# US 12,006,307 B2 · Pharmaceutical compounds for treatment of medical disorders

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- Number: US 12,006,307 B2
- Document ID: US12006307B2
- Status: Granted
- Kind: B2
- Application number: 17/872,104
- Filed: 2022-07-25
- Published: 2023-03-09
- Granted: 2024-06-11
- Earliest claimed: 2017-03-01
- Assignees: Achillion Pharmaceuticals, Inc.
- Applicants: Achillion Pharmaceuticals, Inc.
- Inventors: Jason Allan Wiles; Avinash S. Phadke; Milind Deshpande; Atul Agarwal; Dawei Chen; Venkat Rao Gadhachanda; Akihiro Hashimoto; Godwin Pais; Qiuping Wang; Xiangzhu Wang; Joel Charles Barrish; William Greenlee; Kyle J. Eastman
- Web page: https://patentgrep.com/patent/US12006307B2

## CPC

- C07D 401/14: containing three or more hetero rings
- C07D 403/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 403/10: linked by a carbon chain containing aromatic rings
- C07D 403/14: containing three or more hetero rings
- C07D 405/14: containing three or more hetero rings
- C07D 409/14: containing three or more hetero rings
- C07D 417/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D 487/04: Ortho-condensed systems
- C07D 493/04: Ortho-condensed systems
- C07D 495/04: Ortho-condensed systems
- C07D 513/04: Ortho-condensed systems
- C07F 9/65583: {each of the hetero rings containing nitrogen as ring hetero atom}
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, and Formula IV or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

## Claims

### Claim 1

A compound of structure:
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

### Claim 3 (depends on 1)

A method of treating a disorder mediated by complement Factor D, the method comprising administering to a subject in need thereof an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 3)

The method of claim 3, wherein the subject is a human.

### Claim 5 (depends on 3)

The method of claim 3, wherein the disorder is selected from acute respiratory distress syndrome, age-related macular degeneration, arthritis, asthma, Alzheimer's dementia, amyotrophic lateral sclerosis, antibody-mediated transplant rejection, antineutrophil cytoplasm antibody-associated vasculitis, antiphospholipid syndrome, atypical or typical hemolytic uremic syndrome, a cardiovascular disease, cold agglutinin disease, chronic obstructive pulmonary disease, cirrhosis, Crohn's disease, C3 glomerulonephritis, diabetic retinopathy, dense deposit disease, dermatomyositis, dermatitis, epidermolysis bullosa acquisita, fatty liver, focal segmental glomerulosclerosis, geographic atrophy, glomerulonephritis, graft versus host disease, Guillain Barre syndrome, hemolytic anemia, hidradenitis suppurativa, IgA nephropathy, ischemia/reperfusion injury, liver failure, liver inflammation, lupus nephritis, membrane proliferative glomerulonephritis, multifocal motor neuropathy, multiple sclerosis, myasthenia gravis, neuromyelitis optica, nonalcoholic steatohepatitis (NASH), an ophthalmic disease, pancreatitis, paroxysmal nocturnal hemoglobinuria, pemphigoid, pemphigus vulgaris, pre-eclampsia, reduced glomerular filtration rate, a renovascular disorder, a respiratory disease, retinal detachment, rheumatoid arthritis, scleroderma, sepsis, shiga toxin E. coli-related hemolytic uremic syndrome, spinal cord injury, sickle cell disease, traumatic brain injury, and ulcerative colitis.

### Claim 6 (depends on 5)

The method of claim 5, wherein the disorder is age-related macular degeneration, C3 glomerulonephritis, dense deposit disease, geographic atrophy, IgA nephropathy, lupus nephritis, myasthenia gravis, paroxysmal nocturnal hemoglobinuria, reduced glomerular filtration rate, a renovascular disorder, or sickle cell disease.

### Claim 7

A compound of structure:
or a pharmaceutically acceptable salt thereof.