ATE449090T1 - Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren - Google Patents

Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren

Info

Publication number
ATE449090T1
ATE449090T1 AT02742851T AT02742851T ATE449090T1 AT E449090 T1 ATE449090 T1 AT E449090T1 AT 02742851 T AT02742851 T AT 02742851T AT 02742851 T AT02742851 T AT 02742851T AT E449090 T1 ATE449090 T1 AT E449090T1
Authority
AT
Austria
Prior art keywords
histamine
diazepande
derivatives
receptor modulators
substituted piperazine
Prior art date
Application number
AT02742851T
Other languages
English (en)
Inventor
Florencio Doerwald
Knud Andersen
Jan Sorensen
Original Assignee
High Point Pharmaceuticals Llc
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 High Point Pharmaceuticals Llc filed Critical High Point Pharmaceuticals Llc
Application granted granted Critical
Publication of ATE449090T1 publication Critical patent/ATE449090T1/de

Links

Classifications

    • 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • 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
    • C07D213/56—Amides
    • 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
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/70—Sulfur atoms
    • C07D277/74—Sulfur atoms substituted by carbon atoms
    • 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
    • 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
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • 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
    • C07D295/20—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 carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
    • 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
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen 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
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen 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 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
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D317/10—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 not condensed with other rings
    • C07D317/14—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 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/30—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
    • 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
    • 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
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/60—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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrane Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
AT02742851T 2001-07-02 2002-06-27 Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren ATE449090T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA200101046 2001-07-02
DKPA200101878 2001-12-14
PCT/DK2002/000438 WO2003004480A2 (en) 2001-07-02 2002-06-27 Substituted piperazine and diazepanes as histamine h3 receptor agonists

Publications (1)

Publication Number Publication Date
ATE449090T1 true ATE449090T1 (de) 2009-12-15

Family

ID=26069046

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02742851T ATE449090T1 (de) 2001-07-02 2002-06-27 Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren

Country Status (6)

Country Link
EP (1) EP1421071B1 (de)
JP (1) JP2005502623A (de)
AT (1) ATE449090T1 (de)
AU (1) AU2002344951A1 (de)
DE (1) DE60234453D1 (de)
WO (1) WO2003004480A2 (de)

Families Citing this family (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006503827A (ja) * 2002-09-06 2006-02-02 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ アレルギー性鼻炎治療用薬剤を製造する目的でインドリル誘導体を用いる使用
ATE449766T1 (de) 2002-10-23 2009-12-15 Janssen Pharmaceutica Nv Piperazinyl- und diazapanylbenzamide und- benzothioamide
US7226930B2 (en) * 2003-04-18 2007-06-05 Memory Pharmaceutical Corporation Phosphodiesterase 4 inhibitors
HRP20080541T3 (en) 2003-04-23 2008-12-31 Glaxo Group Limited Piperazine derivatives and their use for the treatment of neurological and psychiatric diseases
CN100522171C (zh) * 2003-09-09 2009-08-05 弗·哈夫曼-拉罗切有限公司 作为甘氨酸摄取抑制剂、用于治疗精神病的1-苯甲酰基哌嗪衍生物
GB0324159D0 (en) 2003-10-15 2003-11-19 Glaxo Group Ltd Novel compounds
JP2007531753A (ja) 2004-03-31 2007-11-08 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 非イミダゾール系複素環式化合物
US7423176B2 (en) * 2004-04-13 2008-09-09 Cephalon, Inc. Bicyclic aromatic sulfinyl derivatives
PL1828154T3 (pl) 2004-12-09 2009-10-30 Hoffmann La Roche Pochodne fenylopiperazynometanonu
MX2007006896A (es) 2004-12-15 2007-06-26 Hoffmann La Roche Fenil-metanonas bi- y triciclicas sustituidas como inhibidores del transportador 1 de glicina (glyt-1) para el tratamiento de la enfermedad de alzheimer.
ATE412636T1 (de) * 2004-12-16 2008-11-15 Hoffmann La Roche Piperazinylpyridinderivate als mittel gegen adipositas
US7485637B2 (en) 2005-01-04 2009-02-03 Hoffmann-La Roche Inc. Benzoyl-tetrahydropiperidine derivatives
ATE472327T1 (de) 2005-01-07 2010-07-15 Hoffmann La Roche Ä4-(heteroaryl)piperazin-1-ylü-(2,5-substituier e phenyl)methanon-derivate als glycin-transporter 1 (glyt-1) hemmer zur behandlung von neurologischen und neuropsychiatrischen erkrankungen
DE602006007682D1 (de) 2005-01-18 2009-08-20 Hoffmann La Roche 2,5-disubstituierte phenylmethanonderivative als glycintransporter-1-inhibitoren (glyt-1) zur behandlung von neurologischen und neuropsychiatrischen störungen
BRPI0607241A2 (pt) 2005-01-26 2009-08-25 Hoffmann La Roche derivados de fenil metanona e o uso dos mesmos como inibidores do transportador de glicina 1
WO2006082001A1 (en) 2005-02-07 2006-08-10 F.Hoffmann-La Roche Ag Heterocyclic substituted phenyl methanones as inhibitors of the glycine transporter 1
DE602006010833D1 (de) * 2005-03-17 2010-01-14 Lilly Co Eli Pyrrolidinderivate als histamin-h3-rezeptorantagonisten
CN101193635A (zh) * 2005-05-13 2008-06-04 莱西肯医药有限公司 多环化合物及其使用方法
CA2609957A1 (en) * 2005-06-20 2007-01-04 Schering Corporation Carbon-linked substituted piperidines and derivatives thereof useful as histamine h3 antagonists
WO2007016496A2 (en) 2005-08-02 2007-02-08 Neurogen Corporation Dipiperazinyl ketones and related analogues
KR101336106B1 (ko) 2005-09-16 2013-12-05 얀센 파마슈티카 엔.브이. 히스타민 ｈ3 수용체의 조절제로서 사이클로프로필 아민
BRPI0707916A2 (pt) * 2006-01-13 2011-05-17 Hoffmann La Roche compostos, processo para a sua manufatura, composições farmacêuticas que os compreendem e uso destes compostos
TW200734313A (en) * 2006-01-17 2007-09-16 Astrazeneca Ab Piperazines and piperidines as mGluR5 potentiators
MX339668B (es) 2006-05-30 2016-06-02 Janssen Pharmaceutica N V * Compuestos de piridil amida sustituidos como moduladores del receptor h3 de la histamina.
CN101511807A (zh) * 2006-06-29 2009-08-19 詹森药业有限公司 组胺h3受体的取代的苯甲酰胺调节剂
US7977358B2 (en) 2007-07-26 2011-07-12 Hoffmann-La Roche Inc. Pyrazol derivatives
BRPI0815591B8 (pt) 2007-08-22 2021-05-25 Astrazeneca Ab composto, composição farmacêutica, e, uso de um composto.
WO2009030716A1 (en) 2007-09-06 2009-03-12 Glaxo Group Limited Piperazine derivative having affinity for the histamine h3 receptor
CN105712977B (zh) 2007-11-20 2021-06-29 詹森药业有限公司 作为组胺h3受体调节剂的环烷基氧基吡啶化合物和杂环烷基氧基吡啶化合物
WO2009067405A1 (en) * 2007-11-20 2009-05-28 Janssen Pharmaceutica N.V. Substituted pyrazinyl amide compounds as modulators of the histamine h3 receptor
US8093248B2 (en) 2007-12-05 2012-01-10 Astrazeneca Ab (Publ) Compounds useful for the treatment of conditions associated with weight gain
WO2009126782A1 (en) * 2008-04-11 2009-10-15 High Point Pharmaceuticals, Llc Histamine h3 receptor ligands
CA2721303C (en) 2008-05-08 2016-06-28 Evotec Ag Azetidines and cyclobutanes as histamine h3 receptor antagonists
US8236792B2 (en) 2008-05-23 2012-08-07 Janssen Pharmaceutica Nv Substituted pyrrolidine amides as modulators of the histamine H3 receptor
JP2011522006A (ja) * 2008-06-04 2011-07-28 アストラゼネカ アクチボラグ 新規化合物ｖ
AU2009313315A1 (en) * 2008-11-07 2011-06-30 The Cleveland Clinic Foundation Compounds and methods of promoting oligodendrocyte precursor differentiation
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
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
CA2768577A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
AU2011218491C1 (en) 2010-02-18 2015-05-14 Astrazeneca Ab Processes for making cyclopropyl amide derivatives and intermediates associated therewith
US8785634B2 (en) 2010-04-26 2014-07-22 Merck Sharp & Dohme Corp 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
ME02320B (me) 2010-09-02 2016-06-20 Suven Life Sciences Ltd Heterociklička jedinjenja kao ligandi histamin h3 receptora
WO2013155223A1 (en) 2012-04-10 2013-10-17 The Regents Of The University Of California Compositions and methods for treating cancer
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
AU2016245864C1 (en) 2015-04-10 2021-09-09 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356347A1 (de) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitoren von kras-g12c-mutanten proteinen
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (de) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitoren von kras-g12c-mutanten proteinen
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤をスクリーニングするための方法
KR102932353B1 (ko) 2015-11-16 2026-02-27 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
EP3573954A1 (de) 2017-01-26 2019-12-04 Araxes Pharma LLC Fusionierte bicyclische benzoheteroaromatische verbindungen und verfahren zur verwendung davon
EP3573971A1 (de) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-on-derivate und ähnliche verbindungen als kras-g12c-modulatoren zur behandlung von krebs
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2101081B1 (de) 1970-08-19 1974-01-11 Rhone Poulenc Sa
DE2304155A1 (de) * 1973-01-29 1974-08-01 Ichthyol Ges Cordes Hermanni & N-acylierte substituierte piperazinbzw. homopiperazinderivate, sowie verfahren zu ihrer herstellung
US4420477A (en) * 1979-11-30 1983-12-13 Fujisawa Pharmaceutical Co., Ltd. Cephem compounds
JPS56120669A (en) * 1980-02-27 1981-09-22 Res Inst For Prod Dev Allophanoylpiperazine compound and analgesic agent containing the same as active constituent
FR2514355A1 (fr) * 1981-10-14 1983-04-15 Fabre Sa Pierre Derives de biphenyl alcoyl carboxylates, leur procede de preparation et leur utilisation comme medicaments
US4457931A (en) * 1982-09-27 1984-07-03 Selvi & C. S.P.A. Piperazine derivatives with anticholinergic and/or antihistaminic activity
JPS6289676A (ja) * 1985-06-05 1987-04-24 Kuraray Co Ltd ３，４−ジヒドロベンゾピラン誘導体類及びその医薬用途
JPS63107968A (ja) * 1986-06-30 1988-05-12 Toyo Jozo Co Ltd ２−置換アルコキシ−３−置換−ピラジン類化合物
JPS6314774A (ja) * 1986-07-07 1988-01-21 Mitsubishi Chem Ind Ltd ピリダジノン誘導体又はその塩類
JPH0720929B2 (ja) * 1988-08-15 1995-03-08 三井東圧化学株式会社 ジヒドロカフェイン酸アミド化合物およびそれを有効成分として含有する治療剤
US5010080A (en) * 1988-12-02 1991-04-23 G. D. Searle & Co. Use of heterocyclic amides to inhibit tumor metastasis
EP0385043A1 (de) * 1989-02-28 1990-09-05 Fabrica Espanola De Productos Quimicos Y Farmaceuticos, S.A. (Faes) 4-Substituierte Piperazinderivate
JPH03275657A (ja) * 1989-07-05 1991-12-06 Kanegafuchi Chem Ind Co Ltd ケイ皮酸アミド誘導体
EP0589985A1 (de) * 1991-06-21 1994-04-06 Boehringer Mannheim Italia S.P.A. 2-amino-4-aryl-thiazole-derivate mit asthma-hemmender und entzündungshemmender wirkung auf der atemwegen
EP0524055A1 (de) * 1991-07-19 1993-01-20 Synthelabo Imidazo(2,1-b)benzothiazolderivate, Verfahren zu ihrer Herstellung und ihre therapeutische Verwendung
FR2722788B1 (fr) * 1994-07-20 1996-10-04 Pf Medicament Nouvelles piperazides derivees d'aryl piperazine, leurs procedes de preparation, leur utilisation a titre de medicament et les compositions pharmaceutiques les comprenant
SK282252B6 (sk) * 1995-01-11 2001-12-03 Samjin Pharmaceutical Co., Ltd. Piperazínové deriváty a farmaceutický prostriedok s ich obsahom
JP3081773B2 (ja) * 1995-03-31 2000-08-28 株式会社資生堂 Ｎ−アシルピペラジン誘導体及び抗菌剤、抗潰瘍剤
JP4263240B2 (ja) 1995-11-09 2009-05-13 サノフィ−アベンティス ５−フェニル−３−（ピペリジン−４−イル）−１，３，４−オキサジアゾール−２（３ｈ）−オン誘導体、及びその５−ｈｔ４又はｈ３レセプターリガンドとしての用途
US6399618B1 (en) * 1997-07-09 2002-06-04 Cardiome Pharma Corp Compositions and methods for modulating sexual activity
GB9803536D0 (en) 1998-02-19 1998-04-15 Black James Foundation Histamine H,receptor ligands
JP2000086603A (ja) * 1998-07-15 2000-03-28 Yoshitomi Pharmaceut Ind Ltd 桂皮酸アミド誘導体および３―フェニルプロピオン酸アミド誘導体
EP0978512A1 (de) 1998-07-29 2000-02-09 Societe Civile Bioprojet Aryloxy- (oder Arylthio)alkylamine ohne Imidazolring als Histamin-H3-Antagonisten und deren therapeutische Anwendung
GB9905010D0 (en) * 1999-03-04 1999-04-28 Merck Sharp & Dohme Therapeutic agents
US6211182B1 (en) * 1999-03-08 2001-04-03 Schering Corporation Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms
WO2000064884A1 (en) 1999-04-26 2000-11-02 Novo Nordisk A/S Piperidyl-imidazole derivatives, their preparations and therapeutic uses
WO2001066534A2 (en) 2000-03-09 2001-09-13 Abbott Laboratories Cyclic and bicyclic diamino histamine-3 receptor antagonists
GB0030304D0 (en) * 2000-12-13 2001-01-24 Lilly Co Eli Compounds
JP2002201178A (ja) * 2000-07-17 2002-07-16 Takeda Chem Ind Ltd スルホン誘導体、その製造法及び用途
US6316475B1 (en) 2000-11-17 2001-11-13 Abbott Laboratories Aminoalkoxybiphenylcarboxamides as histamine-3 receptor ligands and their therapeutic applications
GB0031088D0 (en) * 2000-12-20 2001-01-31 Smithkline Beecham Plc Medicaments

Also Published As

Publication number Publication date
AU2002344951A1 (en) 2003-01-21
WO2003004480A2 (en) 2003-01-16
JP2005502623A (ja) 2005-01-27
WO2003004480A3 (en) 2004-03-25
EP1421071A2 (de) 2004-05-26
EP1421071B1 (de) 2009-11-18
DE60234453D1 (de) 2009-12-31

Similar Documents

Publication Publication Date Title
DE60234453D1 (de) Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren
DE60329330D1 (de) Piperidin- und pyrrolidin-derivate alsantagonisten des histamin-h3-rezeptors
MEP53708A (en) 3-z-[1-(4-(n-((4-methyl-piperazin-1-yl)-methylcarbonyl) -n-methyl -amino) -anilino)-1- phenyl-methylene] -6-methoxycarbonyl -2-indolinone -monoethanesulphonate and the use thereof as a pharmaceutical composition
MY137053A (en) Pyrimidine derivatives and their use as cb2 modulators
BR0316350A (pt) Diaminotriazóis úteis como inibidores de proteìna cinases
BR0314393A (pt) Piperazinas heterocìclicas substituìdas para o tratamento de esquizofrenia
ATE450508T1 (de) Substituierte piperidinen mit selektiver bindungsfähigkeit zu histamin h3-rezeptoren
DE602004014117D1 (de) Thiazole zur verwendung als inhibitoren von protein-kinasen
ATE411985T1 (de) Substituierte piperazine als modulatoren des melanocortinrezeptors
ATE345329T1 (de) Pyridinderivate als modulatoren des cb2-rezeptors
EA200700118A1 (ru) Амидосоединения и их применение в качестве лекарственных средств
CY1111086T1 (el) Παραγωγα 2-αμινο-κιναζολινης χρησιμα ως αναστολεις της βητα-σεκρετασης (bace)
SE0201635D0 (sv) Novel compounds
SE0303180D0 (sv) Novel compounds
BRPI0514738A (pt) derivados de amida de 3-fenil-diidropirimido[4,5-d]pirimidinonas, sua fabricação e aplicação como agentes farmacêuticos
CY1111070T1 (el) Παραγωγα 2-αμινο-κουιναζολινης χρησιμα ως αναστολεις της β-σεκρετασης (bace)
ATE479655T1 (de) Neue aminoazetidin-, aminopyrrolidin- und aminopiperidinderivative
ATE524181T1 (de) Verwendung von 1,4-bis (3-aminoalkyl) piperazin- derivaten bei der behandlung von neurodegenerativen erkrankungen
SE9903894D0 (sv) Novel compounds
AU2003260436A1 (en) Pyrimidine compounds
SE0300456D0 (sv) Novel compounds
TW200800946A (en) Substituted piperazines as metabotropic glutamate receptor antagonists
CY1108837T1 (el) ΝΕΑ ΠΑΡΑΓΩΓΑ ΑΜΙΝΟΠΥΡΙΔΙΝΗΣ ΩΣ ΑΝΤΑΓΩΝΙΣΤΕΣ mGluR5
MXPA05013225A (es) Derivados de 1-aril-4-(ariloxicarbonil)-piperazina para uso como inhibidores de la lipasa sensible a hormonas.
DE60114597D1 (de) Naphthamid-neurokinin antagonisten zur verwendung als medikamente

Legal Events

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