PE20142445A1 - Compuestos de pirazol sustituidos como antagonistas de lpar - Google Patents
Compuestos de pirazol sustituidos como antagonistas de lparInfo
- Publication number
- PE20142445A1 PE20142445A1 PE2014002212A PE2014002212A PE20142445A1 PE 20142445 A1 PE20142445 A1 PE 20142445A1 PE 2014002212 A PE2014002212 A PE 2014002212A PE 2014002212 A PE2014002212 A PE 2014002212A PE 20142445 A1 PE20142445 A1 PE 20142445A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds substituted
- pirazole
- lpar antagonists
- lpar
- antagonists
- Prior art date
Links
- 150000001875 compounds Chemical group 0.000 title abstract 3
- 102000004137 Lysophosphatidic Acid Receptors Human genes 0.000 title 1
- 108090000642 Lysophosphatidic Acid Receptors Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- WRGQSWVCFNIUNZ-GDCKJWNLSA-N 1-oleoyl-sn-glycerol 3-phosphate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](O)COP(O)(O)=O WRGQSWVCFNIUNZ-GDCKJWNLSA-N 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 abstract 2
- 208000027866 inflammatory disease Diseases 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Chemical group 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000003566 oxetanyl group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000005069 pulmonary fibrosis Diseases 0.000 abstract 1
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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S424/00—Drug, bio-affecting and body treating compositions
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Referida a un compuesto derivado de pirazol de formula (I), donde X es oxigeno, nitrogeno o carbono; R1 es alquilo inferior; R2 es hidrogeno, halogeno, alcoxi, entre otros; R3 es ciclobutilo, oxetanilo, entre otros. Tambien esta referida a una composicion farmaceutica. Dichos compuestos tienen actividad antagonista del acido lisofosfatidico (LPA) y son utiles para el tratamiento de enfermedades y trastornos inflamatorios, tales como, por ejemplo, fibrosis pulmonar
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261661958P | 2012-06-20 | 2012-06-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20142445A1 true PE20142445A1 (es) | 2015-01-28 |
Family
ID=48656033
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2014002212A PE20142445A1 (es) | 2012-06-20 | 2013-06-17 | Compuestos de pirazol sustituidos como antagonistas de lpar |
Country Status (22)
Country | Link |
---|---|
US (1) | US20150259295A1 (es) |
EP (1) | EP2864294A1 (es) |
JP (1) | JP2015520201A (es) |
KR (1) | KR20150011003A (es) |
CN (1) | CN104411690A (es) |
AU (1) | AU2013279510A1 (es) |
BR (1) | BR112014031108A2 (es) |
CA (1) | CA2869602A1 (es) |
CL (1) | CL2014003242A1 (es) |
CO (1) | CO7160077A2 (es) |
CR (1) | CR20140516A (es) |
EA (1) | EA201492283A1 (es) |
HK (1) | HK1206341A1 (es) |
IL (1) | IL236091A0 (es) |
IN (1) | IN2014DN09347A (es) |
MA (1) | MA37765A1 (es) |
MX (1) | MX2014014105A (es) |
PE (1) | PE20142445A1 (es) |
PH (1) | PH12014502364A1 (es) |
SG (1) | SG11201407229UA (es) |
UA (1) | UA109867C2 (es) |
WO (1) | WO2013189862A1 (es) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20140067048A (ko) | 2011-08-15 | 2014-06-03 | 인터뮨, 인크. | 라이소포스파티드산 수용체 길항제 |
KR102090231B1 (ko) | 2013-03-15 | 2020-03-17 | 에피젠 바이오싸이언시즈, 아이엔씨. | 질환의 치료에 유용한 헤테로환식 화합물 |
ES2824801T3 (es) | 2014-06-27 | 2021-05-13 | Ube Industries | Sal de compuesto heterocíclico sustituido con halógeno |
JP7301839B2 (ja) * | 2017-12-19 | 2023-07-03 | ブリストル-マイヤーズ スクイブ カンパニー | Lpaアンタゴニストとしてのピラゾールn-連結のカルバモイルシクロヘキシル酸 |
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 |
TWI838626B (zh) | 2020-06-03 | 2024-04-11 | 美商基利科學股份有限公司 | Lpa受體拮抗劑及其用途 |
AU2021282986B2 (en) | 2020-06-03 | 2024-03-07 | Gilead Sciences, Inc. | LPA receptor antagonists and uses thereof |
WO2022240879A1 (en) * | 2021-05-11 | 2022-11-17 | Gilead Sciences, Inc. | Lpa receptor antagonists and uses thereof |
CA3238094A1 (en) | 2021-12-08 | 2023-06-15 | Gilead Sciences, Inc. | Lpa receptor antagonists and uses thereof |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005063241A1 (ja) * | 2003-12-26 | 2005-07-14 | Ono Pharmaceutical Co., Ltd. | 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 |
CN102574822A (zh) * | 2009-08-04 | 2012-07-11 | 阿米拉制药公司 | 作为溶血磷脂酸受体拮抗剂的化合物 |
PH12013501136A1 (en) * | 2010-12-07 | 2013-07-08 | Amira Pharmaceuticals Inc | Lysophosphatidic acid receptor antagonists and uses thereof |
WO2012138648A1 (en) * | 2011-04-06 | 2012-10-11 | Irm Llc | Compositions and methods for modulating lpa receptors |
KR20140067048A (ko) * | 2011-08-15 | 2014-06-03 | 인터뮨, 인크. | 라이소포스파티드산 수용체 길항제 |
-
2013
- 2013-06-17 PE PE2014002212A patent/PE20142445A1/es not_active Application Discontinuation
- 2013-06-17 KR KR1020147035552A patent/KR20150011003A/ko not_active Ceased
- 2013-06-17 SG SG11201407229UA patent/SG11201407229UA/en unknown
- 2013-06-17 EA EA201492283A patent/EA201492283A1/ru unknown
- 2013-06-17 MX MX2014014105A patent/MX2014014105A/es unknown
- 2013-06-17 UA UAA201500427A patent/UA109867C2/ru unknown
- 2013-06-17 EP EP13729940.0A patent/EP2864294A1/en not_active Withdrawn
- 2013-06-17 CN CN201380032266.8A patent/CN104411690A/zh active Pending
- 2013-06-17 BR BR112014031108A patent/BR112014031108A2/pt not_active Application Discontinuation
- 2013-06-17 US US14/402,128 patent/US20150259295A1/en not_active Abandoned
- 2013-06-17 CA CA2869602A patent/CA2869602A1/en not_active Abandoned
- 2013-06-17 WO PCT/EP2013/062458 patent/WO2013189862A1/en active Application Filing
- 2013-06-17 AU AU2013279510A patent/AU2013279510A1/en not_active Abandoned
- 2013-06-17 IN IN9347DEN2014 patent/IN2014DN09347A/en unknown
- 2013-06-17 HK HK15106926.9A patent/HK1206341A1/xx unknown
- 2013-06-17 JP JP2015517702A patent/JP2015520201A/ja active Pending
- 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
Also Published As
Publication number | Publication date |
---|---|
MX2014014105A (es) | 2015-03-05 |
PH12014502364A1 (en) | 2015-01-12 |
IL236091A0 (en) | 2015-02-01 |
HK1206341A1 (en) | 2016-01-08 |
SG11201407229UA (en) | 2014-12-30 |
EA201492283A1 (ru) | 2015-04-30 |
JP2015520201A (ja) | 2015-07-16 |
WO2013189862A1 (en) | 2013-12-27 |
CR20140516A (es) | 2014-12-01 |
CL2014003242A1 (es) | 2015-03-20 |
US20150259295A1 (en) | 2015-09-17 |
CA2869602A1 (en) | 2013-12-27 |
BR112014031108A2 (pt) | 2017-06-27 |
AU2013279510A1 (en) | 2014-10-16 |
UA109867C2 (ru) | 2015-10-12 |
EP2864294A1 (en) | 2015-04-29 |
IN2014DN09347A (es) | 2015-07-17 |
MA37765A1 (fr) | 2017-04-28 |
KR20150011003A (ko) | 2015-01-29 |
CN104411690A (zh) | 2015-03-11 |
CO7160077A2 (es) | 2015-01-15 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FD | Application declared void or lapsed |