Category: 59833-69-1

Iwahashi, Maki; Naganawa, Atsushi; Kinoshita, Atsushi; Shimabukuro, Atsushi; Nishiyama, Toshihiko; Ogawa, Seiji; Matsunaga, Yoko; Tsukamoto, Kohki; Okada, Yutaka; Matsumoto, Ryoji; Nambu, Fumio; Oumi, Rie; Odagaki, Yoshihiko; Katagi, Jun; Yano, Koji; Tani, Kousuke; Nakai, Hisao; Toda, Masaaki published an article in 2011, the title of the article was Discovery of new orally active prostaglandin D2 receptor antagonists.Recommanded Product: 59833-69-1 And the article contains the following content:

To identify an orally available drug candidate, a series of 3-benzoylaminophenylacetic acids were synthesized and evaluated as prostaglandin D2 (PGD2) receptor antagonists. Some of the compounds tested were found to exhibit excellent inhibitory activity against cAMP accumulation in human platelet rich plasma (hPRP), which is one of the indexes of DP antagonism. The optimization process including improvement of the physicochem. properties such as solubility, which may result in an improved pharmacokinetic (PK) profile, is presented. Optimized compounds were studied for their pharmacokinetics and in vivo potential. A structure-activity relation study is also presented. Some of the test compounds were found to have in vivo efficacy towards the inhibition of PGD2-induced and OVA-induced vascular permeability in guinea pig conjunctiva. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).Recommanded Product: 59833-69-1

The Article related to prostaglandin d2 receptor antagonist preparation and structure activity, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 59833-69-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On September 30, 2021, Asada, Masaki; Higuchi, Satonori; Naganawa, Atsushi; Hanada, Keisuke; Takeda, Yasuhiro published a patent.HPLC of Formula: 59833-69-1 The title of the patent was Preparation of phenylacetic acid compound as DP receptor antagonist. And the patent contained the following:

Title compound I [R1 = H, alkyl or benzyl; R2-R4 = independently halo, alkyl (optionally substituted with halo) or alkoxy (optionally substituted with halo); J = bond, -O- or -S-; L = bond, alkylene, alkenylene, etc.; R5 = H, carbocyclyl or heterocyclyl (wherein the carbocycle and heterocycle are optionally substituted with R7); when L is a bond, R5 cannot be H; R7 = halo, alkyl (optionally substituted with halo) or alkoxy (optionally substituted with halo); R11 = H, halo or alkyl (optionally substituted with halo); R12 = H, halo or alkyl (optionally substituted with halo); R11 and R12, together with the carbon atom to which they are attached, may be combined to form a saturated carbocycle; n = 0-4; m = 0-3; or a pharmaceutically acceptable salt thereof] was prepared For example, treatment of Me (4-chloro-3-[2,6-dimethyl-4-[2-(oxan-2-yl)ethoxy]benzamido]phenyl)acetate with Lawesson’s reagent, chiral separation and hydrolsis afforded compound II. The phenylacetic acid compound in the present invention shows high antagonistic activity for DP receptor, e.g., IC50 value of II was 0.0048μM. Compound I is claimed useful for the treat,ent of allergic disease, inflammation, sleep disorder, etc. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).HPLC of Formula: 59833-69-1

The Article related to phenylacetic acid preparation dp receptor antagonist, allergy inflammation sleep disorder treatment phenylacetic acid, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.HPLC of Formula: 59833-69-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Iwahashi, Maki; Takahashi, Eiji; Tanaka, Motoyuki; Matsunaga, Yoko; Okada, Yutaka; Matsumoto, Ryoji; Nambu, Fumio; Nakai, Hisao; Toda, Masaaki published an article in 2011, the title of the article was Design and synthesis of new prostaglandin D2 receptor antagonists.Safety of Methyl 2-(3-amino-4-chlorophenyl)acetate And the article contains the following content:

To identify new cost-effective prostaglandin D2 (DP) receptor antagonists, a series of novel 3-benzoylaminophenylacetic acids containing a benzoxazine moiety were synthesized and biol. evaluated. Among those tested, some representative compounds, e.g., I, were found to be orally available. Receptor selectivity and rat PK profiles were also evaluated. The structure-activity relationship (SAR) study is presented. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).Safety of Methyl 2-(3-amino-4-chlorophenyl)acetate

The Article related to benzoylaminophenylacetic acid benzoxazine derivative preparation prostaglandin receptor antagonist sar, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Safety of Methyl 2-(3-amino-4-chlorophenyl)acetate

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On March 26, 2020, Asada, Masaki; Hanada, Keisuke; Higuchi, Satonori; Naganawa, Atsushi; Takeda, Yasuhiro published a patent.Application of 59833-69-1 The title of the patent was Preparation of benzamide compound as DP antagonist. And the patent contained the following:

The present invention relates to a compound I [R1 = H, alkyl or benzyl; R2-R4 = independently halo, alkyl (optionally substituted with halo) or alkoxy (optionally substituted with halo); when plural R2 or R4 groups exist, they, at each occurrence, are the same or different; J = bond, -O- or -S-; L = bond, alkylene, alkenylene, etc.; R5 = H or carbocyclyl or heterocyclyl (wherein carbocycle and heterocycle are optionally substituted with R7); when L is a bond, R5 cannot be H; R7 = halo, alkyl (optionally substituted with halo) or alkoxy (optionally substituted with halo); Q = oxygen atom or sulfur atom; R6 = H or alkyl; R11 = H, halo or alkyl (optionally substituted with halo); R12 = H, halo or alkyl (optionally substituted with halo); R11 and R12, together with the carbon atom to which they are attached, may combine to form a saturated carbocycle; n = 0-4; m = 0-3; or a pharmaceutically acceptable salt thereof]. For example, compound II was prepared via reaction of Me [4-chloro-3-(4-hydroxy-2,6-dimethylbenzamido)phenyl]acetate with N,N-bis(trifluoromethylsulfonyl)aniline and coupling reaction with 2-[(E)-3-cyclohexylpropen-1-yl]-4,4,5,5-tetramethyl-1,3,2-dioxaborolane. Compound I exhibits high DP antagonistic activity, has excellent ability to migrate to the central nervous system, and therefore is useful for the treatment of disease involving DP receptors located in the central nervous system among DP-receptor-mediated diseases (i.e., sleep-wake disorder). The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).Application of 59833-69-1

The Article related to benzamide preparation dp receptor antagonist, sleep wake disorder treatment benzamide, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Application of 59833-69-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On June 26, 2003, Koppitz, Marcus; Muhn, Hans Peter; Shaw, Ken; Hess-Stumpp, Holger; Paulini, Klaus published a patent.Application of 59833-69-1 The title of the patent was Synthesis of tetrahydrocarbazole derivatives for use as ligands for G-protein coupled receptors and antagonists of gonadotropin-releasing hormone for treatment of disease. And the patent contained the following:

The invention relates to novel tetrahydrocarbazole derivatives [e.g., (I)] which act as ligands for G-protein coupled receptors (GPCR), especially as antagonists of gonadotropin-releasing hormone (GnRH), and pharmaceutical composition containing them. Furthermore, the invention relates to the administration of tetrahydrocarbazole derivatives for the treatment of pathol. conditions mediated by GPCR, especially for the inhibition of GnRH, to mammals, especially humans, requiring such treatment, and to the use of tetrahydrocarbazole derivatives for producing a pharmaceutical agent for treating pathol. conditions mediated by GPCR, especially for the inhibition of GnRH. Limited synthesis of intermediate materials is given, with many tables of products exemplified by general synthesis steps. Thus, beginning from 4,4-ethylenedioxycyclohexanone and phenylhydrazine, I was prepared in seven generalized steps. In in vitro tests with alpha T3-1 cells, I had IC50 for human GnRH of 1.5 x 10-8 M, with Ca2+ release of 4.5 x 10-8 M. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).Application of 59833-69-1

The Article related to protein receptor antagonist tetrahydrocarbazole derivative preparation infertility conception therapy, heterocyclic compound peptide derivative preparation solid phase tumor therapy and other aspects.Application of 59833-69-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On November 27, 1975, Tomari, Masazumi; Miyamatsu, Hiroki; Kiyota, Keiichi; Yasuno, Akio published a patent.Product Details of 59833-69-1 The title of the patent was 2-(Alkoxycarbonylmethylphenyl)-1,3-dihydroisoindoles. And the patent contained the following:

Dihydroisoindoles I (X = H, halo; R = H, Me; R1 = C1-4 alkyl) or their salts are prepared by cyclizing o-(ClCH2)2C6H4 (II) with aminophenylacetate esters III (R2 = C1-4 alkyl). I have antiinflammatory and analgesic effects (no data). Thus, 5.24 g II was refluxed with 6 g III (X = 2-Cl, x = 5, R = H, R2 = Me) (IV) and 6.36 g Na2CO3 in DMF 4 hr to give 70% I (X = 2-Cl, x = 5, R = H, R1 = Me). The ester was hydrolyzed with KOH in MeOH to give 51.5% I (X = 2-Cl, x = 5, R = R1 = H), also prepared in 80% yield by heating II and IV with NaOH in MeOH. Similarly prepared were I (X, x, R, R1 given): 2-Cl, 5, Me, Me; 2-Cl, 5, Me, H; H, 4, H, Me; H, 4, H, H. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).Product Details of 59833-69-1

The Article related to analgesic isoindole, antiinflammatory isoindole, isoindole carboxyalkylphenyl, cyclization bischloromethylbenzene carboxyalkylaniline, chloromethylbenzene dicyclization aniline, aminophenylalkanoate cyclization bischloromethylbenzene and other aspects.Product Details of 59833-69-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On June 30, 2022, Watanabe, Akio; Hirooka, Yasuo; Tsuboi, Kazuma published a patent.SDS of cas: 59833-69-1 The title of the patent was Preparation of N-phenyl-1H-pyrazolecarboxamides, N-phenyl-1H-pyrrolecarboxamides, and N-phenylbenzamides as prostanoid receptor EP2 antagonists. And the patent contained the following:

The title anilides represented by formula I [R1 = CO2 R101, SO3H, SO2NHR102, CONHSO2R103, SO2NHCOR104, CONR105R106, tetrazolyl, or cyano; R101-R106 = each independently H, C1-4 alkyl, C1-4 alkoxy, C1-4 halo alkyl, or dimethylamino; R8, R9 = each independently H, halo, C1-4 alkyl, or HO; when R8 = R9 = C1-4 alkyl, R8 and R9 are bonded to the adjacent benzene ring at o-position to form a C3-7 carbocyclic ring; R2 = H or C1-4 alkyl; R3 = halo, HO, cyano, or each (un)substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, 3-6 membered ring group,NH2, or SH, etc.; R4 = halo or each (un)substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, 3-6 membered ring group, O-(3-6 membered ring group), C1-4 alkylene-(3-5 membered ring group); R5 = CF3 or each (un)substituted C3-10 carbocyclyl or 3-10 membered heterocyclyl; Y = a bond, O, or optionally oxidized S; L = each (un)substituted C1-8 alkylene, C2-8 alkenylene, or C2-8 alkynylene each optionally having the CH2 group replaced with O, S, S(O), or SO2; ring 1 = nitrogen-containing mono- or bicyclic ring; n = 1, 2, 3, or 4; m = 0, 1, 2, or 3] or pharmaceutically acceptable salts thereof are prepared The compounds I have an antagonistic activity against EP2 receptor, good solubility, and high stability against human liver microsome and provide medicines for the prevention and/or treatment of a disease caused by activation of an EP2 receptor. The disease includes endometriosis, uterine myoma, menorrhagia, adenomyosis, dysmenorrhea, chronic pelvic pain syndrome, cancer, inflammatory pain, neuropathic pain, headache, migraine, postoperative pain, interstitial cystitis, leiomyoma, irritable colon syndrome, Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, multiple sclerosis, rheumatism, osteoarthritis, gout, allergic disease, hypertension, brain damage, ischemia , Stroke, renal disease, transplant rejection, atherosclerosis, ischemic heart disease, acne vulgaris, asthma, prostatitis, glomerulonephritis, sarcoidosis, vasculitis, or autoimmune disease. More specifically the cancer is breast cancer, ovarian cancer, colon cancer, lung cancer, prostate cancer, head and neck cancer, lymphoma, uveal melanoma, thymoma, mesoderma, esophageal cancer, gastric cancer, duodenal cancer, hepatocellular carcinoma, bile duct cancer, gallbladder cancer cancer, pancreatic cancer, renal cell carcinoma , renal and urinary tract cancer, bladder cancer, penis cancer, testis cancer, uterine cancer, vaginal cancer, genital cancer, skin cancer (For example, malignant melanoma), malignant bone tumor, Soft tissue sarcoma, chondrosarcoma, leukemia, myelodysplastic syndrome, brain tumor or multiple myeloma. Thus, etherification of Me 2-[3-[[[1-(sec-butyl)-5-[2-[(2-fluoropyridin-4-yl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetate with 2-fluoro-4-hydroxypyridine using cyanomethylenetributylphosphorane in toluene at 90° for 2.5 h gave Me 2-[3-[[[1-(sec-butyl)-5-[2-[(2-fluoropyridin-4-yl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetate which underwent alkali hydrolysis in a mixture of 5 N aqueous NaOH solution and methanol at room temperature for 30 min followed by acidification with 2 N aqueous HCl solution to give [3-[[[1-sec-Butyl-5-[2-[(2-fluoro-4-pyridinyl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetic acid (II). II and [3-[[[1-((2S)-2-butyl)-5-[2-[(2-chloro-6-fluoro-4-pyridinyl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetic acid (III) inhibited the PGE2-induced production of cAMP in CHO cells expressing human EP2 receptor with IC50 of 2.5 and 0.3 nM, resp., and exhibited a selective EP2 selectivity over production DP receptor with a DP/EP2 receptor inhibition selectivity ratio of 2,565 and 3,681, resp. A tablet formulation containing II was described. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).SDS of cas: 59833-69-1

The Article related to anilide preparation prostanoid receptor ep2 selective antagonist, anticancer phenylpyrazolecarboxamide phenylpyrrolecarboxamide phenylbenzamide preparation, cancer endometriosis uterine myoma menorrhagia adenomyosis dysmenorrhea treatment, phenylpyrazolecarboxamide phenylpyrrolecarboxamide phenylbenzamide preparation prostanoid receptor ep2 selective antagonist and other aspects.SDS of cas: 59833-69-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On June 30, 2022, Watanabe, Akio; Hirooka, Yasuo; Tsuboi, Kazuma published a patent.SDS of cas: 59833-69-1 The title of the patent was Preparation of N-phenyl-1H-pyrazolecarboxamides, N-phenyl-1H-pyrrolecarboxamides, and N-phenylbenzamides as prostanoid receptor EP2 antagonists. And the patent contained the following:

The title anilides represented by formula I [R1 = CO2 R101, SO3H, SO2NHR102, CONHSO2R103, SO2NHCOR104, CONR105R106, tetrazolyl, or cyano; R101-R106 = each independently H, C1-4 alkyl, C1-4 alkoxy, C1-4 halo alkyl, or dimethylamino; R8, R9 = each independently H, halo, C1-4 alkyl, or HO; when R8 = R9 = C1-4 alkyl, R8 and R9 are bonded to the adjacent benzene ring at o-position to form a C3-7 carbocyclic ring; R2 = H or C1-4 alkyl; R3 = halo, HO, cyano, or each (un)substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, 3-6 membered ring group,NH2, or SH, etc.; R4 = halo or each (un)substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, 3-6 membered ring group, O-(3-6 membered ring group), C1-4 alkylene-(3-5 membered ring group); R5 = CF3 or each (un)substituted C3-10 carbocyclyl or 3-10 membered heterocyclyl; Y = a bond, O, or optionally oxidized S; L = each (un)substituted C1-8 alkylene, C2-8 alkenylene, or C2-8 alkynylene each optionally having the CH2 group replaced with O, S, S(O), or SO2; ring 1 = nitrogen-containing mono- or bicyclic ring; n = 1, 2, 3, or 4; m = 0, 1, 2, or 3] or pharmaceutically acceptable salts thereof are prepared The compounds I have an antagonistic activity against EP2 receptor, good solubility, and high stability against human liver microsome and provide medicines for the prevention and/or treatment of a disease caused by activation of an EP2 receptor. The disease includes endometriosis, uterine myoma, menorrhagia, adenomyosis, dysmenorrhea, chronic pelvic pain syndrome, cancer, inflammatory pain, neuropathic pain, headache, migraine, postoperative pain, interstitial cystitis, leiomyoma, irritable colon syndrome, Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, multiple sclerosis, rheumatism, osteoarthritis, gout, allergic disease, hypertension, brain damage, ischemia , Stroke, renal disease, transplant rejection, atherosclerosis, ischemic heart disease, acne vulgaris, asthma, prostatitis, glomerulonephritis, sarcoidosis, vasculitis, or autoimmune disease. More specifically the cancer is breast cancer, ovarian cancer, colon cancer, lung cancer, prostate cancer, head and neck cancer, lymphoma, uveal melanoma, thymoma, mesoderma, esophageal cancer, gastric cancer, duodenal cancer, hepatocellular carcinoma, bile duct cancer, gallbladder cancer cancer, pancreatic cancer, renal cell carcinoma , renal and urinary tract cancer, bladder cancer, penis cancer, testis cancer, uterine cancer, vaginal cancer, genital cancer, skin cancer (For example, malignant melanoma), malignant bone tumor, Soft tissue sarcoma, chondrosarcoma, leukemia, myelodysplastic syndrome, brain tumor or multiple myeloma. Thus, etherification of Me 2-[3-[[[1-(sec-butyl)-5-[2-[(2-fluoropyridin-4-yl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetate with 2-fluoro-4-hydroxypyridine using cyanomethylenetributylphosphorane in toluene at 90° for 2.5 h gave Me 2-[3-[[[1-(sec-butyl)-5-[2-[(2-fluoropyridin-4-yl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetate which underwent alkali hydrolysis in a mixture of 5 N aqueous NaOH solution and methanol at room temperature for 30 min followed by acidification with 2 N aqueous HCl solution to give [3-[[[1-sec-Butyl-5-[2-[(2-fluoro-4-pyridinyl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetic acid (II). II and [3-[[[1-((2S)-2-butyl)-5-[2-[(2-chloro-6-fluoro-4-pyridinyl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetic acid (III) inhibited the PGE2-induced production of cAMP in CHO cells expressing human EP2 receptor with IC50 of 2.5 and 0.3 nM, resp., and exhibited a selective EP2 selectivity over production DP receptor with a DP/EP2 receptor inhibition selectivity ratio of 2,565 and 3,681, resp. A tablet formulation containing II was described. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).SDS of cas: 59833-69-1

The Article related to anilide preparation prostanoid receptor ep2 selective antagonist, anticancer phenylpyrazolecarboxamide phenylpyrrolecarboxamide phenylbenzamide preparation, cancer endometriosis uterine myoma menorrhagia adenomyosis dysmenorrhea treatment, phenylpyrazolecarboxamide phenylpyrrolecarboxamide phenylbenzamide preparation prostanoid receptor ep2 selective antagonist and other aspects.SDS of cas: 59833-69-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

On June 30, 2022, Watanabe, Akio; Hirooka, Yasuo; Tsuboi, Kazuma published a patent.SDS of cas: 59833-69-1 The title of the patent was Preparation of N-phenyl-1H-pyrazolecarboxamides, N-phenyl-1H-pyrrolecarboxamides, and N-phenylbenzamides as prostanoid receptor EP2 antagonists. And the patent contained the following:

The title anilides represented by formula I [R1 = CO2 R101, SO3H, SO2NHR102, CONHSO2R103, SO2NHCOR104, CONR105R106, tetrazolyl, or cyano; R101-R106 = each independently H, C1-4 alkyl, C1-4 alkoxy, C1-4 halo alkyl, or dimethylamino; R8, R9 = each independently H, halo, C1-4 alkyl, or HO; when R8 = R9 = C1-4 alkyl, R8 and R9 are bonded to the adjacent benzene ring at o-position to form a C3-7 carbocyclic ring; R2 = H or C1-4 alkyl; R3 = halo, HO, cyano, or each (un)substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, 3-6 membered ring group,NH2, or SH, etc.; R4 = halo or each (un)substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, 3-6 membered ring group, O-(3-6 membered ring group), C1-4 alkylene-(3-5 membered ring group); R5 = CF3 or each (un)substituted C3-10 carbocyclyl or 3-10 membered heterocyclyl; Y = a bond, O, or optionally oxidized S; L = each (un)substituted C1-8 alkylene, C2-8 alkenylene, or C2-8 alkynylene each optionally having the CH2 group replaced with O, S, S(O), or SO2; ring 1 = nitrogen-containing mono- or bicyclic ring; n = 1, 2, 3, or 4; m = 0, 1, 2, or 3] or pharmaceutically acceptable salts thereof are prepared The compounds I have an antagonistic activity against EP2 receptor, good solubility, and high stability against human liver microsome and provide medicines for the prevention and/or treatment of a disease caused by activation of an EP2 receptor. The disease includes endometriosis, uterine myoma, menorrhagia, adenomyosis, dysmenorrhea, chronic pelvic pain syndrome, cancer, inflammatory pain, neuropathic pain, headache, migraine, postoperative pain, interstitial cystitis, leiomyoma, irritable colon syndrome, Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, multiple sclerosis, rheumatism, osteoarthritis, gout, allergic disease, hypertension, brain damage, ischemia , Stroke, renal disease, transplant rejection, atherosclerosis, ischemic heart disease, acne vulgaris, asthma, prostatitis, glomerulonephritis, sarcoidosis, vasculitis, or autoimmune disease. More specifically the cancer is breast cancer, ovarian cancer, colon cancer, lung cancer, prostate cancer, head and neck cancer, lymphoma, uveal melanoma, thymoma, mesoderma, esophageal cancer, gastric cancer, duodenal cancer, hepatocellular carcinoma, bile duct cancer, gallbladder cancer cancer, pancreatic cancer, renal cell carcinoma , renal and urinary tract cancer, bladder cancer, penis cancer, testis cancer, uterine cancer, vaginal cancer, genital cancer, skin cancer (For example, malignant melanoma), malignant bone tumor, Soft tissue sarcoma, chondrosarcoma, leukemia, myelodysplastic syndrome, brain tumor or multiple myeloma. Thus, etherification of Me 2-[3-[[[1-(sec-butyl)-5-[2-[(2-fluoropyridin-4-yl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetate with 2-fluoro-4-hydroxypyridine using cyanomethylenetributylphosphorane in toluene at 90° for 2.5 h gave Me 2-[3-[[[1-(sec-butyl)-5-[2-[(2-fluoropyridin-4-yl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetate which underwent alkali hydrolysis in a mixture of 5 N aqueous NaOH solution and methanol at room temperature for 30 min followed by acidification with 2 N aqueous HCl solution to give [3-[[[1-sec-Butyl-5-[2-[(2-fluoro-4-pyridinyl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetic acid (II). II and [3-[[[1-((2S)-2-butyl)-5-[2-[(2-chloro-6-fluoro-4-pyridinyl)oxy]ethyl]-1H-pyrrol-2-yl]carbonyl]amino]-4-(trifluoromethyl)phenyl]acetic acid (III) inhibited the PGE2-induced production of cAMP in CHO cells expressing human EP2 receptor with IC50 of 2.5 and 0.3 nM, resp., and exhibited a selective EP2 selectivity over production DP receptor with a DP/EP2 receptor inhibition selectivity ratio of 2,565 and 3,681, resp. A tablet formulation containing II was described. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).SDS of cas: 59833-69-1

The Article related to anilide preparation prostanoid receptor ep2 selective antagonist, anticancer phenylpyrazolecarboxamide phenylpyrrolecarboxamide phenylbenzamide preparation, cancer endometriosis uterine myoma menorrhagia adenomyosis dysmenorrhea treatment, phenylpyrazolecarboxamide phenylpyrrolecarboxamide phenylbenzamide preparation prostanoid receptor ep2 selective antagonist and other aspects.SDS of cas: 59833-69-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics