SG11201702576QA - Pyrimidinones as factor xia inhibitors - Google Patents

Pyrimidinones as factor xia inhibitors

Info

Publication number: SG11201702576QA
Authority: SG; Singapore
Prior art keywords: pyrimidinones; factor xia; xia inhibitors; inhibitors; factor
Prior art date: 2014-10-01

Application number

SG11201702576QA

Inventor

Andrew K Dilger

James R Corte

Lucca Indawati De

Tianan Fang

Wu Yang

Yufeng Wang

Kumar Balashanmuga Pabbisetty

William R Ewing

Yeheng Zhu

Ruth R Wexler

Donald J P Pinto

Michael J Orwat

Ii Leon M Smith

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.)

2014-10-01

Filing date

2015-07-29

Publication date

2017-04-27

2015-07-29 Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co

2017-04-27 Publication of SG11201702576QA publication Critical patent/SG11201702576QA/en

Links

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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- 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
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- 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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/61—Halogen atoms or nitro radicals
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
- 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
- C07D403/10—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 aromatic rings

SG11201702576QA 2014-10-01 2015-07-29 Pyrimidinones as factor xia inhibitors SG11201702576QA (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US201462058316P	2014-10-01	2014-10-01
PCT/US2015/042576 WO2016053455A1 (en)	2014-10-01	2015-07-29	Pyrimidinones as factor xia inhibitors

Publications (1)

Publication Number	Publication Date
SG11201702576QA true SG11201702576QA (en)	2017-04-27

Family

ID=53784023

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
SG11201702576QA SG11201702576QA (en)	2014-10-01	2015-07-29	Pyrimidinones as factor xia inhibitors
SG10201911652TA SG10201911652TA (en)	2014-10-01	2015-07-29	Pyrimidinones as factor xia inhibitors

Family Applications After (1)

Application Number	Title	Priority Date	Filing Date
SG10201911652TA SG10201911652TA (en)	2014-10-01	2015-07-29	Pyrimidinones as factor xia inhibitors

Country Status (34)

Country	Link
EP (4)	EP4286372A3 (en)
JP (4)	JP6462865B2 (en)
KR (2)	KR102269999B1 (en)
CN (3)	CN106795161B (en)
AR (1)	AR101367A1 (en)
AU (3)	AU2015324530B2 (en)
CA (1)	CA2963395C (en)
CL (1)	CL2017000712A1 (en)
CO (1)	CO2017003833A2 (en)
CY (2)	CY1119678T1 (en)
DK (2)	DK3293186T3 (en)
EA (1)	EA031590B1 (en)
ES (3)	ES2655884T3 (en)
HR (2)	HRP20171950T1 (en)
HU (2)	HUE052812T2 (en)
IL (2)	IL251434B (en)
LT (2)	LT3089979T (en)
MA (1)	MA40123A1 (en)
MX (2)	MX2017003695A (en)
MY (1)	MY183987A (en)
NO (1)	NO2721243T3 (en)
NZ (2)	NZ731416A (en)
PE (2)	PE20210922A1 (en)
PH (2)	PH12017500580B1 (en)
PL (1)	PL3089979T3 (en)
PT (2)	PT3293186T (en)
RS (2)	RS61183B1 (en)
SG (2)	SG11201702576QA (en)
SI (2)	SI3089979T1 (en)
TN (2)	TN2017000112A1 (en)
TW (2)	TWI692478B (en)
UY (1)	UY36244A (en)
WO (1)	WO2016053455A1 (en)
ZA (1)	ZA201702478B (en)

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JOP20160086B1 (en)	2015-05-08	2021-08-17	2 Katholieke Univ Leuven Ku Leuven Research And Development	Mono- or di-substituted indole derivatives as dengue viral replication inhibitors
JP6742348B2 (en)	2015-06-19	2020-08-19	ブリストル−マイヤーズスクイブカンパニーＢｒｉｓｔｏｌ−ＭｙｅｒｓＳｑｕｉｂｂＣｏｍｐａｎｙ	Diamide macrocycles as factor XIA inhibitors
CN114874222A (en)	2015-07-29	2022-08-09	百时美施贵宝公司	Carrying non-aromatic P2 , Novel macrocyclic form of factor XIA
EP3328851B1 (en) *	2015-07-29	2020-04-22	Bristol-Myers Squibb Company	Factor xia macrocyclic inhibitors bearing alkyl or cycloalkyl p2' moieties
JO3633B1 (en)	2015-09-16	2020-08-27	Katholieke Univ Leuven Ku Leuven Research & Development	Mono- or di-substituted indole derivatives as dengue viral replication inhibitors
JOP20160198B1 (en)	2015-09-16	2022-03-14	Janssen Pharmaceuticals Inc	Mono- or di-substituted indole derivatives as dengue viral replication inhibitors
EP3423458A1 (en)	2016-03-02	2019-01-09	Bristol-Myers Squibb Company	Diamide macrocycles having factor xia inhibiting activity
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WO2018133793A1 (en) *	2017-01-18	2018-07-26	广东东阳光药业有限公司	Blood coagulation factor xia inhibitor and uses thereof
JOP20180025B1 (en)	2017-03-31	2021-08-17	Janssen Pharmaceuticals Inc	Substituted indoline derivatives as dengue viral replication inhibitors
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AU2018274100B2 (en)	2017-05-22	2022-06-23	Janssen Pharmaceuticals, Inc.	Substituted indoline derivatives as dengue viral replication inhibitors
WO2020210613A1 (en) *	2019-04-11	2020-10-15	Bristol-Myers Squibb Company	Novel synthetic options towards the manufacture of (6r,10s)-10- {4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)- pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15 -(metheno)pyrazolo [4,3-b] [1,7] diazacyclotetradecin-5(6h)-one
KR20210151183A (en) *	2019-04-11	2021-12-13	브리스톨-마이어스 스큅 컴퍼니	Enhanced Performance of Amorphous Solids and Solubilized Formulations to Achieve Therapeutic Plasma Concentrations
US20220204508A1 (en) *	2019-04-16	2022-06-30	Medshine Discovery Inc.	Macrocyclic derivatives acting as xia factor inhibitor
CN114008047B (en) *	2019-07-23	2023-03-21	南京明德新药研发有限公司	Macrocyclic derivatives as factor XIa inhibitors
EP4132930A1 (en) *	2020-04-10	2023-02-15	Bristol-Myers Squibb Company	Crystalline forms of (9, 135s)-13- {4-[5-chloro-2-(4-chloro-1h,2,3- triazol- 1 -yl)phenyl] -6-oxo- 1,6-dihydropyrimidin- 1-yl}-3-(difluoromethyl)-9-methyl-3,4,7,15- tetraazatricyclo [ 12.3.1.0] octadeca- 1(18), 2(6), 4, 14, 16-pentaen-8-one
TW202229280A (en) *	2020-10-12	2022-08-01	美商必治妥美雅史谷比公司	A process toward the manufacture of (6r,10s)-10-{4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)-pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(metheno)pyrazolo[4,3-b][1,7]diazacyclotetradecin-5(6h)-one
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2012
- 2012-06-14 NO NO12801069A patent/NO2721243T3/no unknown
2015
- 2015-07-29 SG SG11201702576QA patent/SG11201702576QA/en unknown
- 2015-07-29 WO PCT/US2015/042576 patent/WO2016053455A1/en active Application Filing
- 2015-07-29 ES ES15747721.7T patent/ES2655884T3/en active Active
- 2015-07-29 EA EA201790595A patent/EA031590B1/en not_active IP Right Cessation
- 2015-07-29 PE PE2020001966A patent/PE20210922A1/en unknown
- 2015-07-29 NZ NZ731416A patent/NZ731416A/en unknown
- 2015-07-29 JP JP2017517766A patent/JP6462865B2/en active Active
- 2015-07-29 PT PT171899354T patent/PT3293186T/en unknown
- 2015-07-29 PT PT157477217T patent/PT3089979T/en unknown
- 2015-07-29 AU AU2015324530A patent/AU2015324530B2/en active Active
- 2015-07-29 TN TN2017000112A patent/TN2017000112A1/en unknown
- 2015-07-29 SI SI201530123T patent/SI3089979T1/en unknown
- 2015-07-29 MA MA40123A patent/MA40123A1/en unknown
- 2015-07-29 LT LTEP15747721.7T patent/LT3089979T/en unknown
- 2015-07-29 CN CN201580053079.7A patent/CN106795161B/en active Active
- 2015-07-29 DK DK17189935.4T patent/DK3293186T3/en active
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- 2015-07-29 ES ES20197284T patent/ES2963267T3/en active Active
- 2015-07-29 ES ES17189935T patent/ES2836270T3/en active Active
- 2015-07-29 CN CN201910882473.1A patent/CN110734435B/en active Active
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- 2015-07-29 EP EP23185426.6A patent/EP4286372A3/en active Pending
- 2015-07-29 MX MX2017003695A patent/MX2017003695A/en active IP Right Grant
- 2015-07-29 SI SI201531423T patent/SI3293186T1/en unknown
- 2015-07-29 RS RS20201472A patent/RS61183B1/en unknown
- 2015-07-29 SG SG10201911652TA patent/SG10201911652TA/en unknown
- 2015-07-29 CA CA2963395A patent/CA2963395C/en active Active
- 2015-07-29 LT LTEP17189935.4T patent/LT3293186T/en unknown
- 2015-07-29 TW TW104124664A patent/TWI692478B/en active
- 2015-07-29 KR KR1020187033199A patent/KR102269999B1/en active IP Right Grant
- 2015-07-29 EP EP15747721.7A patent/EP3089979B1/en active Active
- 2015-07-29 RS RS20180046A patent/RS56786B1/en unknown
- 2015-07-29 TN TNP/2018/000229A patent/TN2018000229A1/en unknown
- 2015-07-29 HU HUE17189935A patent/HUE052812T2/en unknown
- 2015-07-29 EP EP20197284.1A patent/EP3828186B1/en active Active
- 2015-07-29 CN CN202210580097.2A patent/CN114957255A/en active Pending
- 2015-07-29 KR KR1020177011233A patent/KR101921436B1/en active IP Right Grant
- 2015-07-29 HU HUE15747721A patent/HUE038061T2/en unknown
- 2015-07-29 DK DK15747721.7T patent/DK3089979T3/en active
- 2015-07-29 TW TW109111475A patent/TWI769442B/en active
- 2015-07-29 MY MYPI2017701150A patent/MY183987A/en unknown
- 2015-07-29 PL PL15747721T patent/PL3089979T3/en unknown
- 2015-07-29 PE PE2017000527A patent/PE20170939A1/en unknown
- 2015-07-29 UY UY0001036244A patent/UY36244A/en active IP Right Grant
- 2015-07-29 EP EP17189935.4A patent/EP3293186B1/en active Active
2017
- 2017-03-21 MX MX2020010840A patent/MX2020010840A/en unknown
- 2017-03-24 CL CL2017000712A patent/CL2017000712A1/en unknown
- 2017-03-28 IL IL251434A patent/IL251434B/en active IP Right Grant
- 2017-03-29 PH PH12017500580A patent/PH12017500580B1/en unknown
- 2017-04-07 ZA ZA2017/02478A patent/ZA201702478B/en unknown
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