# US 2008/0188443 A1 · Tricyclic Compound, Compositions, and Methods

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- Number: US 2008/0188443 A1
- Document ID: US20080188443A1
- Status: Published application
- Kind: A1
- Application number: 12/023,362
- Filed: 2008-01-31
- Published: 2008-08-07
- Earliest claimed: 2007-02-02
- Assignees: Pfizer Inc.
- Inventors: Hengmiao (Henry) Cheng; Rajesh Devraj; Gary A. DeCresenzo; Xiao Hu; Kevin D. Jerome; Mark Obukowicz; Lisa Olson; Paul V. Rucker; Ronald Keith Webber
- Web page: https://patentgrep.com/patent/US20080188443A1

## CPC

- C07D 213/89: with hetero atoms directly attached to the ring nitrogen atom
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 3/14: for calcium homeostasis (vitamin D A61P3/02; parathyroid hormones A61P5/18; calcitonin A61P5/22; osteoporosis A61P19/10; bone metastasis A61P35/04)
- A61P 7/06: Antianaemics
- A61P 7/10: Antioedematous agents; Diuretics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 11/16: Central respiratory analeptics
- A61P 13/12: of the kidneys
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 17/08: Antiseborrheics
- A61P 17/14: for baldness or alopecia
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/06: Antigout agents, e.g. antihyperuricemic or uricosuric agents
- A61P 19/10: for osteoporosis
- A61P 21/04: for myasthenia gravis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/02: Ophthalmic agents
- A61P 27/04: Artificial tears; Irrigation solutions
- A61P 27/14: Decongestants or antiallergics
- A61P 27/16: Otologicals
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/02: specific for leukemia
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 213/72: Nitrogen atoms (nitro radicals C07D213/61)
- C07F 9/58: Pyridine rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)

## Abstract

The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.

## Claims

### Claim 1

A compound of Formula I:
wherein R1 is —P(O)(OH)2;
or salt thereof.

### Claim 2 (depends on 1)

The compound of claim 1, wherein the compound is:
or salt thereof.

### Claim 3 (depends on 1)

The compound of claim 1, wherein the compound is:

### Claim 4 (depends on 1)

The calcium salt of the compound of claim 1.

### Claim 5 (depends on 1)

The sodium salt of the compound of claim 1.

### Claim 6 (depends on 1)

A composition comprising the compound of claim 1 or salt thereof and a carrier.

### Claim 7 (depends on 1)

A method comprising contacting a glucocorticoid receptor with the compound of claim 1 or salt thereof.

### Claim 8

A method of treating a condition mediated by glucocorticoid receptor activity in a subject comprising administering to the subject a compound of Formula I:
wherein R1 is —P(O)(OH)2;
or salt thereof.

### Claim 9 (depends on 8)

The method of claim 8, wherein the condition is an inflammation related condition.

### Claim 10 (depends on 8)

The method of claim 8, wherein the condition is asthma, dermatitis, inflammatory bowel disease, Alzheimer's disease, psychotic major depression, neuropathy, transplant rejection, multiple sclerosis, chronic uveitis, or chronic obstructive pulmonary disease.

### Claim 11 (depends on 8)

The method of claim 8, wherein the condition is rheumatoid arthritis.

### Claim 12 (depends on 8)

The method of claim 8, wherein the condition is dermatitis.

### Claim 13 (depends on 8)

The method of claim 8, wherein the condition is asthma.

### Claim 14 (depends on 8)

The method of claim 8, wherein the condition is Alzheimer's disease.

### Claim 15 (depends on 8)

The method of claim 8, wherein the condition is inflammatory bowel disease.

### Claim 16 (depends on 1)

A method of mitigating side effects associated with glucocorticoid receptor modulation, comprising administering a compound of claim 1 to a subject.