BRPI1013567B8 - Derivados de prolina como inibidores de catepsina - Google Patents

Derivados de prolina como inibidores de catepsina

Info

Publication number
BRPI1013567B8
BRPI1013567B8 BRPI1013567A BRPI1013567A BRPI1013567B8 BR PI1013567 B8 BRPI1013567 B8 BR PI1013567B8 BR PI1013567 A BRPI1013567 A BR PI1013567A BR PI1013567 A BRPI1013567 A BR PI1013567A BR PI1013567 B8 BRPI1013567 B8 BR PI1013567B8
Authority
BR
Brazil
Prior art keywords
proline derivatives
cathepsin inhibitors
cathepsin
inhibitors
proline
Prior art date
Application number
BRPI1013567A
Other languages
English (en)
Inventor
David Banner
Guido Hartmann
Hans Hilpert
Holger Kuehne
Harald Mauser
Jean-Marc Plancher
Peter Hartman
Alvarez Sanchez Ruben
M Ceccarelli Simona
Uwe Grether
Wolfgang Haap
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42261969&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI1013567(B8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BRPI1013567A2 publication Critical patent/BRPI1013567A2/pt
Publication of BRPI1013567B1 publication Critical patent/BRPI1013567B1/pt
Publication of BRPI1013567B8 publication Critical patent/BRPI1013567B8/pt

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
    • 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
    • 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
    • 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
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • 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
    • C07D207/12—Oxygen or sulfur atoms
    • 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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Food Preservation Except Freezing, Refrigeration, And Drying (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Peptides Or Proteins (AREA)

Abstract

derivados de prolina como inibidores de catepsina a invenção se refere um composto da fórmula (i) (i) em que a, r1 a r6 são tais como definidos na descrição e nas reivindicações. o composto da fórmula (i) pode ser usado como um medicamento.
BRPI1013567A 2009-04-20 2010-04-13 Derivados de prolina como inibidores de catepsina BRPI1013567B8 (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP09158212.2 2009-04-20
EP09158212 2009-04-20
EM09158212.2 2009-04-20
PCT/EP2010/054792 WO2010121918A1 (en) 2009-04-20 2010-04-13 Proline derivatives as cathepsin inhibitors

Publications (3)

Publication Number Publication Date
BRPI1013567A2 BRPI1013567A2 (pt) 2020-09-15
BRPI1013567B1 BRPI1013567B1 (pt) 2021-07-20
BRPI1013567B8 true BRPI1013567B8 (pt) 2021-12-07

Family

ID=42261969

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI1013567A BRPI1013567B8 (pt) 2009-04-20 2010-04-13 Derivados de prolina como inibidores de catepsina

Country Status (34)

Country Link
US (1) US8163793B2 (pt)
EP (1) EP2421826B1 (pt)
JP (1) JP5518997B2 (pt)
KR (1) KR101320790B1 (pt)
CN (1) CN102405211B (pt)
AR (1) AR076319A1 (pt)
AU (1) AU2010241084B2 (pt)
BR (1) BRPI1013567B8 (pt)
CA (1) CA2758210C (pt)
CL (1) CL2011002604A1 (pt)
CO (1) CO6430459A2 (pt)
CR (1) CR20110508A (pt)
CY (1) CY1114764T1 (pt)
DK (1) DK2421826T3 (pt)
EC (1) ECSP11011411A (pt)
ES (1) ES2436550T3 (pt)
HK (1) HK1166322A1 (pt)
HR (1) HRP20140030T1 (pt)
IL (1) IL215065A (pt)
MA (1) MA33224B1 (pt)
MX (1) MX2011011094A (pt)
MY (1) MY153880A (pt)
NZ (1) NZ595073A (pt)
PE (1) PE20120911A1 (pt)
PL (1) PL2421826T3 (pt)
PT (1) PT2421826E (pt)
RS (1) RS53122B (pt)
RU (1) RU2535479C2 (pt)
SG (1) SG175264A1 (pt)
SI (1) SI2421826T1 (pt)
TW (1) TWI418555B (pt)
UA (1) UA106748C2 (pt)
WO (1) WO2010121918A1 (pt)
ZA (1) ZA201107668B (pt)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8524710B2 (en) * 2010-11-05 2013-09-03 Hoffmann-La Roche Inc. Pyrrolidine derivatives
DK2776392T3 (en) * 2011-11-11 2016-07-04 Hoffmann La Roche PROCESS FOR THE PREPARATION OF 1-acyl-4-PHENYLSULFONYLPROLINAMID DERIVATIVES AND NEW INTERMEDIATE
JP2014533707A (ja) * 2011-11-25 2014-12-15 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ カテプシンの阻害剤としての新規ピロリジン誘導体
BR112014019180A8 (pt) * 2012-02-07 2017-07-11 Hoffmann La Roche Novos derivados de azetidina
CN104114549A (zh) * 2012-02-17 2014-10-22 霍夫曼-拉罗奇有限公司 新型吡咯烷衍生物
CN104379563B (zh) 2012-04-10 2018-12-21 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
BR112015003217A2 (pt) * 2012-08-21 2017-07-04 Hoffmann La Roche novos derivados de piridina.
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
USD753137S1 (en) * 2014-04-06 2016-04-05 Hsien-Wen Chang Display screen with transitional graphical user interface
WO2016034602A1 (en) * 2014-09-05 2016-03-10 F. Hoffmann-La Roche Ag Solid forms of (2s,4r)-4-[4-(1-methyl-1h-pyrazol-4-yl)-2-trifluoromethyl-benzenesulfonyl]-1-(1-trifluoromethyl-cyclopropanecarbonyl)-pyrrolidine-2-carboxylic acid (1-cyano-cyclopropyl)-amide
WO2016041915A1 (en) 2014-09-18 2016-03-24 F. Hoffmann-La Roche Ag Method for monitoring cathepsin s inhibition
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
AR102094A1 (es) 2014-09-25 2017-02-01 Araxes Pharma Llc Inhibidores de proteínas kras con una mutación g12c
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
BR112017021869A2 (pt) 2015-04-10 2018-12-11 Araxes Pharma Llc compostos quinazolina substituídos e métodos de uso dos mesmos
WO2016168540A1 (en) 2015-04-15 2016-10-20 Araxes Pharma Llc Fused-tricyclic inhibitors of kras and methods of use thereof
US10934244B2 (en) 2015-06-15 2021-03-02 Nmd Pharma A/S Compounds for use in treating neuromuscular disorders
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356339A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 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
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10882847B2 (en) 2015-09-28 2021-01-05 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
CN108779097A (zh) 2015-11-16 2018-11-09 亚瑞克西斯制药公司 包含取代的杂环基的2-取代的喹唑啉化合物及其使用方法
US9938265B2 (en) * 2015-11-30 2018-04-10 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
MX2018009638A (es) * 2016-02-26 2018-09-11 Hoffmann La Roche Derivados novedosos de pirrolidina.
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
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
WO2018139438A1 (ja) 2017-01-24 2018-08-02 アステラス製薬株式会社 フェニルジフルオロメチル置換プロリンアミド化合物
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
US11730714B2 (en) 2017-12-14 2023-08-22 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
US10385028B2 (en) 2017-12-14 2019-08-20 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
US11591284B2 (en) 2017-12-14 2023-02-28 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
US11147788B2 (en) 2017-12-14 2021-10-19 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
TW202023542A (zh) * 2018-09-18 2020-07-01 瑞士商赫孚孟拉羅股份公司 組織蛋白酶(cathepsin)S抑制劑之對抗抗藥抗體形成之用途
CN114105848B (zh) * 2021-11-24 2024-01-12 四川同晟生物医药有限公司 一种顺式-d-羟脯氨酸衍生物的制备方法
WO2023114516A2 (en) * 2021-12-17 2023-06-22 The Board Of Trustees Of The Leland Stanford Junior University Cell-permeant inhibitors of viral cysteine proteases
CN115466225A (zh) * 2022-08-16 2022-12-13 中国科学院上海药物研究所 一种酰胺类化合物及其制备方法、药物组合物和用途

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE40911B1 (en) 1974-04-11 1979-09-12 Schering Ag Imidazole derivatives and process for their manufacture
CA2106768C (en) 1991-04-19 2000-09-19 Donald J. Kyle Bradykinin type peptides
WO1998001133A1 (fr) * 1996-07-08 1998-01-15 Yamanouchi Pharmaceutical Co., Ltd. Inhibiteurs de la resorption osseuse
EP1178958B1 (en) * 1999-03-15 2004-02-18 Axys Pharmaceuticals, Inc. N-cyanomethyl amides as protease inhibitors
DE60030768T2 (de) * 1999-12-24 2007-11-08 F. Hoffmann-La Roche Ag Nitrilderivate als cathepsin k hemmer
US7012075B2 (en) * 2001-03-02 2006-03-14 Merck & Co., Inc. Cathepsin cysteine protease inhibitors
CA2477657C (en) * 2002-03-05 2011-04-26 Merck Frosst Canada & Co./Merck Frosst Canada & Cie Cathepsin cysteine protease inhibitors
CN1798729A (zh) 2003-06-02 2006-07-05 霍夫曼-拉罗奇有限公司 苯甲酰胺腈衍生物
US20060252698A1 (en) * 2005-04-20 2006-11-09 Malcolm Bruce A Compounds for inhibiting cathepsin activity
US7951823B2 (en) * 2006-05-23 2011-05-31 Irm Llc Compounds and compositions as channel activating protease inhibitors

Also Published As

Publication number Publication date
CR20110508A (es) 2011-11-03
IL215065A0 (en) 2011-11-30
CN102405211B (zh) 2015-01-21
JP2012524116A (ja) 2012-10-11
KR101320790B1 (ko) 2013-10-22
KR20110140136A (ko) 2011-12-30
EP2421826B1 (en) 2013-10-23
CL2011002604A1 (es) 2012-03-16
ECSP11011411A (es) 2011-11-30
RU2535479C2 (ru) 2014-12-10
SI2421826T1 (sl) 2014-02-28
SG175264A1 (en) 2011-11-28
NZ595073A (en) 2012-11-30
ZA201107668B (en) 2012-07-25
PL2421826T3 (pl) 2014-03-31
ES2436550T3 (es) 2014-01-02
WO2010121918A1 (en) 2010-10-28
US8163793B2 (en) 2012-04-24
MX2011011094A (es) 2011-11-04
JP5518997B2 (ja) 2014-06-11
MY153880A (en) 2015-04-15
CY1114764T1 (el) 2016-12-14
AU2010241084B2 (en) 2014-10-23
MA33224B1 (fr) 2012-04-02
CA2758210A1 (en) 2010-10-28
PE20120911A1 (es) 2012-08-06
PT2421826E (pt) 2014-01-03
HRP20140030T1 (hr) 2014-02-14
CO6430459A2 (es) 2012-04-30
RS53122B (en) 2014-06-30
CA2758210C (en) 2017-08-29
TWI418555B (zh) 2013-12-11
US20100267722A1 (en) 2010-10-21
CN102405211A (zh) 2012-04-04
AR076319A1 (es) 2011-06-01
UA106748C2 (uk) 2014-10-10
BRPI1013567A2 (pt) 2020-09-15
RU2011146872A (ru) 2013-05-27
DK2421826T3 (en) 2013-11-11
AU2010241084A1 (en) 2011-10-06
BRPI1013567B1 (pt) 2021-07-20
EP2421826A1 (en) 2012-02-29
TW201040164A (en) 2010-11-16
HK1166322A1 (en) 2012-10-26
IL215065A (en) 2016-06-30

Similar Documents

Publication Publication Date Title
BRPI1013567B8 (pt) Derivados de prolina como inibidores de catepsina
BR112015012919A2 (pt) novos derivados de piridina
BR112015013124A2 (pt) novos derivados de piridina
BR112013031463A2 (pt) piridina-2-amidas úteis como agonistas de cb2
BR112014011055A2 (pt) novos derivados de [1,2,3]triazolo[4,5-d]pirimidina
BR112012031343A2 (pt) compostos de heteroarila contendo nitrogênio
BR112015009600A2 (pt) piridina-2-amidas úteis como agonistas cb2
BR112015020795A2 (pt) derivados de pirazol novos
MA33803B1 (fr) Inhibiteur de bromodomaine de benzodiazépine
BR112014010047A2 (pt) novos derivados de pirazina
BR112015009603A2 (pt) novos derivados de pirazina
CO6362015A2 (es) Derivados de acido 1-amino-2ciclobutiletilboronico
BR112013000750A2 (pt) 1-hidroxiimino-3-fenil-propanos
BR112015024272A2 (pt) novos derivados de piridina
BR112012011328A2 (pt) inibidores de akt
CR11251A (es) Depsipeptidos ciclicos y usos de los mismos
BR112014006248A2 (pt) compostos de triazolopiridina como inibidores de pde10a
UY30371A1 (es) Compuestos quimicos
UY32168A (es) Nuevas composiciones de compuestos heterociclicos nitrogenados antibacterianos con otros compuestos antibacterianos y su utilización como medicamentos
BR112015027396A2 (pt) derivados de purina como agonistas do receptor de cb2
BR112014012521A2 (pt) novos derivados de pirrolidina como inibidores de catepsina
BR112014016803A8 (pt) amidas macrocíclicas como inibidoras de protease
BR112015027394A2 (pt) derivados de pirrolo[2,3-d]pirimidina como agonistas de receptor cb2
BR112018011562A2 (pt) novos derivados de fenil
BR112014019220A8 (pt) Novos derivados de pirrolidina

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: AS CLASSIFICACOES ANTERIORES ERAM: C07D 207/16 , C07D 401/04 , C07D 401/06 , C07D 401/12 , C07D 401/14 , C07D 403/04 , C07D 403/06 , C07D 403/12 , C07D 403/14 , C07D 405/04 , C07D 405/06 , C07D 405/12 , C07D 405/14 , C07D 409/14 , C07D 413/12

Ipc: C07D 207/16 (2006.01), C07D 401/04 (2006.01), C07D

B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 13/04/2010, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF, QUE DETERMINA A ALTERACAO DO PRAZO DE CONCESSAO.

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: REF. RPI 2637 DE 20/07/2021 QUANTO AO ENDERECO.