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1.发明申请ANTHRANILIC ACID DERIVATIVES: NOVEL INHIBITORS OF ADVANCED GLYCATION END-PRODUCTS (AGES) FORMATION 审中-公开抗坏血酸衍生物：高级糖化终产物（AGES）形成的新型抑制剂公开(公告)号：US20150051286A1
公开(公告)日：2015-02-19
申请号：US13968071
申请日：2013-08-15
IPC分类号： C07C229/64 , C07C229/58
CPC分类号： A61K31/196
摘要： Anthranilic acid derivatives are used to inhibit the formation of advanced glycation end products to reduce complications in diabetes.
摘要翻译： 邻氨基苯甲酸衍生物用于抑制晚期糖基化终产物的形成，以减少糖尿病的并发症。
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2.发明授权Anthranilic acid derivatives: novel inhibitors of advanced glycation end-products (AGEs) formation 有权邻氨基苯甲酸衍生物：晚期糖基化终产物（AGEs）形成的新型抑制剂公开(公告)号：US09381182B2
公开(公告)日：2016-07-05
申请号：US13968071
申请日：2013-08-15
IPC分类号： A61K31/196
CPC分类号： A61K31/196
摘要： Anthranilic acid derivatives are used to inhibit the formation of advanced glycation end products to reduce complications in diabetes.
摘要翻译： 邻氨基苯甲酸衍生物用于抑制晚期糖基化终产物的形成，以减少糖尿病的并发症。
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公开(公告)号：US20230241079A1
公开(公告)日：2023-08-03
申请号：US18128246
申请日：2023-03-30
申请人： Muhammad Iqbal Choudhary , Atia-tul- Wahab , Humaira Zafar , Ambreen Aziz , Nimra Naveed Shaikh , Atta-ur- Rahman
发明人： Muhammad Iqbal Choudhary , Atia-tul- Wahab , Humaira Zafar , Ambreen Aziz , Nimra Naveed Shaikh , Atta-ur- Rahman
IPC分类号： A61K31/57
CPC分类号： A61K31/57
摘要： Biotransformation of gestonorone acetate (1) with Cunninghamella blakesleeana (ATCC 8688) yielded a new analogue, 17α-actoxy-10β,11β-dihydroxy-progesterone (2). Compound 2 was identified as non-cytotoxic inhibitor of human aromatase enzyme (IC50=0.827±0.066 μM). Compound 2 showed a significant aromatase inhibitory activity, as compared to the standard aromatase inhibitory drug, exemestane (IC50=0.232±0.03 μM).
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4.发明申请公开(公告)号：US20210369740A1
公开(公告)日：2021-12-02
申请号：US17400164
申请日：2021-08-12
申请人： Muhammad Iqbal Choudhary , Atia-tul- Wahab , Mahwish Siddiqui , Almas Jabeen , Nimra Naveed Shaikh , Atta-ur- Rahman
发明人： Muhammad Iqbal Choudhary , Atia-tul- Wahab , Mahwish Siddiqui , Almas Jabeen , Nimra Naveed Shaikh , Atta-ur- Rahman
IPC分类号： A61K31/58
摘要： Four new analogues, 17β-hydroxy-7α,17α-dimethylestr-4,6-diene-3-one (2), 11β,17β-dihydroxy-7α, 17α-dimethyl-estra-1,3,5-triene-3-one (3), 3α,10β,17β-trihydroxy-7α,17α-dimethyl-5α-estrane (4), and 17β-hydroxy-7α,17α-dimethyl-5α-estrane-3,6-dione (5) of anabolic drug mibolerone (1) were synthesized. Derivatives 2 (IC50=3.83 ±0.3 μM) and 3 (IC50=4.24 ±0.2 μM) were identified as potent anti-inflammatory agents against T-cell proliferation. Derivative 4 (IC50=28.5 ±0.07 μM) showed a potent anti-inflammatory activity against TNF-α production. In addition, compounds 1 (IC50=46.0 ±2.4 μM), 2 (IC50=54.4 ±0.3 μM), 3 (IC50=49.1 ±0.4 μM), 4 (IC50=58.0 ±0.1 μM) and 5 (IC50=52.7 ±0.3 μM) showed a remarkable anti-inflammatory activity against NO⋅ production. Metabolite 4 (IC50=0.072 ±0.001 μM) showed a potent inhibitory activity against human placental aromatase. Compound 1 (IC50=24.19 ±2.1 μg/mL) was found to be cytotoxic against BJ normal cell line, while metabolites 2-5 were identified as non-cytotoxic.
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公开(公告)号：US20210308144A1
公开(公告)日：2021-10-07
申请号：US17199481
申请日：2021-03-12
申请人： Atia-tul- Wahab , Muhammad Iqbal Choudhary , Mahwish Siddiqui , Nimra Naveed Shaikh , Nisha Khan , Atta-ur- Rahman
发明人： Atia-tul- Wahab , Muhammad Iqbal Choudhary , Mahwish Siddiqui , Nimra Naveed Shaikh , Nisha Khan , Atta-ur- Rahman
IPC分类号： A61K31/566 , A61K31/567
摘要： New analogues of anti-cancer drugs atamestane (1), drostanolone enanthate ((3), and exemestane (6) were synthesized through biotransformation. New derivatives, 14α-hydroxy-1-methylandrosta-1,4-diene-3,17-dione ((2) (IC50, 9.7±0.72 nM) of 1 (IC50, 13.8±0.2 nM), and 2-methylandrosta-12β,17β-dihydroxy-1,4-diene-3-one (4) (IC50, 4.23±0.133 nM) of 3 (IC50, 6.4±0.06 nM) showed a potent inhibition against human aromatase enzyme and thus have the potential to treat ER+ breast-cancers and other related diseases. New metabolites, 2α-methyl-9α,17β-dihydroxy-5α-androstan-3-one ((5) (IC50=793.0±29.9 nM) of 3, 6-methylene-3α,7β,17β-trihydroxy-5β-androstane (7) (IC50, 46.1±0.81 nM), and 11α,17β-dihydroxy-6-methylene-androsta-1,4-diene-3-one (8) (IC5O=12797.0±844 nM) of exemestane (6) (IC50=232.0±31 nM) also showed a remarkable anti-aromatase activity. Aromatase is an enzyme, involves in the synthesis of estrogen (ER). Increased amount of ER due to overexpression of aromatase in the body, promotes cancerous cells growth in breast. Therefore, aromatase enzyme is a key target for the discovery of chemotherapeutic agents against ER+ breast-cancers.
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公开(公告)号：US20210230214A1
公开(公告)日：2021-07-29
申请号：US17177209
申请日：2021-02-17
申请人： Muhammad Iqbal Choudhary , Atia-tul- Wahab , Mahwish Siddiqui , Nimra Naveed Shaikh , Sammer Yousuf , Atta-ur- Rahman
发明人： Muhammad Iqbal Choudhary , Atia-tul- Wahab , Mahwish Siddiqui , Nimra Naveed Shaikh , Sammer Yousuf , Atta-ur- Rahman
摘要： Biotransformation of an aromatase inhibitor, testolactone (1), yielded five new metabolites, 7α-hydroxy-3-oxo-13,17-secoandrosta-1,4-dieno-17,13α-lactone (2), 7β-hydroxy-3-oxo-13,17-seco-5β-androsta-1-eno-17,13α-lactone (3), 3α,11β-dihydroxy-13,17-seco-5β-androsta-17,13α-lactone (4), 4β,5β-epoxy-3β-hydroxy-13,17-secoandrosta-1-eno-17,13α-lactone (5), and 4β,5β-epoxy-3α-hydroxy-13,17-secoandrosta-1-eno-17,13α-lactone (6). Aromatase (estrogen synthase) involves in the synthesis of estrogen, and promotes the growth of breast cancerous cells. It is a key target for the discovery of chemotherapeutic agents against ER+ (estrogen-positive) breast-cancers and several other diseases caused by overexpression of aromatase enzyme. Metabolites 3 (IC50=8.60±0.402 nM), and 4 (IC50=9.23±1.31 nM) were identified as potent inhibitors against human aromatase enzyme, in comparison to 1 (IC50=0.716±0.031 μM), and the standard aromatase inhibiting drug, exemestane (IC50=0.232±0.031 μM). Derivatives 2 (IC50=11.68±0.73 μM), 5 (IC50=10.37±0.50 μM) and 6 (IC50=0.82±0.059 μM) have also a good inhibition against aromatase enzyme. Therefore, metabolites 2-6 have the potential to serve as therapeutic agents against diseases caused by aromatase enzyme, including breast cancer.
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公开(公告)号：US11065211B2
公开(公告)日：2021-07-20
申请号：US15934539
申请日：2018-03-23
申请人： Atta-ur- Rahman , Muhammad Iqbal Choudhary , Farzana Shaheen , Shabana Usman Simjee , Saba Majeed , Anila Bashir , Kanwal Iftikhar
发明人： Atta-ur- Rahman , Muhammad Iqbal Choudhary , Farzana Shaheen , Shabana Usman Simjee , Saba Majeed , Anila Bashir , Kanwal Iftikhar
摘要： This invention provides an effective method and a composition for treating neurodegenerative diseases and conditions of the central and peripheral nervous system by stimulating neurogenesis by the use isoxylitones or an isomer, acid analog, a salt or a solvate, thereof.
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8.发明申请公开(公告)号：US20170246130A1
公开(公告)日：2017-08-31
申请号：US15053887
申请日：2016-02-25
申请人： Muhammad Iqbal Choudhary , Sumaira Javaid , Khalid M. Khan , Syed Muhammad Saad , Atia-tul Wahab , Atta-ur- Rahman
发明人： Muhammad Iqbal Choudhary , Sumaira Javaid , Khalid M. Khan , Syed Muhammad Saad , Atia-tul Wahab , Atta-ur- Rahman
IPC分类号： A61K31/166
CPC分类号： A61K31/166
摘要： The present invention relates to anti-thymidine phosphorylase compounds. These compounds are derivatives of 4-hydroxybenzohydarzide or generally Schiff bases of hydrazones. The invention evaluates a series of Schiff bases of hydrazones against thymidine phosphorylase, and identified significant inhibitors of thymidine phosphorylase enzyme during in vitro studies.
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公开(公告)号：US11643395B2
公开(公告)日：2023-05-09
申请号：US17396799
申请日：2021-08-09
申请人： Hina Siddiqui , Muhammad Iqbal Choudhary , Atia-tul- Wahab , Atta-ur- Rahman , Fazila Rizvi , Sheeba Wajid
发明人： Hina Siddiqui , Muhammad Iqbal Choudhary , Atia-tul- Wahab , Atta-ur- Rahman , Fazila Rizvi , Sheeba Wajid
IPC分类号： C07D231/48
CPC分类号： C07D231/48
摘要： One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N′-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 μM) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 μM), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 μM (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.
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公开(公告)号：US20210363108A1
公开(公告)日：2021-11-25
申请号：US17396799
申请日：2021-08-09
申请人： Hina Siddiqui , Muhammad Iqbal Choudhary , Atia-tul- Wahab , Atta-ur- Rahman , Fazila Rizvi , Sheeba Wajid
发明人： Hina Siddiqui , Muhammad Iqbal Choudhary , Atia-tul- Wahab , Atta-ur- Rahman , Fazila Rizvi , Sheeba Wajid
IPC分类号： C07D231/48
摘要： One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N′-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 μM) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 μM), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 μM (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.
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