HRP20020221B1 - - Google Patents

Info

Publication number
HRP20020221B1
HRP20020221B1 HR20020221A HRP20020221A HRP20020221B1 HR P20020221 B1 HRP20020221 B1 HR P20020221B1 HR 20020221 A HR20020221 A HR 20020221A HR P20020221 A HRP20020221 A HR P20020221A HR P20020221 B1 HRP20020221 B1 HR P20020221B1
Authority
HR
Croatia
Prior art keywords
alkyl
pyrrolidinyl
piperazinyl
piperidinyl
indolinyl
Prior art date
Application number
HR20020221A
Other languages
English (en)
Inventor
J. Emmanuel Michael
Lynn Frye Leah
R. Hickey Eugene
Liu Weimin
M. Morwick Tina
M. Spero Denice
Sun Sanxing
S. Thomson David
D. Ward Yancey
R. R. Young Erick
Original Assignee
Boehringer Ingelheim Pharmaceuticals 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 Boehringer Ingelheim Pharmaceuticals Inc. filed Critical Boehringer Ingelheim Pharmaceuticals Inc.
Publication of HRP20020221A2 publication Critical patent/HRP20020221A2/hr
Publication of HRP20020221B1 publication Critical patent/HRP20020221B1/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D207/10—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 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
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D207/10—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 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
    • C07D207/16—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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • 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
    • C07D211/66—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 having a hetero atom as the second substituent in position 4
    • 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
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Spoj formule (I): naznačen time, daHet je piperidinil, pirolidinil, azetidinil, tetrahidropiranil, tetrahidrotiopiranil, tetrahidrofuranil, heksahidropirimidinil, heksahidropiridazinil, piperazinil, 1,4,5,6-tetrahidropirimidin-2-ilamin, dihidro-oksazolil, 1,2-tiazinil-1,1-dioksid, 1,2,6-tiadiazinanil-1,1-dioksid, izotiazolidinil-1,1-dioksid ili imidazolidinil-2,4-dion, od kojih je svaki prema pkk,ootrebi supstituiran s jednim ili više R5;Y je O ili S; R1 je C1-5-alkil, C1-5-alkoksi, ariloksi, C3-7-cikloalkil, fenil, benzil, naftil, tetrahidronaftil, C1-5-alkilsulfonil-C1-5-alkil, C3-7-cikloalkilsulfonil-C1-5-alkil, arilsulfonil-C1-5-alkil, pirolidinil, piperidinil, morfolinil, tiomorfolinil, piperazinil, indolinil, piranil, tiopiranil, furanil, tienil, pirolil, oksazolil, izoksazolil, tiazolil, imidazolil, piridinil, pirimidinil, pirazinil, indolil, benzofuranil, benzotienil, benzimidazolil, benzatiazolil, kinolinil, izokinolinil, kinazolinil, benzoksazolil, kinoksalinil, ili amino; pri čemu R1 je prema potrebi supstituiran s jednim ili više Ra;Ra je C1-5-alkil, C3-7-cikloalkil, fenil, naftil, pirolidinil, piperidinil, morfolinil, tiomorfolinil, piperazinil, indolinil, furanil, tienil, pirolil, oksazolil, tiazolil, imidazolil, triazolil, tetrazolil, piridinil, pirimidinil, pirazinil, indolil, benzofuranil, benzotienil, benzimidazolil, benztiazolil, benzoksazolil, benzizoksazolil, kinolinil, izokinolinil, kinazolinil, kinoksalinil, C1-5-alkoksi, C1-5-alkanoil, C1-5-alkanoiloksi, ariloksi, benziloksi, C1-5-alkoksikarbonil, ariloksi-karbonil, aroiloksi, karbamoil pri čemu dušikov atom može biti neovisno mono ili di-supstituiran sa supstituentom iz skupine koju čine C1-8-alkil, aril, pirolidinil, piperidinil, morfolinil, tiomorfolinil, piperazinil, indolinil, furanil, tienil, pirolil, oksazolil, tiazolil, imidazolil, triazolil, tetrazolil, piridinil, pirimidinil, pirazinil, indolil, benzofuranil, benzotienil, benz-imidazolil, benztiazolil, kinolinil, izokinolinil, kinazolinil ili kinoksalinil, ili Ra je C1-5-alkanoilamino, aroilamino, C1-5-alkiltio, ariltio pri čemu sumporni atom može biti oksidiran u sulfoksid ili sulfon, ureido gdje dušikov atom može biti neovisno supstituiran sa supstituentom iz skupine koju čine alkil, aril, pirolidinil, piperidinil, morfolinil, tiomorfolinil, piperazinil, indolinil, furanil, tienil, pirolil, oksazolil, tiazolil, imidazolil, triazolil, tetrazolil, piridinil, pirimidinil, pirazinil, indolil, benzofuranil, benzotienil, benzimidazolil, benz-tiazolil, kinolinil, izokinolinil, kinazolinil ili kinoksalinil, C1-5-alkoksikarbonilamino, ariloksikarbonilamino, C1-5-alkilkarbamoiloksi, arilkarbamoiloksi, C1-5-alkilsulfonilamino,arilsulfonilamino, C1-5-alkilaminosulfonil, arilaminosulfonil, amino gdje dušikov atom može biti neovisno mono ili di-supstituiran sa supstituentom iz skupine koju čine alkil, aril, pirolidinil, piperidinil, morfolinil, tiomorfolinil, piperazinil, indolinil, furanil, tienil, pirolil, oksazolil, tiazo
HR20020221A 1999-09-13 2002-03-12 Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases HRP20020221A2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15373899P 1999-09-13 1999-09-13
US22290000P 2000-08-03 2000-08-03
PCT/US2000/023584 WO2001019816A1 (en) 1999-09-13 2000-08-28 Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases

Publications (2)

Publication Number Publication Date
HRP20020221A2 HRP20020221A2 (en) 2005-10-31
HRP20020221B1 true HRP20020221B1 (hr) 2007-01-31

Family

ID=26850810

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20020221A HRP20020221A2 (en) 1999-09-13 2002-03-12 Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases

Country Status (30)

Country Link
EP (1) EP1218372B1 (hr)
JP (1) JP2003529546A (hr)
KR (1) KR20030024651A (hr)
CN (1) CN100410250C (hr)
AR (1) AR032136A1 (hr)
AT (1) ATE244235T1 (hr)
AU (1) AU782246B2 (hr)
BG (1) BG106483A (hr)
BR (1) BR0013966A (hr)
CA (1) CA2385130C (hr)
CZ (1) CZ2002844A3 (hr)
DE (1) DE60003702T2 (hr)
DK (1) DK1218372T3 (hr)
EE (1) EE200200132A (hr)
ES (1) ES2199856T3 (hr)
HK (1) HK1048807A1 (hr)
HR (1) HRP20020221A2 (hr)
HU (1) HUP0302380A2 (hr)
IL (2) IL148184A0 (hr)
MY (1) MY122696A (hr)
NO (1) NO323354B1 (hr)
NZ (1) NZ518255A (hr)
PL (1) PL364045A1 (hr)
PT (1) PT1218372E (hr)
RU (1) RU2255937C2 (hr)
SA (1) SA00210456B1 (hr)
SK (1) SK286463B6 (hr)
TW (1) TWI230159B (hr)
WO (1) WO2001019816A1 (hr)
YU (1) YU17402A (hr)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL145429A0 (en) 1999-03-15 2002-06-30 Axys Pharm Inc N-cyanomethyl amides, processes for the preparation thereof and pharmaceutical compositions containing the same
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
AR036375A1 (es) 2001-08-30 2004-09-01 Novartis Ag Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos
RS19504A (en) 2001-09-14 2007-02-05 Aventis Pharmaceuticals Inc., Novel compounds and compositions as cathepsin inhibitors
EP1434769A2 (en) 2001-10-02 2004-07-07 Boehringer Ingelheim Pharmaceuticals Inc. Compounds useful as reversible inhibitors of cysteine proteases
WO2003037892A1 (en) * 2001-10-29 2003-05-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
HUP0401906A3 (en) 2001-11-14 2008-07-28 Aventis Pharma Inc Novel cathepsin s inhibitors, process for their preparation and pharmaceutical compositions containing them
WO2003075853A2 (en) 2002-03-08 2003-09-18 Bristol-Myers Squibb Company Cyclic derivatives as modulators of chemokine receptor activity
AU2003256305A1 (en) * 2002-06-24 2004-01-06 Axys Pharmaceuticals, Inc. Peptidic compounds as cysteine protease inhibitors
EA010027B1 (ru) 2002-11-27 2008-06-30 Инсайт Корпорейшн Производные 3-аминопирролидина в качестве модуляторов рецепторов хемокинов
EP1569954A1 (en) * 2002-12-05 2005-09-07 Axys Pharmaceuticals, Inc. Cyanomethyl derivatives as cysteine protease inhibitors
US7384970B2 (en) 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
US7109243B2 (en) 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
WO2004108661A1 (en) * 2003-06-04 2004-12-16 Axys Pharmaceuticals Amidino compounds as cysteine protease inhibitors
US7173051B2 (en) 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
US7256207B2 (en) 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
NZ542865A (en) * 2003-09-18 2009-04-30 Virobay Inc Haloalkyl containing compounds as cysteine protease inhibitors
US7297714B2 (en) * 2003-10-21 2007-11-20 Irm Llc Inhibitors of cathepsin S
JP5154944B2 (ja) 2004-12-02 2013-02-27 ビロベイ，インコーポレイティド システインプロテアーゼインヒビターとしてのスルホンアミド含有化合物
ES2400582T3 (es) 2005-03-21 2013-04-10 Virobay, Inc. Compuestos de alfa cetoamida como inhibidores de cisteína proteasa
WO2006102535A2 (en) 2005-03-22 2006-09-28 Celera Genomics Sulfonyl containing compounds as cysteine protease inhibitors
AR056865A1 (es) * 2005-06-14 2007-10-31 Schering Corp Heterociclos nitrogenados y su uso como inhibidores de proteasas, composiciones farmaceuticas
US8067415B2 (en) 2005-11-01 2011-11-29 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of CCR2
US8067457B2 (en) 2005-11-01 2011-11-29 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of CCR2
UY30090A1 (es) * 2006-01-16 2007-08-31 Syngenta Participations Ag Insecticidas novedosos
ES2392675T3 (es) * 2006-06-01 2012-12-12 Sanofi Nitrilos espirocíclicos como inhibidores de proteasa
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
NZ576105A (en) 2006-10-04 2012-01-12 Virobay Inc Di-fluoro containing compounds as cysteine protease inhibitors
DE102006057036A1 (de) * 2006-12-04 2008-06-05 Bayer Cropscience Ag Biphenylsubstituierte spirocyclische Ketoenole
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases
EP2198879A1 (en) 2008-12-11 2010-06-23 Institut Curie CD74 modulator agent for regulating dendritic cell migration and device for studying the motility capacity of a cell
US8324417B2 (en) 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
WO2012151319A1 (en) 2011-05-02 2012-11-08 Virobay, Inc. Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain
US9278966B2 (en) 2011-06-07 2016-03-08 Kureha Corporation Method for manufacturing oxetane compound, method for manufacturing azolylmethylcyclopentanol compound, and intermediate compound
EP2537532A1 (en) 2011-06-22 2012-12-26 J. Stefan Institute Cathepsin-binding compounds bound to a nanodevice and their diagnostic and therapeutic use
US9187451B2 (en) 2011-11-18 2015-11-17 Heptares Therapeutics Limited Muscarinic M1 receptor agonists
GB201513743D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB202020191D0 (en) 2020-12-18 2021-02-03 Heptares Therapeutics Ltd Pharmaceutical compounds
US11124497B1 (en) 2020-04-17 2021-09-21 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
US11174231B1 (en) 2020-06-09 2021-11-16 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
AU2021286560A1 (en) * 2020-06-09 2023-02-02 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
EP4305021A1 (en) * 2021-03-10 2024-01-17 Vincere Biosciences, Inc. Usp30 inhibitors and uses thereof
WO2023044171A1 (en) * 2021-09-20 2023-03-23 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL322409A1 (en) * 1995-03-24 1998-01-19 Arris Pharm Corp Reversible protease inhibitors
US5776718A (en) * 1995-03-24 1998-07-07 Arris Pharmaceutical Corporation Reversible protease inhibitors
TW438591B (en) * 1995-06-07 2001-06-07 Arris Pharm Corp Reversible cysteine protease inhibitors
IL145429A0 (en) * 1999-03-15 2002-06-30 Axys Pharm Inc N-cyanomethyl amides, processes for the preparation thereof and pharmaceutical compositions containing the same

Also Published As

Publication number Publication date
ATE244235T1 (de) 2003-07-15
AU782246B2 (en) 2005-07-14
MY122696A (en) 2006-04-29
SK286463B6 (sk) 2008-10-07
CN1384830A (zh) 2002-12-11
CA2385130A1 (en) 2001-03-22
EP1218372A1 (en) 2002-07-03
PT1218372E (pt) 2003-11-28
DK1218372T3 (da) 2003-10-20
EE200200132A (et) 2003-12-15
IL148184A (en) 2007-03-08
CA2385130C (en) 2009-10-20
CN100410250C (zh) 2008-08-13
NO323354B1 (no) 2007-04-10
HUP0302380A2 (hu) 2004-03-01
YU17402A (sh) 2004-11-25
DE60003702D1 (de) 2003-08-07
SK4902002A3 (en) 2002-09-10
BR0013966A (pt) 2004-06-15
EP1218372B1 (en) 2003-07-02
ES2199856T3 (es) 2004-03-01
IL148184A0 (en) 2002-09-12
NO20021207D0 (no) 2002-03-12
KR20030024651A (ko) 2003-03-26
HK1048807A1 (zh) 2003-04-17
RU2255937C2 (ru) 2005-07-10
HRP20020221A2 (en) 2005-10-31
SA00210456B1 (ar) 2006-10-03
PL364045A1 (en) 2004-12-13
TWI230159B (en) 2005-04-01
WO2001019816A1 (en) 2001-03-22
AR032136A1 (es) 2003-10-29
CZ2002844A3 (cs) 2002-06-12
BG106483A (bg) 2002-10-31
NZ518255A (en) 2004-11-26
JP2003529546A (ja) 2003-10-07
AU7081800A (en) 2001-04-17
NO20021207L (no) 2002-03-12
DE60003702T2 (de) 2004-04-22

Similar Documents

Publication Publication Date Title
HRP20020221B1 (hr)
MY8200075A (en) Proline derivatives and related compounds
DE3662260D1 (en) Acrylic acid esters and fungicides containing these compounds
ECSP045359A (es) Isoxazolinas 5 metiloximetil sustituidas por 3-heteroarilo utilizadas con herbicidas
ATE173256T1 (de) Azolidindion-derivate und ihre anwendung als antihyperglykämika
ES380579A1 (es) Un procedimiento para la preparacion de un n-(5(6)-acil-2- bencimidazolil) carbamato de alquilo.
ES8201560A1 (es) Un procedimiento para la preparacion de derivados de oxazo- lidona- o tiazolidona.
ES2040213T3 (es) Nuevos derivados de 3-oxadiazol- y 3-(ester de acido carboxilico)-beta-carbolina, su preparacion y su utilizacion como medicamentos.
ES363171A1 (es) Un procedimiento para la preparacion de penicilinas.
YU19892A (sh) Neurolepticki perhidro-1h-pirido /1,2/ pirazini
ES2016279B3 (es) Derivados de ciclohexenona
ATE5881T1 (de) Thiatriazindioxide und diese enthaltende herbizide mittel.
SE7906461L (sv) N-substituerade aziridin-2-karbonsyraderivat
ES2039257T3 (es) Derivados del acido isocianurico.
CO5221051A1 (es) Compuestos peptidil espiroheterociclicos amidino y guanidino, composiciones farmaceuticas que los contienen y su metodo de fabricacion
BR8106485A (pt) Composicao
GB1035918A (en) 1,4-benzodiazepin-2-ones
FR2239476A1 (en) Dialkyl 1-heterocyclic-vinyl phosphates - with insecticidal and acaricidal activity
GB1109309A (en) Heterocyclic acetaldehydes
DK0498179T3 (da) Cyclopropancarboxylsyreamider og -thioamider, fremgangsmåde og mellemprodukter til deres fremstilling, samt deres anvendelse til skadedyrsbekæmpelse
DE59009055D1 (de) N-Heterocyclomethyl-spiroheterocyclen und diese enthaltende Fungizide.
ATE14314T1 (de) 7-beta-(ketooximinoacylamido)-ceph-3-em-4carbons|urederivate, verfahren zur herstellung derselben und diese enthaltende arzneimittel.
ES454285A1 (es) Procedimiento para preparar derivados de 4-amina trans-deca-hidroquinolina.
ES379033A1 (es) Un procedimiento para la preparacion de fenilpiridonas.
ES452592A1 (es) Procedimiento para preparar esteres organicos de acidos fos-foricos.

Legal Events

Date Code Title Description
A1OB Publication of a patent application
ARAI Request for the grant of a patent on the basis of the submitted results of a substantive examination of a patent application
B1PR Patent granted
ODRP Renewal fee for the maintenance of a patent

Payment date: 20070816

Year of fee payment: 8

PBON Lapse due to non-payment of renewal fee

Effective date: 20080829