KR20170035993A - 가용성 구아닐레이트 사이클라제의 활성제로서의 헤테로사이클릭 카복실산 - Google Patents

가용성 구아닐레이트 사이클라제의 활성제로서의 헤테로사이클릭 카복실산 Download PDF

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Publication number: KR20170035993A
Authority: KR; South Korea
Prior art keywords: mmol; mixture; reduced pressure; under reduced; solution
Prior art date: 2014-07-22
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 Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn

Application number

KR1020177004761A

Other languages

English (en)

Korean (ko)

Inventor

제로드 버넷 브렌너먼

존 데이비드 진

크리스토퍼 로날드 사르코

존 웨스트브룩

중화 장

마오린 유

타마라 데니스 홉킨스

마이클 디. 로우

Original Assignee

베링거 인겔하임 인터내셔날 게엠베하

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.)

2014-07-22

Filing date

2015-07-21

Publication date

2017-03-31

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53783363&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR20170035993(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2015-07-21 Application filed by 베링거 인겔하임 인터내셔날 게엠베하 filed Critical 베링거 인겔하임 인터내셔날 게엠베하

2017-03-31 Publication of KR20170035993A publication Critical patent/KR20170035993A/ko

Status Withdrawn legal-status Critical Current

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WXXSNCNJFUAIDG-UHFFFAOYSA-N riociguat Chemical compound N1=C(N)C(N(C)C(=O)OC)=C(N)N=C1C(C1=CC=CN=C11)=NN1CC1=CC=CC=C1F WXXSNCNJFUAIDG-UHFFFAOYSA-N 0.000 description 1
229960000529 riociguat Drugs 0.000 description 1
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BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
229910052938 sodium sulfate Inorganic materials 0.000 description 1
235000011152 sodium sulphate Nutrition 0.000 description 1
AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
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ROUYFJUVMYHXFJ-UHFFFAOYSA-N tert-butyl 4-oxopiperidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCC(=O)CC1 ROUYFJUVMYHXFJ-UHFFFAOYSA-N 0.000 description 1
TZRQZPMQUXEZMC-UHFFFAOYSA-N tert-butyl n-(2-bromoethyl)carbamate Chemical compound CC(C)(C)OC(=O)NCCBr TZRQZPMQUXEZMC-UHFFFAOYSA-N 0.000 description 1
DSPYCWLYGXGJNJ-UHFFFAOYSA-N tert-butyl n-prop-2-ynylcarbamate Chemical compound CC(C)(C)OC(=O)NCC#C DSPYCWLYGXGJNJ-UHFFFAOYSA-N 0.000 description 1
MHYGQXWCZAYSLJ-UHFFFAOYSA-N tert-butyl-chloro-diphenylsilane Chemical compound C=1C=CC=CC=1[Si](Cl)(C(C)(C)C)C1=CC=CC=C1 MHYGQXWCZAYSLJ-UHFFFAOYSA-N 0.000 description 1
YMYHIIMNMWCDJZ-UHFFFAOYSA-N tert-butyl-ethyl-dimethylsilane Chemical compound CC[Si](C)(C)C(C)(C)C YMYHIIMNMWCDJZ-UHFFFAOYSA-N 0.000 description 1
BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical compound CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 description 1
238000012360 testing method Methods 0.000 description 1
DPKBAXPHAYBPRL-UHFFFAOYSA-M tetrabutylazanium;iodide Chemical compound [I-].CCCC[N+](CCCC)(CCCC)CCCC DPKBAXPHAYBPRL-UHFFFAOYSA-M 0.000 description 1
125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
125000003831 tetrazolyl group Chemical group 0.000 description 1
ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 description 1
125000001113 thiadiazolyl group Chemical group 0.000 description 1
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HFRXJVQOXRXOPP-UHFFFAOYSA-N thionyl bromide Chemical compound BrS(Br)=O HFRXJVQOXRXOPP-UHFFFAOYSA-N 0.000 description 1
FYSNRJHAOHDILO-UHFFFAOYSA-N thionyl chloride Chemical compound ClS(Cl)=O FYSNRJHAOHDILO-UHFFFAOYSA-N 0.000 description 1
125000000464 thioxo group Chemical group S=* 0.000 description 1
201000005665 thrombophilia Diseases 0.000 description 1
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125000004306 triazinyl group Chemical group 0.000 description 1
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RMZAYIKUYWXQPB-UHFFFAOYSA-N trioctylphosphane Chemical compound CCCCCCCCP(CCCCCCCC)CCCCCCCC RMZAYIKUYWXQPB-UHFFFAOYSA-N 0.000 description 1
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UTODFRQBVUVYOB-UHFFFAOYSA-P wilkinson's catalyst Chemical compound [Cl-].C1=CC=CC=C1P(C=1C=CC=CC=1)(C=1C=CC=CC=1)[Rh+](P(C=1C=CC=CC=1)(C=1C=CC=CC=1)C=1C=CC=CC=1)P(C=1C=CC=CC=1)(C=1C=CC=CC=1)C1=CC=CC=C1 UTODFRQBVUVYOB-UHFFFAOYSA-P 0.000 description 1
BPICBUSOMSTKRF-UHFFFAOYSA-N xylazine Chemical compound CC1=CC=CC(C)=C1NC1=NCCCS1 BPICBUSOMSTKRF-UHFFFAOYSA-N 0.000 description 1
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Classifications

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- C07—ORGANIC CHEMISTRY
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- 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
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- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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- 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
- Y10S514/866—
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General Health & Medical Sciences (AREA)
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KR1020177004761A 2014-07-22 2015-07-21 가용성 구아닐레이트 사이클라제의 활성제로서의 헤테로사이클릭 카복실산 Withdrawn KR20170035993A (ko)

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US201462027376P	2014-07-22	2014-07-22
US62/027,376		2014-07-22
PCT/US2015/041245 WO2016014463A1 (en)	2014-07-22	2015-07-21	Heterocyclic carboxylic acids as activators of soluble guanylate cyclase

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US (1)	US9353090B2 (2)
EP (1)	EP3172202B1 (2)
JP (1)	JP6602840B2 (2)
KR (1)	KR20170035993A (2)
CN (1)	CN106459017B (2)
AP (1)	AP2016009615A0 (2)
AR (1)	AR101265A1 (2)
AU (1)	AU2015292833B2 (2)
BR (1)	BR112017000943A2 (2)
CA (1)	CA2955937A1 (2)
CL (1)	CL2017000071A1 (2)
CO (1)	CO2017000438A2 (2)
DK (1)	DK3172202T3 (2)
EA (1)	EA032972B1 (2)
ES (1)	ES2784477T3 (2)
HU (1)	HUE049231T2 (2)
IL (1)	IL249587A0 (2)
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PL (1)	PL3172202T3 (2)
PT (1)	PT3172202T (2)
SG (2)	SG11201700507XA (2)
TW (1)	TWI711615B (2)
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WO (1)	WO2016014463A1 (2)

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AU2017216429B2 (en) *	2016-02-01	2022-10-06	Cyclerion Therapeutics, Inc.	Use of sGC stimulators for the treatment of Nonalcoholic Steatohepatitis (NASH)
EP3512825B1 (en)	2016-09-14	2020-10-21	Genomatica, Inc.	1,3-fatty diol compounds and derivatives thereof
CN109890379A (zh)	2016-10-11	2019-06-14	拜耳制药股份公司	包含sGC活化剂和盐皮质激素受体拮抗剂的组合产品
CN106495999B (zh) *	2016-10-18	2019-08-16	亳州学院	一种芳香醛及其合成方法
US12491261B2 (en)	2016-10-26	2025-12-09	Acuitas Therapeutics, Inc.	Lipid nanoparticle formulations
AR112392A1 (es)	2017-07-14	2019-10-23	Glaxosmithkline Ip Dev Ltd	Compuesto tricíclico de pirazol, su uso para fabricar un medicamento y composición farmaceutica que lo comprende
EP4501322A3 (en) *	2017-08-17	2025-04-16	Acuitas Therapeutics, Inc.	Lipids for use in lipid nanoparticle formulations
WO2019081456A1 (en)	2017-10-24	2019-05-02	Bayer Aktiengesellschaft	USE OF SGC ACTIVATORS AND STIMULATORS COMPRISING A BETA2 SUBUNIT
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PE20170249A1 (es)	2017-04-05
AU2015292833B2 (en)	2019-11-28
MX2017000926A (es)	2017-05-04
PL3172202T3 (pl)	2020-07-13
MX378717B (es)	2025-03-10
CL2017000071A1 (es)	2017-06-30
SG11201700507XA (en)	2017-02-27
IL249587A0 (en)	2017-02-28
JP2017521457A (ja)	2017-08-03
BR112017000943A2 (pt)	2017-11-14
CO2017000438A2 (es)	2017-08-31
JP6602840B2 (ja)	2019-11-06
TWI711615B (zh)	2020-12-01
AU2015292833A1 (en)	2016-12-22
AP2016009615A0 (en)	2016-12-31
CA2955937A1 (en)	2016-01-28
ES2784477T3 (es)	2020-09-28
PT3172202T (pt)	2020-05-06
AR101265A1 (es)	2016-12-07
SG10201806565SA (en)	2018-08-30
CN106459017A (zh)	2017-02-22
WO2016014463A1 (en)	2016-01-28
EA032972B1 (ru)	2019-08-30
US20160024059A1 (en)	2016-01-28
CN106459017B (zh)	2020-07-17
PH12017500111A1 (en)	2017-05-29
US9353090B2 (en)	2016-05-31
EP3172202A1 (en)	2017-05-31
EP3172202B1 (en)	2020-01-29
EA201790246A1 (ru)	2017-07-31
TW201617340A (zh)	2016-05-16
DK3172202T3 (da)	2020-04-27
UY36226A (es)	2016-01-29

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