PE20160654A1 - Compuestos de inhibidor de autotaxina - Google Patents
Compuestos de inhibidor de autotaxinaInfo
- Publication number
- PE20160654A1 PE20160654A1 PE2016000669A PE2016000669A PE20160654A1 PE 20160654 A1 PE20160654 A1 PE 20160654A1 PE 2016000669 A PE2016000669 A PE 2016000669A PE 2016000669 A PE2016000669 A PE 2016000669A PE 20160654 A1 PE20160654 A1 PE 20160654A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- inhibitor compounds
- autotaxin inhibitor
- indol
- pyrazol
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 229940122849 Autotaxin inhibitor Drugs 0.000 title 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- KOCAUNIBIIJPAY-UHFFFAOYSA-N 3-[6-chloro-2-cyano-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanylbenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1)C=1C=NN(C1)CCC)C#N)SC=1C=C(C(=O)O)C=CC1 KOCAUNIBIIJPAY-UHFFFAOYSA-N 0.000 abstract 1
- AQYXZSLWKGMODC-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanylbenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1)C=1C=NN(C1)CCC)C1CC1)SC=1C=C(C(=O)O)C=CC1 AQYXZSLWKGMODC-UHFFFAOYSA-N 0.000 abstract 1
- 102100021977 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Human genes 0.000 abstract 1
- 108050004000 Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
Classifications
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- 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
- A61K31/435—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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D405/14—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La presente invencion se refiere a compuestos de formula (III) donde: R1 es -Cl, -Br, -CN O cicloalquilo C3-C6; R2 es H, -OH, entre otros; R3 es H, -CN, entre otros; W es CH, CF o N; cada RA es H, -CN, entre otros; L1 esta ausente, alquileno C1-C6, entre otros; n es 0, 1 o 2; Q es CO2H, OH, entre otros; el anillo B es heteroarilo monociclico donde cada RB es H, -CN, entre otros. Son compuestos preferidos: acido 3-((6-cloro-2-ciano-1-(1-propil-1H-pirazol-4-il)-1H-indol-3-il)tio)benzoico; acido 3-((6-cloro-2-ciclopropil-1-(1-propil-1H-pirazol-4-il)-1H-indol-3-il)tio)benzoico; entre otros. Dichos compuestos son inhibidores de autotaxina siendo utiles en el tratamiento de cancer y enfermedades fibroticas
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361907965P | 2013-11-22 | 2013-11-22 | |
| US201462038121P | 2014-08-15 | 2014-08-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160654A1 true PE20160654A1 (es) | 2016-07-15 |
Family
ID=53180152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016000669A PE20160654A1 (es) | 2013-11-22 | 2014-11-20 | Compuestos de inhibidor de autotaxina |
Country Status (31)
| Country | Link |
|---|---|
| US (7) | US9334261B2 (es) |
| EP (2) | EP3878848A1 (es) |
| JP (1) | JP6501367B2 (es) |
| KR (2) | KR102515248B1 (es) |
| CN (2) | CN105793253B (es) |
| AU (2) | AU2014352888B2 (es) |
| BR (1) | BR112016010220B1 (es) |
| CA (1) | CA2930737C (es) |
| CL (1) | CL2016001231A1 (es) |
| CR (2) | CR20190394A (es) |
| CY (1) | CY1124407T1 (es) |
| DK (1) | DK3071561T3 (es) |
| EA (1) | EA030068B1 (es) |
| ES (1) | ES2875899T3 (es) |
| HR (1) | HRP20210957T1 (es) |
| HU (1) | HUE055213T2 (es) |
| IL (2) | IL245383B (es) |
| LT (1) | LT3071561T (es) |
| MX (2) | MX375706B (es) |
| MY (1) | MY182095A (es) |
| NI (1) | NI201600071A (es) |
| NZ (1) | NZ720478A (es) |
| PE (1) | PE20160654A1 (es) |
| PH (1) | PH12016500862B1 (es) |
| PL (1) | PL3071561T3 (es) |
| PT (1) | PT3071561T (es) |
| RS (1) | RS62027B1 (es) |
| SI (1) | SI3071561T1 (es) |
| SM (1) | SMT202100531T1 (es) |
| WO (1) | WO2015077503A1 (es) |
| ZA (2) | ZA201603083B (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2861566T (pt) | 2012-06-13 | 2017-02-08 | Hoffmann La Roche | Novos diazaspirocicloalcanos e azaspirocicloalcanos |
| HRP20191937T1 (hr) | 2012-09-25 | 2020-01-10 | F. Hoffmann - La Roche Ag | Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| WO2015042053A1 (en) | 2013-09-17 | 2015-03-26 | Pharmakea, Inc. | Vinyl autotaxin inhibitor compounds |
| WO2015042052A1 (en) | 2013-09-17 | 2015-03-26 | Pharmakea, Inc. | Heterocyclic vinyl autotaxin inhibitor compounds |
| US9850203B2 (en) | 2013-09-26 | 2017-12-26 | Pharmakea, Inc. | Autotaxin inhibitor compounds |
| PE20160654A1 (es) | 2013-11-22 | 2016-07-15 | Pharmakea Inc | Compuestos de inhibidor de autotaxina |
| MX2016006688A (es) | 2013-11-22 | 2016-11-29 | Pharmakea Inc | Inhibidores tetraciclicos de autotaxina. |
| PL3074400T3 (pl) | 2013-11-26 | 2018-03-30 | F.Hoffmann-La Roche Ag | Pochodne oktahydrocyklobuta[1,2-c;3,4-c']dipirolu jako inhibitory autotaksyny |
| SG11201607839UA (en) | 2014-03-26 | 2016-10-28 | Hoffmann La Roche | Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| SG11201607845RA (en) | 2014-03-26 | 2016-10-28 | Hoffmann La Roche | Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| EP4026549A1 (en) | 2015-05-27 | 2022-07-13 | Sabre Therapeutics LLC | Autotaxin inhibitors and uses thereof |
| KR20180043837A (ko) | 2015-09-04 | 2018-04-30 | 에프. 호프만-라 로슈 아게 | 페녹시메틸 유도체 |
| BR112017026682A2 (pt) | 2015-09-24 | 2018-08-14 | Hoffmann La Roche | novos compostos bicíclicos como inibidores de dupla ação de atx/ca |
| EP3353178B1 (en) | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| JP6876685B2 (ja) | 2015-09-24 | 2021-05-26 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ａｔｘ阻害剤としての二環式化合物 |
| EP3353180B1 (en) | 2015-09-24 | 2022-03-16 | F. Hoffmann-La Roche AG | Bicyclic compounds as atx inhibitors |
| US11000142B2 (en) | 2016-12-06 | 2021-05-11 | John Joseph Girard | Flexible floor mat incorporating LED lighting |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ．ホフマン－ラ ロシュ アーゲー | Ａｔｘインヒビターとしての新規二環式化合物 |
| PE20191757A1 (es) | 2017-03-16 | 2019-12-12 | Hoffmann La Roche | Compuestos heterociclicos utiles como inhibidores dobles de atx/ca |
| JP7241080B2 (ja) | 2017-08-28 | 2023-03-16 | アンジーエックス・インコーポレーテッド | 抗ｔｍ４ｓｆ１抗体およびそれを使用する方法 |
| MX2021010254A (es) | 2019-02-27 | 2021-09-21 | Angiex Inc | Conjugados de anticuerpo-farmaco que comprenden anticuerpos anti-tm4sf1 y metodos de uso de los mismos. |
| US20250282759A1 (en) * | 2022-05-03 | 2025-09-11 | Sabre Therapeutics Llc | Polymorphic and salt forms of the autotaxin inhibitor cudetaxestat |
| CN116239577A (zh) * | 2023-03-27 | 2023-06-09 | 沈阳药科大学 | 一种制备Cudetaxestat的方法 |
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