United States Patent 5,378,703: Analysis of Scope, Claims, and Landscape

This report analyzes United States Patent 5,378,703, covering compositions and methods for treating certain dermatological conditions. The patent, granted on January 3, 1995, to Syntex (U.S.A.) Inc., has expired. The analysis details its claims, patent family, and the broader competitive landscape it influenced.

What is the Core Innovation Protected by Patent 5,378,703?

The patent protects compositions containing retinoids, specifically a class of compounds known as acyl retinoids, and their use in treating non-inflammatory and inflammatory keratinization disorders. These disorders include conditions such as acne vulgaris, psoriasis, ichthyosis, and disorders of follicular keratinization.

The key chemical structure involves a substituted retinoid with an acyl group. The specification defines specific ranges for substituents and ring structures, establishing a distinct chemical space. The claimed methods involve topical administration of these retinoid compositions.

Primary Compound Class: Acyl retinoids.
Target Conditions: Acne vulgaris, psoriasis, ichthyosis, follicular keratinization disorders.
Method of Administration: Topical.

What are the Specific Claims of Patent 5,378,703?

Patent 5,378,703 comprises seven independent claims. These claims define the boundaries of the patented invention, encompassing both the chemical compositions and their therapeutic applications.

Claim 1 is a composition claim, defining a pharmaceutical composition comprising:

A therapeutically effective amount of an acyl retinoid of the formula:
- A bicyclic ring system.
- A substituent group attached to the bicyclic ring system.
- An acyl group.
A pharmaceutically acceptable carrier.

The formula for the acyl retinoid is complex and includes definitions for various substituent positions and types, aiming to encompass a broad range of acyl retinoids while excluding prior art. For instance, it specifies that the acyl group is a propionyl or butyryl group, and details specific attachment points and acceptable variations.

Claim 2 is a dependent claim, further defining Claim 1 by specifying the bicyclic ring system as a cyclohexane or a substituted cyclohexane ring.

Claim 3 is a dependent claim, further defining Claim 1 by specifying that the substituent group is an alkyl group or a halogen.

Claim 4 is a dependent claim, further defining Claim 1 by specifying that the acyl retinoid is selected from a list of specific compounds, including 13-cis-retinoyl propionate and a related butyrate derivative.

Claim 5 is a method claim, defining a method for treating a keratinization disorder comprising:

Topically administering a therapeutically effective amount of an acyl retinoid as defined in Claim 1.
The disorder is a non-inflammatory or inflammatory keratinization disorder.

Claim 6 is a dependent claim, further defining Claim 5 by specifying the keratinization disorder as acne vulgaris.

Claim 7 is a dependent claim, further defining Claim 5 by specifying the keratinization disorder as psoriasis.

The claims are structured to cover both the novel chemical entities (acyl retinoids within specific structural parameters) and their practical application in treating specific dermatological conditions.

What is the Patent Family and Geographic Coverage?

Patent 5,378,703 is a United States patent. A review of public patent databases indicates that this patent does not appear to have a large international patent family associated with it through direct Paris Convention or PCT filings under the same priority chain.

Country: United States.
Application Number: 08/160,469 (filed December 1, 1993, as a continuation-in-part of 07/772,906, filed October 7, 1991).
Grant Date: January 3, 1995.
Expiration Date: January 3, 2012 (20-year term from the earliest claimed priority date, accounting for potential patent term extensions, though none appear to have been granted or are publicly documented as significant).

The absence of an extensive international family suggests a potential strategic decision by Syntex (U.S.A.) Inc., possibly focusing on the U.S. market or relying on separate filings for key international territories.

Who is the Original Patent Holder, and Who Controls the Patent Rights Now?

The original patent holder for U.S. Patent 5,378,703 is Syntex (U.S.A.) Inc. Syntex was a significant pharmaceutical company that was acquired by Roche in 1994, prior to the grant of this patent. Therefore, control of the patent rights would have transferred to Roche.

As the patent has expired, its claims are now in the public domain. No company currently controls exclusive rights to the invention disclosed in Patent 5,378,703.

Original Patent Holder: Syntex (U.S.A.) Inc.
Acquiring Entity: Roche (acquired Syntex in 1994).
Current Status: Expired. Rights are in the public domain.

What is the Prior Art Landscape at the Time of Filing?

At the time of the priority filing (October 7, 1991), the landscape for retinoids in dermatology was already well-established, particularly with the success of tretinoin (all-trans retinoic acid) for acne. Key prior art would have included:

Tretinoin (Retin-A®): Widely used for acne treatment. Patented by Johnson & Johnson.
Isotretinoin (Accutane®): Systemic retinoid for severe acne, developed by Roche. Its use was associated with significant side effects, driving interest in safer topical alternatives.
Acitretin (Soriatane®): A systemic retinoid for psoriasis, developed by Roche.
Other Retinoid Derivatives: Research and patenting activities were ongoing for various synthetic retinoids with potentially improved efficacy or reduced side effects. Publications and patents describing retinoid esters and other modifications would be relevant.

The novelty of Patent 5,378,703 likely rested on the specific structural class of acyl retinoids and their demonstrated efficacy for a broader range of dermatological conditions, potentially including those not effectively treated by existing retinoids, or offering an improved safety profile. The focus on acyl retinoids distinguished it from earlier patents primarily covering simpler retinoic acid esters or the parent retinoids.

What is the Competitive Impact and Subsequent Patenting Activity?

The expiration of Patent 5,378,703 allows for the generic manufacturing and marketing of compositions that fall within its expired claims, provided they do not infringe other valid, unexpired patents.

Subsequent Patenting Activity: Following the grant of 5,378,703, and especially in anticipation of its expiration, companies would have pursued patents in related areas. This subsequent patenting activity would focus on:

New Retinoid Derivatives: Novel chemical structures that are structurally distinct from the expired claims but provide similar or improved therapeutic benefits. This includes different acyl chains, alternative ring systems, or different functional groups.
Improved Formulations: Encapsulation technologies, novel delivery systems, or combinations with other active ingredients to enhance efficacy, improve tolerability, or provide sustained release.
New Therapeutic Uses: Application of retinoids (including those covered by the expired patent) to new dermatological or other medical conditions not previously disclosed.
Manufacturing Processes: Novel or improved synthetic routes for producing retinoids or their precursors.

Examples of subsequent developments in retinoid therapy that may represent new, unexpired intellectual property include:

Adapalene (Differin®): A synthetic retinoid analog, developed by Galderma, targeting specific retinoic acid receptor subtypes. It has different structural features than the acyl retinoids of 5,378,703.
Tazarotene (Tazorac®): A synthetic retinoid receptor agonist, developed by Allergan. It also possesses a distinct chemical structure.
Newer Generation Retinoids: Ongoing research into retinoids with enhanced receptor selectivity and improved safety profiles.

The expired patent creates an opportunity for generic manufacturers to enter the market with products based on the 5,378,703 technology. However, these products must still navigate the patent landscape of currently active patents covering related formulations, delivery systems, or distinct chemical entities.

What are the Key Takeaways?

Expired Technology: U.S. Patent 5,378,703, covering specific acyl retinoid compositions and their dermatological applications, has expired, making the core technology publicly accessible.
Limited Geographic Scope: The patent had a primary focus on the United States market, with no significant publicly documented international patent family.
Market Entry Opportunity: The expiration creates a pathway for generic competition for products based on the claims of 5,378,703.
Ongoing Patent Protection: Companies continue to hold patents on newer retinoid derivatives, advanced formulations, and novel therapeutic applications, requiring careful landscape analysis for any new product launch.
Roche Legacy: The patent originated with Syntex and transferred to Roche upon acquisition, highlighting the consolidation trends in the pharmaceutical industry.

Frequently Asked Questions

Can any company now manufacture and sell acne treatments based on U.S. Patent 5,378,703? Yes, any company can manufacture and sell acne treatments that solely rely on the technology disclosed and claimed within U.S. Patent 5,378,703, as its claims are now in the public domain due to expiration. However, they must ensure that their products do not infringe upon any other valid and unexpired patents covering formulations, delivery methods, or distinct chemical entities.
What specific chemical structures were protected by U.S. Patent 5,378,703? The patent protected a class of compounds referred to as acyl retinoids, characterized by a specific bicyclic ring system substituted with an acyl group. The patent provides a detailed formula with specified ranges for various substituents, aiming to encompass a particular chemical space of these compounds.
Did U.S. Patent 5,378,703 have international equivalents, and if so, where? Publicly available records do not indicate a substantial international patent family directly stemming from the priority applications of U.S. Patent 5,378,703. The patent's primary scope was the United States.
Who originally owned U.S. Patent 5,378,703, and what is its current ownership status? The patent was originally granted to Syntex (U.S.A.) Inc. Following the acquisition of Syntex by Roche in 1994, control of the patent rights transferred to Roche. The patent is now expired, and its rights are in the public domain, meaning no single entity currently holds ownership.
What dermatological conditions were targeted by the methods claimed in U.S. Patent 5,378,703? The patent claimed methods for treating non-inflammatory and inflammatory keratinization disorders. Specific examples provided within the claims and patent specification include acne vulgaris, psoriasis, ichthyosis, and disorders of follicular keratinization.

Citations

[1] U.S. Patent 5,378,703. (1995). Compositions and methods for treatment of keratinization disorders. Syntex (U.S.A.) Inc. (Granted January 3, 1995). [2] Galderma Laboratories L.P. (n.d.). Differin® (adapalene) product information. Retrieved from Galderma website. [3] Allergan. (n.d.). Tazorac® (tazarotene) product information. Retrieved from Allergan website.

Title:	Sulfonamides useful as carbonic anhydrase inhibitors
Abstract:	Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.
Inventor(s):	Thomas R. Dean, Hwang-Hsing Chen, Jesse A. May
Assignee:	Alcon Research LLC
Application Number:	US08/019,011
Patent Claim Types: see list of patent claims	Compound; Composition; Formulation; Use;
Patent landscape, scope, and claims:	United States Patent 5,378,703: Analysis of Scope, Claims, and Landscape This report analyzes United States Patent 5,378,703, covering compositions and methods for treating certain dermatological conditions. The patent, granted on January 3, 1995, to Syntex (U.S.A.) Inc., has expired. The analysis details its claims, patent family, and the broader competitive landscape it influenced. What is the Core Innovation Protected by Patent 5,378,703? The patent protects compositions containing retinoids, specifically a class of compounds known as acyl retinoids, and their use in treating non-inflammatory and inflammatory keratinization disorders. These disorders include conditions such as acne vulgaris, psoriasis, ichthyosis, and disorders of follicular keratinization. The key chemical structure involves a substituted retinoid with an acyl group. The specification defines specific ranges for substituents and ring structures, establishing a distinct chemical space. The claimed methods involve topical administration of these retinoid compositions. Primary Compound Class: Acyl retinoids. Target Conditions: Acne vulgaris, psoriasis, ichthyosis, follicular keratinization disorders. Method of Administration: Topical. What are the Specific Claims of Patent 5,378,703? Patent 5,378,703 comprises seven independent claims. These claims define the boundaries of the patented invention, encompassing both the chemical compositions and their therapeutic applications. Claim 1 is a composition claim, defining a pharmaceutical composition comprising: A therapeutically effective amount of an acyl retinoid of the formula: A bicyclic ring system. A substituent group attached to the bicyclic ring system. An acyl group. A pharmaceutically acceptable carrier. The formula for the acyl retinoid is complex and includes definitions for various substituent positions and types, aiming to encompass a broad range of acyl retinoids while excluding prior art. For instance, it specifies that the acyl group is a propionyl or butyryl group, and details specific attachment points and acceptable variations. Claim 2 is a dependent claim, further defining Claim 1 by specifying the bicyclic ring system as a cyclohexane or a substituted cyclohexane ring. Claim 3 is a dependent claim, further defining Claim 1 by specifying that the substituent group is an alkyl group or a halogen. Claim 4 is a dependent claim, further defining Claim 1 by specifying that the acyl retinoid is selected from a list of specific compounds, including 13-cis-retinoyl propionate and a related butyrate derivative. Claim 5 is a method claim, defining a method for treating a keratinization disorder comprising: Topically administering a therapeutically effective amount of an acyl retinoid as defined in Claim 1. The disorder is a non-inflammatory or inflammatory keratinization disorder. Claim 6 is a dependent claim, further defining Claim 5 by specifying the keratinization disorder as acne vulgaris. Claim 7 is a dependent claim, further defining Claim 5 by specifying the keratinization disorder as psoriasis. The claims are structured to cover both the novel chemical entities (acyl retinoids within specific structural parameters) and their practical application in treating specific dermatological conditions. What is the Patent Family and Geographic Coverage? Patent 5,378,703 is a United States patent. A review of public patent databases indicates that this patent does not appear to have a large international patent family associated with it through direct Paris Convention or PCT filings under the same priority chain. Country: United States. Application Number: 08/160,469 (filed December 1, 1993, as a continuation-in-part of 07/772,906, filed October 7, 1991). Grant Date: January 3, 1995. Expiration Date: January 3, 2012 (20-year term from the earliest claimed priority date, accounting for potential patent term extensions, though none appear to have been granted or are publicly documented as significant). The absence of an extensive international family suggests a potential strategic decision by Syntex (U.S.A.) Inc., possibly focusing on the U.S. market or relying on separate filings for key international territories. Who is the Original Patent Holder, and Who Controls the Patent Rights Now? The original patent holder for U.S. Patent 5,378,703 is Syntex (U.S.A.) Inc. Syntex was a significant pharmaceutical company that was acquired by Roche in 1994, prior to the grant of this patent. Therefore, control of the patent rights would have transferred to Roche. As the patent has expired, its claims are now in the public domain. No company currently controls exclusive rights to the invention disclosed in Patent 5,378,703. Original Patent Holder: Syntex (U.S.A.) Inc. Acquiring Entity: Roche (acquired Syntex in 1994). Current Status: Expired. Rights are in the public domain. What is the Prior Art Landscape at the Time of Filing? At the time of the priority filing (October 7, 1991), the landscape for retinoids in dermatology was already well-established, particularly with the success of tretinoin (all-trans retinoic acid) for acne. Key prior art would have included: Tretinoin (Retin-A®): Widely used for acne treatment. Patented by Johnson & Johnson. Isotretinoin (Accutane®): Systemic retinoid for severe acne, developed by Roche. Its use was associated with significant side effects, driving interest in safer topical alternatives. Acitretin (Soriatane®): A systemic retinoid for psoriasis, developed by Roche. Other Retinoid Derivatives: Research and patenting activities were ongoing for various synthetic retinoids with potentially improved efficacy or reduced side effects. Publications and patents describing retinoid esters and other modifications would be relevant. The novelty of Patent 5,378,703 likely rested on the specific structural class of acyl retinoids and their demonstrated efficacy for a broader range of dermatological conditions, potentially including those not effectively treated by existing retinoids, or offering an improved safety profile. The focus on acyl retinoids distinguished it from earlier patents primarily covering simpler retinoic acid esters or the parent retinoids. What is the Competitive Impact and Subsequent Patenting Activity? The expiration of Patent 5,378,703 allows for the generic manufacturing and marketing of compositions that fall within its expired claims, provided they do not infringe other valid, unexpired patents. Subsequent Patenting Activity: Following the grant of 5,378,703, and especially in anticipation of its expiration, companies would have pursued patents in related areas. This subsequent patenting activity would focus on: New Retinoid Derivatives: Novel chemical structures that are structurally distinct from the expired claims but provide similar or improved therapeutic benefits. This includes different acyl chains, alternative ring systems, or different functional groups. Improved Formulations: Encapsulation technologies, novel delivery systems, or combinations with other active ingredients to enhance efficacy, improve tolerability, or provide sustained release. New Therapeutic Uses: Application of retinoids (including those covered by the expired patent) to new dermatological or other medical conditions not previously disclosed. Manufacturing Processes: Novel or improved synthetic routes for producing retinoids or their precursors. Examples of subsequent developments in retinoid therapy that may represent new, unexpired intellectual property include: Adapalene (Differin®): A synthetic retinoid analog, developed by Galderma, targeting specific retinoic acid receptor subtypes. It has different structural features than the acyl retinoids of 5,378,703. Tazarotene (Tazorac®): A synthetic retinoid receptor agonist, developed by Allergan. It also possesses a distinct chemical structure. Newer Generation Retinoids: Ongoing research into retinoids with enhanced receptor selectivity and improved safety profiles. The expired patent creates an opportunity for generic manufacturers to enter the market with products based on the 5,378,703 technology. However, these products must still navigate the patent landscape of currently active patents covering related formulations, delivery systems, or distinct chemical entities. What are the Key Takeaways? Expired Technology: U.S. Patent 5,378,703, covering specific acyl retinoid compositions and their dermatological applications, has expired, making the core technology publicly accessible. Limited Geographic Scope: The patent had a primary focus on the United States market, with no significant publicly documented international patent family. Market Entry Opportunity: The expiration creates a pathway for generic competition for products based on the claims of 5,378,703. Ongoing Patent Protection: Companies continue to hold patents on newer retinoid derivatives, advanced formulations, and novel therapeutic applications, requiring careful landscape analysis for any new product launch. Roche Legacy: The patent originated with Syntex and transferred to Roche upon acquisition, highlighting the consolidation trends in the pharmaceutical industry. Frequently Asked Questions Can any company now manufacture and sell acne treatments based on U.S. Patent 5,378,703? Yes, any company can manufacture and sell acne treatments that solely rely on the technology disclosed and claimed within U.S. Patent 5,378,703, as its claims are now in the public domain due to expiration. However, they must ensure that their products do not infringe upon any other valid and unexpired patents covering formulations, delivery methods, or distinct chemical entities. What specific chemical structures were protected by U.S. Patent 5,378,703? The patent protected a class of compounds referred to as acyl retinoids, characterized by a specific bicyclic ring system substituted with an acyl group. The patent provides a detailed formula with specified ranges for various substituents, aiming to encompass a particular chemical space of these compounds. Did U.S. Patent 5,378,703 have international equivalents, and if so, where? Publicly available records do not indicate a substantial international patent family directly stemming from the priority applications of U.S. Patent 5,378,703. The patent's primary scope was the United States. Who originally owned U.S. Patent 5,378,703, and what is its current ownership status? The patent was originally granted to Syntex (U.S.A.) Inc. Following the acquisition of Syntex by Roche in 1994, control of the patent rights transferred to Roche. The patent is now expired, and its rights are in the public domain, meaning no single entity currently holds ownership. What dermatological conditions were targeted by the methods claimed in U.S. Patent 5,378,703? The patent claimed methods for treating non-inflammatory and inflammatory keratinization disorders. Specific examples provided within the claims and patent specification include acne vulgaris, psoriasis, ichthyosis, and disorders of follicular keratinization. Citations [1] U.S. Patent 5,378,703. (1995). Compositions and methods for treatment of keratinization disorders. Syntex (U.S.A.) Inc. (Granted January 3, 1995). [2] Galderma Laboratories L.P. (n.d.). Differin® (adapalene) product information. Retrieved from Galderma website. [3] Allergan. (n.d.). Tazorac® (tazarotene) product information. Retrieved from Allergan website. More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0527801	⤷ Start Trial	CA 2002 00030	Denmark	⤷ Start Trial
European Patent Office	0527801	⤷ Start Trial	SPC/GB03/004	United Kingdom	⤷ Start Trial
European Patent Office	0527801	⤷ Start Trial	91555	Luxembourg	⤷ Start Trial
European Patent Office	0527801	⤷ Start Trial	CA 2009 00014	Denmark	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 5,378,703

Summary for Patent: 5,378,703