EA201000070A1 - Модуляторы калликреина 7 - Google Patents

Модуляторы калликреина 7

Info

Publication number
EA201000070A1
EA201000070A1 EA201000070A EA201000070A EA201000070A1 EA 201000070 A1 EA201000070 A1 EA 201000070A1 EA 201000070 A EA201000070 A EA 201000070A EA 201000070 A EA201000070 A EA 201000070A EA 201000070 A1 EA201000070 A1 EA 201000070A1
Authority
EA
Eurasian Patent Office
Prior art keywords
kallikreina
modulators
kallikrein
crystal structure
application
Prior art date
Application number
EA201000070A
Other languages
English (en)
Other versions
EA018050B1 (ru
Inventor
Штефани Флор
Штефан Андреас Рандль
Нильс Остерманн
Ульрих Хассипен
Фредерик Берст
Урсула Бодендорф
Бернд Герхартц
Андреас Марцинцик
Клаус Эрхардт
Йозеф Готтфрид Майнгасснер
Original Assignee
Новартис Аг
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 Новартис Аг filed Critical Новартис Аг
Publication of EA201000070A1 publication Critical patent/EA201000070A1/ru
Publication of EA018050B1 publication Critical patent/EA018050B1/ru

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
    • C07D207/10—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D209/52—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 condensed with a ring other than six-membered
    • 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
    • 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
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6445—Kallikreins (3.4.21.34; 3.4.21.35)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21034—Plasma kallikrein (3.4.21.34)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Toxicology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)

Abstract

В заявке описаны кристаллическая структура сериновой протеазы калликреина 7 и применение этой кристаллической структуры для создания лекарственных средств. В заявке описаны также соединения, обладающие способностью специфически связываться с указанным активным сайтом калликреина 7.
EA201000070A 2007-06-28 2008-06-26 Модуляторы калликреина 7, фармацевтическая композиция, содержащая эти соединения, способ лечения нарушений, опосредуемых активностью калликреина 7 EA018050B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07111316 2007-06-28
EP07115197 2007-08-29
PCT/EP2008/058139 WO2009000878A1 (en) 2007-06-28 2008-06-26 Kallikrein 7 modulators

Publications (2)

Publication Number Publication Date
EA201000070A1 true EA201000070A1 (ru) 2010-06-30
EA018050B1 EA018050B1 (ru) 2013-05-30

Family

ID=39651437

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201000070A EA018050B1 (ru) 2007-06-28 2008-06-26 Модуляторы калликреина 7, фармацевтическая композиция, содержащая эти соединения, способ лечения нарушений, опосредуемых активностью калликреина 7

Country Status (29)

Country Link
US (2) US8309596B2 (ru)
EP (1) EP2170939A1 (ru)
JP (2) JP2010532162A (ru)
KR (1) KR20100027159A (ru)
CN (1) CN101687913B (ru)
AR (1) AR067336A1 (ru)
AU (1) AU2008267167C1 (ru)
BR (1) BRPI0813230A2 (ru)
CA (1) CA2691849A1 (ru)
CL (1) CL2008001906A1 (ru)
CO (1) CO6251242A2 (ru)
CR (1) CR11134A (ru)
CU (1) CU23944B1 (ru)
EA (1) EA018050B1 (ru)
EC (1) ECSP099829A (ru)
GT (1) GT200900326A (ru)
HN (1) HN2009003484A (ru)
IL (1) IL202284A0 (ru)
MA (1) MA31454B1 (ru)
MX (1) MX2009013952A (ru)
MY (1) MY183252A (ru)
NZ (1) NZ581438A (ru)
PE (1) PE20090484A1 (ru)
SG (1) SG182961A1 (ru)
TN (1) TN2009000520A1 (ru)
TW (1) TWI411433B (ru)
UA (1) UA98647C2 (ru)
WO (1) WO2009000878A1 (ru)
ZA (1) ZA200908159B (ru)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009093119A2 (en) * 2008-01-21 2009-07-30 Med Discovery S.A. Use of serine protease inhibitors in the treatment of skin diseases
EP2766345B1 (en) 2011-10-14 2016-03-16 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US20140179727A1 (en) 2012-12-14 2014-06-26 Trevi Therapeutics, Inc. Methods for treating pruritus
US8987289B2 (en) * 2012-12-14 2015-03-24 Trevi Therapeutics, Inc. Methods for treating pruritus
HUE052990T2 (hu) 2014-01-23 2021-05-28 Sixera Pharma Ab Új kallikrein 7 gátlók
CN107922428B (zh) * 2015-06-25 2021-02-05 普洛麦格公司 噻吩并吡咯化合物及其作为刺虾源性荧光素酶的抑制剂的用途
CN105218545A (zh) * 2015-11-04 2016-01-06 衡阳师范学院 激肽释放酶7小分子抑制剂及其制备方法、用途
CN106518868B (zh) * 2015-11-04 2018-02-23 衡阳师范学院 激肽释放酶7小分子抑制剂及其制备方法、用途
CN105330665B (zh) * 2015-11-04 2017-10-03 衡阳师范学院 一种抑制激肽释放酶klk7的化合物、制备方法和用途
CN106243058B (zh) * 2016-07-28 2018-06-29 三峡大学 一种化合物在制备抑制激肽释放酶klk7的药物上的应用及其合成方法
CN108421034A (zh) * 2018-04-24 2018-08-21 济南磐升生物技术有限公司 激肽释放酶7在皮肤创伤愈合中的应用
SG11202100580UA (en) 2018-07-23 2021-02-25 Trevi Therapeutics Inc Treatment of chronic cough, breathlessness and dyspnea
CN110256417A (zh) * 2019-07-05 2019-09-20 衡阳师范学院 一种激肽释放酶klk7抑制物、制备方法和用途

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3905870A (en) * 1972-11-03 1975-09-16 Bayer Ag Purification of kallikrein
DE3843226A1 (de) 1988-12-22 1990-06-28 Boehringer Ingelheim Kg Chromatographieplatten und verfahren zur duennschicht-chromatographischen trennung von enantiomeren
WO1998003537A2 (en) * 1996-07-24 1998-01-29 Novartis Ag Hirustasin and a hirustasin/kallikrein complex in crystalline form
JPH11292840A (ja) * 1998-04-06 1999-10-26 Soyaku Gijutsu Kenkyusho:Kk ノルスタチン誘導体又はその塩
ES2270898T3 (es) * 1999-12-24 2007-04-16 F. Hoffmann-La Roche Ag Derivados de nitrilo como inhibidores de catepsina k.
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
GB0115515D0 (en) * 2001-06-25 2001-08-15 Ferring Bv Oxytocin agonisys
JP2003185650A (ja) * 2001-12-18 2003-07-03 National Institute Of Advanced Industrial & Technology 薬剤のスクリーニング方法
CA2473740A1 (en) 2002-01-18 2003-07-31 David Solow-Cordero Methods of treating conditions associated with an edg receptor
AU2002953533A0 (en) 2002-12-24 2003-01-16 Arthron Limited Fc receptor modulating compounds and compositions
US7129264B2 (en) * 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
AU2004246766B2 (en) * 2003-06-18 2009-09-17 Merck Patent Gmbh Pyrrolidin-1, 2- dicarboxylic acid- 1- [(4- ethinyl- phenyl) - amid]- 2- [(phenyl)- amid] derivative as inhibitors of coagulation factor Xa and VIIa for the treatment of thrombosis
DE10358814A1 (de) * 2003-12-16 2005-07-21 Merck Patent Gmbh Prolinylarylacetamide
WO2005075667A1 (en) 2004-02-03 2005-08-18 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with kallikrein 7 (klk7)
DE102004014945A1 (de) * 2004-03-26 2005-10-13 Merck Patent Gmbh Prolinylderivate
SG156687A1 (en) 2004-07-28 2009-11-26 Janssen Pharmaceutica Nv Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase

Also Published As

Publication number Publication date
EA018050B1 (ru) 2013-05-30
EP2170939A1 (en) 2010-04-07
UA98647C2 (en) 2012-06-11
CL2008001906A1 (es) 2009-02-20
CU20090229A7 (es) 2012-02-15
JP2010532162A (ja) 2010-10-07
PE20090484A1 (es) 2009-05-27
TWI411433B (zh) 2013-10-11
BRPI0813230A2 (pt) 2014-12-23
CN101687913A (zh) 2010-03-31
TN2009000520A1 (en) 2011-03-31
ECSP099829A (es) 2010-01-29
CU23944B1 (es) 2013-10-29
GT200900326A (es) 2010-05-21
AU2008267167B2 (en) 2011-10-27
SG182961A1 (en) 2012-08-30
TW200906390A (en) 2009-02-16
NZ581438A (en) 2011-03-31
AU2008267167C1 (en) 2012-11-01
US20100256144A1 (en) 2010-10-07
IL202284A0 (en) 2010-06-16
KR20100027159A (ko) 2010-03-10
MA31454B1 (fr) 2010-06-01
HN2009003484A (es) 2012-04-17
CO6251242A2 (es) 2011-02-21
CN101687913B (zh) 2013-09-18
US8309596B2 (en) 2012-11-13
CR11134A (es) 2010-02-04
CA2691849A1 (en) 2008-12-31
US20130028843A1 (en) 2013-01-31
WO2009000878A1 (en) 2008-12-31
ZA200908159B (en) 2010-12-29
AU2008267167A1 (en) 2008-12-31
JP2013166768A (ja) 2013-08-29
MY183252A (en) 2021-02-18
AR067336A1 (es) 2009-10-07
MX2009013952A (es) 2010-01-28

Similar Documents

Publication Publication Date Title
EA201000070A1 (ru) Модуляторы калликреина 7
EA200602221A1 (ru) Новое применение пептидных соединений для лечения боли при тригеминальной невралгии
EA201000784A1 (ru) Антагонисты пути hedgehog и их терапевтические применения
EA200970737A1 (ru) Оксабициклогептаны и оксабициклогептены, их получение и применение
EA200700702A1 (ru) Аналоги локсапина и способы их применения
EA200901166A1 (ru) Соединения и композиции в качестве модуляторов активности gpr 119
EA201100037A1 (ru) Органические соединения
BR112012019042A2 (pt) "inibidores de serina protease tipo tripsina, e sua preparação e uso".
EA201490922A1 (ru) ПРОИЗВОДНЫЕ ГИДАНТОИНА, ПОЛЕЗНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ Kv3-КАНАЛОВ
EA200500203A1 (ru) Новый способ синтеза и новая кристаллическая форма агомелатина и фармацевтические композиции, которые её содержат
DE602006004463D1 (de) Kristallform von asenapinmaleat
EA201300242A1 (ru) Фармацевтические композиции, содержащие замещенные ациланилиды
ATE528007T1 (de) Lagerstabile infusionslösung von dihydropteridinonen
CY1112653T1 (el) Κρυσταλλικες τροποποιησεις της πυρακλοστροβινης
EA201070544A1 (ru) Новый класс терапевтических веществ, усиливающих диффузию низкомолекулярных соединений
EA200701396A1 (ru) Триазолофталазины в качестве ингибиторов pde-2
EA200801997A1 (ru) Новые соединения
DE602008003911D1 (de) Co-kristalle von propiconazol
ATE541848T1 (de) Diaryl-purin, azapurine und deazapurine als nichtnukleoside reverse-transkriptase-inhibitoren zur behandlung von hiv
EA200700400A1 (ru) Производные n-(1h-индолил)-1н-индол-2-карбоксамидов, их получение и их применение в терапии
CY1118976T1 (el) Κρυσταλλικες τροποποιησεις της (1r,2r)-3-(3-διμεθυλαμινο-1-αιθυλ-2-μεθυλ-προπυλ)-φαινολης
EA200601267A1 (ru) Модуляторы рецепторов андрогена
EA200702336A1 (ru) ПРИМЕНЕНИЕ 24-норУДХК
DE602006020585D1 (de) Neue cysteinproteasehemmer und ihre therapeutische anwendung
ITMI20050477A1 (it) Cerotto transdermico

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): BY KZ RU