AU2013279510A1 - Substituted pyrazole compounds as LPAR antagonists - Google Patents
Substituted pyrazole compounds as LPAR antagonists Download PDFInfo
- Publication number
- AU2013279510A1 AU2013279510A1 AU2013279510A AU2013279510A AU2013279510A1 AU 2013279510 A1 AU2013279510 A1 AU 2013279510A1 AU 2013279510 A AU2013279510 A AU 2013279510A AU 2013279510 A AU2013279510 A AU 2013279510A AU 2013279510 A1 AU2013279510 A1 AU 2013279510A1
- Authority
- AU
- Australia
- Prior art keywords
- phenyl
- methyl
- pyrazol
- biphenyl
- acid
- Prior art date
- 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.)
- Abandoned
Links
- 108090000642 Lysophosphatidic Acid Receptors Proteins 0.000 title description 8
- 102000004137 Lysophosphatidic Acid Receptors Human genes 0.000 title description 8
- 239000005557 antagonist Substances 0.000 title description 6
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 21
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- SSMIBGPOHRVNGJ-UHFFFAOYSA-N 1-(2-chlorophenyl)ethyl n-[4-(2-fluorophenyl)-2-methylpyrazol-3-yl]carbamate Chemical compound C=1C=CC=C(Cl)C=1C(C)OC(=O)NC(N(N=C1)C)=C1C1=CC=CC=C1F SSMIBGPOHRVNGJ-UHFFFAOYSA-N 0.000 claims description 3
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- HNTJWMPUBJHPLD-UHFFFAOYSA-N methyl 1-(4-bromophenyl)cyclopropane-1-carboxylate Chemical compound C=1C=C(Br)C=CC=1C1(C(=O)OC)CC1 HNTJWMPUBJHPLD-UHFFFAOYSA-N 0.000 description 1
- XQQDYMOXTLWTIM-UHFFFAOYSA-N methyl 1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]cyclopropane-1-carboxylate Chemical compound C=1C=C(B2OC(C)(C)C(C)(C)O2)C=CC=1C1(C(=O)OC)CC1 XQQDYMOXTLWTIM-UHFFFAOYSA-N 0.000 description 1
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- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
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- BHMBVRSPMRCCGG-UHFFFAOYSA-N prostaglandine D2 Natural products CCCCCC(O)C=CC1C(CC=CCCCC(O)=O)C(O)CC1=O BHMBVRSPMRCCGG-UHFFFAOYSA-N 0.000 description 1
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- 239000003549 soybean oil Substances 0.000 description 1
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- 229960001967 tacrolimus Drugs 0.000 description 1
- QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- ZVQXQPNJHRNGID-UHFFFAOYSA-N tetramethylsuccinonitrile Chemical compound N#CC(C)(C)C(C)(C)C#N ZVQXQPNJHRNGID-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
- SEDZOYHHAIAQIW-UHFFFAOYSA-N trimethylsilyl azide Chemical compound C[Si](C)(C)N=[N+]=[N-] SEDZOYHHAIAQIW-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
- C07D231/38—Nitrogen atoms
- C07D231/40—Acylated on said nitrogen atom
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261661958P | 2012-06-20 | 2012-06-20 | |
| US61/661,958 | 2012-06-20 | ||
| PCT/EP2013/062458 WO2013189862A1 (en) | 2012-06-20 | 2013-06-17 | Substituted pyrazole compounds as lpar antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2013279510A1 true AU2013279510A1 (en) | 2014-10-16 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2013279510A Abandoned AU2013279510A1 (en) | 2012-06-20 | 2013-06-17 | Substituted pyrazole compounds as LPAR antagonists |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20150259295A1 (pt-PT) |
| EP (1) | EP2864294A1 (pt-PT) |
| JP (1) | JP2015520201A (pt-PT) |
| KR (1) | KR20150011003A (pt-PT) |
| CN (1) | CN104411690A (pt-PT) |
| AU (1) | AU2013279510A1 (pt-PT) |
| BR (1) | BR112014031108A2 (pt-PT) |
| CA (1) | CA2869602A1 (pt-PT) |
| CL (1) | CL2014003242A1 (pt-PT) |
| CO (1) | CO7160077A2 (pt-PT) |
| CR (1) | CR20140516A (pt-PT) |
| EA (1) | EA201492283A1 (pt-PT) |
| HK (1) | HK1206341A1 (pt-PT) |
| IL (1) | IL236091A0 (pt-PT) |
| IN (1) | IN2014DN09347A (pt-PT) |
| MA (1) | MA37765A1 (pt-PT) |
| MX (1) | MX2014014105A (pt-PT) |
| PE (1) | PE20142445A1 (pt-PT) |
| PH (1) | PH12014502364A1 (pt-PT) |
| SG (1) | SG11201407229UA (pt-PT) |
| UA (1) | UA109867C2 (pt-PT) |
| WO (1) | WO2013189862A1 (pt-PT) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8975235B2 (en) | 2011-03-20 | 2015-03-10 | Intermune, Inc. | Lysophosphatidic acid receptor antagonists |
| US10000459B2 (en) | 2013-03-15 | 2018-06-19 | Epigen Biosciences, Inc. | Heterocyclic compounds useful in the treatment of disease |
| RU2689315C2 (ru) | 2014-06-27 | 2019-05-27 | Убе Индастриз, Лтд. | Соль гетероциклического соединения, замещенного галогеном |
| KR20200100712A (ko) * | 2017-12-19 | 2020-08-26 | 브리스톨-마이어스 스큅 컴퍼니 | Lpa 길항제로서의 피라졸 n-연결된 카르바모일 시클로헥실 산 |
| CN111434655A (zh) * | 2019-01-15 | 2020-07-21 | 武汉朗来科技发展有限公司 | 溶血磷脂酸受体拮抗剂及其制备方法 |
| JP7431961B2 (ja) | 2019-11-15 | 2024-02-15 | ギリアード サイエンシーズ， インコーポレイテッド | Ｌｐａ受容体アンタゴニストとしてのトリアゾールカルバメートピリジルスルホンアミド及びその使用 |
| KR20230019880A (ko) | 2020-06-03 | 2023-02-09 | 길리애드 사이언시즈, 인코포레이티드 | Lpa 수용체 길항제 및 이의 용도 |
| AU2021285747A1 (en) | 2020-06-03 | 2023-01-19 | Gilead Sciences, Inc. | LPA receptor antagonists and uses thereof |
| TW202400561A (zh) * | 2021-05-11 | 2024-01-01 | 美商基利科學股份有限公司 | Lpa受體拮抗劑及其用途 |
| US11939318B2 (en) | 2021-12-08 | 2024-03-26 | Gilead Sciences, Inc. | LPA receptor antagonists and uses thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JPWO2005063241A1 (ja) * | 2003-12-26 | 2007-07-19 | 小野薬品工業株式会社 | ミトコンドリアベンゾジアゼピン受容体介在性疾患の予防および／または治療剤 |
| TW200827346A (en) | 2006-11-03 | 2008-07-01 | Astrazeneca Ab | Chemical compounds |
| US20090036425A1 (en) | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
| GB2466121B (en) * | 2008-12-15 | 2010-12-08 | Amira Pharmaceuticals Inc | Antagonists of lysophosphatidic acid receptors |
| GB2470833B (en) * | 2009-06-03 | 2011-06-01 | Amira Pharmaceuticals Inc | Polycyclic antagonists of lysophosphatidic acid receptors |
| WO2011017350A2 (en) * | 2009-08-04 | 2011-02-10 | Amira Pharmaceuticals, Inc. | Compounds as lysophosphatidic acid receptor antagonists |
| BR112013014019A2 (pt) * | 2010-12-07 | 2016-09-13 | Amira Pharmaceuticals Inc | antagonistas do receptor do ácido lisofosfatídico e seus usos |
| US8975235B2 (en) * | 2011-03-20 | 2015-03-10 | Intermune, Inc. | Lysophosphatidic acid receptor antagonists |
| WO2012138648A1 (en) * | 2011-04-06 | 2012-10-11 | Irm Llc | Compositions and methods for modulating lpa receptors |
-
2013
- 2013-06-17 AU AU2013279510A patent/AU2013279510A1/en not_active Abandoned
- 2013-06-17 UA UAA201500427A patent/UA109867C2/ru unknown
- 2013-06-17 IN IN9347DEN2014 patent/IN2014DN09347A/en unknown
- 2013-06-17 EA EA201492283A patent/EA201492283A1/ru unknown
- 2013-06-17 PE PE2014002212A patent/PE20142445A1/es not_active Application Discontinuation
- 2013-06-17 EP EP13729940.0A patent/EP2864294A1/en not_active Withdrawn
- 2013-06-17 US US14/402,128 patent/US20150259295A1/en not_active Abandoned
- 2013-06-17 JP JP2015517702A patent/JP2015520201A/ja active Pending
- 2013-06-17 BR BR112014031108A patent/BR112014031108A2/pt not_active Application Discontinuation
- 2013-06-17 MX MX2014014105A patent/MX2014014105A/es unknown
- 2013-06-17 CN CN201380032266.8A patent/CN104411690A/zh active Pending
- 2013-06-17 SG SG11201407229UA patent/SG11201407229UA/en unknown
- 2013-06-17 WO PCT/EP2013/062458 patent/WO2013189862A1/en active Application Filing
- 2013-06-17 KR KR1020147035552A patent/KR20150011003A/ko not_active Application Discontinuation
- 2013-06-17 CA CA2869602A patent/CA2869602A1/en not_active Abandoned
- 2013-06-17 MA MA37765A patent/MA37765A1/fr unknown
-
2014
- 2014-10-22 PH PH12014502364A patent/PH12014502364A1/en unknown
- 2014-11-11 CR CR20140516A patent/CR20140516A/es unknown
- 2014-11-28 CL CL2014003242A patent/CL2014003242A1/es unknown
- 2014-12-04 IL IL236091A patent/IL236091A0/en unknown
- 2014-12-19 CO CO14279332A patent/CO7160077A2/es unknown
-
2015
- 2015-07-21 HK HK15106926.9A patent/HK1206341A1/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SG11201407229UA (en) | 2014-12-30 |
| US20150259295A1 (en) | 2015-09-17 |
| MX2014014105A (es) | 2015-03-05 |
| IL236091A0 (en) | 2015-02-01 |
| KR20150011003A (ko) | 2015-01-29 |
| EP2864294A1 (en) | 2015-04-29 |
| PH12014502364A1 (en) | 2015-01-12 |
| CL2014003242A1 (es) | 2015-03-20 |
| JP2015520201A (ja) | 2015-07-16 |
| EA201492283A1 (ru) | 2015-04-30 |
| BR112014031108A2 (pt) | 2017-06-27 |
| CA2869602A1 (en) | 2013-12-27 |
| PE20142445A1 (es) | 2015-01-28 |
| CO7160077A2 (es) | 2015-01-15 |
| UA109867C2 (ru) | 2015-10-12 |
| IN2014DN09347A (pt-PT) | 2015-07-17 |
| WO2013189862A1 (en) | 2013-12-27 |
| HK1206341A1 (en) | 2016-01-08 |
| CN104411690A (zh) | 2015-03-11 |
| MA37765A1 (fr) | 2017-04-28 |
| CR20140516A (es) | 2014-12-01 |
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