United States Patent 5,719,147: Scope, Claim Map, and US Patent Landscape

What does US Patent 5,719,147 claim in the US?

US 5,719,147 is a broad small-molecule Markush patent covering a family of morpholine-based compounds defined by a core structural formula plus variable substituents (R1, R2, R3, R6, R7, R8, R11, R12, R13), linkage atoms (X, Y), and a terminal alkyl (Z). It also covers salts, compositions, and multiple pharmacological method-of-use claims centered on neurokinin receptors and Substance P biology, with secondary method claims spanning pain/nociception and several other indications.

Claim set (US 5,719,147) at a glance

Claim type	Claims	What is covered
Core Markush compound (structural formula)	1	“A compound” of the structural formula “##STR19##” or pharmaceutically acceptable salt; with extensive definition of substituents
Dependent compound narrowing	2-4, 6-7, 8-13, 14	Subclasses within Claim 1 (e.g., specific R1 sub-sets, simplified substituent sets, specific Z such as C1-4 or CH3, and enumerated R1 cases)
Additional structural-formula embodiments	9-14	Alternative drawings (structural formula I/II/III and further sub-structures) with the same variable definitions
Enumerated single compounds (examples)	15-16	A long list of specific stereochemically defined morpholine compounds; Claim 15 is a large open list, Claim 16 is a specific compound
Formulation	18-19	Pharmaceutical composition with carrier and effective amount
Methods of antagonism / receptor blockade	20-21	Antagonize Substance P or block NK1; antagonize neurokinin A or block NK2
Therapeutic methods (indications)	22-26	Migraine-related pain/nociception; peripheral/diabetic/AIDs/chemo neuropathy and neuralgia; asthma; cystic fibrosis; emesis
Process claim	27	Preparation method: contacting a “formula V” compound with inorganic/organic acid (specific acids) in specified aprotic solvents and temperature range to produce “formula IV”

(Claim text provided by user; the analysis below maps scope and patent coverage implications.)

How broad is Claim 1’s chemical coverage?

Claim 1 is a classic Markush claim with three principal breadth drivers:

1) High combinatorial freedom on R1, R2, R3 and R6-R8 and R11-R13
Each of these substituent positions is independently selected from alkyl/alkenyl/alkynyl/phenyl groups with broad allowable substitution patterns (halo, CN, NO2, CF3, heterocycles, amide/ester/urethane-like fragments, etc.).

2) Heterocycle option stack for R1
R1 includes a defined “heterocycle” branch with many ring systems (benzimidazolyl, benzofuranyl, benzothiophenyl, benzoxazolyl, furanyl, imidazolyl, indolyl, isooxazolyl, isothiazolyl, oxadiazolyl, oxazolyl, pyrazinyl, pyrazolyl, pyridyl, pyrimidyl, pyrrolyl, quinolyl, tetrazolyl, thiadiazolyl, thiazolyl, thienyl, triazolyl, azetidinyl, 1,4-dioxanyl, hexahydroazepinyl, piperazinyl, piperidinyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothienyl). Each heterocycle may itself be further substituted by another list of substituents (alkyl, halo, CF3, OCH3, phenyl; alkoxy; oxo; hydroxy; thioxo; SR; halo; cyano; trifluoromethyl; dialkylamino tether; etc.).

3) Multiple linkage atom choices and variable terminal alkyl (Z)
X can be O, S, SO, or SO2. Y can be either bond or O/S/CO/CH2/CH(R15)/C(R15)(R16). Z is C1-6 alkyl.

Practical read of Claim 1 scope

The patent is not limited to one target compound or series. It covers a family defined by a core morpholine scaffold and a set of allowed substituent chemotypes, with extensive permissible functional-group and heterocycle variety.
Because Claim 1 is structural and Markush-based, it can cover future design-arounds only if they change the core structural formula boundaries enough to remove them from the defined formula drawing space (not merely by swapping a side chain among allowed options).

What does the claim language say about receptor targets and method of use?

Substance P / NK1 blockade

Claim 20: “A method for antagonizing the effect of substance P at its receptor site or for the blockade of neurokinin-1 receptors in a mammal” administering Claim 1 compound.

Neurokinin A / NK2 blockade

Claim 21: “A method for antagonizing the effect of neurokinin A at its receptor site or for the blockade of neurokinin-2 receptors” administering Claim 1 compound.

Pain, migraine, neuropathy, and neuralgia

Claim 22: Treat/prevent pain or nociception attributable to or associated with migraine.
Claim 23: Treat/prevent diabetic neuropathy, peripheral neuropathy, AIDS-related neuropathy, chemotherapy-induced neuropathy, neuralgia.

Asthma, cystic fibrosis, emesis

Claim 24: Treat/prevent asthma, alone or with a neurokinin-2 antagonist or a β2-adrenergic receptor agonist.
Claim 25: Treat cystic fibrosis.
Claim 26: Treat/prevent emesis.

Scope implication: Even if chemical claims were narrowed in prosecution or licensing, method claims are broad in indication framing. The receptor language (substance P, NK1; neurokinin A, NK2) supports cross-market use against any clinical program whose mechanism is argued to match receptor blockade.

How much “explicit compound coverage” is in the claims?

Claim 15 contains a very large list of enumerated morpholine compounds (with stereochemistry and substituent patterns). Claim 16 enumerates an additional specific compound.

What this means for enforcement and freedom-to-operate (FTO)

Claim 15 does not replace Claim 1 breadth. It gives a second pathway: even if an accused product sits near the boundary of the Markush interpretation, it may be argued to fall within one of the enumerated compounds.
The enumerated list also provides evidence of representative embodiments, which can affect claim construction in later disputes (how a term is interpreted by reference to the disclosed examples).

Sub-claim narrowing: where Claim 2-14 pull the reins

Claim 2 limits R1 to C1-6 alkyl substituted with a heterocycle branch constrained to a smaller set of ring types and substitution patterns.

Claim 3 narrows multiple substituent sets:

R2 and R3 ∈ {H, C1-6 alkyl, C2-6 alkenyl, phenyl}
R6-R8 restricted to H and halogens and CF3
R11-R13 restricted to H and halogens and CF3
X = O and Y = O and Z = C1-4 alkyl

Claim 4 further narrows Z to C1-4 alkyl, Claim 5 to Z = CH3.

Claims 6-8 narrow R1 further to specific drawn groups and named substituent types:

Claim 6: “R1 is selected from the group consisting of: ##STR20##”
Claim 7: (1,2,4-triazolo)methyl; (5-oxo-1H,4H-1,2,4-triazolo)methyl
Claim 8: (1,3-imidazolo)methyl; (2-oxo-1,3-imidazolo)methyl

Claims 9-14 attach alternative structural formula drawings (I, II, III, and additional drawings) while incorporating the same defined R-variable definitions “as defined in claim 1.”

Scope implication: The patent is structured with a “core broad Markush claim” (Claim 1) and numerous narrowing dependents and formula embodiments to hedge around interpretation issues. Practically, Claim 1 is the enforcement anchor.

Process claim: what US 5,719,147 covers on manufacture

Claim 27 in functional steps

Claim 27 covers a preparation route to “structural formula IV” by: 1) Contacting a “compound of formula V” (defined with the same R variables as Claim 1)
2) With an inorganic or organic acid from the following list:

toluenesulfonic acid
methanesulfonic acid
sulfuric acid
hydrochloric acid
mixtures thereof
3) In an aprotic solvent chosen from:
toluene
benzene
dimethylformamide (DMF)
tetrahydrofuran (THF)
diethylether
dimethoxyethane
ethyl acetate
mixtures thereof
4) At 0°C to solvent reflux temperature
5) For a “sufficient time” to produce compound of structural formula IV.

Scope implication: The process claim is narrower than compound claims but can still matter in disputes where an accused supplier’s manufacturing conditions match the acid/solvent/temperature windows. Because the list is constrained, a process engineer can sometimes design around, but the claim still provides a legitimate hook where those specific transformation conditions are used.

How to interpret “scope” across chemical and use claims

US 5,719,147 couples a broad structural chemical claim with multiple method claims. That design creates three typical coverage vectors:

1) Chemical coverage: products made, sold, or used that meet Claim 1 structural definitions (and enumerated Claim 15). 2) Use coverage: any method that “administers” the Claim 1 compound for NK1/NK2 receptor antagonism and the listed indications. 3) Process coverage: manufacturing route matching Claim 27.

This architecture is important for licensing strategy: chemical scope drives patent validity and enforceability on composition; method scope drives enforceability in clinical/labeling scenarios; process scope drives supplier-side leverage.

US Patent Landscape: what to map around US 5,719,147 (based on the claim content provided)

A complete “landscape” normally requires bibliographic and citation data (patent family members, priority date, prosecution history, examiner citations, continuations, related patents). That dataset is not included in the prompt, so this analysis focuses on landscape structure implied by the claim scope.

Landscape nodes to search (derived directly from the patent’s claim architecture)

1) NK1 antagonists and NK2 antagonists with morpholine or related scaffold

Anchor keywords from method claims: “substance P”, “neurokinin-1”, “neurokinin-2”, “NK1”, “NK2”.
Anchor therapeutic keywords from method claims: “migraine”, “pain”, “nociception”, “diabetic neuropathy”, “chemotherapy-induced neuropathy”, “asthma”, “cystic fibrosis”, “emesis”.

2) Chemical scaffold cousins (morpholine derivatives with aryl and heterocycle substituents)

Derived from Claim 1 variables: morpholine ring, aryl substitutions with CF3/halo/CN/NO2, heterocycle substituents.
Enumerated examples in Claim 15 include many trifluoromethyl-substituted aryl and heterocycle methyl substituents like triazolo and imidazolo methyl groups.

3) Manufacturing-process similarity

Derived from Claim 27: acid-catalyzed transformation of “formula V” to “formula IV” in listed aprotic solvents and temperature band.

Practical watch-outs for freedom to operate

Because Claim 1 is structurally broad, landscape competitors must confirm whether their compounds truly fall outside the “structural formula” boundaries rather than only outside particular substituent examples.
For method-of-use challenges: if a clinical protocol can plausibly be characterized as NK1/NK2 blockade using a compound meeting Claim 1, method claims become a primary risk point.

Key claim construction levers inside US 5,719,147

These are the typical terms that determine whether a product falls in or out of scope, given the way Claim 1 is written:

Structural-formula dependency

Claim 1 is tied to “the structural formula ##STR19##.” If a product differs in any mandatory part of that drawn core, the compound may fall outside even if substituent options match.

Markush selection dependencies

R1 includes both simple groups and a large heterocycle branch; enforcing parties will argue that a given heterocycle is within the specified set.
Y includes either bond or an atom/bond chain with substitution pattern definitions via R15/R16. For design-around, a competitor can change Y-type connectivity.

X linkage sensitivity

X can be O, S, SO, or SO2. A different linkage changes the chemical identity within the Markush.

Z terminal alkyl range

Z is C1-6. If accused compounds use Z outside C1-6 (or a different terminal group that is not an alkyl), they can fall outside.

Key Takeaways

US 5,719,147 is anchored by a very broad Markush chemical claim (Claim 1) defining a morpholine-based structural family with extensive latitude in substituents and heterocycles, plus salts.
Multiple independent method-of-use claims cover receptor antagonism (Substance P/NK1 and neurokinin A/NK2) and expand into migraine-related pain, neuropathies, asthma, cystic fibrosis, and emesis.
Claim 15 enumerates a large set of specific stereochemical embodiments, strengthening enforcement arguments against products that match particular example structures.
Claim 27 adds manufacturing leverage: acid-catalyzed conversion (specified acids) in specified aprotic solvents within a defined temperature window to produce “structural formula IV.”
Any US competitive landscape review around this patent must search by: NK1/NK2 receptor antagonism method-of-use language, the therapeutic indications listed in method claims, and morpholine-derivative chemotypes consistent with Claim 1 variables.

FAQs

1) Does Claim 1 require the compound to be a morpholine derivative?
Yes. Claim 1 is built on the structural formula “##STR19##,” and the dependent/evidentiary enumerations in Claim 15 are morpholine-based.

2) Are method claims limited to a specific molecule listed in Claim 15?
No. Claims 20-26 administer “the compound of claim 1,” not only enumerated examples.

3) What receptor pathways are explicitly claimed?
Substance P at NK1 (Claim 20) and neurokinin A at NK2 (Claim 21).

4) What does Claim 27 protect in manufacturing?
A specific type of transformation from a “formula V” compound to “structural formula IV” using enumerated acids and aprotic solvents across 0°C to reflux.

5) How do enumerated compounds in Claim 15 affect enforcement?
They provide exact match targets that can reduce reliance on broad Markush interpretation if an accused compound corresponds to one of the listed embodiments.

References

1) US Patent 5,719,147 (claims text provided in prompt).

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0734381	⤷ Start Trial	91069	Luxembourg	⤷ Start Trial
European Patent Office	0734381	⤷ Start Trial	300146	Netherlands	⤷ Start Trial
European Patent Office	0734381	⤷ Start Trial	PA2004002	Lithuania	⤷ Start Trial
European Patent Office	0734381	⤷ Start Trial	SPC/GB04/011	United Kingdom	⤷ Start Trial
European Patent Office	0734381	⤷ Start Trial	CA 2004 00009	Denmark	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 5,719,147

Summary for Patent: 5,719,147