UnfoldIPThemes

Company patents

Arena Pharmaceuticals, Inc.

Arena Pharmaceuticals, Inc. demonstrates a focused patent strategy, with 85.5% of its portfolio in Pharmaceutical Preparations, yet surprisingly, its patenting activity in this core area has seen a significant decline of 64.7% so far in 2026 compared to 2025. While most categories show a downward trend in 2026, the 100.0% year-over-year growth in Acyclic / Carbocyclic Compounds in 2025 (6 patents) suggests a brief, but now shifting, priority in that specific chemical area.

Patent Trend by Technology Area

Yearly patent publications since 2023

Product themes

Product-level themes inferred from filings since 2023, with category chips showing where each theme appears. Select a theme to filter the patents below.

69 US filings (since 2023) · 6 categories · 7 themes

Targeted Small Molecule Therapeutics

Design and synthesis of acyclic or carbocyclic organic compounds that selectively modulate specific biological targets or pathways for the treatment of diseases.

Pharmaceutical PreparationsHeterocyclic Compounds (Pharma)Acyclic / Carbocyclic Compounds
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51since 2023
-6.7%YoY
Targeted Drug Formulation Delivery

Delivery systems specifically engineered to administer advanced drug formulations (e.g., microparticles, biologics, extended-release systems) to achieve precise targeting, controlled release kinetics, or enhanced therapeutic efficacy within the body.

Pharmaceutical Preparations
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15since 2023
+50.0%YoY
Recombinant Protein & Peptide Therapeutics

Development and application of therapeutic proteins or peptides produced through recombinant DNA technology, including fusion proteins and modified growth factors.

Therapeutic Activity (Pharma)
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8since 2023
+50.0%YoY
API Solid Form Engineeringfiltered

Techniques for preparing and characterizing specific solid forms, such as crystal forms, salts, co-crystals, or amorphous forms, of active pharmaceutical ingredients to optimize properties like stability, solubility, and bioavailability.

Heterocyclic Compounds (Pharma)General Organic Chemistry Methods
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4since 2023
+100.0%YoY
Drug Candidate Synthesis

Methods and intermediates for preparing complex organic molecules intended as active pharmaceutical ingredients (APIs), often involving multi-step synthesis and optimization of reaction pathways.

General Organic Chemistry Methods
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2since 2023
new
Advanced Cell & Gene Therapies

Development of therapeutic approaches involving the genetic modification of cells (e.g., T cells, stem cells, macrophages) or the use of viral/non-viral vectors to deliver genetic material for disease treatment.

Pharmaceutical Preparations
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2since 2023
0.0%YoY
Antibody Engineering & Therapeutics

Design and modification of antibodies or antibody-derived fragments for targeted therapeutic intervention, including bispecific formats, Fc region modifications, and activatable constructs.

Pharmaceutical PreparationsTherapeutic Activity (Pharma)
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1since 2023
n/a

Patents

Showing 1-6 of 6

API Solid Form Engineering
Page 1 of 1
US 20250346560 A1APPLICATION
C07D209/94

CRYSTALLINE L-ARGININE SALT OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3, 4-TETRAHYDROCYCLO-PENTA [B]INDOL-3-YL)ACETIC ACID(COMPOUND1) FOR USE IN SIPI RECEPTOR-ASSOCIATED DISORDERS

Filed:2025-07-17Pub:2025-11-13
Applicant:Arena Pharmaceuticals, Inc.

The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P 1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

US 12378198 B2GRANTED
C07D209/70

Crystalline l-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(compound1) for use in SIPI receptor-associated disorders

Filed:2023-12-18Pub:2025-08-05
Applicant:Arena Pharmaceuticals, Inc.

The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P 1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

US 20240140911 A1APPLICATION
C07D209/94

CRYSTALLINE L-ARGININE SALT OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3, 4-TETRAHYDROCYCLO-PENTA [B]INDOL-3-YL)ACETIC ACID(COMPOUND1) FOR USE IN SIPI RECEPTOR-ASSOCIATED DISORDERS

Filed:2023-12-18Pub:2024-05-02
Applicant:Arena Pharmaceuticals, Inc.

The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P 1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

US 11560369 B2GRANTED
C07D403/04

Crystalline forms and processes for the preparation of cannabinoid receptor modulators

Filed:2021-03-16Pub:2023-01-24
Applicant:Arena Pharmaceuticals, Inc.

The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB 2 receptor and are therefore useful in the treatment of CB 2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.

US 20210380560 A1APPLICATION
C07D403/04

CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF CANNABINOID RECEPTOR MODULATORS

Filed:2021-03-16Pub:2021-12-09
Applicant:Arena Pharmaceuticals, Inc.

The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB 2 receptor and are therefore useful in the treatment of CB 2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.

US 10981895 B2GRANTED
C07D403/04

Crystalline forms and processes for the preparation of cannabinoid receptor modulators

Filed:2018-12-10Pub:2021-04-20
Applicant:Arena Pharmaceuticals, Inc.

The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB 2 receptor and are therefore useful in the treatment of CB 2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.

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