ATE411985T1 - Substituierte piperazine als modulatoren des melanocortinrezeptors - Google Patents

Substituierte piperazine als modulatoren des melanocortinrezeptors

Info

Publication number
ATE411985T1
ATE411985T1 AT02761189T AT02761189T ATE411985T1 AT E411985 T1 ATE411985 T1 AT E411985T1 AT 02761189 T AT02761189 T AT 02761189T AT 02761189 T AT02761189 T AT 02761189T AT E411985 T1 ATE411985 T1 AT E411985T1
Authority
AT
Austria
Prior art keywords
melanocortin receptor
modulators
compounds
substituted piperazines
prophylaxis
Prior art date
Application number
AT02761189T
Other languages
English (en)
Inventor
Christopher Fotsch
Premilla Arasasingham
Yunxin Bo
Ning Chen
Martin Goldberg
Nianhe Han
Feng-Yin Hsieh
Michael Kelly
Qingyian Liu
Mark Norman
Duncan Smith
Markian Stec
Nuria Tamayo
Ning Xi
Shimin Xu
Original Assignee
Amgen 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
Application filed by Amgen Inc filed Critical Amgen Inc
Application granted granted Critical
Publication of ATE411985T1 publication Critical patent/ATE411985T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/60—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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • C07D213/60—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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • C07D215/16—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 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/06—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • 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
    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/60—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
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
    • C07D317/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06147—Dipeptides with the first amino acid being heterocyclic and His-amino acid; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Seasonings (AREA)
  • Indole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
AT02761189T 2001-07-25 2002-07-25 Substituierte piperazine als modulatoren des melanocortinrezeptors ATE411985T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30783101P 2001-07-25 2001-07-25
US10/202,823 US7115607B2 (en) 2001-07-25 2002-07-24 Substituted piperazinyl amides and methods of use

Publications (1)

Publication Number Publication Date
ATE411985T1 true ATE411985T1 (de) 2008-11-15

Family

ID=26898056

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02761189T ATE411985T1 (de) 2001-07-25 2002-07-25 Substituierte piperazine als modulatoren des melanocortinrezeptors

Country Status (11)

Country Link
US (2) US7115607B2 (de)
EP (1) EP1417190B1 (de)
JP (1) JP2005503369A (de)
AT (1) ATE411985T1 (de)
AU (1) AU2002326469B2 (de)
CA (1) CA2454903A1 (de)
DE (1) DE60229530D1 (de)
ES (1) ES2315390T3 (de)
MX (1) MXPA04000761A (de)
PL (1) PL370381A1 (de)
WO (1) WO2003009850A1 (de)

Families Citing this family (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004523529A (ja) * 2001-01-23 2004-08-05 イーライ・リリー・アンド・カンパニー メラノコルチンレセプターアゴニスト
US7456184B2 (en) 2003-05-01 2008-11-25 Palatin Technologies Inc. Melanocortin receptor-specific compounds
US7354923B2 (en) 2001-08-10 2008-04-08 Palatin Technologies, Inc. Piperazine melanocortin-specific compounds
US20030158209A1 (en) * 2001-10-09 2003-08-21 Neurocrine Biosciences Inc. Ligands of melanocortin receptors and compositions and methods related thereto
US20050119251A1 (en) * 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
US7390813B1 (en) * 2001-12-21 2008-06-24 Xenon Pharmaceuticals Inc. Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents
EP1503761A1 (de) * 2002-05-10 2005-02-09 Neurocrine Biosciences, Inc. Substituierte piperazine als melanokortin-rezeptor liganden
US7132539B2 (en) * 2002-10-23 2006-11-07 The Procter & Gamble Company Melanocortin receptor ligands
WO2004081643A1 (en) * 2002-12-20 2004-09-23 Kaiser Aerospace & Electronics Corp. Lenslet array with polarization conversion
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US7153858B2 (en) 2003-01-31 2006-12-26 Epix Delaware, Inc. Arylpiperazinyl compounds
EP1460070B1 (de) * 2003-03-20 2007-05-16 Santhera Pharmaceuticals (Schweiz) AG Substituierte Piperidin- und Piperazin-Derivative als Melanocortin-4 Receptor Modulatoren
KR20060026011A (ko) 2003-05-09 2006-03-22 노보 노르디스크 에이/에스 비만 치료용 펩티드
CA2539596A1 (en) 2003-09-30 2005-04-07 Kilian Waldemar Conde-Frieboes Melanocortin receptor agonists
US20050119252A1 (en) * 2003-10-22 2005-06-02 Neurocrine Biosciences, Inc. Ligands of melanocortin receptors and compositions and methods related thereto
CN1883145B (zh) * 2003-11-21 2010-12-08 松下电器产业株式会社 多天线接收装置、多天线接收方法、多天线发送装置以及多天线通信系统
EP1538159A1 (de) * 2003-12-05 2005-06-08 Santhera Pharmaceuticals (Schweiz) GmbH Substituierte N-Benzyl-lactam Derivate als Melanocortin-4 Rezeptor Agonisten
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
WO2005110989A1 (en) * 2004-04-07 2005-11-24 Neurogen Corporation Substituted 1-heteroaryl-4-substituted piperazine and piperidine analogues
WO2005110982A2 (en) * 2004-04-07 2005-11-24 Neurogen Corporation Substituted 1-benzyl-4-substituted piperazine analogues
WO2005118573A1 (en) * 2004-05-28 2005-12-15 Smithkline Beecham Corporation Novel diazepine compounds as ligands of the melanocortin 1 and/or 4 receptors
CN101090724A (zh) * 2004-09-20 2007-12-19 泽农医药公司 用于抑制人硬脂酰CoA去饱和酶的吡啶衍生物
WO2006034279A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
CN101084207A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
EP1807085B1 (de) 2004-09-20 2013-08-21 Xenon Pharmaceuticals Inc. Heterozyklische Derivate und ihre Verwendung als Stearoyl-Coa-Desaturase-Inhibitoren
CN101084212A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶介导剂的用途
AU2005286793A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes
JP5149009B2 (ja) * 2004-09-20 2013-02-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド ヒトステアロイル−ＣｏＡデサチュラーゼを阻害するためのピリダジン誘導体
CA2580857A1 (en) * 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
CN101083986A (zh) * 2004-09-20 2007-12-05 泽农医药公司 双环杂环衍生物及其作为硬脂酰CoA去饱和酶(SCD)抑制剂的用途
US20070021433A1 (en) 2005-06-03 2007-01-25 Jian-Qiang Fan Pharmacological chaperones for treating obesity
AU2006343359A1 (en) * 2005-06-03 2007-11-15 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
KR20080048502A (ko) 2005-09-29 2008-06-02 머크 앤드 캄파니 인코포레이티드 멜라노코르틴-4 수용체 조절제로서의 아실화스피로피페리딘 유도체
WO2007047496A2 (en) 2005-10-18 2007-04-26 Merck & Co., Inc. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
JP2009519976A (ja) * 2005-12-15 2009-05-21 スミスクライン・ビーチャム・コーポレイション Ｔｒｐｖ４チャネル受容体のアゴニストとしてのピペラジン化合物
AU2008261102B2 (en) 2007-06-04 2013-11-28 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
US20100120694A1 (en) 2008-06-04 2010-05-13 Synergy Pharmaceuticals, Inc. Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders
US10022558B1 (en) 2008-01-07 2018-07-17 Salutaris Medical Devices, Inc. Methods and devices for minimally-invasive delivery of radiation to the eye
US9056201B1 (en) 2008-01-07 2015-06-16 Salutaris Medical Devices, Inc. Methods and devices for minimally-invasive delivery of radiation to the eye
DK3108933T3 (da) 2008-01-07 2019-11-25 Salutaris Medical Devices Inc Indretninger til minimal-invasiv extraokulær levering af radiation til posterior del af øjet
US8602959B1 (en) 2010-05-21 2013-12-10 Robert Park Methods and devices for delivery of radiation to the posterior portion of the eye
US9873001B2 (en) 2008-01-07 2018-01-23 Salutaris Medical Devices, Inc. Methods and devices for minimally-invasive delivery of radiation to the eye
US8608632B1 (en) 2009-07-03 2013-12-17 Salutaris Medical Devices, Inc. Methods and devices for minimally-invasive extraocular delivery of radiation and/or pharmaceutics to the posterior portion of the eye
JP2011519973A (ja) * 2008-05-12 2011-07-14 アムネスティックス・インコーポレーテッド 学習及び記憶を改善するための化合物関連出願に関する情報
ES2624828T3 (es) 2008-07-16 2017-07-17 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros
MX2011004258A (es) 2008-10-22 2011-06-01 Merck Sharp & Dohme Derivados de bencimidazol ciclicos novedosos utiles como agentes anti-diabeticos.
JP5557845B2 (ja) 2008-10-31 2014-07-23 メルク・シャープ・アンド・ドーム・コーポレーション 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体
UA99555C2 (en) 2008-11-12 2012-08-27 Элджи Лайф Саенсез Лтд. Melanocortin receptor agonists
JP5514831B2 (ja) 2008-11-17 2014-06-04 メルク・シャープ・アンド・ドーム・コーポレーション 糖尿病の治療のための置換二環式アミン
USD691268S1 (en) 2009-01-07 2013-10-08 Salutaris Medical Devices, Inc. Fixed-shape cannula for posterior delivery of radiation to eye
USD691267S1 (en) 2009-01-07 2013-10-08 Salutaris Medical Devices, Inc. Fixed-shape cannula for posterior delivery of radiation to eye
USD691269S1 (en) 2009-01-07 2013-10-08 Salutaris Medical Devices, Inc. Fixed-shape cannula for posterior delivery of radiation to an eye
USD691270S1 (en) 2009-01-07 2013-10-08 Salutaris Medical Devices, Inc. Fixed-shape cannula for posterior delivery of radiation to an eye
NZ596205A (en) * 2009-04-16 2013-01-25 Takeda Pharmaceutical Derivatives of n-acyl-n'-phenylpiperazine useful (inter alia) for the prophylaxis or treatment of diabetes
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
CA2768577A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
US9044606B2 (en) 2010-01-22 2015-06-02 Ethicon Endo-Surgery, Inc. Methods and devices for activating brown adipose tissue using electrical energy
US8476227B2 (en) 2010-01-22 2013-07-02 Ethicon Endo-Surgery, Inc. Methods of activating a melanocortin-4 receptor pathway in obese subjects
CA2786314A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
BR112012021231A2 (pt) 2010-02-26 2015-09-08 Basf Plant Science Co Gmbh método para acentuar o rendimento em plantas, planta, construto, uso de um construto, método para a produção de uma planta transgênica, partes coletáveis de uma planta, produtos derivados de uma planta, uso de um ácido nucleíco e método para a produção de um produto
WO2011104378A1 (en) 2010-02-26 2011-09-01 Novo Nordisk A/S Peptides for treatment of obesity
WO2011137024A1 (en) 2010-04-26 2011-11-03 Merck Sharp & Dohme Corp. Novel spiropiperidine prolylcarboxypeptidase inhibitors
WO2011143057A1 (en) 2010-05-11 2011-11-17 Merck Sharp & Dohme Corp. Novel prolylcarboxypeptidase inhibitors
EP2579873A4 (de) 2010-06-11 2013-11-27 Merck Sharp & Dohme Neuartige prolylcarboxypeptidase-hemmer
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
US9018395B2 (en) 2011-01-27 2015-04-28 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
EP2677869B1 (de) 2011-02-25 2017-11-08 Merck Sharp & Dohme Corp. Neue cyclische azabenzimidazolderivate als antidiabetika
CA2880901A1 (en) 2012-08-02 2014-02-06 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
MX2015010935A (es) 2013-02-22 2015-10-29 Merck Sharp & Dohme Compuestos biciclicos antidiabeticos.
EP2970119B1 (de) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Neuartige indolderivate als antidiabetika
HK1220611A1 (zh) 2013-03-15 2017-05-12 Bausch Health Ireland Limited 用於治疗胃肠道病症的组成物
US9708367B2 (en) 2013-03-15 2017-07-18 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase and their uses
EP3004138B1 (de) 2013-06-05 2024-03-13 Bausch Health Ireland Limited Ultrareine agonisten von guanylatcyclase c, verfahren zur herstellung und verwendung davon
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US10092738B2 (en) 2014-12-29 2018-10-09 Ethicon Llc Methods and devices for inhibiting nerves when activating brown adipose tissue
US10080884B2 (en) 2014-12-29 2018-09-25 Ethicon Llc Methods and devices for activating brown adipose tissue using electrical energy
AU2016367914A1 (en) * 2015-12-11 2018-06-28 The Board Of Regents Of The University Of Texas System Substituted benzimidazolium, pyrido-imidazolium, or pyrazino-imidazolium compounds as chemotherapeutics
USD814637S1 (en) 2016-05-11 2018-04-03 Salutaris Medical Devices, Inc. Brachytherapy device
USD815285S1 (en) 2016-05-11 2018-04-10 Salutaris Medical Devices, Inc. Brachytherapy device
USD814638S1 (en) 2016-05-11 2018-04-03 Salutaris Medical Devices, Inc. Brachytherapy device
WO2017216805A1 (en) * 2016-06-15 2017-12-21 Lakshmi Prasad Alaparthi Intermediates and processes for preparation of vortioxetine
ES2880174T3 (es) * 2016-07-19 2021-11-23 Astellas Pharma Inc Derivado de piperazina
USD808529S1 (en) 2016-08-31 2018-01-23 Salutaris Medical Devices, Inc. Holder for a brachytherapy device
USD808528S1 (en) 2016-08-31 2018-01-23 Salutaris Medical Devices, Inc. Holder for a brachytherapy device
WO2018106518A1 (en) 2016-12-06 2018-06-14 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
US10968232B2 (en) 2016-12-20 2021-04-06 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
US10519121B2 (en) 2016-12-30 2019-12-31 Apicore Us Llc Process and novel polymorphic form of vortioxetine and its pharmaceutically acceptable salts
SG11202012071TA (en) 2018-06-05 2021-01-28 Crinetics Pharmaceuticals Inc Melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof
EP4054583A4 (de) 2019-11-07 2023-10-25 Crinetics Pharmaceuticals, Inc. Melanocortin-subtyp-2-rezeptor(mc2r)-antagonisten und deren verwendungen
KR20220129553A (ko) 2019-12-18 2022-09-23 크리네틱스 파마슈티칼스, 인크. Gem-이치환된 피페리딘 멜라노코르틴 아형-2 수용체(mc2r) 길항제 및 이의 용도
US12466829B2 (en) 2019-12-23 2025-11-11 Crinetics Pharmaceuticals, Inc. Spirocyclic piperidine melanocortin subtype-2 receptor (MC2R) antagonists and uses thereof
IL305952A (en) 2021-03-19 2023-11-01 Crinetics Pharmaceuticals Inc Melanocortin subtype 2 receptor (MC2R) antagonist for disease treatment
CN113549038B (zh) * 2021-07-07 2023-05-23 常州大学 多取代异苯并呋喃化合物及其用途

Family Cites Families (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6051556A (en) * 1988-04-28 2000-04-18 Mycogen Corporation Hybrid pesticidal toxins
WO1992008709A1 (de) * 1990-11-15 1992-05-29 Pentapharm Ag Meta-substituierte phenylalanin-derivate
JPH069402A (ja) * 1991-05-15 1994-01-18 Hiroyoshi Hidaka 抗潰瘍剤
FR2680508B1 (fr) * 1991-08-20 1995-03-03 Adir Nouveaux composes amidiques des 1-(alcoxybenzyl)piperazines, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent.
DE59309867D1 (de) 1992-09-03 1999-12-16 Boehringer Ingelheim Pharma Neue aminosäurederivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende pharmazeutische zusammensetzungen
WO1994022460A1 (en) 1993-04-05 1994-10-13 University Patents, Inc. Diagnosis and treatment of erectile dysfunction
US5681954A (en) * 1993-05-14 1997-10-28 Daiichi Pharmaceutical Co., Ltd. Piperazine derivatives
US5721251A (en) * 1993-12-10 1998-02-24 Merck & Co., Inc. Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone
AU2695795A (en) 1994-06-13 1996-01-05 Merck & Co., Inc. Piperazine compounds promote release of growth hormone
US6054556A (en) * 1995-04-10 2000-04-25 The Arizona Board Of Regents On Behalf Of The University Of Arizona Melanocortin receptor antagonists and agonists
KR0173034B1 (ko) 1995-04-28 1999-03-30 성재갑 선택적 트롬빈 억제제
US5575290A (en) * 1995-06-30 1996-11-19 Siemens Medical Systems, Inc. Coarse-fine ultrasound transducer array for medical imaging
US5935959A (en) 1995-07-13 1999-08-10 Senju Pharmaceutical Co., Ltd. Piperazine derivatives and use as cysteine inhibitors
ATE230389T1 (de) * 1995-10-25 2003-01-15 Senju Pharma Co Angiogenese inhibitoren
AU7710596A (en) 1995-11-29 1997-06-19 Nihon Nohyaku Co., Ltd. Phenylalanine derivatives, optically active substances, salts or coordination compounds thereof, and their use as fungicides
WO1997019919A1 (en) 1995-11-30 1997-06-05 C & C Research Laboratories Sulfamide derivatives
JP2000509039A (ja) 1996-04-23 2000-07-18 ファルマシア・アンド・アップジョン・カンパニー マトリックスメタロプロテイナーゼ・インヒビターとして有用なチアジアゾリル（チオ）尿素
EP1440976B1 (de) * 1996-09-10 2008-07-23 Boehringer Ingelheim Pharma GmbH & Co.KG Abgewandelte Aminosäuren, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE69819349T2 (de) * 1997-08-29 2004-07-22 Tularik Ltd. 1-amino-7-isochinolin-derivate als serin protease inhibitoren
JP2002517444A (ja) 1998-06-11 2002-06-18 メルク エンド カムパニー インコーポレーテッド メラノコルチン受容体作動薬としてのスピロピペリジン誘導体
US6303637B1 (en) 1998-10-30 2001-10-16 Merck & Co., Inc. Heterocyclic potassium channel inhibitors
ES2238870T3 (es) 1998-12-17 2005-09-01 Wyeth Derivados amida de arilpiperidina y aril-1,2,5,6-tetrahidropiridina que presentan actividad en el receptor 5ht1a.
EP1140831A1 (de) 1998-12-17 2001-10-10 American Home Products Corporation Arylpiperidin- und aryl-1,2,5,6-tetrahydropyridinharnstoff-derivate mit 5ht1a rezeptor aktivität
JP2003505435A (ja) 1999-06-04 2003-02-12 メルク エンド カムパニー インコーポレーテッド メラノコルチン−４受容体ゴニストとしての置換ピペリジン
JP2003502373A (ja) 1999-06-23 2003-01-21 メルク エンド カムパニー インコーポレーテッド インテグリン受容体アンタゴニスト
AU6621600A (en) 1999-08-04 2001-03-05 Millennium Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
EP1086947A1 (de) 1999-09-01 2001-03-28 Pfizer Products Inc. Somatostatin Antagonisten und Agonisten, die an der SST Subtyp 2 Rezeptor wirken
WO2001034586A2 (en) * 1999-11-12 2001-05-17 Wyeth Branched adamantyl and noradamantyl aryl- and aralkylpiperazines with serotonin 5-ht1a activity
EP1320366A4 (de) * 2000-08-23 2005-04-06 Merck & Co Inc Substituierte piperidine als melanocortin-rezeptoragonisten
US20020091090A1 (en) * 2000-12-28 2002-07-11 Cole Bridget M. Somatostatin antagonists and agonists
JP2004523529A (ja) 2001-01-23 2004-08-05 イーライ・リリー・アンド・カンパニー メラノコルチンレセプターアゴニスト
US7169777B2 (en) 2001-01-23 2007-01-30 Eli Lilly And Company Melanocortin receptor agonists
WO2002059107A1 (en) 2001-01-23 2002-08-01 Eli Lilly And Company Substituted piperidines/piperazines as melanocortin receptor agonists
WO2002062766A2 (en) 2001-02-07 2002-08-15 Millennium Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
ATE341327T1 (de) 2001-02-28 2006-10-15 Merck & Co Inc Acylierte piperidin-derivate als melanocortin-4- rezeptor-agonisten
US7012084B2 (en) 2001-02-28 2006-03-14 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists
MXPA03007785A (es) 2001-02-28 2003-12-08 Merck & Co Inc Derivados de piperidina acilados como agonistas del receptor de melanocortina 4.
EP1370211A4 (de) 2001-03-02 2005-02-09 Bristol Myers Squibb Co Gleichzeitige verabreichung eines melanocortin rezeptor-agonists und eines phosphodiesterase-hemmers zur behandlung von erkrankungen im zusammenhang mit zyklischer amp
CA2437594A1 (en) 2001-03-02 2002-09-12 Graham S. Poindexter Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same
US6977264B2 (en) * 2001-07-25 2005-12-20 Amgen Inc. Substituted piperidines and methods of use
US20030158209A1 (en) 2001-10-09 2003-08-21 Neurocrine Biosciences Inc. Ligands of melanocortin receptors and compositions and methods related thereto
JP2005527492A (ja) 2002-01-23 2005-09-15 イーライ・リリー・アンド・カンパニー メラノコルチン受容体アゴニスト
WO2003063781A2 (en) 2002-01-29 2003-08-07 Merck & Co., Inc. Substituted imidazoles as cannabinoid receptor modulators

Also Published As

Publication number Publication date
US20030220324A1 (en) 2003-11-27
US7560460B2 (en) 2009-07-14
PL370381A1 (en) 2005-05-30
EP1417190A1 (de) 2004-05-12
CA2454903A1 (en) 2003-02-06
JP2005503369A (ja) 2005-02-03
EP1417190B1 (de) 2008-10-22
US20070265248A1 (en) 2007-11-15
WO2003009850A1 (en) 2003-02-06
US7115607B2 (en) 2006-10-03
DE60229530D1 (de) 2008-12-04
ES2315390T3 (es) 2009-04-01
AU2002326469B2 (en) 2006-03-30
MXPA04000761A (es) 2004-07-08

Similar Documents

Publication Publication Date Title
ATE411985T1 (de) Substituierte piperazine als modulatoren des melanocortinrezeptors
DE60224404D1 (de) Substiuierte piperidine als melanocortinrezeptor-modulatoren
ATE404552T1 (de) Substituierte isochinolinderivate und anwendungsverfahren
ATE453636T1 (de) Substituierte 2,3-dihydro-1h-isoindol-1-one derivate und anwendungsverfahren
MY177111A (en) Substituted amide derivatives and methods of use
BR0311494A (pt) Novos indóis substituìdos
SE0303180D0 (sv) Novel compounds
SE0302232D0 (sv) Novel Compounds
SE0203713D0 (sv) Novel compounds
NO20033181D0 (no) Substituerte alkylaminderivater og fremgangsmater for anvendelse
DE60118003D1 (de) Harnstoffderivate und ihre verwendung
MXPA05013366A (es) Derivados de benzazepina utiles para el tratamiento de enfermedades asociadas con el receptor 5ht2c.
ATE388708T1 (de) Piperazinderivate und anwendungsverfahren
ATE440834T1 (de) Substituierte arylaminderivate und verwendungsverfahren
MX2009003981A (es) Agentes moduladores del receptor de calcio.
NO20063275L (no) Anvendelse av substituerte 2-aminotetraliner for forebyggende behandling av Parkinsons sykdom
EA200601194A1 (ru) Новые производные бензофурана, используемые для профилактики или лечения нарушений, связанных с 5-ht-рецептором
EA200600071A1 (ru) Производные n-фенилпиперазина и способы профилактики или лечения заболеваний, связанных с 5ht-рецептором
TW200800946A (en) Substituted piperazines as metabotropic glutamate receptor antagonists
DE602004009099D1 (de) Verwendung von 2-thia-dibenzoäe,hüazulenen zur behandlung und prävention von erkrankungen und störungen des zentralen nervensystems
DE60312154D1 (de) 2-oxo-1,3,4-trihydrochinazolin derivative zur behandlung von zellproliferationskrankheiten
PL377470A1 (pl) Zastosowanie lewocetyryzyny do leczenia przetrwałego alergicznego nieżytu nosa

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties