Category: 596114-50-0

On January 14, 2010, Bertram, Lisa Sarah; Fyfe, Matthew Colin Thor; Jeevaratnam, Revathy Perpetua; Keily, John; Krulle, Thomas Martin; Rasamison, Chrystelle Marie; Sambrook-Smith, Colin Peter; Swain, Simon Andrew published a patent.Related Products of 596114-50-0 The title of the patent was Piperidinyl compounds as GPCR agonists and their preparation, and use in the treatment of diabetes and obesity. And the patent contained the following:

The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity. Compounds of formula I wherein Q is CH and N; one of W, Y and Z is N and CH and the others are CR5; R1 is SO2Me and CONH2 and derivatives; R2, R3 and R4 are independently H and Me; n is 0, 1, and 2; R5 is C1-4 alkyl, C1-4 alkoxy, F, Cl, C1-3 fluoroalkyl and Bn; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their GPCR agonistic activity (some data given). The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to piperidinyl compound preparation gpcr agonist treatment diabetes obesity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 7, 2013, Bradley, Stuart Edward; Bell, James Charles; Keily, John; Morrison, Angus; Hanrahan, Patrick Eric; Morgan, Trevor; Rasamison, Chrystelle; Curtis, Eleanor; Smyth, Donald; Bloxham, Jason; Sambrook-Smith, Colin Peter published a patent.Recommanded Product: 596114-50-0 The title of the patent was Preparation of 3-(N-heterocyclylpiperidin-4-yl)butyloxyphenyl derivatives as agonists of GPR119 and GPR40 receptors. And the patent contained the following:

Title compounds I, II and III [R3 = H, F or propyn-1-yl; R5, R6 and R7 = independently H or halogen; E = O, NR8 or S; R8 =H, Me, Et, Pr or i-propyl; V = bond, C(CH3)2, (un)substituted spirocycloalkyl or spiroheterocycle; W = CH2 or form cycloalkyl or heterocyclyl when taken together with V; A = (un)substituted Ph or heteroaryl; B = H, F, OH, propyn-1-yl, etc.; X = O, CH2, N or S; Y = CH2, (CH3)CH, FCH, CH2CH2, etc.; R9 and R10 = independently H, halogen, (un)substituted alkyl, or form azabicyclo[3.3.1]nonane, 3-oxa-7-azabicyclo[ 3.3.1]nonane or azabicyclo[3.2.1]octane when taken together; R11 = H, halogen, alkoxy or (un)substituted alkyl; p and q = 0-2; Z = Ph, benzyl, heteroaryl or CH2-heteroaryl, etc.], and their pharmaceutically acceptable salts, are prepared as agonists of GPR119 and GPR40 receptors. Compound IV was prepared by coupling reaction of compound V (preparation given) and compound VI (preparation given) followed by hydrolysis of the ester group. CompoundIV exhibited activities with EC50 values of less than 1 μM in both GPRl19 cAMP assay and GPR40 FLIPR assay. The invention compounds are useful for the treatment of type II diabetes. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Recommanded Product: 596114-50-0

The Article related to heterocyclylpiperidinylbutyloxyphenyl derivative preparation gpr119 gpr40 receptor agonist typeii diabetes, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 14, 2013, Nagase, Hiroshi; Fujii, Hideaki; Nakata, Eriko; Watanabe, Yoshikazu; Takahashi, Toshihiro published a patent.HPLC of Formula: 596114-50-0 The title of the patent was Preparation of morphinan derivatives as opioid δ receptor agonists. And the patent contained the following:

Title compounds I [R1 = H, alkyl, aryl, etc.; R2 = H, alkyl, cycloalkyl, etc.; R3-R5 = independently H, hydroxy, halo, etc.; R6a, R6b = independently H, F or hydroxy; R6a and R6b may combine to form oxo; R7, R8 = independently H, F or hydroxy; R9, R10 = independently H, alkyl, aryl, etc.; X = O or CH2; Y = C:O, C:S, SO2, etc.; or pharmacol. acceptable salts thereof] were prepared For example, reaction of (1S,3aS,5aS,6R,11bR,11cR)-3-benzyl-14-(cyclopropylmethyl)-3a,11-dihydroxy-10-methoxy-1,3,3a,4,5,6,7,11c-octahydro-2H-6,11b-(iminoethano)-1,5a-expoxynaphtho[1,2-e]indol-2-one with BH3·THF, treatment with PhBr/K2CO3/Cu, exposure to ethylenediamine/sodium silica-gel (stage I), debenzylation, benzoylation, and demethylation using BBr3 afforded compound II. In opioid receptor agonist activity test, the selected invention compounds, e.g., II, showed EC50 of <1 nM for opioid δ receptor. Compounds I are claimed useful for the treatment of pain. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).HPLC of Formula: 596114-50-0

The Article related to morphinan preparation opioid delta receptor agonist, analgesic morphinan opioid delta receptor agonist, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.HPLC of Formula: 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 6, 2018, Fan, Pingchen; Lange, Christopher W.; Lui, Rebecca M.; Malathong, Viengkham; Mali, Venkat Reddy; Punna, Sreenivas; Singh, Rajinder; Tanaka, Hiroko; Zeng, Yibin; Zhang, Penglie published a patent.Category: pyrimidines The title of the patent was 6-5 Fused ring as C5a inhibitors and their preparation. And the patent contained the following:

The disclosure provides, inter alia, compounds of formula I or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathol. activation from C5a and non-pharmaceutical applications. Compounds of formula I wherein A0 is Nh and CO; A1 and A3 are independently N, NH, CH, CO and CR4; A2, A5 and A6 are independently N, CH and CR4; A4 is N, NC1-4 alkyl, CH and CR4; provided that no more than two of A3, A4, A5 and A6 are N; dashed bonds are single and double bonds; n is 0, 1, 2 and 3; R1 is heteroaryl, C6-10 aryl, C1-8 alkylene-heteroaryl, etc.; each R2a is independently C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, etc.; each R2b is independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, CN, etc.; each R3 is independently C1-4 alkyl, C1-4 haloalkyl, and OH; two R3 groups can be taken together to form oxo; each R4 is independently C1-6 alkyl, C1-6 alkoxy, C1-6 hydroxyalkyl, halo, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their C5a inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 5 nM. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Category: pyrimidines

The Article related to indazole preparation c5a inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 6, 2018, Fan, Pingchen; Lange, Christopher W.; Lui, Rebecca M.; Malathong, Viengkham; Mali, Venkat Reddy; Punna, Sreenivas; Zeng, Yibin; Zhang, Penglie published a patent.Related Products of 596114-50-0 The title of the patent was 5-5 Fused ring as C5a inhibitors and their preparation. And the patent contained the following:

The disclosure provides, inter alia, compounds of formula I or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathol. activation from C5a and non-pharmaceutical applications. Compounds of formula I wherein A1 is N, CH, CO and CR4; A2 is N, CH and CR4; A3, A4, A5 and A6 are independently CH and CR4; dashed bonds are single and double bonds; n is 0, 1, 2 and 3; R1 is C1-8 alkylene-C6-10 aryl, C1-8 alkylene-heteroaryl, C1-8 alkyl, etc.; each R2a is independently C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, etc.; each R2b is independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, CN, etc.; each R3 is independently C1-4 alkyl, C1-4 haloalkyl, halo and OH; two R3 groups can be taken together to form oxo or a 3- to 5-membered ring; each R4 is independently C1-6 alkyl, C1-6 alkoxy, C1-6 hydroxyalkyl, halo, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their C5a inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 5 nM. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to pyrrolopyrazole preparation c5a inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 14, 2010, Bertram, Lisa Sarah; Fyfe, Matthew Colin Thor; Jeevaratnam, Revathy Perpetua; Keily, John; Krulle, Thomas Martin; Rasamison, Chrystelle Marie; Sambrook-Smith, Colin Peter; Swain, Simon Andrew published a patent.Related Products of 596114-50-0 The title of the patent was Piperidinyl compounds as GPCR agonists and their preparation, and use in the treatment of diabetes and obesity. And the patent contained the following:

The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity. Compounds of formula I wherein Q is CH and N; one of W, Y and Z is N and CH and the others are CR5; R1 is SO2Me and CONH2 and derivatives; R2, R3 and R4 are independently H and Me; n is 0, 1, and 2; R5 is C1-4 alkyl, C1-4 alkoxy, F, Cl, C1-3 fluoroalkyl and Bn; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their GPCR agonistic activity (some data given). The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to piperidinyl compound preparation gpcr agonist treatment diabetes obesity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 7, 2013, Bradley, Stuart Edward; Bell, James Charles; Keily, John; Morrison, Angus; Hanrahan, Patrick Eric; Morgan, Trevor; Rasamison, Chrystelle; Curtis, Eleanor; Smyth, Donald; Bloxham, Jason; Sambrook-Smith, Colin Peter published a patent.Recommanded Product: 596114-50-0 The title of the patent was Preparation of 3-(N-heterocyclylpiperidin-4-yl)butyloxyphenyl derivatives as agonists of GPR119 and GPR40 receptors. And the patent contained the following:

Title compounds I, II and III [R3 = H, F or propyn-1-yl; R5, R6 and R7 = independently H or halogen; E = O, NR8 or S; R8 =H, Me, Et, Pr or i-propyl; V = bond, C(CH3)2, (un)substituted spirocycloalkyl or spiroheterocycle; W = CH2 or form cycloalkyl or heterocyclyl when taken together with V; A = (un)substituted Ph or heteroaryl; B = H, F, OH, propyn-1-yl, etc.; X = O, CH2, N or S; Y = CH2, (CH3)CH, FCH, CH2CH2, etc.; R9 and R10 = independently H, halogen, (un)substituted alkyl, or form azabicyclo[3.3.1]nonane, 3-oxa-7-azabicyclo[ 3.3.1]nonane or azabicyclo[3.2.1]octane when taken together; R11 = H, halogen, alkoxy or (un)substituted alkyl; p and q = 0-2; Z = Ph, benzyl, heteroaryl or CH2-heteroaryl, etc.], and their pharmaceutically acceptable salts, are prepared as agonists of GPR119 and GPR40 receptors. Compound IV was prepared by coupling reaction of compound V (preparation given) and compound VI (preparation given) followed by hydrolysis of the ester group. CompoundIV exhibited activities with EC50 values of less than 1 μM in both GPRl19 cAMP assay and GPR40 FLIPR assay. The invention compounds are useful for the treatment of type II diabetes. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Recommanded Product: 596114-50-0

The Article related to heterocyclylpiperidinylbutyloxyphenyl derivative preparation gpr119 gpr40 receptor agonist typeii diabetes, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 14, 2013, Nagase, Hiroshi; Fujii, Hideaki; Nakata, Eriko; Watanabe, Yoshikazu; Takahashi, Toshihiro published a patent.HPLC of Formula: 596114-50-0 The title of the patent was Preparation of morphinan derivatives as opioid δ receptor agonists. And the patent contained the following:

Title compounds I [R1 = H, alkyl, aryl, etc.; R2 = H, alkyl, cycloalkyl, etc.; R3-R5 = independently H, hydroxy, halo, etc.; R6a, R6b = independently H, F or hydroxy; R6a and R6b may combine to form oxo; R7, R8 = independently H, F or hydroxy; R9, R10 = independently H, alkyl, aryl, etc.; X = O or CH2; Y = C:O, C:S, SO2, etc.; or pharmacol. acceptable salts thereof] were prepared For example, reaction of (1S,3aS,5aS,6R,11bR,11cR)-3-benzyl-14-(cyclopropylmethyl)-3a,11-dihydroxy-10-methoxy-1,3,3a,4,5,6,7,11c-octahydro-2H-6,11b-(iminoethano)-1,5a-expoxynaphtho[1,2-e]indol-2-one with BH3·THF, treatment with PhBr/K2CO3/Cu, exposure to ethylenediamine/sodium silica-gel (stage I), debenzylation, benzoylation, and demethylation using BBr3 afforded compound II. In opioid receptor agonist activity test, the selected invention compounds, e.g., II, showed EC50 of <1 nM for opioid δ receptor. Compounds I are claimed useful for the treatment of pain. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).HPLC of Formula: 596114-50-0

The Article related to morphinan preparation opioid delta receptor agonist, analgesic morphinan opioid delta receptor agonist, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.HPLC of Formula: 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 6, 2018, Fan, Pingchen; Lange, Christopher W.; Lui, Rebecca M.; Malathong, Viengkham; Mali, Venkat Reddy; Punna, Sreenivas; Singh, Rajinder; Tanaka, Hiroko; Zeng, Yibin; Zhang, Penglie published a patent.Category: pyrimidines The title of the patent was 6-5 Fused ring as C5a inhibitors and their preparation. And the patent contained the following:

The disclosure provides, inter alia, compounds of formula I or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathol. activation from C5a and non-pharmaceutical applications. Compounds of formula I wherein A0 is Nh and CO; A1 and A3 are independently N, NH, CH, CO and CR4; A2, A5 and A6 are independently N, CH and CR4; A4 is N, NC1-4 alkyl, CH and CR4; provided that no more than two of A3, A4, A5 and A6 are N; dashed bonds are single and double bonds; n is 0, 1, 2 and 3; R1 is heteroaryl, C6-10 aryl, C1-8 alkylene-heteroaryl, etc.; each R2a is independently C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, etc.; each R2b is independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, CN, etc.; each R3 is independently C1-4 alkyl, C1-4 haloalkyl, and OH; two R3 groups can be taken together to form oxo; each R4 is independently C1-6 alkyl, C1-6 alkoxy, C1-6 hydroxyalkyl, halo, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their C5a inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 5 nM. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Category: pyrimidines

The Article related to indazole preparation c5a inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On December 6, 2018, Fan, Pingchen; Lange, Christopher W.; Lui, Rebecca M.; Malathong, Viengkham; Mali, Venkat Reddy; Punna, Sreenivas; Zeng, Yibin; Zhang, Penglie published a patent.Related Products of 596114-50-0 The title of the patent was 5-5 Fused ring as C5a inhibitors and their preparation. And the patent contained the following:

The disclosure provides, inter alia, compounds of formula I or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathol. activation from C5a and non-pharmaceutical applications. Compounds of formula I wherein A1 is N, CH, CO and CR4; A2 is N, CH and CR4; A3, A4, A5 and A6 are independently CH and CR4; dashed bonds are single and double bonds; n is 0, 1, 2 and 3; R1 is C1-8 alkylene-C6-10 aryl, C1-8 alkylene-heteroaryl, C1-8 alkyl, etc.; each R2a is independently C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, etc.; each R2b is independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, CN, etc.; each R3 is independently C1-4 alkyl, C1-4 haloalkyl, halo and OH; two R3 groups can be taken together to form oxo or a 3- to 5-membered ring; each R4 is independently C1-6 alkyl, C1-6 alkoxy, C1-6 hydroxyalkyl, halo, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their C5a inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 5 nM. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Related Products of 596114-50-0

The Article related to pyrrolopyrazole preparation c5a inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 596114-50-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia