http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-108185-A1
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| filingDate | 2017-04-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
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| publicationDate | 2018-07-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-108185-A1 |
| titleOfInvention | TERTIARY AMIDAS AND METHOD FOR USE |
| abstract | Compounds and pharmaceutically acceptable salts thereof, useful in the treatment of conditions and disorders that are prevented or improved by modulating lysophosphatidic acid receptor 1. Claim 1: A compound characterized in that it is of formula (1) or a pharmaceutically acceptable salt thereof, wherein: G¹ is selected from the compounds of the group of formulas (2); where RG¹ᵃ is selected from the group consisting of hydrogen and fluorine; RG¹ᵇ and RG¹ᵈ are independently selected from the group consisting of hydrogen, C₁₋₃alkoxy, and halogen; where C₁₋₃alkoxy is not substituted or is optionally substituted with one, two or three fluorine atoms; RG¹ᶜ is selected from the group consisting of hydrogen, C₁₋₃alkoxy, C₁₋₃alkyl, C₃₋₅cycloalkyl, halogen, and -NO₂; where the C₁₋₃alkyl and C₁₋₃alkoxy are not substituted or are optionally substituted with a hydroxyl or one, two or three fluorine atoms; where at least one of RG¹ᵇ, RG¹ᶜ, and RG¹ᵈ is not hydrogen; RG¹ᵉ and RG¹ᶠ are independently selected from the group consisting of hydrogen, C₁₋₃alkoxy, and -NHC (O) Rˣ; where the C₁₋₃alkoxy is not substituted or is optionally substituted with one, two or three fluorine atoms; Rˣ is C₁₋₃alkyl; where the C₁₋₃alkyl is not substituted or is optionally substituted with one, two or three fluorine atoms; RG¹ᵍ is selected from the group consisting of halogen and C₁₋₃alkoxy; where the C₁₋₃alkoxy is not substituted or is optionally substituted with one, two or three fluorine atoms; RG¹ʰ and RG¹ⁱ are independently selected from the group consisting of hydrogen, C₁₋₃alkoxy, and C₁₋₃alkyl; where C₁₋₃alkyl and C₁₋₃alkoxy are not substituted or are optionally substituted with one, two or three fluorine atoms; RG¹ʲ is selected from the group consisting of hydrogen or halogen; RG¹ᵏ and RG¹ˡ are independently selected from the group consisting of hydrogen and fluorine; RG¹ᵐ, RG¹ᵒ, RG¹ᵖ, RG¹q, and RG¹ˢ are independently selected in each case from the group consisting of hydrogen and C₁₋₃alkyl; where the C₁₋₃alkyl is not substituted or is optionally substituted with one, two or three fluorine atoms; RG¹ⁿ is selected from the group consisting of halogen and C₁₋₃alkoxy; where the C₁₋₃alkoxy is not substituted or is optionally substituted with one, two or three fluorine atoms; RG¹ʳ is independently selected in each case from the group consisting of hydrogen, C₁₋₃alkoxy, C₁₋₃alkyl, C₃₋₅cycloalkyl, halogen, and -NO₂; where the C₁₋₃alkyl and C₁₋₃alkoxy are not substituted or are optionally substituted with a hydroxyl or one, two or three fluorine atoms; one of X¹ and X² is O and the other is CH; m is one, two or three; n is one, two or three; L¹ is a union or C (R¹R²); R¹ and R² are independently selected from the group consisting of hydrogen, C₁₋₃alkoxy, and C₁₋₃alkyl; where C₁₋₃alkyl and C₁₋₃alkoxy are not substituted or are optionally substituted with one, two or three fluorine atoms; or R¹ and R² and the carbon atom to which they are attached form a C₃₋₆cycloalkylene or oxetane; wherein the C₃₋₆cycloalkylene is not substituted or is optionally substituted with one, two or three substituents selected from C₁₋₃alkoxy, C₁₋₃alkyl and oxo; where C₁₋₃alkyl and C₁₋₃alkoxy are not substituted or are optionally substituted with one, two or three fluorine atoms; G² is selected from the group consisting of phenyl, 2-furanyl and 2-thiophenyl; where the phenyl is not substituted or is optionally substituted with 1, 2 or 3 substituents independently selected from C₁₋₃alkoxy, C₁₋₃alkyl, or halogen, where the C₁₋₃alkyl and C₁₋₃alkoxy are not substituted or are optionally substituted with one, two or three fluorine atoms; and where 2-furanyl and 2-thiophenyl are not substituted or are optionally substituted with 1 or 2 substituents independently selected from halogen or C₁₋₃alkyl, where the C₁₋₃alkyl is not substituted or is optionally substituted with one, two or three fluorine atoms; L² is -CH₂CH₂CH₂-, where -CH₂CH₂CH₂- is not substituted or is optionally substituted with C₁₋₃alkyl, where the substituent -CH₂CH₂CH₂- or C₁₋₃alkyl are optionally independently substituted with one, two or three fluorine atoms , and where the central carbon of -CH₂CH₂CH₂- may optionally be connected with a methylene bridge to G²; G³ is selected from the group consisting of -CO₂H, -P (O) (OH) ₂, -P (O) (OH) (OC₁₋₆alkyl), -P (O) (CH₃) (OH), -B (OH) ₂, -SO₃H, -CH (OH) CF₃, -C (O) NH (OH), -C (O) NH (CN), -C (O) NHSO₂RG³ᵃ, -SO₂NHC (O) RG³ᵃ, - C (O) NHSO₂NHRG³ᵃ, -NHSO₂NHC (O) RG³ᵃ, -OC (O) NHSO₂RG³ᵃ, -SO₂NH₂, -SO₂NHRG³ᵃ, -C (O) NHS (O) (RG³ᵃ) = NC (O) RG³ᵃ, C (O) NHS (O) (RG³ᵃ) = NRG³ᵇ, or a remainder of the formula group (3); where, RG³ᵃ is C₁₋₆alkyl, C₁₋₆haloalkyl, or GA; RG³ᵇ is hydrogen, C₁₋₆alkyl, C₁₋₆haloalkyl, or GA; GA is cycloalkyl, cycloalkenyl, aryl, or heteroaryl, each of which is not substituted or is independently substituted with 1, 2, or 3 independently selected Rᵘ groups; where Rᵘ, in each case, is independently C₁₋₆alkyl, C₂₋₆alkenyl, C₂₋₆alquinyl, halogen, C₁₋₆haloalkyl, -CN, oxo, -NO₂, -ORʲ, -OC (O) Rᵏ, -OC ( O) N (Rʲ) ₂, -S (O) ₂Rʲ, -S (O) ₂N (Rʲ) ₂, -C (O) Rᵏ, -C (O) ORʲ, -C (OR) N (Rʲ) ₂ , -N (Rʲ) C (O) Rᵏ, -N (Rʲ) S (O) ₂Rᵏ, -N (Rʲ) C (O) O (Rʲ) ₂ or -N (Rʲ) C (O) N (Rʲ ) ₂; Rʲ, in each case, is independently selected from the group consisting of hydrogen, C₁₋₆alkyl, or C₁₋₆haloalkyl; Rᵏ, in each case, is independently selected from the group consisting of C₁₋₆alkyl or C₁₋₆haloalkyl; L³ is selected from the group consisting of - (CH₂) ₂₋₅-, - (CH₂) ₁₋₄- (CR³R⁴) -, - (CH₂) - (CR⁵R⁶) ₁₋₃- (CH₂) -, - ( CR⁷R⁸) ₁₋₄- (CH₂) -, -CH₂CH₂-X³- (CR⁹R¹⁰) ₁₋₂-, - (CH₂) ₁₋₂CH = CH- (CH₂) ₁₋₂- and -CH₂C (O) NH (CR¹¹R¹² ) -; R³ and R⁴ are selected from the group consisting of hydrogen, C₁₋₆alkyl, - (C₁₋₆alkylene) -GB, and hydroxyl, where one of R³ and R⁴ is not hydrogen; or R³ and R⁴ and the carbon to which they are attached form a C₃₋₆cycloalkylene; GB is aryl or heteroaryl, each of which is not substituted or is independently substituted with 1, 2, or 3 independently selected Rᵘ groups; R⁵ is independently selected, in each case, from the group consisting of hydrogen and C₁₋₆alkyl; an R⁶ is hydroxyl, and any additional R⁶ is independently selected, in each case, from the group consisting of hydrogen and C₁₋₆alkyl; R⁷ and R⁸ are independently selected, in each case, from the group consisting of hydrogen and C₁₋₆alkyl; R⁹ and R¹⁰ are independently selected, in each case, from the group consisting of hydrogen and C₁₋₆alkyl; or an R⁹ and R¹⁰ and the carbon to which they are attached form a C₃₋₆cycloalkylene and any additional R⁹ and R¹⁰ are independently selected, in each case, from the group consisting of hydrogen and C₁₋₆alkyl; X³ is O, S, or S (O) ₁₋₂; and R¹¹ and R¹² are independently selected from the group consisting of hydrogen, C₁₋₆alkyl, and - (C₁₋₆alkylene) -GB; or R¹¹ and R¹² and the carbon to which they are attached form a C₃₋₆cycloalkylene, where the C₃₋₆cycloalkylene is not substituted or is optionally substituted with one, two or three C₁₋₆alkyl or the C₃₋₆cycloalkylene is optionally fused to a phenyl ring . |
| priorityDate | 2016-04-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 131.