ES2655540T3 - Inhibidores de factor XIa macrocíclicos condensados con heterociclos - Google Patents

Inhibidores de factor XIa macrocíclicos condensados con heterociclos Download PDF

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Publication number: ES2655540T3
Authority: ES; Spain
Prior art keywords: independently selected; chf2; pharmaceutically acceptable; alkyl; tautomer
Prior art date: 2014-01-31
Legal status (The legal status 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 status listed.): Active

Application number

ES15705427.1T

Other languages

English (en)

Spanish (es)

Inventor

Andrew K. DILGER

James R. Corte

Indawati De Lucca

Tianan Fang

Wu Yang

Yufeng Wang

Kumar Balashanmuga PABBISETTY

William R. Ewing

Yeheng Zhu

Ruth R. Wexler

Donald J.P. Pinto

Michael J. Orwat

Leon M. Smith Ii

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Bristol Myers Squibb Co

Original Assignee

Bristol Myers Squibb Co

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.)

2014-01-31

Filing date

2015-01-30

Publication date

2018-02-20

2015-01-30 Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co

2018-02-20 Application granted granted Critical

2018-02-20 Publication of ES2655540T3 publication Critical patent/ES2655540T3/es

Status Active legal-status Critical Current

2035-01-30 Anticipated expiration legal-status Critical

Links

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229960003009 clopidogrel Drugs 0.000 description 1
229940126051 coagulation factor XIa Drugs 0.000 description 1
229940072645 coumadin Drugs 0.000 description 1
125000000753 cycloalkyl group Chemical group 0.000 description 1
230000007812 deficiency Effects 0.000 description 1
230000037213 diet Effects 0.000 description 1
235000005911 diet Nutrition 0.000 description 1
SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 description 1
229950003499 fibrin Drugs 0.000 description 1
229940012952 fibrinogen Drugs 0.000 description 1
210000001035 gastrointestinal tract Anatomy 0.000 description 1
230000002068 genetic effect Effects 0.000 description 1
210000004392 genitalia Anatomy 0.000 description 1
210000004247 hand Anatomy 0.000 description 1
229960002897 heparin Drugs 0.000 description 1
229920000669 heparin Polymers 0.000 description 1
238000001727 in vivo Methods 0.000 description 1
208000027866 inflammatory disease Diseases 0.000 description 1
230000003993 interaction Effects 0.000 description 1
239000000543 intermediate Substances 0.000 description 1
230000003870 intestinal permeability Effects 0.000 description 1
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
208000017169 kidney disease Diseases 0.000 description 1
150000002605 large molecules Chemical class 0.000 description 1
229920002521 macromolecule Polymers 0.000 description 1
230000035800 maturation Effects 0.000 description 1
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
238000012544 monitoring process Methods 0.000 description 1
230000014508 negative regulation of coagulation Effects 0.000 description 1
201000001119 neuropathy Diseases 0.000 description 1
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238000003199 nucleic acid amplification method Methods 0.000 description 1
230000037361 pathway Effects 0.000 description 1
208000033808 peripheral neuropathy Diseases 0.000 description 1
210000003800 pharynx Anatomy 0.000 description 1
239000000106 platelet aggregation inhibitor Substances 0.000 description 1
229940020573 plavix Drugs 0.000 description 1
230000001323 posttranslational effect Effects 0.000 description 1
230000000644 propagated effect Effects 0.000 description 1
229940121649 protein inhibitor Drugs 0.000 description 1
239000012268 protein inhibitor Substances 0.000 description 1
102000004169 proteins and genes Human genes 0.000 description 1
230000002797 proteolythic effect Effects 0.000 description 1
230000020964 regulation of blood coagulation Effects 0.000 description 1
230000004268 retinal thickening Effects 0.000 description 1
238000012552 review Methods 0.000 description 1
150000003384 small molecules Chemical class 0.000 description 1
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230000001225 therapeutic effect Effects 0.000 description 1
231100001274 therapeutic index Toxicity 0.000 description 1
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WCYWZMWISLQXQU-FIBGUPNXSA-N trideuteriomethane Chemical compound [2H][C]([2H])[2H] WCYWZMWISLQXQU-FIBGUPNXSA-N 0.000 description 1
108010036927 trypsin-like serine protease Proteins 0.000 description 1

Classifications

- 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
- C07D471/12—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 three hetero rings
- C07D471/18—Bridged systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- 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
- A61P9/06—Antiarrhythmics
- 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
- 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
- C07D487/08—Bridged systems

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Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Veterinary Medicine (AREA)
Life Sciences & Earth Sciences (AREA)
Public Health (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Heart & Thoracic Surgery (AREA)
Cardiology (AREA)
Vascular Medicine (AREA)
Urology & Nephrology (AREA)
Diabetes (AREA)
Hematology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)

ES15705427.1T 2014-01-31 2015-01-30 Inhibidores de factor XIa macrocíclicos condensados con heterociclos Active ES2655540T3 (es)

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US201461933948P		2014-01-31
PCT/US2015/013647 WO2015116882A1 (en)	2014-01-31	2015-01-30	Macrocyclic factor xia inhibitors condensed with heterocycles

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TW (1)	TWI703144B (2)
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JP7286001B2 (ja) *	2019-07-23	2023-06-02	メッドシャインディスカバリーインコーポレイテッド	第ＸＩａ因子阻害剤としての大環状誘導体
TW202229280A (zh) *	2020-10-12	2022-08-01	美商必治妥美雅史谷比公司	（６ｒ，１０ｓ）－１０－｛４－［５－氯－２－（４－氯－１ｈ－１，２，３－三唑－１－基）苯基］－６－側氧基－１（６ｈ）－嘧啶基｝－１－（二氟甲基）－６－甲基－１，４，７，８，９，１０－六氫－１１，１５－（亞甲橋基）吡唑并［４，３－ｂ］［１，７］二氮雜環十四炔－５（６ｈ）－酮之製備方法
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- 2012-08-31 NO NO12780535A patent/NO2760821T3/no unknown
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Publication number	Publication date
BR112016016741B1 (pt)	2023-01-17
EP3099688B1 (en)	2017-10-18
EP3099688A1 (en)	2016-12-07
PL3099688T3 (pl)	2018-03-30
LT3099688T (lt)	2017-12-27
AR099228A1 (es)	2016-07-06
MX2016009385A (es)	2016-09-16
EA032650B1 (ru)	2019-06-28
NO2760821T3 (2)	2018-03-10
CN106459051B (zh)	2018-10-16
SMT201800024T1 (it)	2018-03-08
CA2937738C (en)	2023-01-17
SI3099688T1 (sl)	2017-12-29
TWI703144B (zh)	2020-09-01
DK3099688T3 (en)	2018-01-15
US20170342071A1 (en)	2017-11-30
TW201615640A (zh)	2016-05-01
PT3099688T (pt)	2018-01-15
EA201691561A1 (ru)	2017-01-30
CY1120534T1 (el)	2019-07-10
RS56785B1 (sr)	2018-04-30
WO2015116882A1 (en)	2015-08-06
US20180222907A1 (en)	2018-08-09
US10273236B2 (en)	2019-04-30
HRP20172002T1 (hr)	2018-02-09
CN106459051A (zh)	2017-02-22
UY35972A (es)	2015-07-31
BR112016016741A2 (2)	2017-08-08
CA2937738A1 (en)	2015-08-06
HUE038060T2 (hu)	2018-09-28
JP6419836B2 (ja)	2018-11-07
JP2017504640A (ja)	2017-02-09
US20170057961A1 (en)	2017-03-02

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