CN101896178A - 作为crth2受体拮抗剂的杂环化合物 - Google Patents
作为crth2受体拮抗剂的杂环化合物 Download PDFInfo
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- CN101896178A CN101896178A CN2008801092963A CN200880109296A CN101896178A CN 101896178 A CN101896178 A CN 101896178A CN 2008801092963 A CN2008801092963 A CN 2008801092963A CN 200880109296 A CN200880109296 A CN 200880109296A CN 101896178 A CN101896178 A CN 101896178A
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- 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
- C07D471/14—Ortho-condensed systems
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- 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61P19/00—Drugs for skeletal disorders
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
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- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P5/00—Drugs for disorders of the endocrine system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
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- A—HUMAN NECESSITIES
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- 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
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- 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
- A61P9/12—Antihypertensives
Abstract
Description
Cd | A | B | C | D | R | X | Ar | n | m |
1 | N | CH | CH | CH | CH3 | CH2 | Ph | 2 | 1 |
2 | N | CH | CH | CH | CH3 | CH2 | Ph | 1 | 1 |
3 | N | CH | CH | CH | H | SCH2 | Ph | 2 | 1 |
4 | N | CH | CH | CH | CH3 | SCH2 | Ph | 1 | 1 |
5 | N | CH | CH | CH | H | CH2 | 4-FPh | 2 | 1 |
6 | N | CH | CH | CH | CH3 | CH2 | 4-CF3Ph | 1 | 1 |
7 | N | CH | CH | CH | CH3 | SCH2 | 4-ClPh | 2 | 1 |
8 | N | CH | CH | CH | CH3 | SCH2 | 3,4-diFPh | 1 | 1 |
9 | N | CCF3 | CH | CH | CH3 | CH2 | Ph | 2 | 1 |
10 | N | CCH3 | CH | CH | CH3 | CH2 | Ph | 2 | 1 |
11 | N | CH | CCH3 | CH | CH3 | CH2 | 4-FPh | 2 | 1 |
12 | CH | N | CH | CH | CH3 | CH2 | Ph | 2 | 1 |
13 | CH | N | CH | N | CH3 | CH2 | Ph | 1 | 1 |
14 | CH | N | CH | CH | CH3 | SCH2 | 4-MeSO2Ph | 2 | 1 |
15 | CH | N | CH | CH | CH3 | SCH2 | Ph | 1 | 1 |
16 | CH | N | CH | CH | H | CH2 | 4-FPh | 2 | 1 |
17 | CH | N | CH | CH | CH3 | CH2 | 4-CF3Ph | 1 | 1 |
18 | CH | N | CH | CH | CH3 | SCH2 | 4-ClPh | 2 | 1 |
Cd | A | B | C | D | R | X | Ar | n | m |
19 | CH | N | CH | CH | CH3 | SCH2 | 3,4-diFPh | 1 | 1 |
20 | CH | N | CH | CH | CH3 | CH2 | Ph | 2 | 1 |
21 | Ci-Pr | N | CH | CH | CH3 | CH2 | Ph | 2 | 1 |
22 | N | CH | CH | N | CH3 | CH2 | Ph | 2 | 1 |
23 | CH | N | CH | CH | C2H5 | CH2 | Ph | 2 | 1 |
24 | CH | N | CH | CH | CH3 | CH2 | Ph | 2 | 1 |
25 | N | CH | CH | CH | c-Pr | CH2 | Ph | 2 | 1 |
26 | CH | CH | CCH3 | N | CH3 | CH2 | Ph | 2 | 1 |
27 | CH | CH | C-iPr | N | CH3 | CH2 | Ph | 1 | 1 |
28 | CH | CH | C-cPr | N | CH3 | SCH2 | Ph | 2 | 1 |
29 | CH | N | CH | N | CH3 | SCH2 | Ph | 1 | 1 |
30 | CH | N | CCH3 | N | CH3 | CH2 | 4-FPh | 2 | 1 |
31 | CH | CH | CSCH3 | N | CH3 | CH2 | 4-CF3Ph | 1 | 1 |
32 | CH | CH | CH | N | CH3 | SCH2 | 4-ClPh | 2 | 1 |
33 | CH | CH | CH | N | CH3 | SCH2 | 3,4-diFPh | 1 | 1 |
34 | CH | CCF3 | CH | N | H | CH2 | Ph | 2 | 1 |
35 | CH | CCH3 | CH | N | CH3 | CH2 | Ph | 2 | 1 |
36 | CH | CH | CH | N | CH3 | CH2 | Ph | 2 | 1 |
37 | CH | CH | CH | N | CH3 | CH2 | Ph | 1 | 1 |
38 | CH | CH | CH | N | CH3 | SCH2 | Ph | 2 | 1 |
39 | CH | CH | CH | N | CH3 | SCH2 | Ph | 1 | 1 |
40 | CH | CH | CH | N | CH3 | CH2 | 4-FPh | 2 | 1 |
41 | CH | CH | CH | N | CH3 | CH2 | 4-CF3Ph | 1 | 1 |
42 | CH | CH | N | CH | CH3 | CH2 | Ph | 2 | 1 |
43 | CH | CH | N | C-iPr | H | CH2 | Ph | 1 | 1 |
44 | CH | CH | N | CH | CH3 | SCH2 | Ph | 2 | 1 |
45 | CH | CH | N | CH | CH3 | SCH2 | Ph | 1 | 1 |
46 | CH | CH | N | CH | CH3 | CH2 | 4-FPh | 2 | 1 |
Cd | A | B | C | D | R | X | Ar | n | m |
47 | CH | CH | N | CH | CH3 | CH2 | 4-CF3Ph | 1 | 1 |
48 | CH | CH | N | CH | CH3 | SCH2 | 4-ClPh | 2 | 1 |
49 | CH | CH | N | CH | CH3 | SCH2 | 3,4-diFPh | 1 | 1 |
50 | CH | CCF3 | N | CH | H | CH2 | Ph | 2 | 1 |
51 | CH | CCH3 | N | CH | CH3 | CH2 | Ph | 2 | 1 |
52 | CH | CH | N | CH | CH3 | CH2 | 3-噻吩 | 2 | 1 |
53 | CCH3 | CH | N | CH | H | CH2 | Ph | 1 | 1 |
54 | CCl | CH | N | CH | CH3 | SCH2 | 2-噻吩 | 2 | 1 |
55 | CF | CH | N | CH | CH3 | SCH2 | Ph | 1 | 1 |
56 | N | CH | N | CH | CH3 | CH2 | 4-吡啶基 | 2 | 1 |
57 | N | CH | N | CH | CH3 | CH2 | 4-Cl-Ph | 1 | 1 |
58 | N | CH | N | CH | cPr | CH2 | 3,4-diCl-Ph | 2 | 1 |
59 | N | CH | N | CH | iPr | OCH2 | 4-Br-Ph | 2 | 1 |
实施例 | 浓度 | %抑制 |
实施例2A | 20nM | 97 |
实施例2B | 20nM | 0 |
实施例4A | 20nM | 91 |
实施例4B | 20nM | 0 |
Claims (33)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US99829807P | 2007-10-10 | 2007-10-10 | |
US60/998,298 | 2007-10-10 | ||
PCT/US2008/079303 WO2009049021A1 (en) | 2007-10-10 | 2008-10-09 | Heterocyclic compounds as crth2 receptor antagonists |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101896178A true CN101896178A (zh) | 2010-11-24 |
CN101896178B CN101896178B (zh) | 2013-11-20 |
Family
ID=40549546
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2008801092963A Active CN101896178B (zh) | 2007-10-10 | 2008-10-09 | 作为crth2受体拮抗剂的杂环化合物 |
Country Status (13)
Country | Link |
---|---|
US (1) | US8772312B2 (zh) |
EP (1) | EP2197438B1 (zh) |
JP (2) | JP2011500584A (zh) |
KR (2) | KR101442663B1 (zh) |
CN (1) | CN101896178B (zh) |
AU (1) | AU2008310874B2 (zh) |
BR (1) | BRPI0815948A2 (zh) |
CA (1) | CA2700824C (zh) |
ES (1) | ES2548577T3 (zh) |
HK (1) | HK1147674A1 (zh) |
IL (1) | IL204823A0 (zh) |
RU (1) | RU2451019C2 (zh) |
WO (1) | WO2009049021A1 (zh) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2020143781A1 (zh) * | 2019-01-10 | 2020-07-16 | 石药集团中奇制药技术(石家庄)有限公司 | 作为crth2受体拮抗剂的杂环化合物的晶型 |
WO2020143793A1 (zh) | 2019-01-10 | 2020-07-16 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物盐及其应用 |
WO2020233713A1 (zh) * | 2019-05-22 | 2020-11-26 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物及其盐的应用 |
Families Citing this family (17)
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WO2010008864A2 (en) | 2008-06-24 | 2010-01-21 | Amira Pharmaceuticals, Inc. | Cycloalkane[b]indole angtagonists of prostaglandin d2 receptors |
CA2737483A1 (en) | 2008-09-22 | 2010-03-25 | Merck Frosst Canada Ltd. | Indole derivatives as crth2 receptor antagonists |
AU2009295231A1 (en) * | 2008-09-22 | 2010-03-25 | Merck Canada Inc. | Azaindole derivatives as CRTH2 receptor antagonists |
GB2465062B (en) * | 2008-11-06 | 2011-04-13 | Amira Pharmaceuticals Inc | Cycloalkane(B)azaindole antagonists of prostaglandin D2 receptors |
CA2764387A1 (en) | 2009-06-05 | 2010-12-09 | Link Medicine Corporation | Aminopyrrolidinone derivatives and uses thereof |
KR101444572B1 (ko) | 2010-03-22 | 2014-09-24 | 액테리온 파마슈티칼 리미티드 | 3-(헤테로아릴-아미노)-1,2,3,4-테트라히드로-9h-카르바졸 유도체 및 이의 프로스타글란딘 d2 수용체 조절제로서의 용도 |
EP2457900A1 (en) | 2010-11-25 | 2012-05-30 | Almirall, S.A. | New pyrazole derivatives having CRTh2 antagonistic behaviour |
WO2012107364A1 (en) * | 2011-02-07 | 2012-08-16 | Scipharm Sàrl | Novel composition for the treatment of cystic fibrosis |
ES2596581T3 (es) | 2011-04-14 | 2017-01-10 | Actelion Pharmaceuticals Ltd. | Derivados de ácido 7-(heteroaril-amino)-6,7,8,9-tetrahidropirido[1,2-a]indol acético y su uso como moduladores del receptor de prostaglandina D2 |
MY179356A (en) | 2014-03-17 | 2020-11-05 | Idorsia Pharmaceuticals Ltd | Azaindole acetic acid derivatives and their use as prostaglandin d2 receptor modulators |
CA2938107A1 (en) | 2014-03-18 | 2015-09-24 | Actelion Pharmaceuticals Ltd | Azaindole acetic acid derivatives and their use as prostaglandin d2 receptor modulators |
WO2016128565A1 (en) * | 2015-02-13 | 2016-08-18 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Ptgdr-1 and/or ptgdr-2 antagonists for preventing and/or treating systemic lupus erythematosus |
WO2017005759A1 (en) * | 2015-07-07 | 2017-01-12 | Intervet International B.V. | A process to make azaindole derivatives |
WO2017005764A1 (en) * | 2015-07-07 | 2017-01-12 | Intervet International B.V. | A process to make tricycloketone intermediates of crth2 antagonists |
TWI711616B (zh) | 2015-09-15 | 2020-12-01 | 瑞士商愛杜西亞製藥有限公司 | 結晶型式 |
PT3356329T (pt) * | 2015-09-29 | 2020-07-15 | Novartis Ag | Processo para a preparação de ácido 1-(4-metanossulfonil-2-trifluorometil-benzil)-2-metil-1h-pirrolo[2,3-b]piridin-3-il-acético |
JOP20190223A1 (ar) * | 2017-04-01 | 2019-09-26 | Novartis Ag | عملية لتحضير حمض 1-(4- ميثان سلفونيل -2- تراي فلورو ميثيل - بنزيل)-2- ميثيل -1h- بيرولو [2، 3-b] بيريدين -3- يل- أسيتيك |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2002094830A2 (en) * | 2001-05-23 | 2002-11-28 | Merck Frosst Canada & Co. | DIHYDROPYRROLO[1,2-A]INDOLE AND TETRAHYDROPYRIDO[1,2-a]-INDOLE DERIVATIVES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS |
CN1732171A (zh) * | 2002-10-30 | 2006-02-08 | 麦克弗罗斯特(加拿大)公司 | 吡啶并吡咯里嗪和吡啶并吲嗪衍生物 |
CA2503767C (en) | 2002-10-30 | 2009-09-22 | Merck Frosst Canada & Co./Merck Frosst Canada & Cie | Pyridopyrrolizine and pyridoindolizine derivatives |
CN1930162B (zh) * | 2004-03-11 | 2010-06-16 | 埃科特莱茵药品有限公司 | 四氢吡啶并吲哚衍生物 |
JP4708885B2 (ja) * | 2005-07-06 | 2011-06-22 | 日本電気株式会社 | 符号化装置、携帯端末装置及びそれらに用いる画素色情報符号化方法 |
EP1915372B1 (en) * | 2005-08-12 | 2013-11-20 | Merck Canada Inc. | Indole derivatives as crth2 receptor antagonists |
US20110112134A1 (en) * | 2008-05-16 | 2011-05-12 | Amira Pharmaceuticals, Inc. | Tricyclic Antagonists of Prostaglandin D2 Receptors |
-
2008
- 2008-10-09 CN CN2008801092963A patent/CN101896178B/zh active Active
- 2008-10-09 RU RU2010117156/04A patent/RU2451019C2/ru active
- 2008-10-09 US US12/681,356 patent/US8772312B2/en active Active
- 2008-10-09 AU AU2008310874A patent/AU2008310874B2/en active Active
- 2008-10-09 EP EP08838211.4A patent/EP2197438B1/en active Active
- 2008-10-09 CA CA2700824A patent/CA2700824C/en active Active
- 2008-10-09 WO PCT/US2008/079303 patent/WO2009049021A1/en active Application Filing
- 2008-10-09 KR KR1020107010092A patent/KR101442663B1/ko active IP Right Grant
- 2008-10-09 KR KR1020137011440A patent/KR20130069840A/ko not_active Application Discontinuation
- 2008-10-09 JP JP2010529022A patent/JP2011500584A/ja active Pending
- 2008-10-09 ES ES08838211.4T patent/ES2548577T3/es active Active
- 2008-10-09 BR BRPI0815948A patent/BRPI0815948A2/pt not_active IP Right Cessation
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2010
- 2010-03-28 IL IL204823A patent/IL204823A0/en unknown
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2011
- 2011-02-22 HK HK11101706.0A patent/HK1147674A1/zh unknown
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Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2020143781A1 (zh) * | 2019-01-10 | 2020-07-16 | 石药集团中奇制药技术(石家庄)有限公司 | 作为crth2受体拮抗剂的杂环化合物的晶型 |
WO2020143793A1 (zh) | 2019-01-10 | 2020-07-16 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物盐及其应用 |
CN113330013A (zh) * | 2019-01-10 | 2021-08-31 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物盐及其应用 |
CN113382995A (zh) * | 2019-01-10 | 2021-09-10 | 石药集团中奇制药技术(石家庄)有限公司 | 作为crth2受体拮抗剂的杂环化合物的晶型 |
CN113330013B (zh) * | 2019-01-10 | 2022-12-27 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物盐及其应用 |
WO2020233713A1 (zh) * | 2019-05-22 | 2020-11-26 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物及其盐的应用 |
CN114502164A (zh) * | 2019-05-22 | 2022-05-13 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物及其盐的应用 |
CN114502164B (zh) * | 2019-05-22 | 2024-01-26 | 石药集团中奇制药技术(石家庄)有限公司 | 杂环化合物及其盐的应用 |
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KR101442663B1 (ko) | 2014-09-22 |
AU2008310874A1 (en) | 2009-04-16 |
US20100222270A1 (en) | 2010-09-02 |
HK1147674A1 (zh) | 2011-08-19 |
AU2008310874B2 (en) | 2012-03-15 |
JP2011500584A (ja) | 2011-01-06 |
JP2013209425A (ja) | 2013-10-10 |
EP2197438B1 (en) | 2015-07-15 |
RU2010117156A (ru) | 2011-11-20 |
RU2451019C2 (ru) | 2012-05-20 |
CA2700824A1 (en) | 2009-04-16 |
EP2197438A1 (en) | 2010-06-23 |
CA2700824C (en) | 2013-12-10 |
CN101896178B (zh) | 2013-11-20 |
WO2009049021A1 (en) | 2009-04-16 |
US8772312B2 (en) | 2014-07-08 |
BRPI0815948A2 (pt) | 2019-09-24 |
ES2548577T3 (es) | 2015-10-19 |
JP5680146B2 (ja) | 2015-03-04 |
KR20130069840A (ko) | 2013-06-26 |
KR20100065398A (ko) | 2010-06-16 |
IL204823A0 (en) | 2010-11-30 |
EP2197438A4 (en) | 2011-10-12 |
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