Organic Active Ingredients TRIZ Cases

Repurposing abemaciclib suppresses TLR4-driven neuroinflammation, tau phosphorylation, and amyloid plaques to improve memory in degenerative brain disease.

Novel lipidoid lipid nanoparticles improve nucleic acid delivery efficiency while reducing acute toxicity and side-effects in cells.

Localized lipolysis drugs and an elastic ring reduce epicardial fat and loosen pericardial tissue to improve heart filling space.

Small-molecule compounds inhibit mutant KRAS activity, addressing the lack of effective targeted therapies for pancreatic, colorectal, and lung cancers.

A selective multi-kinase pyrimidopyrimidinone targets GCK and ACK1 to overcome RAS pathway compensation in NRAS-driven cancers.

Dual BRD4 and PI3K inhibitors such as MDP5 suppress MYC activity, promote apoptosis, and reduce tumor growth with minimal toxicity.

Combining ALK and TNKS inhibitors suppresses drug-tolerant persister cells, lowers β-catenin, and prolongs control of ALK-positive cancer.

Small molecule modulators target calcitonin and amylin receptors to improve blood glucose control and support weight loss in metabolic disorders.

Heteroaryl compounds block AXL and MERTK together to limit resistance and improve anti-tumor immune responses in TAM-associated disorders.

A Brevundimonas LPS feed or water additive broadens poultry immune defense against avian influenza and related viruses without strain-specific vaccines.

Pathway-selective indazole macrocycles inhibit STING to curb chronic inflammation with lower toxicity and preserved metabolic stability.

GalNAc-linked double-stranded RNAi targets hepatocytes to persistently lower angiotensinogen and improve 24-hour blood pressure control.

Novel heterobicyclic amide scaffolds expand EP4 antagonist diversity to improve inhibition of PGE2 signaling in pain, inflammation, and cancer.

Ground placental membrane with glue helps fill irregular cartilage defects by injection while improving retention and hyaline-like regeneration.

New alkynyl quinazoline compounds target oncogenic ErbB mutants to address variable patient response in cancers such as glioblastoma and NSCLC.

Low-cationic QTsome lipid ratios improve intramuscular mRNA delivery while limiting systemic gene expression and myocarditis-related side effects.

Double-stranded RNAi agents silence KRAS mRNA to lower protein production, improving treatment of KRAS-driven cancers while limiting off-target effects.

Blocking ROCK1/2 and related kinases raises mutant FXN transcription to restore frataxin and improve mitochondrial and cardiac function.

Small-molecule 5-HT2A agonists reduce inflammatory signaling while avoiding the treatment complexity of biologics and limiting CNS side effects.

A water-free co-solution uses propyl glycol, N-methyl pyrrolidone, and coconut oil to prevent precipitation and reduce injection-site irritation.

A quinazoline derivative targets EGFR C797S and related mutations to inhibit osimertinib-resistant NSCLC and CNS metastases.

Selective AhR ligands drive Tr1 cell differentiation to suppress autoimmune responses without the broad toxicity of conventional immunosuppression.

A tricyclic heterocyclic scaffold offers a distinct antiviral mechanism for COVID-19 while preserving oral use and reducing resistance risk.

A heterocyclic prodrug approach improves CNS treatment breadth by enabling rapid absorption, in vivo brexpiprazole conversion, and weeks-long blood levels.

Stable macropa-chelated 225Ac PSMA antibodies improve tumor targeting while reducing radionuclide dissociation, liver uptake, and off-target toxicity.

Fatty acid-modified CDK4/6 inhibitors target resistant cancer stem cells to curb recurrence, metastasis, and chemotherapy resistance.

Localized lung delivery of imidazolo indazole JAK inhibitors targets respiratory inflammation while minimizing systemic immunosuppression.

Jet-milled ibuprofen at a controlled micron size boosts dissolution and Cmax, enabling earlier and longer-lasting pain relief at lower doses.

Selective MGL inhibition raises 2-AG where it is naturally produced, treating pain and mood disorders while limiting CB1 agonist side effects.

A DOPC/DOPG/cholesterol liposomal steroid formulation sustains joint pain relief while reducing cartilage damage and chondrocyte apoptosis.

Combining pridopidine with CNM-Au8 targets ALS progression by supporting motor neurons, neuromuscular junctions, and respiratory function.

Combining dacomitinib with nintedanib improves pulmonary fibrosis treatment efficacy by reducing fibrosis and inflammation versus monotherapy.

A hydrophobic balloon coating with biodegradable drug micro-reservoirs extends vessel-wall delivery after brief inflation while resisting blood wash-off.

Novel 2-methoxyestradiol derivatives target underlying liver and pulmonary fibrosis where current drugs mainly slow disease progression.

Maternal sphingomyelin supplementation supports fetal and infant myelination, brain structure, and later cognitive function during pregnancy and lactation.

By inhibiting sclerostin, this composition reduces inflammation, angiogenesis, and oxidative stress in diabetic eye disease without inducing cell death.

Selective small-molecule PARG inhibitors bind the adenine pocket to improve potency, specificity, membrane permeability, and in vivo utility in cancer.

Targeted SMN2 base edits correct exon 7 and disable degrons to raise SMN protein stability and support longer-lasting SMA treatment.

Measuring sgp130 and sIL6R before CAR T therapy helps identify patients at high risk of severe CRS for earlier intervention.

A Formula 1 carbamate compound inhibits TGF-β1-driven fibrosis and inflammation, including radiation-induced lung injury.

Modified double-stranded siRNA with GalNAc conjugation improves LPA silencing stability, duration, and specificity for lowering Lp(a).

Targeting CCT2 helps suppress tumor growth and metastasis while improving response to cell cycle inhibitors in drug-resistant breast cancer.

Site-specific 2'-OMe, 2'-F, and phosphorothioate modifications improve serum stability while preserving gene-silencing activity.

Polymer-encapsulated drug particles on balloon catheters enable sustained local delivery to strictures, helping reduce repeat interventions.

Pyrimidoindole compounds activate the CUL3-KBTBD4 ligase to degrade RCOR1 and disrupt LSD1/HDAC2 complexes for selective anti-cancer action.

A low-solubility tetrahydronaphthalene suspension enables weeks-long drug release, avoiding patch-related skin reactions and dosing gaps.

A phytic acid-metal-protein nanomaterial uses pH-triggered tumor retention to improve imaging and therapy while maintaining biocompatibility.

A cyclodextrin-based sublingual cladribine film improves solubility and stability while bypassing GI degradation and first-pass metabolism.

Epigallocatechin promotes ammonia metabolism and urea production to lower blood ammonia, easing fatigue and hyperammonemia.

A dual BTK/ITK heterocyclic amine compound improves autoimmune disease treatment by modulating both B-cell and T-cell activity.

Strong apo(a) binding in cyclic amine derivatives lowers Lp(a) and inhibits LDL-apo(a) assembly while minimizing toxic side effects.

A sulfonamide scaffold blocks KAT6A/KAT6B while improving selectivity, bioavailability, and clearance to limit toxic in-vivo accumulation.

Reducing membrane-surface CAPRIN-1 with antibodies, nucleic acids, enzymes, and pathway modulators helps suppress tumorigenesis.

Using at least two solubilizers, this self-emulsifying formulation improves sulfonamide solubility and membrane permeability after oral dosing.

Combining hyaluronidase with a plasminogen activator speeds local fibrosis breakdown and improves function with less invasive treatment.

DGLA-EE topical compositions reduce inflammation and itch in chronic skin disease while avoiding the side effects of steroids and FK-506.

A bipolymeric depot swells from a thin rod into a compact coil in the eye, enabling months-long release with less tissue trauma and migration.

Selective SSTR5 antagonists promote growth hormone secretion while avoiding unwanted release of other anterior pituitary hormones.

Combining ribociclib with an aromatase inhibitor targets HR+ breast cancer more effectively while reducing reliance on toxic single-agent therapy.

Selective 2,4,6-tri-substituted pyrimidines inhibit ATR kinase to improve cancer treatment while reducing toxic effects on normal cells.

Targeted PanK modulators regulate CoA levels for PKAN and diabetes while balancing neuronal efficacy against off-target metabolic effects.

A compound series spanning Formulas I-XV improves treatment and risk reduction across cancers, inflammatory diseases, and autoimmune disorders.

Combining CDK inhibition with anti-hormonal therapy improves HR+ breast cancer treatment while balancing efficacy, dosing flexibility, and toxicity.

Selective oral BTK inhibition with fenebrutinib reduces autoimmune disease activity while lowering adverse effects seen with current therapies.

Engineered acyclic lipids and a tropism screening platform improve cargo protection while enabling targeted delivery to immune cells.

Gold nanoparticles stabilized with thiohexoses make amphotericin B water-dispersible, less toxic, and more effective against biofilms and intracellular infection.

Selective small molecules inhibit TRAP-1 to improve tissue penetration and enable oral or eye drop treatment of neovascular diseases.

Administered fibroblasts or their derived products help protect renal function, lower serum creatinine, and support recovery from kidney injury.

A stable crystalline Form A enables reproducible production of Compound (I) while preserving solvent solubility for conversion into other solid forms.

Targeting SOC and CRAC calcium channels helps curb cytokine release in ALI and ARDS while preserving lung function.

Water-soluble polymer nanoaggregates and sodium bicarbonate improve taxane solubility, stabilize pH, and reduce hypersensitivity and toxicity.

Novel macrocyclic compounds improve LRRK2 inhibition potency and selectivity to help slow disease progression in neurological and inflammatory disorders.

Specific imidazopyridine substituents improve selective protein kinase inhibition, supporting treatment of cancer and other kinase-related diseases.

A tailored cationic lipid composition improves nucleic acid encapsulation and spleen delivery while reducing cytotoxicity and liver toxicity.

A novel oral BCR-ABL inhibitor targets T315I and other resistant CML mutations, improving antiproliferative activity and clinical response.

Crystalline salt formation improves plasma kallikrein inhibitor stability and pharmacokinetics for oral use while reducing reocclusion and bleeding risk.

FabI inhibition offers an alternative to ceftriaxone, helping treat resistant N. gonorrhoeae with low side effects.

Blocking CD73 lowers adenosine-mediated immunosuppression, re-sensitizes tumors to therapy, and strengthens immune response.

Defined XRPD crystal forms improve BCL-2 inhibitor selectivity, stability, solubility, and pharmacokinetics for cancer therapy use.

Mutant COCH mRNA is selectively degraded by antisense oligonucleotides to prevent cytotoxic cochlin dimers while preserving wildtype protein.

A cyclic amine derivative binds advillin to improve actin turnover, accelerate axon extension, and support accurate nerve rejoining.

A bis-HCl tenapanor tablet with acidifier and antioxidant improves dissolution in gastrointestinal fluids while maintaining chemical stability.

Controlled impurity limits, pH, mannitol, and low-temperature lyophilization improve disodium levofolinate stability for oncology use.

A liver-targeted PCSK9 siRNA conjugate improves gene silencing stability and lowers LDL-c and cholesterol for hypercholesterolemia treatment.

Specific aniline substituents improve RORγt inhibition, subtype selectivity, and bioavailability for treating autoimmune disease.

Zinc meloxicam microparticles in multivesicular liposomes improve encapsulation and sustain synovial release while lowering systemic GI toxicity.

Dual DAT modulation and nicAChR partial agonism help reduce alcohol and nicotine reinforcement while limiting abuse liability and withdrawal.

Bifunctional compounds link IRAK binding to cereblon recruitment, driving targeted ubiquitination and degradation for multiple myeloma therapy.

Self-assembled glucosamine derivative nanoparticles improve skin penetration and cellular uptake while reducing cytotoxicity and bypassing oral bioavailability loss.

A modular isoindoline-glutarimide scaffold improves CRBN binding and substrate protein degradation to expand low-toxicity cancer degrader options.

ATS-linked PLGA nanoparticles improve delivery of poorly soluble obesity drugs to liver and adipose tissue while reducing off-target effects.

A fibrin-laminin-hyaluronic acid hydrogel patch targets herniated disc pain while reducing recurrence and avoiding invasive surgery.

Cleavable target-binding moieties guide prodrugs to specific sites, enabling local drug release with higher efficacy and lower toxicity.

Complementary antisense oligomers target processed UBE3A mRNA to sharply lower protein expression in disorders linked to UBE3A overexpression.

A pyridone derivative reduces collagen deposition and inflammation to treat intestinal and non-alcoholic liver fibrosis at low dose.

Small molecules bind ATXN3 pre-mRNA to shift splicing, lower full-length ATXN3, and reduce toxic aggregates linked to SCA3.

Stable crystalline GLP-1R agonist salt synthesis improves solubility, formulation, and Type 2 diabetes treatment efficacy with fewer side effects.

dsRNA targeting C5 mRNA uses RISC-mediated cleavage to sustain inhibition, reduce infusion burden, and limit breakthrough hemolysis.

Remimazolam nasal delivery bypasses first-pass metabolism to speed CNS action while avoiding injections and improving patient compliance.

A sublingual artemether, artesunate, and berberine regimen addresses poor ACT bioavailability and allergy risk in Dengue treatment.