KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 1 of 37
`
`
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 1 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 2 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 3 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 4 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 5 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 6 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 7 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 8 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 9 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 10 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 11 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 12 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 13 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 14 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 15 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 16 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 17 of 37
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 18 of 37
`
`
`
`⑲ FRENCH REPUBLIC
`
`
`
`
`
`
`
`NATIONAL INSTITUTE
`OF INDUSTRIAL PROPERTY
`PARIS
`
`
`
`
`
`
`
`⑪ Publication No.:
`
`(for use only when ordering duplicates)
` National registration No:
`
`2 993 457
`12 02095
`
`
`
`
`
` Int Cl8: A 61 K 36/00 (2013.01), A 61 K36/20, A 61 P 3/10
`
`
`
`
`
`
`
`⑫
`
`Date filed: 07/12/20
`Priority:
`
`PATENT APPLICATION
`
`A1
`
`
`
`
`
`
`
`
` Date application was made publicly available:
`01/24/14 Bulletin 14/04
` List of documents cited in the preliminary
`search report: The latter not been drawn up as of
`the application publishing date.
` References to other related national
`documents:
`
`Applicant(s): QUTISHAT LAITH — FR.
`
`Inventor(s): QUTISHAT LAITH.
`
`
`
`
`
`
`
`Owner(s): QUTISHAT LAITH.
`
`Agent(s): QUTISHAT LAITH.
`
` LIQUID PHARMACEUTICAL PREPARATION BASED ON CERTIFIED ORGANIC AGAVE SYRUP.
`
`
`
`There is a growing interest in organic products and low-
`calorie products, especially
`for
`liquid pharmaceutical
`compositions. Most liquid oral forms are made of refined
`sugar syrup, which is not suitable for diabetic patients or for
`those seeking a low-calorie intake or for those wishing to use
`(certified) organic ingredients. This invention is therefore
`based on (certified) organic agave syrup as a vehicle for liquid
`dosage forms, active pharmaceutical ingredients (soluble,
`insoluble and poorly soluble) alone or in combination,
`suspending agents and natural flavorings. These liquid forms
`can be filled in a single dose to avoid adding preservatives to
`the formulations. This invention also provides a simple
`method for preparing the formulations.
`
`
`
`
`
`
`
`
`
`
`
`
`FR 2 993 457 – A1
`
`[barcode]
`
`
`
`1
`
`2993457
`
`5
`
`Description of the invention
`
`Technical field
`to novel liquid pharmaceutical
`This invention relates
`formulations for oral administration. These novel general
`formulations are based on (certified) organic agave syrup with
`a low glycemic index.
`
`State of the art
`Dosage forms consist of active ingredients and excipients.
`Excipients are the major component by weight of a
`preparation. Excipients have various sources: animal (for
`example, gelatin), plant (sugars, cellulose), mineral (silica),
`and synthetic (polysorbate). Most liquid oral forms are made
`of refined sugar syrup which is not suitable for diabetic
`patients or for people seeking a low calorie intake. Some
`sugar substitutes such as aspartame have limited use due to
`phenylketonuria. Other excipients such as thickening agents
`(for example gums), solubilizers/wetting agents, colorants,
`synthetic flavorings and preservatives of some additives are
`not completely safe. Moreover, there is tremendous public
`concern about paraben derivatives.
`
`Natural excipients derived from ordinary agricultural
`practices and their extractions are not well controlled; as a
`result, traces of pesticides, heavy metals, and other pollutants
`may be present in these products.
`
`Synergistic toxicity may occur between active ingredients,
`pesticide residues and/or fertilizers in natural excipients.
`
`10
`
`15
`
`20
`
`25
`
`30
`
`
`
`
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 20 of 37
`
`
`
`2
`
`2993457
`
`As with the toxic impact observed on the environment,
`pollutants could have a synergistic effect. A recent review by
`Mauderly and Samet (1/January 117/number volume 2009 •
`Environmental Health Perspectives).
`
`Solid dosage forms are not suitable for children or for the
`elderly. This is why they are formulated in liquid dosage
`forms, either in a clear syrup or a suspension. Furthermore,
`some drugs such as antitussives are preferably prepared in
`liquid dosage forms. Some drugs are formulated
`in
`suspension, either due to insufficient solubility or to mask an
`unpleasant taste.
`
`Pharmaceutical suspensions and syrups consist of water,
`sugar, suspending agents, wetting agents, co-solvents,
`solubilizers, preservatives, flavorings, acid pH modifiers and
`alkali salts thereof or alkaline pH modifiers and salts thereof,
`sweetening agents, colorants.
`
`Formulations based on natural syrups are not easy to obtain
`and must be heated to obtain homogenized suspensions.
`Therefore, gums should be blended with care to avoid too
`much particle agglomeration.
`
`
`
`
`35
`
`40
`
`45
`
`50
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 21 of 37
`
`
`
`3
`
`2993457
`
`Summary of the invention
`
`The present invention provides pharmaceutical suspensions
`or syrups for oral administration based on syrups with low
`glycemic indexes. They consist mainly of certified organic
`agave syrup alone or in combination with other syrups and of
`an active ingredient used alone or in combination with at least
`one suspending agent, with or without gelling agents, without
`preservatives in the case of single-dose preparations and with
`preservatives when in multiple doses, and of natural
`flavorings. Natural sweeteners such as Rebaudioside and
`steviol glycoside may be added as well as natural colorants.
`
`These formulations are based on syrups with a low glycemic
`index such as organic agave syrup and use as few additives as
`possible, thus avoiding the use of artificial sweeteners and of
`any colorants. These formulas are suitable for people with
`diabetes and those seeking a low calorie intake. Most of the
`dosage forms used do not take into account the low toxicity
`of the excipients and the cumulative effect of the toxins
`present in the excipients and the potential interactions with
`drugs. This can be prevented by using organically-sourced
`products.
`
`that may be
`ingredients
`The active pharmaceutical
`incorporated must be compatible with the other essential
`ingredients and compatible in combination with other active
`ingredients or added compounds and may be present in
`concentrations ranging from about 0.01% to about 90%,
`preferably from about 0.1% to about 75%, more preferably
`from about 1.0% to about 50% and more preferably from
`about 1.0% to about 25%.
`
`55
`
`60
`
`65
`
`70
`
`75
`
`80
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 22 of 37
`
`
`
`4
`
`2993457
`
`85
`
`90
`
`95
`
`100
`
`105
`
`The active ingredients may be chosen from, but are not
`limited
`to,
`the following: bronchodilators, anorectics,
`antihistamines, dietary supplements (vitamins, minerals, fatty
`acids, amino acids and analogs thereof), laxatives, analgesics,
`antacids, H2
`receptor
`antagonists,
`antidiarrheals,
`decongestants, antitussives, antinauseants, antimicrobials,
`antifungals, antivirals, expectorants, anti-inflammatory
`agents, antipyretics, their pharmaceutically-acceptable salts
`and mixtures thereof.
`
`“Pharmaceutically-acceptable salts” refers to salts prepared
`from non-toxic, pharmaceutically-acceptable bases including,
`but not limited to, inorganic and organic bases. Salts derived
`from inorganic bases include sodium, potassium, lithium,
`ammonia, calcium, magnesium, iron, zinc, manganese,
`aluminum, ferric salts, manganics and analogs thereof. Salts
`derived from organic bases include primary, secondary,
`tertiary and quaternary amine salts comprising naturally-
`occurring substituted amines, cyclic amines and basic ion
`exchange resins, such as triethylamine, tripropylamine, 2-
`dimethylaminoethanol,
`2-diethylaminoethanol,
`lysine,
`arginine, histidine, caffeine, procaine, N-ethylpiperidine,
`hydrabamine,
`choline,
`betaine,
`ethylenediamine,
`glucosamine, N-methylglycamine,
`theobromine, purines,
`piperazine, piperidine, polyamine resins and analogs thereof.
`
`Examples of decongestants useful in the compositions of the
`present
`invention
`include
`pseudoephedrine,
`phenylpropanolamine, phenylephrine and ephedrine, their
`pharmaceutically-acceptable salts, and mixtures thereof.
`
`110
`
`
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 23 of 37
`
`
`
`5
`
`2993457
`
`115
`
`120
`
`125
`
`130
`
`Examples of antitussives useful in the compositions of the
`present invention include dextromethorphan, chlophedianol,
`carbetapentane, caramiphen, noscapine, diphenhydramine,
`codeine,
`hydrocodone,
`hydromorphone,
`their
`pharmaceutically-acceptable salts, and mixtures thereof.
`
`Examples of expectorants (also known as mucolytic agents)
`useful in the present invention include: guaifenesin, terpin
`hydrate, ammonium chloride, N-acetyl cysteine, and
`ambroxol,
`their pharmaceutically-acceptable salts, and
`mixtures thereof.
`
`Examples of analgesics useful in the present invention
`include: morphine, codeine, meperidine, pentazocine,
`propoxyphene, paracetamol, allopurinol, acetylsalicylic acid,
`choline
`salicylate,
`ketoprofen, magnesium
`silicate,
`fenoprofen, ibuprofen, flurbiprofen, indomethacin, naproxen,
`etc., and their pharmaceutically-acceptable salts and mixtures
`thereof.
`
`Examples of antihistamines useful in the present invention
`include: brompheniramine, chlorpheniramine, clemastine,
`dexchlorpheniramine,
`diphenhydramine,
`doxylamine,
`promethazine, terfenadine, triprolidine and many others, and
`their pharmaceutically-acceptable salts and mixtures thereof.
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 24 of 37
`
`
`
`6
`
`2993457
`
`135
`
`140
`
`145
`
`150
`
`155
`
`Analgesics, antihistamines, decongestants, expectorants and
`antitussives and their acceptable dosage ranges are described
`in US Patent No. 4783465, Sunshine et al., granted on
`November 8, 1988, and in US Patent No. 4619934 Sunshine
`et al., which are included in the references hereto.
`
`Examples of gastrointestinal agents that may be used in the
`present invention include anticholinergics such as atropine,
`clidinium, and dicyclomine; antacids, including aluminum
`hydroxide, bismuth salicylate, calcium carbonate, and
`magaldrate; H2 receptor antagonists, including: cimetidine,
`famotidine, nizatidine, and ranitidine; laxatives, including:
`phenolphthalein and casanthrol; and antidiarrheals,
`in
`particular: diphenoxylate and loperamide.
`
`Other examples of appropriate analgesics, decongestants,
`antitussives, expectorants and antihistamines as well as
`bronchodilators,
`anorectics,
`laxatives,
`antiemetics,
`antimicrobials,
`antibacterials,
`antifungals,
`anti-
`inflammatories, antivirals, antipyretics, dietary supplements,
`anticholinergics,
`antacids, H2
`receptor
`antagonists,
`antidiarrheals, and various other gastrointestinal compounds
`and
`their acceptable dosage ranges are described
`in
`Remington’s Pharmaceutical Sciences, pp. 734-789, 791-799,
`861-868, 907-945, 875-888, 1002-1034, 1098-1121,1124-
`1131, 1173-1224, 1232-1241 (Alfonso R. Gennaro, editor)
`(18th ed. 1990), included in the references hereto.
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 25 of 37
`
`
`
`7
`
`2993457
`
`160
`
`165
`
`170
`
`175
`
`180
`
`185
`
`Natural syrups come from organic farming and from agave
`syrup alone or combined with other syrups such as, but not
`limited to, maple syrup, orbitol [sic: sorbitol], xylitol, corn
`syrup and erythritol.
`
`The suspending agent may be natural or natural organic, for
`example, but not limited to: guar gum, locust bean gum,
`tragacanth gum, xanthan gum, colloidal silica dioxide,
`hypromellose, hydroxypropyl
`cellulose, hydroxyethyl
`cellulose, hydroxypropyl methyl cellulose, bentonite,
`propylene glycol alginate, sodium alginate, povidone,
`magnesium and aluminum silicate, kaolin, gelatin, inulin and
`mixtures thereof.
`
`In single-dose form, these syrups are formulated with or
`without preservatives. If they are filled in glass or plastic
`phials in multi-dose form, preservatives will be used, for
`example, but not limited to: benzoic acid, sodium benzoate,
`potassium sorbate, sorbic acid, domiphen bromide, sodium
`propionate, propylene glycol, ethanol and mixtures thereof.
`
`The pH regulating agent is chosen from the group of
`anhydrous citric acid, citric acid monohydrate, lactic acid,
`tartaric acid, fumaric acid, malic acid, their corresponding
`alkali salts and mixtures thereof.
`
`The flavorings can be natural from floral waters, or natural
`flavorings derived from natural extracts. If colorants are used,
`they will be natural.
`
`Wetting agents chosen from the group may be glycerol,
`propylene glycol, liquid polyethylene glycol, sorbitol and
`mixtures thereof.
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 26 of 37
`
`
`
`8
`
`2993457
`
`190
`
`195
`
`the preparation of
`for
`is a general method
`This
`suspensions/solutions at room temperature with easy handling
`of xanthan gum and agar-agar in the formulation. Agar-agar
`and xanthan gum are mixed with glycerin in a separate
`container and even mixed with a spatula to provide Solution
`A. The active pharmaceutical ingredient(s) is (are) dispersed
`or dissolved in agave syrup to make Solution B. Solution A is
`added to Solution B. Water is added and mixed in. Then the
`other ingredients are added and mixed in and then placed in 5
`ml or 100 ml vials.
`
`Example 1
`
`%w/v
`Ingredients
`2.5 g
`Paracetamol
`45 g
`Certified Agave Syrup
`0.4 g
`Xanthan gum
`0.2 g
`Certified agar
`5 g
`Glycerin
`0.5 g
`Sodium Citrate
`0.4 g
`Anhydrous Citric Acid
`Natural Strawberry Flavoring 0.01 g
`Purified water
`Up to 100 ml
`
`
`
`200
`
`Preparation method
`
`The xanthan gum and the agar-agar are mixed with glycerin
`to obtain Solution A. The paracetamol is suspended in syrup
`to obtain Solution B. Solution A is included in Solution B and
`mixed well. The water is topped up to 100 ml and mixed in.
`Then the other ingredients are added and mixed in and then
`placed in 5 ml or 100 ml vials.
`
`205
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 27 of 37
`
`
`
`9
`
`2993457
`
`Example 2
`
`Ingredients
`Diphenhydramine hydrochloride
`Certified Agave syrup
`Glycerin
`Sodium Citrate
`Anhydrous Citric Acid
`Natural Flavoring-Lemon
`Purified water
`
`%w/v
`0.200 g
`45 g
`10 g
`0.75 g
`0.4 g
`0.01 g
`Up to 100 ml
`
`210
`
`The diphenhydramine hydrochloride is dissolved in the syrup.
`The water is topped up to 100 ml and mixed in, then the other
`ingredients are added and mixed in and then placed in 5 ml or
`100 ml vials.
`
`Example 3
`
`Ingredients
`Ibuprofen
`Certified Agave Syrup
`Xanthan gum
`Certified agar-agar
`
`
`
`
`
`%w/v
`4.0 g
`45 g
`0.4 g
`0.2 g
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 28 of 37
`
`
`
`10
`
`2993457
`
`Glycerin
`Sodium Citrate
`Anhydrous Citric Acid
`Natural Strawberry Flavoring
`Purified water
`
`5 g
`0.70 g
`0.6 g
`0.01 g
`Up to 100 ml
`
`215
`
`The xanthan gum and the agar-agar are mixed with glycerin
`to make Solution A. The ibuprofen is suspended in the agave
`syrup to make Solution B. Solutions A are added to B. Then,
`the water is added and mixed in. Then, the other ingredients
`are added and mixed in and then placed in 5 ml or 100 ml
`vials.
`
`220
`
`Example 4
`
`Ingredients
`Ibuprofen
`Paracetamol
`Certified Agave Syrup
`Xanthan gum
`Certified Agar-Agar
`Glycerin
`Sodium Citrate
`Anhydrous Citric Acid
`Natural Strawberry Flavoring
`Purified water
`
`%w/v
`2.0 g
`3.25
`35 g
`0.4 g
`0.2 g
`5 g
`0.70 g
`0.6 g
`0.01 g
`Up to 100 ml
`
`Agar-agar and xanthan gum are mixed with glycerin to obtain
`Solution A. The ibuprofen and the paracetamol are suspended
`in the agave syrup to make Solution B. Then, the other
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 29 of 37
`
`
`
`11
`
`2993457
`
`225
`
`ingredients are added and mixed in and then placed in 5 ml or
`100 ml vials.
`
`230
`
`235
`
`A 50-liter batch of a liquid suspension in accordance with the
`invention in this application can be prepared as follows. The
`resulting preparation contains 100 mg of ibuprofen and 162.5
`mg of paracetamol per 5 ml.
`
`In a 10 L stainless-steel container, 2.75 kg of glycerin is
`weighed and 110 g of agar-agar and 220 g of xanthan gum are
`added and mixed in with a spatula. A homogenized
`suspension is easily obtained to make Solution A.
`
`19.25 kg of agave syrup is placed in the 100 L mixer and 1.1
`kg of ibuprofen is added and 1.788 kg of paracetamol is
`added. The ingredients are mixed well until the mixture is
`thoroughly homogenized, Solution A is added. Then, 29
`litters [sic: liters] of purified water is added and mixed, then
`the rest of the ingredients are added. Then put into 5 ml vials.
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 30 of 37
`
`
`
`2993457
`
`5
`
`10
`
`15
`
`20
`
`25
`
`30
`
`Claims
`
`1- The claimed invention consists of [a] novel general
`formulation of an aqueous liquid pharmaceutical composition
`for oral administration based on a suspension or solution of
`agave syrup. The agave syrup with a concentration ranging
`from 1% to 50%, but more generally used at 45%.
`
`2-The novel general formulation of claim 1, which may
`contain other certified organic syrups in combination chosen
`from the list, for example, but not limited to, marple [sic:
`maple] syrup, sorbitol, xylitol, corn syrup, erythritol,
`
`3-The novel general formulation of claim 1, which contains
`either natural or organic suspending agents, for example, but
`not limited to: guar gum, locust bean gum, tragacanth gum,
`xanthan gum, colloidal silica dioxide, hypromellose,
`hydroxypropyl
`cellulose,
`hydroxyethyl
`cellulose,
`hydroxypropyl methyl cellulose, bentonite, propylene glycol,
`alginate,
`sodium alginate, povidone, aluminum and
`magnesium silicates, kaolin, gelatin, inulin and mixtures
`thereof.
`
`4-The novel general formulation of claim 1, which contains
`The [sic] active ingredients may be chosen among, without
`being limited to, the following compounds: bronchodilators,
`anorectics, antihistamines, dietary supplements (vitamins,
`minerals, fatty acids, amino acids and analogs thereof),
`laxatives, analgesics, antacids, H2 receptor antagonists,
`antidiarrheals, decongestants, antitussives, antinauseants,
`antimicrobials, antifungals, antivirals, expectorants, anti-
`inflammatory agents, antipyretics, their pharmaceutically-
`acceptable salts and mixtures thereof.
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 31 of 37
`
`
`
`2993457
`
`35
`
`40
`
`45
`
`50
`
`55
`
`“Pharmaceutically-acceptable salts” refers to salts prepared
`from non-toxic, pharmaceutically-acceptable bases including,
`but not limited to, inorganic and organic bases. Salts derived
`from inorganic bases include sodium, potassium, lithium,
`ammonia, calcium, magnesium, iron, zinc, manganese,
`aluminum, ferric salts, manganics and analogs thereof. Salts
`derived from organic bases include primary, secondary,
`tertiary and quaternary amine salts comprising naturally-
`occurring substituted amines, cyclic amines and basic ion
`exchange resins, such as triethylamine, tripropylamine, 2-
`dimethylaminoethanol,
`2-diethylaminoethanol,
`lysine,
`arginine, histidine, caffeine, procaine, N-ethylpiperidine,
`hydrabamine,
`choline,
`betaine,
`ethylenediamine,
`glucosamine, N-methylglycamine,
`theobromine, purines,
`piperazine, piperidine, polyamine resins and analogs thereof.
`
`Examples of decongestants useful in the compositions of the
`present
`invention
`include
`pseudoephedrine,
`phenylpropanolamine, phenylephrine and ephedrine, their
`pharmaceutically-acceptable salts, and mixtures thereof.
`
`Examples of antitussives useful in the compositions of the
`present invention include dextromethorphan, chlophedianol,
`carbetapentane, caramiphen, noscapine, diphenhydramine,
`codeine,
`hydrocodone,
`hydromorphone,
`their
`pharmaceutically[-acceptable] salts
`
`
`
`
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 32 of 37
`
`
`
`2993457
`
`60
`
`65
`
`70
`
`75
`
`80
`
`85
`
`Examples of expectorants (also known as mucolytic agents)
`useful in the present invention include: guaifenesin, terpin
`hydrate, ammonium chloride, N-acetyl cysteine, and
`ambroxol,
`their pharmaceutically-acceptable salts, and
`mixtures thereof.
`
`Examples of analgesics useful in the present invention
`include: morphine, codeine, meperidine, pentazocine,
`propoxyphene, paracetamol, allopurinol, acetylsalicylic acid,
`choline
`salicylate,
`ketoprofen, magnesium
`silicate,
`fenoprofen, ibuprofen, flurbiprofen, indomethacin, naproxen,
`etc., and their pharmaceutically-acceptable salts and mixtures
`thereof.
`
`Examples of antihistamines useful in the present invention
`include: brompheniramine, chlorpheniramine, clemastine,
`dexchlorpheniramine,
`diphenhydramine,
`doxylamine,
`promethazine, terfenadine, triprolidine and many others, and
`their pharmaceutically-acceptable salts and mixtures thereof.
`
`Analgesics, antihistamines, decongestants, expectorants and
`antitussives and their acceptable dosage ranges are described
`in US Patent No. 4783465, Sunshine et al., granted on
`November 8, 1988, and in US Patent No. 4619934 Sunshine
`et al., which are included in the references hereto.
`
`Examples of gastrointestinal agents that may be used in the
`present invention include anticholinergics such as atropine,
`clidinium, and dicyclomine; antacids, including aluminum
`hydroxide, bismuth salicylate, calcium carbonate, and
`magaldrate; H2 receptor antagonists, including: cimetidine,
`famotidine, nizatidine, and ranitidine; laxatives, including:
`phenolphthalein and casanthrol; and antidiarrheals,
`in
`particular: diphenoxylate and loperamide.
`
` KINDERFARMS Ex. 1042
` KINDERFARMS LLC. v. GENEXA INC.
` PGR2023-00051
`
`
`Page 33 of 37
`
`
`
`2993457
`
`90
`
`95
`
`100
`
`Other examples of appropriate analgesics, decongestants,
`antitussives, expectorants and antihistamines as well as
`bronchodilators,
`anorectics,
`laxatives,
`antiemetics,
`antimicrobials,
`antibacterials,
`antifungals,
`anti-
`inflammatories, antivirals, antipyretics, dietary supplements,
`anticholinergics,
`antacids, H2
`receptor
`antagonists,
`antidiarrheals, and various other gastrointestinal compounds
`and
`their acceptable dosage ranges are described
`in
`Remington’s Pharmaceutical Sciences, pp. 734-789, 791-799,
`861-868, 907-945, 875-888, 1002-1034, 1098-1121, 1124-
`1131, 1173-1224, 1232-1241 (Alfonso R. Gennaro, editor)
`(18th ed. 1990), included in the references hereto.
`
`
`
` KINDERFARMS Ex. 1042
`
Accessing this document will incur an additional charge of $.
After purchase, you can access this document again without charge.
Accept $ Charge
Still Working On It
This document is taking longer than usual to download. This can happen if we need to contact the court directly to obtain the document and their servers are running slowly.
Give it another minute or two to complete, and then try the refresh button.
A few More Minutes ... Still Working
It can take up to 5 minutes for us to download a document if the court servers are running slowly.
Thank you for your continued patience.
This document could not be displayed.
We could not find this document within its docket. Please go back to the docket page and check the link. If that does not work, go back to the docket and refresh it to pull the newest information.
Your account does not support viewing this document.
You need a Paid Account to view this document. Click here to change your account type.
Your account does not support viewing this document.
Set your membership
status to view this document.
With a Docket Alarm membership, you'll
get a whole lot more, including:
- Up-to-date information for this case.
- Email alerts whenever there is an update.
- Full text search for other cases.
- Get email alerts whenever a new case matches your search.
One Moment Please
The filing “” is large (MB) and is being downloaded.
Please refresh this page in a few minutes to see if the filing has been downloaded. The filing will also be emailed to you when the download completes.
Your document is on its way!
If you do not receive the document in five minutes, contact support at support@docketalarm.com.
Sealed Document
We are unable to display this document, it may be under a court ordered seal.
If you have proper credentials to access the file, you may proceed directly to the court's system using your government issued username and password.
Access Government Site
