Acefylline

April 9, 2019, 2:55 am

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New Drug Approvals

Acefylline Skeletal formula of acefylline

Acefylline

Molecular FormulaC₉H₁₀N₄O₄
Average mass238.200 Da

(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)acetic acid

1,2,3,6-Tetrahydro-1,3-dimethyl-2,6-dioxo-7H-purine-7-acetic Acid

1,3-Dimethylxanthine-7-acetic acid

211-490-2 [EINECS]

652-37-9 [RN]

7-(Carboxymethyl)theophylline

7H-Purine-7-acetic acid, 1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-

CAS Registry Number: 652-37-9

CAS Name: 1,2,3,6-Tetrahydro-1,3-dimethyl-2,6-dioxopurine-7-acetic acid

Additional Names: carboxymethyltheophylline; 7-theophyllineacetic acid

Molecular Formula: C9H10N4O4

Molecular Weight: 238.20

Percent Composition: C 45.38%, H 4.23%, N 23.52%, O 26.87%

Literature References: Prepn: DE 352980 (1922 to E. Merck); Frdl. 14, 1320; S. M. Ride et al., Pharmazie 32, 672 (1977). Prepn of salts: J. Baisse, Bull. Soc. Chim. Fr. 1949, 769; M. Milletti, F. Virgili, Chimica 6, 394 (1951), C.A. 46, 8615h (1952). GC determn in urine: J. Zuidema, H. Hilbers, J. Chromatogr. 182, 445 (1980). HPLC determn in serum and pharmacokinetics: S. Sved et al.,Biopharm. Drug Dispos. 2, 177 (1981).

Properties: Crystals from water, mp 271°.

Melting point: mp…

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Thiotepa, チオテパ ,тиотепа , ثيوتيبا , 塞替派 ,

April 18, 2019, 3:27 am

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New Drug Approvals

ChemSpider 2D Image | thiotepa | C6H12N3PS

Thiotepa, チオテパ

Use:antineoplastic, alkylating agent
Chemical name:1,1′,1”-phosphinothioylidynetrisaziridine
Formula:C₆H₁₂N₃PS

MW:189.22 g/mol
CAS:52-24-4
EINECS:200-135-7
LD₅₀:14500 μg/kg (M, i.v.); 38 mg/kg (M, p.o.);
9400 μg/kg (R, i.v.)
Aziridine, 1,1′,1”-phosphinothioylidynetris-

Aziridine, 1-[bis(1-aziridinyl)phosphinothioyl]-

N,N’,N”-Triethylenethiophosphoramide

Phosphorothioic tri(ethyleneamide)

SZ2975000

T3NTJ APS&- AT3NTJ&- AT3NTJ [WLN]

Thiofozil

Thiotef

1,1′,1”-Phosphorothioyltriaziridine

JAPAN APPROVED, Rethio, PMDA, 2019/3/26

тиотепа [Russian] [INN]

ثيوتيبا [Arabic] [INN]

塞替派 [Chinese] [INN]

Thiotepa (INN,^[1] chemical name: N,N′,N′′-triethylenethiophosphoramide) is an alkylating agent used to treat cancer.

Thiotepa is an organophosphorus compound with the formula SP(NC₂H₄)₃.^[2] It is an analog of N,N′,N′′-triethylenephosphoramide (TEPA), which contains tetrahedral phosphorus and is structurally akin to phosphate. It is manufactured by heating aziridine with thiophosphoryl chloride.

History

Thiotepa was developed…

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SRT 1720

May 6, 2019, 3:57 am

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New Drug Approvals

SRT-1720 diHCl

CAY10559

CAS: 1001645-58-4 (di HCl) , 925434-55-5 (free base) 1001645-58-4 (HCl)
Chemical Formula: C25H25Cl2N7OS
Molecular Weight: 542.483
Elemental Analysis: C, 55.35; H, 4.65; Cl, 13.07; N, 18.07; O, 2.95; S, 5.91

SRT-1720 HCl, SRT-1720 hudrochloride; SRT1720; SRT-1720; SRT 1720; CAY10559; CAY-10559; CAY 10559; SIRT-1933; SIRT 1933; SIRT1933.

N-(2-(3-(piperazin-1-ylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)quinoxaline-2-carboxamide dihydrochloride

Molecular FormulaC₂₅H₂₃N₇OS
Average mass469.561 Da

SRT-1720, also known as CAY10559 and is a drug developed by Sirtris Pharmaceuticals intended as a small-molecule activator of the sirtuin subtype SIRT1. It has similar activity in the body to the known SIRT1 activator resveratrol, but is 1000x more potent. In animal studies it was found to improve insulin sensitivity and lower plasma glucose levels in fat, muscle and liver tissue, and increased mitochondrial and metabolic function. A study of SRT1720 conducted by the National Institute on Aging found that the drug may extend the lifespan…

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AK 3280

August 16, 2019, 3:15 am

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New Drug Approvals

AK-3280

AK 3280; GDC3280; RG 6069

C₁₉ H₁₅ F₃ N₄ O_2, 388.34

CAS 1799412-33-1

4H-Benzimidazol-4-one, 1,5-dihydro-1-methyl-7-(1-methyl-1H-pyrazol-4-yl)-5-[4-(trifluoromethoxy)phenyl]-

Ci8Hi₄N50₂F₃, mass 389.3 g/mol),

ROCHE,

Ark Biosciences , under license from Roche , is developing AK-3280, an antifibrotic agent, for the potential oral treatment of IPF. In July 2018, Ark intended to further clinical development of the drug, for IPF. In June 2019, a phase I trial was planned in Sweden.

Originator Genentech
Mechanism of Action Undefined mechanism

Phase I Interstitial lung diseases

19 Jun 2019Ark Biosciences plans a phase I trial for Idiopathic pulmonary fibrosis (In volunteers) in Sweden (PO, Tablet), in August 2019 , (NCT03990688)
28 Sep 2018GDC 3280 is still in phase I trials for Interstitial lung diseases (Genentech pipeline, September 2018)
28 Jun 2018No recent reports of development identified for phase-I development in Fibrosis(In…

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Lurbinectedin

December 27, 2020, 4:16 am

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New Drug Approvals

Lurbinectedin

(1’R,6R,6aR,7R,13S,14S,16R)-5-(Acetyloxy)-2′,3′,4′,6,6a,7,9′-decahydro-8,14-dihydroxy-6′,9-dimethoxy-4,10,23-trimethyl-spiro(6,16-(epithiopropaneoxymethano)-7.13-imino-12H-1,3-dioxolo[7,8]soquino[3,2-b][3]benzazocine-20,1′-[1H]pyrido[3,4-b]indol]-19-one

Molecular Weight	784.87
Formula	C41H44N4O10S
CAS No.	497871-47-3 (Lurbinectedin);
Chemical Name	Spiro[6,16-(epithiopropanoxymethano)-7,13-imino-12H-1,3-dioxolo[7,8]isoquino[3,2-b][3]benzazocine-20,1′-[1H]pyrido[3,4-b]indol]-19-one, 5-(acetyloxy)-2′,3′,4′,6,6a,7,9′,13,14,16-decahydro-8,14-dihydroxy-6′,9-dimethoxy-4,10,23-trimethyl-, (1’R,6R,6aR,7R,13S,14S,16R)- (9CI)

fda approved , 6/15/2020,ZEPZELCA, Pharma Mar S.A.

To treat metastatic small cell lung cancer
Drug Trials Snapshot

Research Code：PM-01183;PM-1183

MOA：RNA polymerase inhibitor

Indication：Ovarian cancer;Breast cancer;Non small cell lung cancer (NSCLC)лурбинектединلوربينيكتيدين芦比替定(1R,1’R,2’R,3’R,11’S,12’S,14’R)-5′,12′-Dihydroxy-6,6′-dimethoxy-7′,21′,30′-trimethyl-27′-oxo-2,3,4,9-tetrahydrospiro[β-carboline-1,26′-[17,19,28]trioxa[24]thia[13,30]diazaheptacyclo[12.9.6.1^3,11…^2,13.0^4,9.0^15,23.0^16,20]triaconta[4,6,8,15,20,22]hexaen]-22′-yl acetate[ACD/IUPAC Name]2CN60TN6ZS497871-47-3[RN]9397

Lurbinectedin is in phase III clinical development for the treatment of platinum refractory/resistant ovarian cancer.

Phase II clinical trials are also ongoing for several oncology indications: non-small cell lung cancer, breast cancer, small cell lung cancer, head and neck carcinoma, neuroendocrine tumors, biliary tract carcinoma, endometrial carcinoma, germ cell tumors and Ewing’s family of tumors.

Lurbinectedin, sold under the brand nameZepzelca, is a medication for the treatment of adults with metastatic small cell lung cancer (SCLC) with disease progression on or after…

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MAX 40279

September 13, 2021, 7:10 pm

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New Drug Approvals

Thieno(3,2-d)pyrimidin-2-amine, 7-(4-fluoro-2-methoxyphenyl)-6-methyl-N-(1-(4-piperidinyl)-1H-pyrazol-4-yl)-.png

MAX 40279,EX-A4057

Max 4; MAX-40279; MAX-40279-001; MAX-40279-01

UNII-DL772G3NN7

2070931-57-4

C₂₂H₂₃FN₆OS,438.5

7-(4-fluoro-2-methoxyphenyl)-6-methyl-N-(1-piperidin-4-ylpyrazol-4-yl)thieno[3,2-d]pyrimidin-2-amine

Thieno[3,2-d]pyrimidin-2-amine, 7-(4-fluoro-2-methoxyphenyl)-6-methyl-N-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-

7-(4-FLUORO-2-METHOXYPHENYL)-6-METHYL-N-(1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL) THIENO (3,2-D)PYRIMIDIN-2-AMINE SEMI-FUMARATE CAS2388506-43-0

7-(4-Fluoro-2-methoxyphenyl)-6-methyl-N-[1-(4-piperidinyl)-1H-pyrazol-4-yl]thieno[3,2-d]pyrimidin-2-amine

OriginatorMaxinovel Pharmaceuticals
ClassAntineoplastics
Mechanism of ActionFibroblast growth factor receptor antagonists; Fms-like tyrosine kinase 3 inhibitors
Orphan Drug StatusYes – Acute myeloid leukaemia
Phase IAcute myeloid leukaemia; Solid tumours

Most Recent Events

28 Nov 2019Phase-I clinical trials in Solid tumours (Late-stage disease, Metastatic disease) in China (PO) (NCT04183764)
16 Apr 2019Phase-I clinical trials in Acute myeloid leukaemia (Second-line therapy or greater) in China (PO) (NCT04187495)
23 Jan 2019Guangzhou Maxinovel Pharmaceuticals plans a phase I trial in China (ChiCTR1900020971)
MaxiNovel Pharmaceuticals, Inc. Announces FDA Orphan Drug Designation for MAX-40279 for the Treatment of Acute Myeloid Leukemia (AML)

March 29, 2018 11:24 AM Eastern Daylight Timehttps://www.businesswire.com/news/home/20180329005826/en/MaxiNovel-Pharmaceuticals-Inc.-Announces-FDA-Orphan-Drug-Designation-for-MAX-40279-for-the-Treatment-of-Acute-Myeloid-Leukemia-AML

GUANGZHOU, China–(BUSINESS…

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LANSOPRAZOLE

November 1, 2021, 3:11 am

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New Drug Approvals

Lansoprazole

Molecular FormulaC₁₆H₁₄F₃N₃O₂S
Average mass369.362 Da

Lansoprazole, AG-1749, ABT-006, CG-4801, A-65006, Ogast, Lanzor, Lanzo, Agopton, Opiren, Bamalite, Takepron, Lansox, Lansox, Ogastro, Monolitum, Prevacid, Zoton103577-45-3[RN]
1H-Benzimidazole, 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-
лансопразол[Russian][INN],لانسوبرازول[Arabic][INN],兰索拉唑[Chinese][INN]

CAS Registry Number:103577-45-3
CAS Name:2-[[[3-Methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole
Additional Names:2-(2-benzimidazolylsulfinylmethyl)-3-methyl-4-(2,2,2-trifluoroethoxy)pyridine
Manufacturers’ Codes:A-65006; AG-1749
Trademarks:Agopton (Takeda); Lansox (Takeda); Lanzor (Aventis); Limpidex (Sigma-Tau); Ogast (Takeda); Prevacid (TAP); Takepron (Takeda); Zoton (Wyeth)
Molecular Formula:C16H14F3N3O2S,Molecular Weight:369.36
Percent Composition:C 52.03%, H 3.82%, F 15.43%, N 11.38%, O 8.66%, S 8.68%
Literature References:Gastric proton-pump inhibitor. Prepn: A. Nohara, Y. Maki,EP174726;eidem,US4628098(both 1986 to Takeda).HPLC determn in plasma: T. Unoet al.,J. Chromatogr. B816, 309 (2005). Pharmacology: H. Satohet al.,J. Pharmacol. Exp. Ther.248,806 (1989). Mechanism…

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ARIMOCLOMOL

May 30, 2022, 12:44 am

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New Drug Approvals

ARIMOCLOMOL

アリモクロモル;

Formula	C14H20ClN3O3
Exact mass	313.1193
Mol weight	313.7799

CAS289893-25-0

289893-26-1 (Arimoclomol maleate);

INN 8300

N-[(2R)-2-hydroxy-3-piperidin-1-ylpropoxy]-1-oxidopyridin-1-ium-3-carboximidoyl chloride

BRX 220

Arimoclomol maleate is in a phase III clinical trials by Orphazyme for the treatment of Niemann-Pick disease type C (NP-C). It is also in phase II clinical studies for the treatment of amyotrophic lateral sclerosis (ALS).

Arimoclomol(INN; originally codenamedBRX-345, which is a citrate salt formulation ofBRX-220) is an experimental drug developed byCytRx Corporation, a biopharmaceutical company based inLos Angeles, California. In 2011 the worldwide rights to arimoclomol were bought by Danish biotech company Orphazyme ApS.^[1]TheEuropean Medicines Agency(EMA) andU.S. Food & Drug Administration(FDA) granted orphan drug designation to arimoclomol as a potential treatment forNiemann-Picktype C in 2014 and 2015 respectively.^[2]^[3]

Fig. 1Structures of (±)-bimoclomol (1) and (R)-(+)-arimoclomol…

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‘Top 10 Prominent & Great Personalities of the year 2022’ campaign by Fame Finders. ANTHONY CRASTO

January 16, 2023, 7:20 pm

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New Drug Approvals

‘Top 10 Prominent & Great Personalities of the year 2022’ campaign by Fame Finders.
Feeling great to be selected in the ‘Top 10 Prominent & Great Personalities of the year 2022’ campaign by Fame Finders. It is an online campaign to honour inspiring personalities and feature them in the upcoming edition of the top news sites, including – Deccan Chronicle/Asian Age/Deccan Herald, ANI, Zee5, Latestly, Lokmat Times, DailyHunt, Google News, JioNews, MSN and 70+ sites.Jan 16 2023

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SMARTCHEM FROM ROW2 TECHNOLOGIES

March 9, 2023, 5:36 am

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New Drug Approvals

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