CN106132940B - 新的激肽释放酶7抑制剂 - Google Patents

新的激肽释放酶7抑制剂 Download PDF

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Publication number
CN106132940B
CN106132940B CN201580005402.3A CN201580005402A CN106132940B CN 106132940 B CN106132940 B CN 106132940B CN 201580005402 A CN201580005402 A CN 201580005402A CN 106132940 B CN106132940 B CN 106132940B
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acetate
phenyl
propyl
ethyl
oxo
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CN106132940A (zh
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M·林斯霍滕
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Xikesi Pull Pharmaceutical Co
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Xikesi Pull Pharmaceutical Co
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    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/42—Amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/16—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/38—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with 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
    • C07D261/14—Nitrogen 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Birds (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Cosmetics (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
CN201580005402.3A 2014-01-23 2015-01-22 新的激肽释放酶7抑制剂 Active CN106132940B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE1430004 2014-01-23
SE1430004-0 2014-01-23
PCT/SE2015/050060 WO2015112079A1 (en) 2014-01-23 2015-01-22 New kallikrein 7 inhibitors

Publications (2)

Publication Number Publication Date
CN106132940A CN106132940A (zh) 2016-11-16
CN106132940B true CN106132940B (zh) 2019-04-23

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US (1) US9744148B2 (enExample)
EP (1) EP3097084B1 (enExample)
JP (2) JP6552010B2 (enExample)
CN (1) CN106132940B (enExample)
AU (1) AU2015209759B2 (enExample)
CA (1) CA2934024C (enExample)
CY (1) CY1123707T1 (enExample)
DK (1) DK3097084T3 (enExample)
ES (1) ES2834851T3 (enExample)
HR (1) HRP20201915T1 (enExample)
HU (1) HUE052990T2 (enExample)
LT (1) LT3097084T (enExample)
PL (1) PL3097084T3 (enExample)
PT (1) PT3097084T (enExample)
RS (1) RS61142B1 (enExample)
SI (1) SI3097084T1 (enExample)
SM (1) SMT202000653T1 (enExample)
WO (1) WO2015112079A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9744148B2 (en) * 2014-01-23 2017-08-29 Sixera Pharma Ab Kallikrein 7 inhibitors
EP3305781A1 (en) * 2016-10-07 2018-04-11 Deutsches Krebsforschungszentrum Chemical substances which inhibit the enzymatic activity of human kallikrein-related peptidase 6 (klk6)
US20200040103A1 (en) 2018-03-14 2020-02-06 Genentech, Inc. Anti-klk5 antibodies and methods of use
GB201809378D0 (en) * 2018-06-07 2018-07-25 Glaxosmithkline Ip Dev Ltd Novel compounds
AR119997A1 (es) 2019-09-18 2022-01-26 Genentech Inc Anticuerpos anti-klk7, anticuerpos anti-klk5, anticuerpos multiespecíficos anti-klk5 / klk7 y métodos de uso
CN117084936A (zh) * 2023-09-22 2023-11-21 南京盛德生物科技研究院有限公司 多萜类化合物作为激肽释放酶抑制剂在化妆品中的应用

Citations (4)

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Publication number Priority date Publication date Assignee Title
WO2003101941A2 (en) * 2002-05-31 2003-12-11 Genzyme Corporation Alpha acyloxyacetamides for kallikrein and urokinase inhibition
WO2004108139A2 (en) * 2003-06-06 2004-12-16 Arexis Ab Use of fused heterocyclic compounds as scce inhibitors for the treatment of skin conditions or cancer
WO2008062035A2 (en) * 2006-11-23 2008-05-29 Vib Vzw Activators of lateral root formation
WO2009024528A1 (en) * 2007-08-17 2009-02-26 Novartis Ag Use of cyclic depsipeptides to inhibit kallikrein 7

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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
US8309596B2 (en) 2007-06-28 2012-11-13 Novartis Ag Kallikrein 7 modulators
CN103298827B (zh) 2007-08-17 2017-05-31 诺华股份有限公司 环状酯肽
US8143269B2 (en) 2008-10-03 2012-03-27 Calcimedica, Inc. Inhibitors of store operated calcium release
EP2545916A1 (en) 2011-07-15 2013-01-16 Universite Pierre Et Marie Curie - Paris 6 Use of coumarin derivatives for the preparation of drugs for treating skin diseases
US9744148B2 (en) * 2014-01-23 2017-08-29 Sixera Pharma Ab Kallikrein 7 inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003101941A2 (en) * 2002-05-31 2003-12-11 Genzyme Corporation Alpha acyloxyacetamides for kallikrein and urokinase inhibition
WO2004108139A2 (en) * 2003-06-06 2004-12-16 Arexis Ab Use of fused heterocyclic compounds as scce inhibitors for the treatment of skin conditions or cancer
WO2008062035A2 (en) * 2006-11-23 2008-05-29 Vib Vzw Activators of lateral root formation
WO2009024528A1 (en) * 2007-08-17 2009-02-26 Novartis Ag Use of cyclic depsipeptides to inhibit kallikrein 7

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
"Nimesulide Based Novel Glycolamide Esters:Their Design, Synthesis, and Pharmacological Evaluation";Kavitha Kankanala et al.;《Journal of Chemistry》;20131231;第2013卷;第1-8页 *
"Piperazine and thiourea containing analogs of phenyl acetic acid: Synthesis and their antimicrobial activity";Navin B. Patel et al.;《Chemistry & Biology Interface》;20111231;第1卷(第1期);第79-94页 *
"Versatile, Fragrant, Convertible Isonitriles";Michael C. Pirrung et al.;《J. AM. CHEM. SOC.》;20060819;第128卷(第36期);第11772-11773页 *
提供的产品目录;来源：Aurora Building Blocks等;《数据库REGISTRY（在线）》;20120927;CAS登记号：1009280-55-0等 *

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US9744148B2 (en) 2017-08-29
EP3097084A4 (en) 2017-10-04
LT3097084T (lt) 2020-12-28
PL3097084T3 (pl) 2021-02-22
CA2934024A1 (en) 2015-07-30
DK3097084T3 (da) 2020-12-21
JP6552010B2 (ja) 2019-07-31
CN106132940A (zh) 2016-11-16
HUE052990T2 (hu) 2021-05-28
RS61142B1 (sr) 2020-12-31
CY1123707T1 (el) 2022-03-24
AU2015209759A1 (en) 2016-07-07
AU2015209759B2 (en) 2018-11-29
US20170000753A1 (en) 2017-01-05
SI3097084T1 (sl) 2021-01-29
PT3097084T (pt) 2020-12-09
SMT202000653T1 (it) 2021-01-05
JP6932386B2 (ja) 2021-09-08
HRP20201915T1 (hr) 2021-01-22
EP3097084A1 (en) 2016-11-30
JP2019163296A (ja) 2019-09-26
CA2934024C (en) 2022-08-23
ES2834851T3 (es) 2021-06-18
JP2017505299A (ja) 2017-02-16
WO2015112079A1 (en) 2015-07-30
EP3097084B1 (en) 2020-09-30

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