09 Université de Bretagne Occidentale Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US20220298120A1 (en) 2019-08-15 2022-09-22 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021195206A1 (en) 2020-03-24 2021-09-30 Black Diamond Therapeutics, Inc. Polymorphic forms and related uses
WO2022043556A1 (en) 2020-08-31 2022-03-03 Novartis Ag Stable radiopharmaceutical composition
EP4204021A1 (en) 2020-08-31 2023-07-05 Advanced Accelerator Applications International S.A. Method of treating psma-expressing cancers
WO2022043558A1 (en) 2020-08-31 2022-03-03 Advanced Accelerator Applications International Sa Method of treating psma-expressing cancers
WO2022140472A1 (en) 2020-12-22 2022-06-30 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
WO2022152821A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
WO2022170052A1 (en) 2021-02-05 2022-08-11 Black Diamond Therapeutics, Inc. Quinazoline derivatives, pyridopyrimidine derivatives, pyrimidopyrimidine derivatives, and uses thereof
WO2022219407A1 (en) 2021-04-14 2022-10-20 Monte Rosa Therapeutics Ag Isoindolinone compounds
EP4323349A1 (en) 2021-04-14 2024-02-21 Monte Rosa Therapeutics AG Isoindolinone amide compounds useful to treat diseases associated with gspt1
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4370522A1 (en) 2021-07-14 2024-05-22 Nikang Therapeutics, Inc. Alkylidene derivatives as kras inhibitors
US20230303509A1 (en) 2022-03-28 2023-09-28 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
WO2023240024A1 (en) 2022-06-08 2023-12-14 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
WO2024102849A1 (en) 2022-11-11 2024-05-16 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE479651T1 (de) * 1997-11-05 2010-09-15 Novartis Pharma Gmbh Dipeptide nitrile
AU2560300A (en) 1999-02-20 2000-09-04 Astrazeneca Ab Acetamido acetonitrile derivatives as inhibitors of cathepsin l and/or cathepsins
CN1364155A (zh) * 1999-03-15 2002-08-14 Axys药物公司 用作蛋白酶抑制剂的n－氰基甲基酰胺
EP1212302A1 (en) * 1999-09-16 2002-06-12 Axys Pharmaceuticals, Inc. Compounds and pharmaceutical compositions as cathepsin s inhibitors
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
DE60113406T2 (de) * 2000-05-15 2006-06-29 Novartis Ag N-substituierte peptidylnitrile als cystein-cathepsin-inhibitoren
AU2002254099B2 (en) * 2001-03-02 2006-07-06 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
EP1595363B1 (en) * 2001-08-15 2016-07-13 The Board of Governors for Higher Education State of Rhode Island and Providence Plantations Scsi-to-ip cache storage device and method
WO2003041649A2 (en) * 2001-11-13 2003-05-22 Merck Frosst Canada & Co. Cyanoalkylamino derivatives as protease inhibitors
AU2003219953B8 (en) 2002-03-05 2008-09-25 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
KR20060079143A (ko) * 2003-09-18 2006-07-05 액시스 파마슈티컬스 인코포레이티드 시스테인 프로테아제 억제제로서의 할로알킬 함유 화합물
AR055283A1 (es) * 2004-11-23 2007-08-15 Merck Frosst Canada Ltd Inhibidores de cisteinproteasa de catepsina
EP1891003A4 (en) * 2005-06-02 2010-07-21 Merck Frosst Canada Ltd FLUORALKYLAMINE DERIVATIVES AS CATHEPSIN INHIBITORS

Also Published As

Publication number Publication date
NO20044207L (no) 2004-11-24
RU2312861C2 (ru) 2007-12-20
US20110230446A1 (en) 2011-09-22
HRP20040800B1 (en) 2012-11-30
PL215865B1 (pl) 2014-02-28
IS2549B (is) 2009-10-15
AU2003219953B8 (en) 2008-09-25
HRP20040800A2 (en) 2005-04-30
ES2305452T3 (es) 2008-11-01
US8318748B2 (en) 2012-11-27
IL163748A0 (en) 2005-12-18
KR100975784B1 (ko) 2010-08-17
AU2003219953B2 (en) 2007-11-01
EP1482924A4 (en) 2006-03-08
DK1482924T3 (da) 2008-09-29
SI1482924T1 (sl) 2008-12-31
MXPA04008621A (es) 2004-12-06
AU2003219953A1 (en) 2003-09-22
MA27295A1 (fr) 2005-05-02
CA2477657C (en) 2011-04-26
CY1111130T1 (el) 2015-06-11
RU2004129587A (ru) 2005-05-10
JP4918456B2 (ja) 2012-04-18
CN1638757A (zh) 2005-07-13
BRPI0308208B8 (pt) 2021-05-25
EP1482924A2 (en) 2004-12-08
US20080188529A1 (en) 2008-08-07
US8772336B2 (en) 2014-07-08
JP2005526753A (ja) 2005-09-08
WO2003075836A2 (en) 2003-09-18
IS7400A (is) 2004-08-12
ATE395911T1 (de) 2008-06-15
HK1080375A1 (en) 2006-04-28
JP4201716B2 (ja) 2008-12-24
NZ534583A (en) 2006-11-30
US20130035312A1 (en) 2013-02-07
EP1482924B1 (en) 2008-05-21
PT1482924E (pt) 2008-08-27
US20140256743A1 (en) 2014-09-11
PL372204A1 (en) 2005-07-11
BRPI0308208B1 (pt) 2017-04-18
KR20040095262A (ko) 2004-11-12
US20030232863A1 (en) 2003-12-18
DE60321141D1 (en) 2008-07-03
CA2477657A1 (en) 2003-09-18
NO335099B1 (no) 2014-09-15
US7973037B2 (en) 2011-07-05
JP2008115177A (ja) 2008-05-22
CL2003001743A1 (es) 2005-05-06
IL163748A (en) 2013-10-31
US20050240023A1 (en) 2005-10-27
ECSP045261A (es) 2004-10-26
US7375134B2 (en) 2008-05-20
WO2003075836A3 (en) 2004-07-15
CN100430052C (zh) 2008-11-05

Similar Documents

Publication Publication Date Title
BR0308208A (pt) Composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, métodos para inibir a atividade de catepsina em um mamìfero que disto necessita, para tratar ou prevenir uma doença, para tratar condições dependentes de catepsina em um mamìfero que disto necessita, para inibir ressorção óssea, para incrementar a densidade mineral óssea, e, para reduzir o risco de fraturas
DE60229114D1 (en) Cathepsincystein-proteasehemmer
BR0211119A (pt) Composto, método de tratar um paciente que tenha, ou de prevenir um paciente de pegar, uma doença ou condição, uso de um composto, e, método para fabricar um composto
BR0211364A (pt) Composição farmacêutica para tratamento de doenças associadas com redução na massa óssea compreendendo o agonista ep4 como componente ativo
BR0211118A (pt) Composto, métodos para o tratamento ou prevenção de doenças e para fabricar um composto, intermediário, e, uso de um composto ou sal
BR0017075A (pt) Derivados de piridopirimidinona para tratamento de doença neurodegenerativa
BR0315597A (pt) Processos de baixa dose para tratamento de distúrbios em que a atividade de tnf(alfa)é prejudicial
BR0310092A (pt) Combinação de compostos orgânicos
BR0306724A (pt) carboxamidas amino substituìdas para tratamento de doença de alzheimer
ATE450265T1 (de) Pharmazeutische mischung zur behandlung von krebs,die dioxolan nukleosidanalogen enthält
BR0211122A (pt) Composto, métodos para o tratamento ou prevenção de doenças e para fabricar um composto, intermediário, e, uso de um composto ou sal
DE60120691D1 (de) Zusammensetzungen zur verwendung bei der behandlung der osteoporose und/oder der entzündlichen gelenkerkrankungen
ATE232874T1 (de) Prostaglandin-konjugate zur behandlung von knochenkrankheiten
WO2004098617A3 (en) Controlled release composition containing a strontium salt
ATE553090T1 (de) Cathepsincysteinproteasehemmer
BR0215395A (pt) Compostos; processo para a preparação de um composto; composição farmacêutica; e método para o tratamento e/ou profilaxia de doenças que estão relacionadas com o nìvel de glicose no sangue
BR0316458A (pt) Composto, composição farmacêutica, método de tratamento ou prevenção de doenças, método para intensificar a cognição em um paciente saudável, e, uso de um composto
BR0209128A (pt) Compostos, composições farmacêuticas, métodos para o tratamento de dores, métodos para a modulação de uma resposta farmacológica e usos de compostos
DE60024120D1 (de) Substituierte (aminoiminomethyl oder aminomethyl) dihydrobenzofurane und benozopyrane
BR0214359A (pt) Método para tratar ou prevenir o mal de alzheimer e uma doença e para tratar um paciente que tem, ou para prevenir que um paciente adquira uma doença ou condição, para inibir a atividade de beta-secretase, a clivagem de um isotipo de proteìna de precursor amilóide e a produção de peptìdeo e de placa beta-amilóide e para produzir um complexo de beta-secretase, uso de um composto e, composição
BR9508185A (pt) Composto de tetraésteres de ácido piridinil-aminometilideno- bisfônico composição farmacêutica processo para fabricar uma composição farmacêutica e método para tratar doenças ósseas
AU2003251728A8 (en) Placental growth factor as a target for the treatment of osteoporosis
BRPI0410657A (pt) composto, composição farmacêutica, uso de um composto, método para tratar um distúrbio de um paciente, e, processo para a preparação de um composto
BR0211121A (pt) Composto, métodos para o tratamento ou prevenção de doenças e para fabricar um composto, intermediário, e, uso de um composto ou sal
BR0308118A (pt) Método para o tratamento de osteoartrite

Legal Events

Date Code Title Description
B25A Requested transfer of rights approved

Owner name: AXYS PHARMACEUTICALS, INC (US) , MERCK FROSST CANA

Free format text: TRANSFERIDO DE: MERCK FROSST CANADA AND CO.

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: PARA: INT. CL. A61K 31/275, 31/281, 31/404, 31/417, 31/42, 31/4245, 31/426, 31/427, 31/44, 31/4406," 31/4409, 31/4465, 31/47, 31/495, 31/505, 31/5375, 45/00 "25, 255/29, 255/46, 255/58, 311/37, 317/32, 317/36 /61, 213/64, 213/70, 213/71, 213/74, 213/89, 215/12, 231/12, 233/54, 233/64, 239/26, 241/12, 261/08,263/32, 271/06, 277/28, 295/12, 295/135, 295/22, 307/52, 333/20, 401/04, 417/04

Ipc: A61K 31/275 (2011.01), A61K 31/381 (2011.01), A61K

Free format text: PARA: INT. CL. A61K 31/275, 31/281, 31/404, 31/417, 31/42, 31/4245, 31/426, 31/427, 31/44, 31/4406, 31/4409, 31/4465, 31/47, 31/495, 31/505, 31/5375, 45/00; A61P 19/02, 19/08, 19/10, 29/00; C07C 255/25, 255/29, 255/46, 255/58, 311/37, 317/32, 317/36; C07D 209/08, 211/26, 211/38, 213/36, 213/38, 213/61, 213/64, 213/70, 213/71, 213/74, 213/89, 215/12, 231/12, 233/54, 233/64, 239/26, 241/12, 261/08, 263/32, 271/06, 277/28, 295/12, 295/135, 295/22, 307/52, 333/20, 401/04, 417/04

Ipc: A61K 31/275 (2011.01), A61K 31/381 (2011.01), A61K

B25D Requested change of name of applicant approved

Owner name: AXYS PHARMACEUTICALS, INC (US) , MERCK CANADA INC.

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]
B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 28/02/2003 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 20A ANUIDADE.

B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2711 DE 20-12-2022 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.