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1. 发明申请

WO2023089632A1 PYRAZOLE AMIDE BASED COMPOUNDS AND USES AGAINST BREAST CANCER THEREOF 审中-公开
公开(公告)号：WO2023089632A1
公开(公告)日：2023-05-25
申请号：PCT/IN2022/051006
申请日：2022-11-16
申请人： COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN. OF SOC. ACT (ACT XXI OF 1860)
发明人： SULOCHANA, Priya , SASIDHAR BALAPPA, Somappa , KOZHIPARAMBIL GOPALAN, Raghu , SREERENJINI, Lakshmi , KIZHAKKAN THIRUTHI, Ashitha
IPC分类号： A61P35/00 , A61K31/415 , C07D231/14
摘要： The present disclosure provides new derivatives of pyrazole amide represented by the formula (Formula I) in which when R= -CH2-, then R1 may be one among benzene, 4-methyl benzene, 4-methoxy benzene, 4-chloro benzene, 4-fluoro benzene, 2-chloro benzene, 3,4-dichloro benzene, 3,5-trifluoromethylbenzene, and when R= -SO2-, then R1 may be one among benzene, 4-methoxy benzene, 4-chloro benzene, 4-bromo benzene, 4-trifluoromethyl benzene, 3-trifluoromethyl benzene, 2-bromo benzene, 2-chlorothiophen, 2,3-dichlorothiophen substituents. The disclosure also relates to compounds of formula (I) for its use as an anticancer agent in triple negative breast cancer (TNBC) cells. The disclosure established the effectiveness of the pyrazole amide derivative of formula I (I-8), against TNBC cells by inducing cell death by various mechanisms through interaction with diverse cellular pathways.

2. 发明申请

WO2023075178A1 자가나노유화 약물전달시스템을 이용한 셀레콕시브 함유 경구 투여용 제제 및 이의 제조방법 审中-公开
公开(公告)号：WO2023075178A1
公开(公告)日：2023-05-04
申请号：PCT/KR2022/014506
申请日：2022-09-28
申请人： 단국대학교 천안캠퍼스 산학협력단
发明人： 진성규 , 최한곤 , 김종오 , 김정석 , 우미란 , 천승현
IPC分类号： A61K9/107 , A61K47/02 , A61K47/38 , A61K9/16 , A61K47/26 , A61K47/22 , A61K31/415 , A61P29/00
摘要： 본 발명은 셀레콕시브, 오일, 계면활성제 및 보조계면활성제를 함유하는 자가나노유화 액상기제 조성물; 및 고체운반체를 포함하고, 상기 고체운반체는 규소를 포함하는 화합물인 것인, 셀레콕시브 함유 경구 투여용 제제와 이의 제조방법에 관한 것으로, 상기 제제는 셀레콕시브의 수용해도를 현저히 증가시키는 효과가 있고, 이에 더하여 용출량 및 경구 생체 이용률을 증가시킬 수 있다.

3. 发明申请

WO2023009612A1 ACORAMIDIS (3-(3-(3,5-DIMETHYL-1H-PYRAZOL-4-YL)PROPOXY)-4-FLUOROBENZOIC ACID) DERIVATIVES FOR STABILIZING TRANSTHYRETIN (TTS) AND INHIBITING TTS MISFOLDING FOR THE TREATMENT OF E.G. PERIPHERAL TTR AMYLOIDOSIS 审中-公开
公开(公告)号：WO2023009612A1
公开(公告)日：2023-02-02
申请号：PCT/US2022/038506
申请日：2022-07-27
申请人： PROTEGO BIOPHARMA, INC.
发明人： LABAUDINIERE, Richard, F. , TAIT, Bradley, Dean
IPC分类号： C07D231/12 , C07D403/12 , A61K31/415 , A61K31/4155 , A61K31/4439 , A61K31/4178 , A61P25/00 , A61P25/28 , A61P27/02 , A61P13/04 , A61P9/00 , A61P43/00
摘要： Provided herein are acoramidis (3-(3-(3,5-dimethyl-lH-pyrazol-4-yl) propoxy)-4-fluorobenzoic acid) derivatives of formula (I) wherein A is having activity against transthyretin (TTR) related conditions. Also provided are the compounds for use in methods for inhibiting and preventing TTR aggregation and/or amyloid formation in the peripheral nerves, kidney, cardiac tissue, eye and CNS, and of treating a subject with peripheral TTR amyloidosis, ocular or cerebral amyloid angiopathy, familial amyloid polyneuropathy, familial amyloid cardiomyopathy, localized nodular cutaneous amyloidosis, TTR oculoleptomeningeal amyloidosis or senile systemic amyloidosis. An exemplary compound is e.g. 2-(dimethylamino)ethyl 3-(3-(3,5- dimethyl-lH-pyrazol-4-yl)propoxy)-4-fluorobenzoate (example 1, compound 1) Results of biological assays are provided.

4. 发明申请

WO2023283743A1 SULFAMOYL BENZENE DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：WO2023283743A1
公开(公告)日：2023-01-19
申请号：PCT/CA2022/051102
申请日：2022-07-15
申请人： APHIOTX INC.
发明人： TRANG, Tuan , DERKSEN, Darren Jason , NAVIS, Kathleen , GOROBETS, Evgueni , PAPATZIMAS, James
IPC分类号： C07C311/29 , A61K31/145 , A61K31/415 , A61K31/416 , A61K31/505 , A61K31/4418 , A61P25/36 , C07D213/74 , C07D231/12 , C07D231/56 , C07D239/42
摘要： The present invention provides compounds of formula (I): NR1R2SOOYR3 (I) or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), and use of the compounds and the pharmaceutical compositions for treating or ameliorating opioid withdrawal syndrome in a subject.

5. 发明申请

WO2023281449A1 METHOD OF PRODUCTION OF THE COMPOSITION OF CYCLOOXYGENASE-2 (COX-2) INHIBITORS 审中-公开
公开(公告)号：WO2023281449A1
公开(公告)日：2023-01-12
申请号：PCT/IB2022/056309
申请日：2022-07-08
申请人： US NANO FOOD & DRUG INC
发明人： PUI, Hing Sang , PUI, Yip Ching , PUI, Yip Shu
IPC分类号： A61K31/415 , A61K31/4015 , A61K31/41 , A61K31/4422 , A61K47/02 , A61K47/12 , A61K47/22 , A61K9/00 , A61K9/46 , A61K9/48
摘要： The disclosure is directed to the method of production of the composition of a cyclooxygenase-2 (COX-2) inhibitor comprising a water soluble excipient comprising HPMC, an organic acid and one or more other components. The composition may be in the form of pellets, a tablet, a capsule or granules with higher dissolution of the API or fast disintegration in the aqueous medium. In some embodiments, the composition further contains a carbonate salt to form a weakly effervescent disintegration formulation.

6. 发明申请

WO2022262657A1 N-取代苯基磺酰胺类化合物及其用途审中-公开
公开(公告)号：WO2022262657A1
公开(公告)日：2022-12-22
申请号：PCT/CN2022/098183
申请日：2022-06-10
申请人：上海璃道医药科技有限公司
发明人：王友鑫 , 张玲玲 , 丁强
IPC分类号： C07D307/52 , C07D307/79 , C07D417/12 , C07D405/12 , C07D409/12 , C07D333/20 , C07D333/34 , C07D207/335 , C07D277/28 , C07D231/12 , C07D261/08 , C07D233/64 , C07D307/54 , C07D409/14 , C07D249/06 , A61P29/00 , A61P1/00 , A61P1/04 , A61P25/00 , A61K31/341 , A61K31/428 , A61K31/443 , A61K31/4178 , A61K31/381 , A61K31/40 , A61K31/426 , A61K31/415 , A61K31/4164 , A61K31/402 , A61K31/4192
摘要：本发明涉及N-取代苯基磺酰胺类化合物及其用途。具体地，本发明提供一种如式I化合物，或其光学异构体，或其外消旋体、或其药学上可接受的盐。本发明所述的化合物对瞬时受体电位通道蛋白具有优异的抑制作用，并对瞬时受体电位通道蛋白相关的疾病如炎症性肠病、肠易激综合征、疼痛和炎症等具有优异的治疗作用。

7. 发明申请

WO2022226172A1 COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES 审中-公开
公开(公告)号：WO2022226172A1
公开(公告)日：2022-10-27
申请号：PCT/US2022/025732
申请日：2022-04-21
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： JOHN, Varghese , MODY, Istvan , CAMPAGNA, Jesus, J. , JAGODZINSKA, Barbara , WEI, Xiaofei
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , A61K31/415 , A61K31/4155 , A61K31/454 , A61P25/00 , A61P25/28 , A61P43/00
摘要： The present disclosure relates to compounds which increase y-oscillations in the brain. The disclosure further relates to methods of treating neurodegenerative diseases or disorders with the compounds disclosed herein.

8. 发明申请

WO2022197577A1 HETEROAROYL AMIDES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF 审中-公开
公开(公告)号：WO2022197577A1
公开(公告)日：2022-09-22
申请号：PCT/US2022/020110
申请日：2022-03-14
申请人： MERCK SHARP & DOHME LLC , CHILDERS, Kaleen Konrad , ELLIS, J. Michael , FULLER, Peter, J. , GUNAYDIN, Hakan , SCOTT, Jack, D. , TANG, Haiqun , YEUNG, Charles, S.
发明人： CHILDERS, Kaleen Konrad , ELLIS, J. Michael , FULLER, Peter, J. , GUNAYDIN, Hakan , SCOTT, Jack, D. , TANG, Haiqun , YEUNG, Charles, S.
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/427 , C07D231/10 , C07D231/12 , C07D231/14
摘要： The present invention is directed to certain (hetero)aroyl 4-aminopyrazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, R1, R2, and R3 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

9. 发明申请

WO2022189459A2 D-GALACTOPYRANOSIDE DERIVATIVES AS INHIBITORS OF GALECTIN 审中-公开
公开(公告)号：WO2022189459A2
公开(公告)日：2022-09-15
申请号：PCT/EP2022/055945
申请日：2022-03-08
申请人： GALECTO BIOTECH AB
发明人： PETERSON, Kristoffer , ZETTERBERG, Fredrik
IPC分类号： C07H19/04 , C07D405/04 , C07D405/14 , A61K31/7056 , A61K31/415 , A61P29/00 , A61P35/00 , A61K45/06
摘要： The present invention relates to beta D-galactopyranose compound of formula (I). Wherein the pyranose ring is β-D-galactopyranose, and these compounds are high affinity galectin-3 inhibitors for use in treatment of inflammation; fibrosis, such as pulmonary fibrosis, liver fibrosis, kidney fibrosis, ophthalmological fibrosis and fibrosis of the skin and heart; scarring; keloid formation; aberrant scar formation; surgical adhesions; scleroderma; systemic sclerosis; septic shock; cancer, such as carcinomas, sarcomas, leukemias and lymphomas, such as T-cell lymphomas; metastasising cancers; autoimmune diseases, such as psoriasis, rheumatoid arthritis, Crohn's disease, ulcerative colitis, intestinal fibrosis, ankylosing spondylitis, systemic lupus erythematosus; metabolic disorders; heart disease; heart failure; aortic stenosis, atherosclerosis, pathological angiogenesis, such as ocular angiogenesis or a disease or condition associated with ocular angiogenesis, e.g. neovascularization related to cancer; and eye diseases, such as age-related macular degeneration and corneal neovascularization; atherosclerosis; metabolic diseases such as diabetes; type 2 diabetes; insulin resistance; obesity; Diastolic HF; asthma and other interstitial lung diseases, including Hermansky-Pudlak syndrome, pulmonary arterial hypertension, RA-ILD, SSc-ILD, Lung disease with fibrosis such as COPD and asthma. Otosclerosis, mesothelioma; liver disorders, such as non-alcoholic steatohepatitis or non-alcoholic fatty liver disease, Liver cirrhosis of various origins, such as alcoholic and non-alcoholic, autoimmune cirrhosis such as primary biliary cirrhosis and sclerosing cholangitis, virally induced cirrhosis, cirrhosis induced by genetic disease. Liver cancer, cholangiocarcinoma, biliary tract cancer; neurodegenerative disorders such as Parkinsons disease, Alzheimers disease, cognitive impairment, cerebrovascular diseases such as stroke, traumatic brain injury, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, peripheral nephropathy.

10. 发明申请

WO2022185338A1 STABLE ORAL SUSPENSION OF CELECOXIB AND METHOD OF PREPARATION THEREOF 审中-公开
公开(公告)号：WO2022185338A1
公开(公告)日：2022-09-09
申请号：PCT/IN2022/050180
申请日：2022-03-02
申请人： ALKEM LABORATORIES LIMITED
发明人： DHUPPAD, Ulhas , GANGWAL, Jitendra , SHARMA, Akhilesh , AWARE, Babasaheb , KADAM, Sainath , GHAG, Suraj
IPC分类号： A61K31/415
摘要： The disclosure describes a stable oral pharmaceutical suspension and a method of preparation of the stable oral pharmaceutical suspension. The stable oral pharmaceutical suspension comprises about 2% w/v of celecoxib, suspending agents and pharmaceutically acceptable excipients. The stable pharmaceutical suspension is suitable for oral administration, and improves palatability, ensuring adequate therapeutic levels of drug concentration in comparison to the commercial capsule dosage form.

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