# US 2013/0158036 A1 · N,n-disubstituted aminoalkylbiphenyl antagonists of prostaglandin d2 receptors

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- Number: US 2013/0158036 A1
- Document ID: US20130158036A1
- Status: Published application
- Kind: A1
- Application number: 13/666,703
- Filed: 2012-11-01
- Published: 2013-06-20
- Earliest claimed: 2008-02-01
- Assignees: Panmira Pharmaceuticals, LLC
- Inventors: John Howard HUTCHINSON; Brian Andrew STEARNS; Jill Melissa SCOTT; Yen Pham TRUONG; Jeffrey Roger ROPPE; Nicholas Simon STOCK; Jeannie M. ARRUDA; Thomas Jon SEIDERS; Bowei WANG; Deborah VOLKOTS
- Web page: https://patentgrep.com/patent/US20130158036A1

## CPC

- A61K 31/5375: 1,4-Oxazines, e.g. morpholine
- A61K 31/17: having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine (isoureas, isothioureas A61K31/155; sulfonylureas A61K31/64)
- A61K 31/27: of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
- A61K 31/277: having a ring, e.g. verapamil
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/41: having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K 31/415: 1,2-Diazoles
- A61K 31/4164: 1,3-Diazoles
- A61K 31/4196: 1,2,4-Triazoles
- A61K 31/421: 1,3-Oxazoles, e.g. pemoline, trimethadione
- A61K 31/4412: having oxo groups directly attached to the heterocyclic ring
- A61K 31/47: Quinolines; Isoquinolines
- A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 11/08: Bronchodilators
- A61P 11/14: Antitussive agents
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 27/02: Ophthalmic agents
- A61P 27/16: Otologicals
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- C07C 233/47: having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
- C07C 233/54: having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
- C07C 233/63: having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
- C07C 271/22: to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
- C07C 271/24: with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
- C07C 271/28: to a carbon atom of a non-condensed six-membered aromatic ring
- C07C 271/34: with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C 275/24: containing six-membered aromatic rings
- C07C 275/26: having nitrogen atoms of urea groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C 311/08: having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C 317/50: at least one of the nitrogen atoms being part of any of the groups [IMAGE cpc-sch-C07C-0976.gif], X being a hetero atom, Y being any atom
- C07C 323/63: the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
- C07C 2601/02: with a three-membered ring
- C07C 2601/04: with a four-membered ring
- C07C 2601/08: the ring being saturated
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

## Claims

### Claim at position 1

1-99. (canceled)

### Claim 100

A method for treating a respiratory disease or condition in a mammal comprising administering to the mammal a therapeutically effective amount of an antagonist of DP2, wherein the antagonist is selective for DP2.

### Claim 101 (depends on 100)

The method of claim 100, wherein the respiratory disease or condition is asthma, adult respiratory distress syndrome, allergic asthma, non-allergic asthma, acute severe asthma, chronic asthma, clinical asthma, nocturnal asthma, allergen-induced asthma, aspirin-sensitive asthma, exercise-induced asthma, neutrophilic asthma, isocapnic hyperventilation, child-onset asthma, adult-onset asthma, cough-variant asthma, occupational asthma, steroid-resistant asthma, seasonal asthma, seasonal allergic rhinitis, perennial allergic rhinitis, chronic obstructive pulmonary disease, including chronic bronchitis or emphysema, pulmonary hypertension, interstitial lung fibrosis, airway inflammation, cystic fibrosis, or hypoxia.

### Claim 102 (depends on 100)

The method of claim 100, wherein the respiratory disease or condition is asthma.

### Claim 103 (depends on 100)

The method of claim 100, wherein the respiratory disease or condition is adult respiratory distress syndrome, allergic asthma, non-allergic asthma, acute severe asthma, chronic asthma, clinical asthma, nocturnal asthma, allergen-induced asthma, aspirin-sensitive asthma, exercise-induced asthma, neutrophilic asthma, isocapnic hyperventilation, child-onset asthma, adult-onset asthma, cough-variant asthma, occupational asthma, steroid-resistant asthma, or seasonal asthma.

### Claim 104 (depends on 100)

The method of claim 100, wherein the respiratory disease or condition is rhinitis.

### Claim 105 (depends on 100)

The method of claim 100, wherein the respiratory disease or condition is allergic rhinitis, non-allergic rhinitis, chronic rhinitis, allergen-induced rhinitis, aspirin-sensitive rhinitis, child-onset rhinitis, adult-onset rhinitis, occupational rhinitis, steroid-resistant rhinitis, seasonal rhinitis, perennial rhinitis, rhinosinusitis, or rhinopolyposis.

### Claim 106 (depends on 100)

The method of claim 100, wherein the antagonist of DP2 is administered to the mammal by intravenous injection, oral administration, inhalation, nasal administration, topical administration, ophthalmic administration or otic administration.

### Claim 107 (depends on 100)

The method of claim 100, wherein the method further comprises administering to the mammal a second therapeutic agent selected from 5-lipoxygenase-activating protein inhibitors, 5-lipoxygenase inhibitors, CYSLTR1 antagonists, CYSLTR2 antagonists, BLT1 antagonists, BLT2 antagonists, thromboxane antagonists, DP1 receptor antagonists, DP1 receptor agonists, IP receptor agonists, anti-IgE, chemokine receptor antagonists, IL5 antibody, bronchodilators, theophylline, leukotriene receptor antagonists, leukotriene formation inhibitors, decongestants, antihistamines, mucolytics, corticosteroids, glucocorticoids, anticholinergics, antitussives, analgesics, expectorants, and β-2 agonists

### Claim 108

A method for treating an allergic disease or condition in a mammal comprising administering to the mammal a therapeutically effective amount of an antagonist of DP2, wherein the antagonist is selective for DP2.

### Claim 109 (depends on 108)

The method of claim 108, wherein the allergic disease or condition is allergic rhinitis, asthma, dermatitis, or allergic conjunctivitis.

### Claim 110 (depends on 108)

The method of claim 108, wherein the antagonist of DP2 is administered to the mammal by intravenous injection, oral administration, inhalation, nasal administration, topical administration, ophthalmic administration or otic administration.

### Claim 111 (depends on 108)

The method of claim 108, wherein the method further comprises administering to the mammal a second therapeutic agent selected from 5-lipoxygenase-activating protein inhibitors, 5-lipoxygenase inhibitors, CYSLTR1 antagonists, CYSLTR2 antagonists, BLT1 antagonists, BLT2 antagonists, thromboxane antagonists, DP1 receptor antagonists, DP1 receptor agonists, IP receptor agonists, anti-IgE, chemokine receptor antagonists, IL5 antibody, bronchodilators, theophylline, leukotriene receptor antagonists, leukotriene formation inhibitors, decongestants, antihistamines, mucolytics, corticosteroids, glucocorticoids, anticholinergics, antitussives, analgesics, expectorants, and 13-2 agonists

### Claim 112

A method for treating an inflammatory disease or condition in a mammal comprising administering to the mammal a therapeutically effective amount of an antagonist of DP2, wherein the antagonist is selective for DP2.

### Claim 113 (depends on 112)

The method of claim 112, wherein the inflammatory disease or condition is asthma, rhinitis, chronic obstructive pulmonary disease, pulmonary hypertension, or interstitial lung fibrosis.

### Claim 114 (depends on 112)

The method of claim 112, wherein the antagonist of DP2 is administered to the mammal by intravenous injection, oral administration, inhalation, nasal administration, topical administration, ophthalmic administration or otic administration.

### Claim 115 (depends on 112)

The method of claim 112, wherein the method further comprises administering to the mammal a second therapeutic agent selected from 5-lipoxygenase-activating protein inhibitors, 5-lipoxygenase inhibitors, CYSLTR1 antagonists, CYSLTR2 antagonists, BLT1 antagonists, BLT2 antagonists, thromboxane antagonists, DP1 receptor antagonists, DP1 receptor agonists, IP receptor agonists, anti-IgE, chemokine receptor antagonists, IL5 antibody, bronchodilators, theophylline, leukotriene receptor antagonists, leukotriene formation inhibitors, decongestants, antihistamines, mucolytics, corticosteroids, glucocorticoids, anticholinergics, antitussives, analgesics, expectorants, and β-2 agonists.